Dissertations / Theses on the topic 'Analgesic properties of plants'

The work presented in this thesis is divided into two projects, the isolation and characterisation of analgesic activity in the bark of Barringtonia acutangula and the initiation of an assay for protein phosphatase activity which could be used as a high throughput screen. Analgesic activity had been reported in the bark of Barringtonia acutangula, a tree which grows across northern Australia, by aboriginal people living in the Kimberley district of NorthWwestern Australia. B. acutangula is one of four species of Barringtonia which grow in Australia and one of many which grow in tropical regions worldwide. In addition to its analgesic properties B. acutangula has been put to many uses by local peoples. These include use as medicines, construction materials and as foods. Commonly B. acutangula is used as a fish poison in the collecting of fish for human consumption.
Thesis (PhD Doctorate)
Doctor of Philosophy (PhD)
School of Science
Science, Environment, Engineering and Technology
Full Text

The antiphlogistic and analgesic of American ginseng was confirmed in a model organism of zebrafish, and the possibility of commercial production of fine powder of American ginseng roots, ground to the level of destruction of the plant cell wall, was studied. Zebrafish were used as a model for assessing antiphlogistic activity. Next models were designed: an endotoxin lipopolysaccharide, phenylthiourea, 2,4,6-trinitrobenzene sulfonic acid, -induced inflammation model and model is the tail fin amputation model. The zebrafish activity results showed that all of the aforementioned models of inflammation confirmed the antiphlogistic activity of Panax quinquefolium in a dose-dependent manner within a safe dose. Ultra-grinding of American ginseng roots has increased the release rate of the drug, improved dissolution of active pharmaceutical ingredients and improved absorption in the body, providing a solid theoretical basis and support for the development of industrial research.
Протизапальну активність і знеболюючу активність американського женьшеню було підтверджено на модельному організмі рибок даніо. Вивчено можливість промислового виробництва дрібнодисперсного порошку коренів американського женьшеню, з руйнуванням рослинної клітинної стінки. Рибок даніо використовували як модель для оцінки протизапальної активності. Були індуковані моделі запалення з ліпополісахаридом ендотоксину, фенілтіомочевиною, 2,4,6-тринітробензолсульфоновою кислотою і модель індукованого запалення після ампутації хвостового плавцю (травматична). Результати дослідження активності рибок даніо показали, що на всіх вищезгаданих моделях запалення підтвердили протизапальну активність Panax quinquefolium дозозалежним чином у межах безпечної дози. Ультраподрібнення коренів американського женьшеню збільшує швидкість вивільнення лікарської речовини, покращує розчинення активних фармацевтичних інгредієнтів та сприяє їх всмоктуванню в організмі, забезпечуючи міцну теоретичну основу та підтримку для розвитку промислових досліджень.

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Cryptolepine is the major alkaloid of the West African shrub, Cryptolepis sanguinolenta. Cryptolepine has been shown to inhibit nitric oxide production, and DNA binding of Nuclear Factor-kappa B following inflammatory stimuli in vitro. In order to validate the anti-inflammatory property of this compound in vivo, we investigated its effects on a number of animal models of inflammation. Cryptolepine (10¿40 mg/kg i.p.) produced significant dose-dependent inhibition of the carrageenan-induced rat paw oedema, and carrageenaninduced pleurisy in rats. These effects were compared with those of the non-steroidal anti-inflammatory drug indomethacin (10 mg/kg). At doses of 10¿40 mg/kg i.p., cryptolepine inhibited lipopolysaccharide (LPS)-induced microvascular permeability in mice in a dose-related fashion. Oral administration of up to 40 mg/kg of the compound for four consecutive days did not induce gastric lesion formation in rats. Analgesic activity was also exhibited by cryptolepine through a dose-related (10¿40 mg/kg i.p.) inhibition of writhing induced by i.p. administration of acetic acid in mice. The results of this study reveal that cryptolepine possesses in vivo anti-inflammatory activity.Copyright © 2009 John Wiley & Sons, Ltd.

Chronic pain and excessive alcohol consumption are individually problems in our society today. Alcohol Use Disorder (AUD) affects 15.1 million adult Americans each year. Chronic pain affects over 100 million people annually in the United States. However, there is growing evidence suggesting that these two conditions can often be interrelated with chronic pain increasing consumption of alcohol, and excessive alcohol consumption increasing pain that leaves a feedback cycle trapping millions of patients in an ever worsening spiral. Large population-based studies show an association between pain and alcohol abuse, suggesting a link between increased alcohol use and reduced pain. While rodent studies consistently demonstrate antinociception following acute ethanol administration in hot-plate and tail-flick tests. However, little is currently known about the effects of alcohol in chronic pain models. We hypothesize that acute ethanol administration will possess analgesic-like properties in models of chronic pain by engaging opioid receptors in addition to its more commonly studied action at the GABA receptor. The first aim of this study was to characterize the antinociceptive effects of alcohol in Complete Freund’s Adjuvant (CFA) and Chronic Constriction Injury (CCI) mouse models of chronic inflammatory and neuropathic pain models, respectively. The second aim of this study is to investigate the mechanisms behind ethanol's analgesic like effects including tolerance, receptor activation and correlates with blood alcohol content. Lastly, we investigated whether alcohol maintains its analgesic-like effects in non-reflexive assays in addition to effects in reflexive assays.

Endogenous opiates, the enkephalins, have been identified in the brain and intestine. Their physiological role in the gut has yet to be determined, but since opiates have anti-diarrhoeal actions it was thought possible that they might be involved in the control of mucosal ion transport in addition to their known effects on motility. This possibility was studied using the lq'in vitro' technique of Ussing and Zerahn. Morphine (10^-6 to 10^-4M) induced a significant fall in potential difference (PD) and short-circuit current (I_sc) across stripped rabbit ileal mucosa, with no change in tissue resistance. A maximal electrical response was dependent on the presence of Na, Cl and HCO₃ in the bathing medium. A significant increase in Cl absorption due to a decrease in serosa to mucosa flux was provoked in response to morphine (2 x 10^-5M), accompanied by an increase in residual ion flux (J^R/_net), possibly due to HCO₃ secretion. Na transport was unaffected. Dextromoramide (10^-5M) mimicked the response to morphine, but the inactive isomer laevomoramide (10^-5M) had no effect. Naloxone (10^-6M) inhibited the response to morphine (2 x 10^-5M) and this inhibition was competitive in nature supporting the existence of mucosal opiate receptors. The enkephalin analogue Me-Tyr-D-Met-Gly-Phe-Pro-NH₂ also decreased the PD and I_sc and produced a similar increase in Cl absorption and J^R/_net. This analogue had a more rapid action and provoked a response at a lower dose (10^-8M) than morphine. Tetrodotoxin (10^-7M) inhibited the response to morphine (10^-4M) but blockade of cholinergic, α and β adrenergic and dopaminergic mechanisms had no effect. Morphine (10^-4M) inhibited the secretion produced by three secretagogues, prostaglandin E₂ (10^-5M), acetylcholine (10^-4M) and cholera toxin (1 μg/ml). Adenyl cyclase and cyclic AMP levels were unaffected by morphine, but the electrical response to morphine was increased by omitting Ca^+ + from the medium. Thus these studies provide evidence for the presence of mucosal opiate receptors which may have a physiological role, and demonstrate that opiates enhance Cl absorption and inhibit secretion provoked by three secretagogues. The mechanism of action may be related to an antagonism to intracellular calcium.

3 pp.
Tips for Arizona's Rural Landowners Series -- Plants Unit
The Tips for Arizona's Rural Landowners Fact Sheet Series is intended to educate homeowners who have recently purchased small acreages in Arizona. The purpose of the series is to give homeowners information about living in rural settings. The Plant Unit includes fact sheets on Arizona's native plant law, small-scale gardening, pasture establishment, invasive plants, and assessing plant damage.

Fusion power is the production of electricity from a hot plasma of deuterium and tritium, reacting to produce particles and 14 MeV neutrons, which are collected by a cooling system. Their kinetic energy is transformed into heat and electricity via steam turbines. The constant ux of neutrons on the rst wall of the reactor produces atomic displacement damage through collisions with nuclei, and gas bubbles as a result of transmutation reactions. This leads eventually to hardening and embrittlement. Designing a material able to withstand such intensity of damage is one of the main aims of research in the field of controlled fusion. In the past decades, many experiments have been carried out to understand the formation of radiation-induced damage and quantify the changes in mechanical properties of irradiated steels, but the lack of facilities prevents us from testing candidate materials in a fusion-like environment. Modelling techniques are utilised here to extract information and principles which can help estimate changes in steels due to damage. The elongation and yield strength of various low-activation ferritic/martensitic steels were modelled by neural networks and Gaussian processes. These models were used to make predictions which were compared to experimental values. Combined with other techniques and thermodynamic tools, it was possible to understand the evolution of the mechanical properties of irradiated steel, with a particular focus on the role of chromium and the roles of irradiation temperature and irradiation dose. They were also used to extrapolate data related to fission and attempt to make predictions in fusion conditions. A set of general recommendations concerning the database used to train the neural networks were made and the usage of such a modelling technique in materials science is discussed. An attempt to optimise the performance of neural networks by suppressing some random aspects of the training is presented. Models of the elongation, yield strength and ductile-to-brittle transition temperature trained following this procedure were created and compared to classical models.

3 pp. / Originally published 01/2010.
Invasive plants are plants that have been accidentally or intentionally introduced to an area outside their original range and become problematic in their new environment by interfering with native or desirable species. Landowners can help prevent the spread and assist in controlling these invasive plants. Revised 11/2016. Originally published 01/2010.

South Africa with its vast biodiversity and use of plants in traditional medicine provides a platform for natural drug research and development through the discovery of new chemical entities. The present study was based on the identification of plants as a natural resource for compounds conveying potential antioxidant properties. Free radicals and related molecules, collectively termed reactive oxygen/nitrogen species (ROS/RNS), in excess, promotes oxidative stress within cells and ultimately neurodegeneration. The role of the antioxidant defenses is to eliminate the excess in ROS/RNS and therefore the interest in prevention and/or treatment of neurodegenerative diseases. These compounds have the ability to scavenge free radicals and prevent oxidative stress and related diseases such as neurodegenerative diseases; Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis. For this study, Plumbago auriculata and Tarchonanthus camphoratus were selected from an initial screening (ORAC/FRAP) of a selection of 21 plant species. P. auriculata and T. camphoratus were extracted by Soxhlet extraction, using four solvents, petroleum ether, dichloromethane, ethyl acetate and ethanol, in order of increasing polarity. The extracts were bleached using an ultra-violet irradiation apparatus. Each extract of both plants were then subjected to in vitro assays to determine the antioxidant properties thereof. Both, the thiobarbituric acid (TBA) and nitro-blue tetrazolium (NBT) assays of Ottino & Duncan (1996) were used for antioxidant activity screening of the extracts in rat brain homogenates. The TBA assay relies on the assessment of lipid peroxidation, via hydroxyl anions (OH), on the basis of the complex formation between malondialdehyde (MDA) and TBA, generating a pink colour to be measured spectrophotometrically at 532 nm. The principal of the NBT assay is the reduction of NBT to nitro-blue diformazan (NBD), signified as a purple colour formation, in the presence of the superoxide anions (02 0-). The intensity of the purple colour is then measured spectrophotometrically at 650 nm. The experimental data showed that all of the extracts of P. auricufata and T. camphorates were able to scavenge for OH• and O2.-, which were then correlated to the antioxidant activity of the extracts. The best results were obtained with the EtOAc and EtOH-extracts of T. camphoratus. In comparison to the toxin (H20 2), 0.0270 ± 0.00045 nmole MDAlmg tissue, the extracts showed significant decrease in MDA formation (TBA assay). The EtOH-extract of T. camphoratus attenuated the lipid peroxidation to 0.00386 ± 0.00015 nmole MDAlmg tissue. The extracts were also compared to the toxin (KCN), 30.5006 ± 0.7812 pmole/mg proteins (NBT assay) and showed significant reduction of NBO formation and O2'.scavenging ability. The EtOAc-extract of T. camphoratus obtained the best O2'. Scavenging results 3.5891 ± 0.5029 I-lmole/mg protein reduction in NBO formation. However, based on the correlation of TBA, FRAP and ORAC results the EtOH-extract was chosen for further research. Plant extracts were also subjected to toxicity testing via the MTT (3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The extracts showing toxicity were; PE (10 mg/ml) of both plants and OCM (10 mg/ml) of T. camphoratus. All other extracts showed non-significant toxicity against HeLa cell growth. The EtOH-extracts of T. camphoratus was submitted to bioassay-guided fractionation to isolate the compound responsible for these properties. Compound MVHS9 was isolated through column chromatography and purified by solid phase extraction. 1H, 13C, COSY NMR and IR spectral data were used for structure elucidation and a phthalate ester was proposed for MVHS9.
Thesis (M.Sc. (Pharmaceutical Chemistry))--North-West University, Potchefstroom Campus, 2009.

The methanol extract of Helichrisum pedunculatum was screened for antimicrobial activity up to a concentration of 5 mg/ml using the agar dilution technique. A number of test bacterial isolates, comprising both Gram negative and Gram positive organisms were susceptible to the crude extract of the plant. The minimum inhibitory concentrations (MICs) of the extract ranged between 1 and 5 mg/ml for the susceptible organisms. The MICs of the selected antibiotics, chloramphenicol and penicillin, ranged between 2 and 4 mg/L, and 2 and 32 mg/L respectively against Bacillus cereus, Proteus vulgaris and Staphylococcus aureus OKOH1. Bactericidal activity was determined by the time kill assay. The methanol extract of the plant was not bactericidal at 1 × MIC for B. cereus, P. vulgaris and Staph. aureus OKOH1. At 2 × MIC the extract was bacteriostatic against B. cereus but bactericidal against P. vulgaris and Staph. aureus OKOH1. Combination studies were done at 1/2 × MIC, 1 × MIC and 2 × MIC of the plant extract with 1 × MIC of the antibiotics. Combinations of the plant extract and chloramphenicol resulted in mostly indifferent interactions against P. vulgaris and Staph. aureus OKOH1 but synergistic interactions at higher concentration of the plant extract for B. cereus. Penicillin combinations gave synergistic interactions at lower concentrations of the plant for P.vulgaris and Staph. aureus OKOH1 but was mostly indifferent for B. cereus.

Ganoderma species are one of the most widely researched fungi because of their reported potent bioactive properties. Although there is much information related to American, European and Asian isolates, little research has been conducted on Australian Ganoderma isolates. Ganoderma may only be imported into Australia under strict quarantine conditions, therefore, the isolation of a native strain that possesses bioactivity may be industrially and commercially significant. Three Australian species of this wood-decomposing fungus were isolated in northern Queensland. In this study, they have been identified as three separate species. Further, they have been studied to determine their optimal growth conditions in liquid culture and assessed for their antibacterial properties. Phylogeny inferred from the Internal Transcribed Spacer Regions (ITS) from the DNA sequences resolved the three Australian Ganoderma species into separate clades. Two isolates were identified to be isolates of Ganoderma cupreum (H1) and Ganoderma weberianum (H2). The third isolate could only be identified to the genus level, Ganoderma species, due to the lack of informative data that could be used for comparison. The effects of short term and long term storage on the viability of the fungi were investigated on agar plates, agar slants and balsa wood at varying temperatures ranging from 10 to 45�C. The most appropriate storage conditions were determined to be �80�C on balsa wood chips for periods of up to 2 years without subculture, and on agar slants at 4�C for up to a maximum of eight weeks. Light was observed to be detrimental to the survival of Ganoderma H1 and Ganoderma H2 during storage. Growth trials using potato dextrose agar plates determined the optimal temperature and pH for mycelial growth to be 30�C and a pH of 6, for all isolates. Subsequent growth trials in liquid media found that glucose, as the carbohydrate source, supported the greatest mycelial growth of Ganoderma H1 and Ganoderma H2 and that galactose and fructose supported the greatest growth of Ganoderma H3. Abstract ii Aqueous (hot water) and organic (hexane (HEX), dichloromethane (DCM), ethyl acetate (EtOAc), methanol (MeOH)) extracts from the liquid cultivated mycelium were assessed for their antibacterial activity using disc diffusion assays. Extracts from the mycelium of Ganoderma H1 exhibited activity against a greater number of Gram positive bacteria than those from Ganoderma H2 and H3. Subsequent studies on the DCM and EtOAc extracts from Ganoderma H1 determined the MIC and MBC against a number of Gram positive bacteria, including Bacillus cereus, B. subtilis, Enterococcus faecalis, Streptococcus pyogenes, Staphylococcus aureus, S. epidermidis and Listeria monocytogenes, as well as Clostridium species, including Clostridium perfringens, C. sporogenes and C. difficile, and some methicillin resistant Staphylococcus aureus (MRSA) strains. Time course growth assays confirmed that the DCM and EtOAc extracts predominantly exhibited bactericidal activity. Finally, the active compounds were determined to be terpenoid in structure with some phenolic groups attached.

Xyloglucan endotransglucosylase activity (XET), one of the two main activities of wall xyloglucan endotransglucosylase/hydrolase proteins (XTHs), is of interest because it is responsible for cutting and re-joining xyloglucan of the hemicellulose-cellulose microfibril network in the plant cell wall. XET activity causes transient matrix cleavage without hydrolysis, thus providing a molecular mechanism for controlled, turgor-driven wall expansion. XET activity can be involved in both wall-loosening, thus facilitating cell expansion, and wall-tightening, thus suppressing cell expansion depending on the molecular size, location and age of the participating xyloglucan chains. I have studied the existence of an ‘XET activating factor’ (XAF) in the cold-water-extractable polymers of cauliflower florets. Remaining water-soluble on boiling but losing activity upon proteinase K- and trypsin-digestions implied a heavily glycosylated glycoprotein. XAF was extracted from a wide range of plants and organs. XAF solubilised Arabidopsis cell-wall XTHs, increasing their XET activity on soluble xyloglucan up to 120-fold, tested by a novel method developed in my project. XAF had effects similar to those of 15 mM Ca2+ and 100 mM Na+ in this respect, although it was only weakly ionic. Interestingly, XAF had the unique ability to solubilise XET activity but no other tested wall enzymes from Arabidopsis cell walls, suggesting a specific interaction of XAF to XTH proteins. XAF was successfully purified by the use of several methods, developed in this project. These included cation-exchange column chromatography followed by anion-exchange column chromatography, resulting in two main XAF-activity fractions; or a native- PAGE electro-elution, resulting in three main fractions. Purified XAF contained a major amount of glucose, arabinose, galactose and uronic acid residues. Both boiled cauliflower preparation (BCP) and partially purified XAF were positive with AGP antibodies but the purification of AGP from BCP by the use of Yariv reagent did not enrich XAF activity. Mass-spectrometry analyses of the purified XAF fractions showed some candidates for XAF, including fasciclin-like arabinogalactan-protein 7 (FLA7), stress-responsive protein (LTI65, LTI140) and early nodulin-like protein 14 (ENODL14). Homozygous Arabidopsis mutants (confirmed by genotyping) defective in these genes were used to determine XAF as well as its biological role on plant cell growth. Although there was no phenotype observed, several organs of the mutant plants had significant increases or decreases in XAF activity compared to that of wild type plants. This is the first work that suggests a role of fla7, enodl14 and lti65 in the solubilisation, and thus activation, of Arabidopsis XET.

Considerable evidence suggests the involvement of the ventrolateral periaqueductal gray (PAG) in both inhibitory and facilitatory actions within modulatory pathways for pain, The PAG is a critical nucleus in these pain networks and receives and sends extensive projections within these networks. Chronic pain is a major side effect in 30-70% of cancer patients receiving chemotherapeutic regimen. Endocannabinoids, such as anandamide (AEA), are lipid neuromodulators in the CNS that affect nociception. AEA is known to activate cannabinoid (CB1) as well as transient receptor potential vanilloid 1 (TRPV1) receptors, which are involved in nociception. Previous studies have shown that PAG is a crucial site for EC- mediated analgesia. Hypothesis one of my project is blockade of AEA uptake in the PAG will induce analgesic effects, which are mediated by CB1 and/or TRPV1 receptors. My results indicate that focal bilateral microinjection of AM404, an AEA uptake inhibitor, into the PAG induced analgesia to noxious thermal stimuli (radiant heat) both in normal and paclitaxel-treated (2 mg/kg i.p. for 4 alternate days). This analgesia was mainly mediated by both CB1 and TRPV1 receptors in the PAG in normal and by CB1 receptors in paxlitaxel-treated rats. Several studies have demonstrated that post-ictal analgesia is observed following drug-induced generalized seizures in rats. My second hypothesis is that post-ictal analgesia will occur after audiogenic seizure (AGS) induction, in genetically epilepsy prone rats (GEPR-9s), and blockade of CB1 receptors in the PAG will inhibit the analgesic effects that occur during the post-ictal period. My results indicate that induction of AGS resulted in post-ictal analgesia in GEPR-9s to noxious thermal stimuli, which was blocked upon microinjection of a CB1 receptor antagonist into the PAG suggesting a crucial role of PAG in post-ictal analgesia in GEPR-9s. Hypothesis three of my project is that, neuroplastic changes will occur in the PAG, leading to increases in neuronal firing during neuropathic pain, which will be altered by analgesic drugs. To evaluate this hypothesis, I studied the firing pattern of PAG neurons in awake behaving rats to noxious thermal stimuli. This involved evaluation of extracellular single unit activity using 8 channel microwire electrodes chronically-implanted in the PAG of unrestrained awake rats and examining responses to noxious thermal stimulation (Peltier device). The results indicate the presence of the three types of neuronal populations in the PAG that exhibit either "excitatory" or "Inhibitory" responses or were "non-responsive", to noxious thermal stimulus administered to the paw. Subsequently, I also investigated effects of pentobarbital on spontaneous and thermal stimulus evoked PAG neuronal firing, as has often been done in previous pain studies. Administration of low doses of pentobarbital significantly decreased PAG spontaneous firing and evoked excitatory and inhibitory PAG neuronal responses. These results suggest that the use of barbiturates to study PAG neuronal responses might have resulted in significant un-intended modifications of the fundamental properties of PAG neuron, as compared to the unanesthetized state. The PAG is important part of pain modulatory network, but the electrophysiological characteristics of PAG neurons in chronic neuropathic pain conditions are still unclear. This issue was addressed by administering a standard chronic pain protocol, using the cancer chemotherapeutic drug, paclitaxel, (2 mg/kg i.p. for 4 alternate days) which induced chronic neuropathic pain, Ten days after treatment, mean spontaneous firing rates of PAG neurons were increased significantly after paclitaxel treatment compared to the pre-paclitaxel treatment levels. PAG neurons in the neuropathic state exhibited significantly increased excitatory neuronal responses to non-noxious stimulus, similar to noxious thermal stimulation and significantly increased excitatory-like neuronal responses as compared to pre-treatment levels. Gabapentin is an anticonvulsant that acts on N type voltage sensitive calcium channels and possesses analgesic properties in chronic pain syndromes. Gabapentin did not significantly affect PAG neuronal responses to acute pain in my initial studies However, gabapentin did produce significant changes in spontaneous and thermal stimuli evoked PAG neuronal firing in paclitaxel-treated rats. Gabapentin induced significant dose-dependent decreases in the elevated spontaneous and evoked PAG neuronal firing to both non-noxious and noxious thermal stimuli in the paclitaxel model of neuropathic pain. I also investigated effects of AM404 on spontaneous and thermal stimuli evoked PAG neuronal firing in paclitaxel-treated rats, I observed that AM404 dose-dependently inhibited elevated spontaneous and evoked PAG neuronal firing in paclitaxel-treated rats. These effects were blocked by pre-treatment with CB1 receptor antagonist (AM251) suggesting a crucial role of CB1 receptor in AM404 mediated analgesic effects. These findings suggest that paclitaxel treatment could lead to plasticity in the PAG that might contribute to generation and maintenance of neuropathic pain. These findings provide the evidence that targeting endogenous cannabinoid system or inhibiting presynaptic calcium channels may be effective in treating neuropathic pain, in part, by actions on the PAG.

Philosophiae Doctor - PhD
Over the years, microorganisms have become resistant to commonly used antimicrobial agents leading to multidrug resistance. This is believed to occur even with new classes of therapeutic agents thus creating a challenge on the global healthcare system. The study of medicinal plants allows for their possible use as alternative therapeutic agents. Galenia africana (G. africana) is a South African medicinal plant with numerous health benefits. The purpose of this study was to evaluate the potential antimicrobial, antifungal and anticancer properties of the ethanolic extract of G. africana. Prior to evaluating these properties, in vitro and in vivo acute toxicity studies were conducted to assess the toxicity profile of G. africana. The toxicity profile of the G. africana extract was evaluated using acute toxicity studies conducted in animal and reconstituted human epidermis skin models. The results of the acute oral and dermal toxicity studies revealed that the median lethal dosage (LD50) for G. africana extract in Sprague-Dawley rats was considered to exceed 2000 mg/kg. In the dermal sensitization study, the stimulation index (SI) values for the mice treated with the G. africana extract at concentrations of 25% (50 mg/ml), 50% (100 mg/ml), and 100% (200 mg/ml), when compared to the control group, were 1.3, 0.9 and 1.3, respectively which did not result in an SI value of ? 3 in any group. Hence, it did not elicit a hypersensitivity response. In the irritation test, the G. africana (concentrate) and G. africana (in-use dilution) extracts were non-irritant on the reconstituted human epidermis.

In this PhD it has been analyzed the antioxidant activity of five plants: Camelia sinensis, Gentian lutea, Betula pendula, Convolvulus arvensis and Arctostaphylos uva-ursi. An Electronic Paramagnetic Resonance has been tuned up to determine the antiradical activity of white tea against the methoxy radical using ferulic acid as a standard. It has been proven that the components with more antiradical activity, against the methoxy radical, are the ones with the gallate group, EGCG and ECG. Active ingredients of the Gentian root have been obtained with hydroalcoholic extraction and their antioxidant activity has been demonstrated in both in vitro methods and food models. The antiradical activity of such extracts was determined by FRAP, DPPH, TEAC and ORAC assays. The lyophilized extract, added to the ecological beef meat in a proportion of 2% (by mass), inhibited the meat oxidation (measured by TBARS assay) in high oxygen content atmospheres (80% in volume) as well as in low oxygen content ones (20% in volume). The simultaneous addition of ascorbic acid (0.5% by mass) resulted in significant improvements in color and stability. The lyophilized extract (0.5% by mass) also inhibited oxidation in model systems, oil-in-water emulsions, stored in forced oxidation conditions and constant agitation. The protein BSA addition (0.1% by mass) showed synergic effect and increased the emulsion stability against oxidation. HPLC quantitative analysis found that gentian contained secoiridoid-glycosides (gentiopiocroside and sweroside) and the post-column addition of ABTS cationic radical demonstrated the scavenging activity of each of its compounds. For Convolvulus and Betula, the effect of the solvent polarity in the total polyphenol extraction (by the Folin Ciocalteau assay) was determined. The 50% ethanol extract was the best performer. The scavenging activity of the Convolvulus extract was analyzed by TEAC, FRAP and ORAC assays and against methoxy radical (by EPR). Furthermore, lyophilized extract was added to minced meat hamburgers in different proportions (0.1 and 0.3% by mass). They were stored in a modified atmosphere (80% of O2 and 20% of CO2). Lastly, an edible gelatin film, with Convolvulus extract, was designed. All the assays showed capacity to protect the hamburgers against oxidation. The antiradical activity of the Betula extract was also determined by TEAC, ORAC and FRAP assays and against methoxy radical (by EPR). Some of its phenolic acids were identified by HPLC. Hamburgers, with a proportion of 0.1% and 0.3% by mass of the lyophilized extract, were made and stored under refrigeration (4ºC) and in a modified atmosphere (80% of O2 and 20% of CO2). Colour and percentage of metmyoglobin changes were analyzed as well as the oxidation degree (by TBARS assay). Both percentages provided significant improvements in all the studied parameters. The last part of this thesis was focused in the study of Arctostaphylos uva-ursi. The scavenging activity against ABTS+ and methoxy radical was determined (by EPR). A percentage of 0.1% by mass of the lyophilized extract was added to oil-in-water emulsions. Oxidation was measured by VP and TBARS. There was a significant delay in oxidation. Extract was incorporated to edible gelatin films with 0.1% by mass. If such a film protects the hamburger, its life is increased. In conclusion, all five plants presented in this study have antioxidant activity (in the used proportions) that made them suitable to formulate new foods, more stable over time against oxidation without using the controversial synthetic antioxidants. Moreover, they will be able to provide additional advantages (incorporating natural antioxidants), which would provide functional foods.
Se ha analizado la actividad antioxidante de cinco plantas: Camelia sinensis, Gentian lutea, Betula pendula, Convolvulus arvensis y Arctostaphylos uva-ursi. Se ha puesto a punto, con el té blanco, la Resonancia Paramagnética Electrónica (EPR) para determinar la actividad antiradicalaria frente al radical metoxi, usando como patrón el ácido ferúlico. Se ha demostrado que los componentes del té con más actividad antiradicalaria, frente a los radicales metoxi, son los que tienen el grupo galato, EGCG y ECG. Se han obtenido, por extracción hidroalcohólica, los principios activos de la raíz de genciana y se ha demostrado su actividad antioxidante tanto en métodos in vitro como en modelos de alimentos. La actividad antiradicalaria de dichos extractos se determinó por FRAP, DPPH, TEAC y ORAC. El liofilizado del extracto, añadido a la carne de ternera ecológica en proporción 0,2 % (en masa), inhibió la oxidación de la carne (medida por TBARs), tanto en atmósferas de alto contenido en oxígeno (80% en volumen) como de bajo contenido (20% en volumen). La adición simultánea de ácido ascórbico (0,5% en masa) produjo mejoras significativas en el color y en la estabilidad. El extracto liofilizado (0,5 % en masa) también inhibió la oxidación en sistemas modelo, emulsiones de aceite en agua, almacenadas en condiciones de oxidación forzada y con agitación constante. La adición de la proteína BSA (0,1 % en masa) mostró efecto sinérgico y aumento la estabilidad de la emulsión frente a la oxidación. El análisis cuantitativo mediante HPLC mostró que la genciana contenía glucósidos secoiridoides (gentiopiocrosido y swerosido) y la adición post-columna del radical catiónico ABTS, demostró la actividad antiradicalaria de cada uno de sus compuestos. Para Convulvuvus y Betula se determinó el efecto de la polaridad del disolvente en la extracción de los polifenoles totales (por el método de Folin Ciocalteau). El extracto de etanol al 50% fue el que obtuvo mejores resultados. Se analizó la actividad antiradicalaria del extracto de Convulvuvus mediante el TEAC, el FRAP, el ORAC y frente al radical metoxi (por EPR). Además se añadió el extracto liofilizado a hamburguesas de carne picada en diferentes proporciones (0,1 y 0,3 % en masa). Se almacenó en atmósfera modificada (80% de O2 y 20% de CO2). Finalmente se diseñó un film comestible de gelatina con el extracto de Convulvuvus. Todos los ensayos mostraron capacidad de proteger las hamburguesas frente a la oxidación. Se determinó la actividad antiradicalaria del extracto de Betula por TEAC, ORAC, FRAP y frente al radical metoxi (por EPR). Se identificaron por HPLC algunos de sus ácidos fenólicos. Se hicieron hamburguesas con una proporción de 0,1% y 0,3%, en masa, del extracto liofilizado y se almacenaron en refrigeración (4ºC) y en atmósfera modificada (80% O2 y 20% CO2). Se analizó el cambio de color y el cambio en el porcentaje de metamioglobina, así como el grado de oxidación (a través del TBARs). Los dos porcentajes proporcionaron mejoras significativas en todos los parámetros estudiados. La última parte de esta tesis se centró en el estudio de la Arctostaphylos uva-ursi. Se determinó la actividad antiradicalaria frente al ABTS·+ y frente al radical metoxi (por EPR). Se añadió a emulsiones de aceite en agua un porcentaje de 0,1 % en masa del extracto liofilizado. Se midió la oxidación por VP y TBARs. Se produjo un retraso significativo en la oxidación. Se incorporó extracto a films comestibles de gelatina con 0,1 % en masa. Si dicho film protege la hamburguesa, aumenta su vida útil. En conclusión, las 5 plantas presentadas en este estudio tienen una actividad antioxidante (en las proporciones utilizadas) que las hace aptas para formular nuevos alimentos, más estables en el tiempo frente a la oxidación sin el uso de los controvertidos antioxidantes sintéticos. Además podrán proporcionar ventajas adicionales (incorporación de antioxidantes naturales), lo que permitiría obtener alimentos funcionales.

Cancer and malaria are among the most life-threatening diseases globally. Cancer is responsible for about 125,000 annual deaths globally. In 2015, the World Health Organization report estimated that 236000-635000 people died of malaria. These diseases are complicated by the development of resistance to available chemotherapeutic agents. Natural products have been recognized for their major applications in the identification of drug leads in drug discovery. Viola philippica Car, Viola yedoensis Makino (Violaceae), Triclisia subcordata Oliv (Menispermeaceae) and Cyclicodiscus gabunensis Harms (Fabaceae) are medicinal plants traditionally used for the treatment of various diseases including malaria or cancer in China and West Africa. However, the bioactive compounds are unknown. Therefore, this study evaluated the in vitro anticancer and antimalarial activities of the four medicinal plants and searched their bioactive compounds. The in vitro anti-ovarian cancer and antimalarial assays were demonstrated respectively using sulforhodamine B dye and Syber green 1 fluorescence assay methods. Bioassay-guided fractionation and purification were performed. Structural elucidation was performed by nuclear magnetic resonance spectroscopy and mass spectrometry analysis. Results revealed the anticancer and antimalarial activities of T. subcordata; V. philippica, and V. yedoensis to be bisbenzylisoquinoline alkaloids (cycleanine, isochondodendrine and 2′-norcocsuline) and/or cyclotides. The cycleanine analogues were synthesized and found to be more potent than cycleanine. Induction of apoptosis by these alkaloids has also been determined. This study could serve as basis for the support of use of these plants in cancer and/or malaria treatment. The BBIQ alkaloids and analogues could serve as lead compounds in drug discovery. Future in vivo studies need to be carried out on these alkaloids to get drug approval.

Leaf tensile strength was measured for four resurrection plants, Craterostigma wilmsii Engl, Xerophyta schlecteri (Baker) N.L. Menezes, Xerophyta humilis (Baker) T. Durand & Schinz and Sporobolus stapfianus Gandoger, as well as two desiccation-sensitive controls, Zea mays L. and Arabidopsis thaliana (L.) Heynh. (ecotype Columbia) at full hydration and after dehydration, both on the plant (naturally-dried) and rapidly off the plant causing death (flash-dried). In the desiccation-tolerant plants, leaf tensile strength was higher in the monocots than the dicots at full hydration. Three different mechanisms of cell protection occur in resurrection plants on drying: cell-wall folding, packing vacuoles with non-aqueous solute or a combination of the two. Tensile strength in C. wilmsii ( dicot) increased when naturally-dried but decreased when flash-dried, possibly due to the nature of the drying mechanisms (wall folding). The, leaf tensile strength of the Xerophyte species, both monocots, increased when naturally dried and when flashdried. Xerophyte species pack their vacuoles during desiccation. S. stapfianus, a grass which uses a combination of wall folding and vacuole packing, had the highest tensile strength possibly due to its unique architectural structure. Differences in leaf architecture, in terms of lignin content, were examined using light microscopy after histo-chemical staining for lignin, which showed that monocotyledons had a higher percentage of lignin per unit leaf cross-sectional area than dicotyledons. A regression analysis revealed that leaf tensile strength and lignin content were positively correlated in fully hydrated leaves I but no relationship existed between lignin content and naturally dried leaves. This may be due to variations of protective mechanisms induced during desiccation by the four resurrection plants. Notching was observed in X schlechteri, behaving differently to grasses which are notch-insensitive, possibly due to large lignin contents on the outer edges of the leaves.

The rapid development of seriously drug-resistant pathogen strains has created a dangerous problem to public health. The discovery of new effective antimicrobials remains an urgent task to control microbial resistance. Natural products can offer special stereochemistry and unlimited diversity of natural leads which are biologically active or ready for development and structure optimization strategies. Four medicinal plants Cylicodiscus gabunensis (CG), Pogostemon cablin (PC), Perilla frutescens (PF) and Magnolia biondii (MB) were selected for investigation of their phytochemical composition and antiplasmodial and/or antibacterial properties. A bioassay guided fractionation method has been followed to characterize the antiplasmodial and antibacterial constituents of CG. Flash column chromatography and preparative HPLC were used to obtain the bioactive compounds. GC-MS, LC-MS, and NMR have been used for chemical analysis purposes. For evaluation of the antibacterial activity, disk diffusion assay, alamar blue microplate assay, time kill kinetic and scanning electron microscopy (SEM) methods have been used. The work led to the isolation of the most potent antiplasmodial fraction of CG with IC50 of 4.7.

To investigate nematicidal activity against the root-lesion nematode, Pratylenchus coffeae, the methanolic extracts were obtained from 5 medicinal plants in Vietnam. Methanol extracts of the 5 samples were screened for nematicidal activity against Pratylenchus coffeae in vitro. Of the plant extracts tested, a 5 mg/ml concentration of Terminalia nigrovenulosa extract showed the highest level (95.0%) of nematicidal activity against Pratylenchus coffeae at 9 h after treatment. The remainder of the plant extracts was followed by Cinnamomum camphora (66.7%), Jasminum suptriplinerve (30.8%), Premna integrifolia (6.7%), and Treptocaulon juventas (5.8%). A 2.0 mg/ml concentration of T. nigrovenulosa resulted in 13.3, 42.5, 62.5 and 86.7% at 1, 3, 5 and 7 h after treatment, respectively against Pratylenchus coffeae. Concentration of 0.1, 0.5, 1.0 and 2.0 mg/ml of T. nigrovenulosa resulted in 26.7, 71.7, 78.3 and 86.7% effectiveness respectively, at 7 h after treatment. Also, at 3 days after exposure to T. nigrovenulosa, hatch was inhibited by 60.0, 45.8, 17.5 and 5.8% at 0.1, 0.5, 1.0 and 2.0 mg/ml, respectively. Hatch was inhibited by 65.0, 50.8, 21.7 and 6.7% at 0.1, 0.5, 1.0 and 2.0 mg/ml respectvely, at 6 days after exposure to T. nigrovenulosa. The mortality rate and hatch inhibition increased with increasing incubation time for crude extract of T. nigrovenulosa
Trong nghiên cứu này, 5 cây thuốc (Cinnamomum camphora, Jasminum suptriplinerve, Premna integrifolia, Terminalia nigrovenulosa, Treptocaulon juventas) đã được sử dụng làm nguyên liệu chiết xuất bằng methanol để thử hoạt tính kháng tuyến trùng Pratylenchus coffeae. Kết quả cho thấy chiết xuất từ cây Terminalia nigrovenulosa biểu hiện hoạt tính kháng tuyến trùng cao nhất (95,0%) sau 9 giờ xử lý với nồng độ 5 mg/ml. Hoạt tính kháng tuyến trùng của các chất chiết xuất được biểu hiện theo thứ tự giảm dần lần lượt là C. camphora (66,7%), J. suptriplinerve (30,8%), P. integrifolia (6,7%) và T. juventas (5,8%). Với nồng độ 2 mg/ml của chất chiết xuất từ T. nigrovenulossa biểu hiện hoạt tính gây chết tuyến trùng Pratylenchuss coffeae là 13,3; 42,5; 62,5 và 86,7% sau 1, 3, 5 và 7 giờ xử lý theo thứ tự. Ở cùng thời điểm sau xử lý 7 giờ, các nồng độ 0,1; 0,5; 1,0 và 2,0 mg/ml chiết xuất của T. nigrovenulossa có hoạt tính gây chết tuyến trùng Pratylenchus coffeae lần lượt là 26,7; 71,7; 78,3 và 86,7%. Bên cạnh đó, chất chiết xuất của T. nigrovenulossa cũng cho thấy tỷ lệ ức chế trứng nở cao. Cụ thể là sau 3 ngày xử lý với chất chiết xuất của T. nigrovenulossa, tỷ lệ ức chế trứng không nở là 60,0; 45,8; 17,5 và 5,8% at 0,1; 0,5; 1,0 và 2,0 mg/ml theo thứ tự. Sau 6 ngày xử lý với chất chiết xuất của T. nigrovenulossa, tỷ lệ ức chế trứng nở là 65,0; 50,8; 21,7 và 6,7% tại nồng độ 0,1; 0,5; 1,0 và 2,0 mg/ml theo thứ tự. Tỷ lệ gây chết và tỷ lệ ức chế của chất chiết xuất phụ thuộc vào cả thời gian và nồng độ xử lý

Drug-resistant pathogenic and opportunistic bacteria are increasing in occurrence and prevalence, and pose a dangerous threat to human health. In the search for novel antibiotics with which to combat this threat, plants, specifically those used in traditional medicine with ascribed antibacterial properties, offer a promising and potentially vast source of such therapeutic compounds. The purpose of this study was therefore to screen chemical extracts created from various plant species for antibacterial properties versus pathogenic bacterial species. In the course of these antibacterial assays, we successfully identified a methanol extract derived from Artemisia tridentata tridentata plant material as capable of inhibiting the growth of the opportunistic pathogen Staphylococcus aureus. Three sub-fractions were created using hexane, ethyl acetate and water solvents. Each of these extracts displayed significant antibacterial activity versus a wild-type strain over a period of six hours, at concentrations as low as 62.5 µg/ml. The extracts also demonstrated an enhancement of antibiotic effects when combined with ampicillin, G418 sulfate or amikacin, for a period of up to twelve hours. Though the efficacy of the extracts was lessened when tested against an ampicillin-resistant strain, significant enhancement of the efficacy of this antibiotic was still observed. Gas chromatography-mass spectrometry analysis of these three extracts revealed the sesquiterpene lactone achillin as present in each. Column chromatography of the hexane extract resulted in a fraction retaining its antibacterial activity, and still containing this compound, further implicating it as responsible for the antibacterial activity of this plant. The results of serial dilution and plating of extract-treated samples, along with those of ethidium bromide assays and transmission electron microscopy analysis, indicated a bacteriostatic mechanism of action involving disruption of the bacterial membrane, which is in agreement with the literature on the antibacterial properties of this plant, and those of sesquiterpene lactones, respectively. We therefore conclude that achillin, likely produced as a secondary metabolite by Artemisia tridentata tridentata, possesses growth inhibitory properties versus Staphylococcus aureus, and should be isolated and studied further for the purposes of evaluating its potential use, either as a stand-alone antibiotic, or as an adjunctive therapeutic, in the treatment of drug-resistant bacterial pathogens.

A follow-up of traditional medicinal plants uses is an important tool in highlighting their therapeutic potentials, as they have been found to be a source of a wide range of bioactive compounds that can be used as base compounds for new pharmaceutical drugs. This study therefore focuses on assessing the anti-Listerial properties of the seeds of Garcinia kola (Heckel) plant, which is a traditional medicinal plant of west and central African origin, and was and is still used to traditionally treat several ailments. Four different solvents crude extracts of the seeds were assessed for their anti-Listerial activities in-vitro, against a panel of 42 Listeria bacteria, which included Listeria monocytogenes, Listeria ivanovii and Listeria grayi species. At 10 mg/ml concentration the aqueous extract had activity against 29% of the test isolates while the other three crude extracts namely dichloromethane, n-hexane and the methanol extracts had activity against 45% of the test bacteria. The minimum inhibitory concentration (MIC) ranges of the extracts were 0.079-0.313 mg/ml for the dichloromethane extract; 0.079-0.625 mg/ml for the n-hexane extract; 0.157-0.625 mg/ml for the methanol extract; and 10->10 mg/ml for the aqueous extract. The minimum bactericidal concentration (MBC) ranges of the extracts were 0.625–10 mg/ml for both the n-hexane and the dichloromethane extract; 5-10 mg/ml for the methanol extract; and those for the aqueous extract were above 10 mg/ml against all the susceptible Listeria isolates. The rate of kill analysis was then determined for the three most active crude extracts that is excluding the aqueous extract and it was assessed against four representative Listeria species namely L. monocytogenes (LAL 8), L. grayi (LAL 15), L. ivanovii (LEL 30) and L. ivanovii (LEL 18). All the three extracts showed a general trend of being concentration and time dependent in their rate of kill profiles such that most bacteria cells were killed at the highest test concentration of 4× MIC value after the maximum exposure time of 2 h. The n-hexane, dichloromethane and methanol extracts were bactericidal against 4, 3 and 1 isolates out of the four test Listeria isolates respectively.

This thesis examines the cytochrom P450 (CYP) drug metabolizing enzyme inhibition and antimicrobial properties of 46 common food plants available in the Canadian Market and the inhibitory properties of 17 traditional Cree antidiabetic medicines on aldose reductase. Inhibitory activity profiles of CYP 3A4, 3A5, 3A7 and 2D6 were created for the 46 samples. The most active plants in the CYP inhibition assay were the spices, belonging to the Apiaceae and Lamiaceae. Similarly, the most active plants in the antimicrobial assay were also the Apiaceae and Lamiaceae. Swine lens homogenate was tested as a novel model for the aldose reductase inhibition assay. Several Cree plants selected for the aldose reductase study showed a high activity, primarily in samples which also contained high levels of phenolics. A positive correlation was observed between total phenolics content and aldose reductase inhibition r2=0.44, p=0.05. Crude extracts of Rhododendron groenlandicum exhibited inhibitory activities of 35.11 ± 0.16 %. The subfractionation and HPLC analysis of R. groenlandicum revealed high levels of phenolics compounds including, catechin, epicatechin, quercetin and quercetin glycosides. This study found that medicinal and food plants contain phytochemicals that may have both beneficial and detrimental biological effects.
Nous avons étudié dans cette thèse les capacités de 46 plantes comestibles, disponibles sur le marché canadien, à inhiber le cytochrome P450 (CYP), enzyme responsable du métabolisme des médicaments, les propriétés antimicrobiennes, et les propriétés inhibitrices de l'aldose réductase à partir de 17 médicaments antidiabétiques traditionnellement utilisés par les Cris. Les profils de l'activité inhibitrice du CYP 3A4, 3A5, 3A7 et 2D6 ont été réalisés pour les 46 plantes à l'étude. Les plantes les plus actives dans le test d'inhibition du CYP furent les épices, plantes appartenant aux familles des Apiaceae et Lamiaceae. De même, les plantes les plus actives dans le bioessai antimicrobien furent aussi les plantes de ces deux mêmes familles. Un homogénat de cristallin de porc a été utilisé comme modèle nouveau pour le test d'inhibition de l'aldose réductase. Plusieurs plantes, utilisées par la nation Cri, qui ont été sélectionnées pour l'étude ont montré une forte activité inhibitrice de l’aldose réductase, principalement dans les échantillons qui contenaient des teneurs élevées en composés phénoliques. Une corrélation positive a été observée entre la teneur totale en composés phénoliques et l'inhibition de l'aldose réductase (r2 = 0.44, p = 0.05). Des extraits bruts de Rhododendron groenlandicum ont montré des activités inhibitrices de 35.11 ± 0.16%. Le sous-fractionnement et l'analyse HPLC de R. groenlandicum ont aussi révélé des teneurs élevées des composés phénoliques, incluant la catéchine, l'épicatéchine, la quercétine et les glycosides de quercétine. Cette étude a montré que les plantes médicinales et alimentaires contiennent des composés phytochimiques qui peuvent avoir à la fois des effets biologiques bénéfique et préjudiciable.

To investigate nematicidal activity against the root-lesion nematode, Pratylenchus coffeae, the methanolic extracts were obtained from 5 medicinal plants in Vietnam. Methanol extracts of the 5 samples were screened for nematicidal activity against Pratylenchus coffeae in vitro. Of the plant extracts tested, a 5 mg/ml concentration of Terminalia nigrovenulosa extract showed the highest level (95.0%) of nematicidal activity against Pratylenchus coffeae at 9 h after treatment. The remainder of the plant extracts was followed by Cinnamomum camphora (66.7%), Jasminum suptriplinerve (30.8%), Premna integrifolia (6.7%), and Treptocaulon juventas (5.8%). A 2.0 mg/ml concentration of T. nigrovenulosa resulted in 13.3, 42.5, 62.5 and 86.7% at 1, 3, 5 and 7 h after treatment, respectively against Pratylenchus coffeae. Concentration of 0.1, 0.5, 1.0 and 2.0 mg/ml of T. nigrovenulosa resulted in 26.7, 71.7, 78.3 and 86.7% effectiveness respectively, at 7 h after treatment. Also, at 3 days after exposure to T. nigrovenulosa, hatch was inhibited by 60.0, 45.8, 17.5 and 5.8% at 0.1, 0.5, 1.0 and 2.0 mg/ml, respectively. Hatch was inhibited by 65.0, 50.8, 21.7 and 6.7% at 0.1, 0.5, 1.0 and 2.0 mg/ml respectvely, at 6 days after exposure to T. nigrovenulosa. The mortality rate and hatch inhibition increased with increasing incubation time for crude extract of T. nigrovenulosa.
Trong nghiên cứu này, 5 cây thuốc (Cinnamomum camphora, Jasminum suptriplinerve, Premna integrifolia, Terminalia nigrovenulosa, Treptocaulon juventas) đã được sử dụng làm nguyên liệu chiết xuất bằng methanol để thử hoạt tính kháng tuyến trùng Pratylenchus coffeae. Kết quả cho thấy chiết xuất từ cây Terminalia nigrovenulosa biểu hiện hoạt tính kháng tuyến trùng cao nhất (95,0%) sau 9 giờ xử lý với nồng độ 5 mg/ml. Hoạt tính kháng tuyến trùng của các chất chiết xuất được biểu hiện theo thứ tự giảm dần lần lượt là C. camphora (66,7%), J. suptriplinerve (30,8%), P. integrifolia (6,7%) và T. juventas (5,8%). Với nồng độ 2 mg/ml của chất chiết xuất từ T. nigrovenulossa biểu hiện hoạt tính gây chết tuyến trùng Pratylenchuss coffeae là 13,3; 42,5; 62,5 và 86,7% sau 1, 3, 5 và 7 giờ xử lý theo thứ tự. Ở cùng thời điểm sau xử lý 7 giờ, các nồng độ 0,1; 0,5; 1,0 và 2,0 mg/ml chiết xuất của T. nigrovenulossa có hoạt tính gây chết tuyến trùng Pratylenchus coffeae lần lượt là 26,7; 71,7; 78,3 và 86,7%. Bên cạnh đó, chất chiết xuất của T. nigrovenulossa cũng cho thấy tỷ lệ ức chế trứng nở cao. Cụ thể là sau 3 ngày xử lý với chất chiết xuất của T. nigrovenulossa, tỷ lệ ức chế trứng không nở là 60,0; 45,8; 17,5 và 5,8% at 0,1; 0,5; 1,0 và 2,0 mg/ml theo thứ tự. Sau 6 ngày xử lý với chất chiết xuất của T. nigrovenulossa, tỷ lệ ức chế trứng nở là 65,0; 50,8; 21,7 và 6,7% tại nồng độ 0,1; 0,5; 1,0 và 2,0 mg/ml theo thứ tự. Tỷ lệ gây chết và tỷ lệ ức chế của chất chiết xuất phụ thuộc vào cả thời gian và nồng độ xử lý.

Thesis (Ph. D.)--School of Geosciences, Faculty of Science, University of Sydney, 2004.
Degree awarded 2004; thesis submitted 2003. Submitted in fulfilment of the requirements for the degree of Doctor of Philosophy to the School of Geosciences, Faculty of Science. Title from title screen (viewed 13 January 2009). Includes bibliographical references. Also available in print form.

Mestrado em Engenharia Alimentar - Qualidade e Segurança Alimentar - Instituto Superior de Agronomia
In the present work, leaves of four wild plants (Rumex crispus (curly dock), Sinapis arvensis (wild mustard), Beta maritima (sea beet) and Sonchus oleraceus (sow thistle)) were studied in order to analyse for their mineral composition, phenolic content, antioxidant capacity, and detection of lectins (anti-nutritive compound). The mineral and antioxidant study of different species was compared with cultivated plants of same family (rhubarb, turnip greens, common chard and lettuce). In wild plants, per 100 g of part edible, the elements most notably were magnesium (52.70 mg), iron (2.69 mg) and zinc (0.46 mg). The phenolic content varied between 891.55 and 105.84 mg GAE/ 100 g dry weight and the leaves of Rumex crispus had an antioxidant capacity three times higher than other species. All extracts, except Rumex crispus, revealed presence of lectins in leaves subject to thermal treatment. These results suggest that leaves of Rumex cripus may have potential in the food industry and the lectins of other species could have various applications. Further research is needed for a more complete characterization these plants and its uses

In many developing countries, farmers and pastoralists still rely on their indigenous knowledge, practices and locally available plants to control nematode parasitic infections, both in livestock and humans. The overall aim of my thesis was to undertake bioassay-guided phyto-chemical study of extracts and their constituents from Ethiopian anti-parasitic plants used by healers to control gastrointestinal nematode parasites in livestock to validate their ethno-medicinal use and to characterise and identify their active ingredients. As a first experiment (Chapter Three), four types of crude extracts (water, 70% methyl-alcohol, absolute methanol and acetone) of four indigenous Ethiopian medicinal plants (Adenia species, Cissus ruspolii, Ipomoea eriocarpa and Euphorbia thymifolia) were screened against Teladorsagia circumcincta egg hatching in vitro, not only as a first step to validate the traditional healers claim but also to choose the most promising plant extract(s) for further phyto-chemical studies. The egg hatching inhibition (EHI) test results revealed that the anti-parasitic properties of these plants depended on plant species, dose, and solvent polarity. The water extracts of both C. ruspolii and Adenia sp. exhibited largest, up to 100% EHI but also larval migration inhibition activities, and were selected for further studies. The second experiment (Chapter Four) assessed the nature of active constituents in these extracts by physico-chemical methods. It was observed that the major constituents of both plant extracts responsible for the EHI activities are likely highly polar, water-soluble, small and moderately heat-labile molecules. The third and fourth experiments (Chapters Five and Six) consisted of separating Cissus ruspolii and Adenia sp. water extracts into discrete fractions by gel-permeation chromatography, EHI tests of Bio-Gel P-2 fractions followed by thin layer chromatography (TLC) profiling of these fractions to detect separated spots (in day light, under UV-light or after staining with various staining reagents) and also to see how elution patterns of separated spots affected by column parameters. The EHI tests on the fractions obtained revealed that the active constituents of C. ruspolii and Adenia sp. water crude extracts were eluted into few fractions based on their molecular sizes. The TLC profilings of these fractions identified spot patterns of active and inactive fractions, which allowed pooling of active constituents based on their EHI and TLC profiling into three pools for each plant. The fifth experiment (Chapter Seven) was to isolate and purify compounds from these pools using various preparative planar and column chromatographic methods. Sequential applications of column chromatography followed by preparative thin layer chromatography isolated and purified five active compounds from C. ruspolii and two active compounds from Adenia sp. The sixth experiment (Chapter Eight) was to characterize and propose/elucidate structures of compounds from the active fractions using chromatographic, analytical and spectroscopic methods. In this regard, the structures of two oleanane type triterpenoid saponins isolated from one of active fractions of Adenia sp. were proposed based on their mass spectrometry (MS) and nuclear magnetic resonance (NMR) data with support of compounds property, TLC and literature. Similar outcomes for C. ruspolii were not achieved due to lack of sufficient sample to run 13C-nuclear magnetic resonance spectroscopy and distortionless enhancement by polarization transfer (DEPT), contamination of some purified compounds with ill-characterised substance from the preparative TLC matrix and in some cases mass spectrometry (MS) and nuclear magnetic resonance (NMR) data did not support each other. The last experiment (Chapter Nine) was to assess anthelmintic efficacy and safety of C. ruspolii and Adenia sp. crude water extracts in Heligmosomoides bakeri infected mice. This in vivo test revealed that both plant extracts exhibited significant reduction in worm burdens and worm egg excretion, with moderate effects on haematology and organ weights at tolerated dosages. In conclusion, both in vitro and in vivo data revealed that Adenia sp. and C. ruspolii have anthelmintic properties, thus validating traditional healer claims and supporting ethno-medicinal use. The bioassay-guided phytochemical study resulted in the isolation of a number of active compounds from these plants, for some of which a structure has been proposed.

Thesis (M. Tech. (Biomedical Technology)) -- Central University of Technology, Free State, 2014.
Traditional medicine has been known by mankind since ancient times as a healthcare system. All cultures have used herbs throughout history and it was an integral part of the development of modern civilization. Primitive man observed and appreciated the great diversity of plants available to him. Plants provided food, clothes, shelter and medicine and still play a vital role in rural villages of South Africa. The medicinal uses of plants and animals have been developed through trial and error. Herbal plants produce and contain a wide variety of chemical substances that act upon the body’s immune system. The medicinal properties of Ipomoea oblongata (E.Mey.ex Choisy) in this study was to determine the phytochemical content, antioxidant, anti-cancer and anti-diabetic properties of I. oblongata (Mothokho), a medicinal plant used by traditional medical practitioners of Thaba-Nchu in the Free State. The study was carried out in order to validate the ethnomedicinal claims made by the traditional medical practitioners and to evaluate the plant’s potential as a novel therapeutic agent. Twelve traditional medical practitioners of the Kopanang Dingaka Association were interviewed on the knowledge and use of I. oblongata (Mothokho). The phytochemical constituents of the plant were determined using standard screening methods. Testing for antioxidant properties (free radical scavenging activity) was carried out by means of the 2, 2- diphenylpicrylhydrazyl (DPPH) assays. The Sulforhodamine B assay was used to screen for anti-cancer activity in breast (MCF7), colon (HCT116) and prostate (PC3) cancer cell lines. Glucose uptake in C2C12 muscle cells was used to evaluate the anti- iii diabetic potential of I. oblongata. Methanol extract was fractionated using Ultra-Pure Liquid Chromatography (UPLC) to identify active compounds. The traditional medical practitioners cited the plant roots as the main ingredient in the treatment of respiratory infections, sexually transmitted infections, postnatal womb treatments, inflammation, arthritis, wounds and cancer. The methanol extract of I. oblongata showed remarkable (99.03%, 98.39, 71.31%) antioxidant potential in all triplicates tested which explains its use in oxidative stress-related diseases such as arthritis and cancer. Phytochemical tests showed the presence of carbohydrates, glycosides, steroids, terpenoids, alkaloids, flavonoids and tannins. However, the extracts were inactive against the cancer cell lines used. Glucose uptake by the C2C12 muscle cells was increased by over 150% and was comparable to that of insulin and metformin, suggesting good anti-diabetic activity. Predicted compounds found were dihydroquercetin pentaacetate, actinorhodin and actinorhodine, using Chemspider analysis. These are possible compounds that could be found in the Ipomoea oblongata extracts when using nuclear magnetic resonance (NMR) to determine the structure and names of the active compounds. Ethnobotanical uses of Ipomoea oblongata were found to have a link with other ethnobotanical studies to capture the indigenous knowledge, culture and therapeutic uses. The phytochemical results of Ipomoea oblongata can contribute to the knowledge of new drug development as indicated by literature (Harbone; 1973, Soforowa, 1993; De et al., 2010) that plants contain phytochemical contents and phenolic compounds that are valuable as medicinal properties. Methanolic extract of Ipomoea oblongata presented high levels of antioxidant activity respectively, which can become a potential iv antimicrobial agent and remedy oxidative stress related diseases. The anticancer properties were inactive and the cytotoxicity levels were found to below in I. oblongata. Low levels of cytotoxicity allow medicinal plants to be consumed by humans with fewer side effects however doses must be standardized. High levels of glucose uptake in muscle cells were indicated from the aqueous extract of Ipomoea oblongata, therefore showing great potential as an antidiabetic agent. Many medicinal plants have been validated as antidiabetic therapeutic agents in South Africa and the world. New treatment of cancer, diabetes, bacterial and viral infections is required from natural products that are cost effective with minimal side effects that can be used in health care systems. There is a correlation between the medicinal properties found in I. oblongata and the ethnomedicinal uses cited by the traditional medical practitioners. The plant I. oblongata has six ethno-pharmaceutical uses. I. oblongata is a good source of anti-diabetic and antioxidant agents that can be developed further. However the plant is not a good source of anticancer properties. Future research will be into the isolation and identification of the active compounds.

Hermannia incana Cav. (Sterculiaceae), known as sweet yellow bells, is a medicinal plant used by the people of the Eastern Cape for the treatment of stomach-ache and diarrhoea. It has purgative and diaphoretic effects. It is a prostrate herb with yellow flowers and sparsely hairy and slightly glandular leaves, occurring in grassland and marshes in the Eastern Cape Province of South Africa. Based on the ethnomedical uses of this plant, the research project was designed to evaluate its antidiarrhoeal and toxicological properties. An ethnobotanical study of plants used for the treatment of diarrhoea in the Eastern Cape Province was carried out, using a questionnaire which was administered to herbalists, traditional healers and rural dwellers. This survey indicated a total of 17 plant species from 14 families. Elephantorrhiza elephantine (Burch.) Skeels, Hermannia incana Cav., Pelargonium reniforme Curt., Alepidea amatymbica Eckl. & Zeyh. and Bulbine latifolia (L.f.) Roem. et Schult. were the most frequently mentioned and highly recommended plants for the treatment of diarrhoea by both the traditional healers and rural dwellers. The root, bark and leaves are the common parts of plants used, while decoctions and infusions are the main methods of preparation. The agar dilution method was used to study the antimicrobial activity. The methanol extracts of the plant showed appreciable activity against Gram-positive and Gram-negative bacteria at concentrations ranging from 0.5 to 7.0 mg/ml. The acetone and water extracts of both the leaves and the roots showed moderate activity against Gram positive bacteria and less activity against Gram negative bacteria. All the extracts inhibited the growth of the fungi Aspergillus flavus, Aspergillus niger, and Mucor hiemalis with growth inhibition ranging from 54.31 percent to 96.67 percent at 0.1-10 mg/ml. None of the extracts suppressed the growth of Candida albicans at the maximum concentration (10 mg/ml) tested. iii In the in vivo antidiarrhoeal evaluation using Wistar rats, the aqueous extract at all the doses tested, significantly prolonged the time of induction of diarrhoea and also reduced the frequency of diarrhoeal episodes and fecal parameters (total number, number of wet, fresh and dry weight and water content of the faeces). The percentage inhibition of defecation and intestinal content (enteropooling) were increased in dose dependent manner. The doses also reduced the intestinal transit time of charcoal, masses and volumes of intestinal fluid (gastrointestinal motility). These results are indications of antidiarrhoeal property of H. incana leaf extract with the 600 mg/kg body weight of the extract being the most effective. In the toxicological evaluation using Wistar rats, the oral administration of the extract did not produce any significant effect on the liver and kidney body weight ratios, RBC, HB, PCV, MCV MCH, MCHC, RCDW, WBC, neutrophils, monocytes and basophils cholesterol, triacylglycerol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol and atherogenic index. The extract also did not affect the levels of sodium, potassium, chloride, inorganic phosphorus, urea, creatinine, total protein, globulin, albumin, total and conjugated bilirubin. The activities of alkaline phosphatase, gamma glutamyl transferase and alanine aminotransaminase in the serum were increased by the extract whereas aspartate aminotransaminase was decreased. The levels of LUC, platelets, lymphocytes and eosinophils were significantly affected at 600 mg/kg body weight. The available evidence in this study suggests that the extract of H. incana leaf is mild, parameter and dose specific. The structure and distribution of foliar appendages on the leaves of this plant were investigated with the JEOL (JSM-6390LV) scanning electron microscope (SEM). Both glandular and non-glandular trichomes were observed. Long stalked glandular trichomes were present on both the abaxial and adaxial surfaces while short stalked glandular trichomes were present only on the adaxial surface. Glandular trichomes were capitate while nonglandular trichomes were stellate with many arms. Energy dispersive X-ray spectroscopyiv SEM showed that Al, Ca, K, Na, Ti and Si were the major constituents of the crystals analyzed from the leaf surfaces. The phytochemical screening of H. incana revealed the presence of bioactive antidiarrhoeal agents such as alkaloids, tannins, saponins, phenolics, triterpenes, cardiac glycosides, flavonoids, cardenolides and dienolides. Two flavonoids, epicatechin and 3, 5, 7, 2’ tetra-hydroxy flavone-3- O--D-glucopyranoside were isolated from the leaves of the plant through bio-active guided fractionation. Both these compounds were screened against diarrhoea causative organisms (Echerichia coli, Shigella flexneri, Bacillus cereus and Staphylococcus aureus) and exhibiting minimum inhibitory concentrations ranging from 12.5 to 100 μg/ml. The findings from this research have generally justified the traditional use of this plant for the treatment of diarrhoea in this province.

Thesis (PhD)--Stellenbosch University, 2014.
ENGLISH ABSTRACT: Concentrating solar power plants are a promising means of generating electricity. However, they are dependent on the sun as a source of energy, and require thermal storage to supply power on demand. At present thermal storage – usually molten salt – although functional, is expensive, and a cheaper solution is desired. It is proposed that sensible heat storage in a packed bed of rock, with air as heat transfer medium, is suitable at temperatures of 500 – 600 °C. To determine if this concept is technically feasible and economically competitive with existing storage, rock properties, packed bed pressure drop and thermal characteristics must be understood. This work addresses these topics. No previously published data is available on thermal cycling resistance of South African rock, and there is limited data from other countries in the proposed temperature range for long-term thermal cycling, so samples were thermally cycled. There is rock which is suitable for thermal storage applications at temperatures of 500 – 600 °C. New maps of South Africa showing where potentially suitable rock is available were produced. Dolerite, found extensively in the Karoo, is particularly suitable. Friction factors were measured for beds of different particles to determine the importance of roughness, shape, and packing arrangement. Five sets of rock were also tested, giving a combined dataset broader than published in any previous study. Limitations of existing correlations are shown. The friction factor is highly dependent on particle shape and, in the case of asymmetric particles, packing method. The friction factor varied by up to 70 % for crushed rock depending on the direction in which it was poured into the test section, probably caused by the orientation of the asymmetric rock relative to the air flow direction. This has not been reported before for rock beds. New isothermal correlations using the volume equivalent particle diameter are given: they are within 15 % of the measurements. This work will allow a techno-economic evaluation of crushed rock beds using more accurate predictions of pumping power than could previously be made. Thermal tests below 80 °C show that bed heat transfer is insensitive to particle shape or type. A heat transfer correlation for air in terms of the volume equivalent diameter was formulated and combined with the E-NTU method. The predicted bed outlet temperatures are within 5 °C of the measurements for tests at 530 °C, showing that the influence of thermal conduction and radiation can be reasonably negligible for a single charge/discharge cycle at mass fluxes around 0.2 kg/m2s. A novel method for finding the optimum particle size and bed length is given: The Biot number is fixed, and the net income (income less bed cost) from a steam cycle supplied by heat from the bed is calculated. A simplified calculation using the method shows that the optimum particle size is approximately 20 mm for bed lengths of 6 – 7 m. Depending on the containment design and cost, the capital cost could be an order of magnitude lower than a nitrate salt system.
AFRIKAANSE OPSOMMING: Gekonsentreerde son-energie kragstasies is n belowende manier om elektrisiteit op te wek, maar hulle is afhanklik van die son as n bron van energie. Om drywing op aanvraag te voorsien moet hulle energie stoor. Tans is termiese stoor – gewoonlik gesmelte sout – hoewel funksioneel, duur, en n goedkoper oplossing word gesoek. Daar word voorgestel dat stoor van voelbare warmte-energie in n gepakte rotsbed met lug as warmteoordrag medium geskik is by temperature van 500 – 600 °C. Om te bepaal of dié konsep tegnies gangbaar en ekonomies mededingend met bestaande stoorstelsels is, moet rotseienskappe, gepakte bed drukval en hitteoordrag verstaan word. Hierdie werk spreek hierdie aspekte aan. Geen voorheen gepubliseerde data is beskikbaar oor die termiese siklus weerstand van Suid-Afrikaanse rots nie, en daar is beperkte data van ander lande in die voorgestelde temperatuurbereik, dus is monsters onderwerp aan termiese siklusse. Daar bestaan rots wat geskik is vir termiese stoor toepassings by temperature van 500 – 600 °C. Nuwe kaarte van Suid-Afrika is opgestel om te wys waar potensieel geskikte rots beskikbaar is. Doleriet, wat wyd in die Karoo voor kom, blyk om veral geskik te wees. Wrywingsfaktore is gemeet vir beddens van verskillende partikels om die belangrikheid van grofheid, vorm en pak-rangskikking te bepaal. Vyf rotsstelle is ook getoets, wat n saamgestelde datastel gee wyer as in enige gepubliseerde studie. Beperkings van bestaande korrelasies word aangetoon. Die wrywingsfaktor is hoogs sensitief vir partikelvorm en, in die geval van asimmetriese partikels, pakkings metode. Die wrywingsfaktor het met tot 70 % gevarieer vir gebreekte rots, afhanklik van die rigting waarin dit in die toetsseksie neergelê is. Dit is waarskynlik veroorsaak deur die oriëntasie van die asimmetriese rots relatief tot die lugvloei rigting, en is nie voorheen vir rotsbeddens gerapporteer nie. Nuwe isotermiese korrelasies wat gebruik maak van die volume-ekwivalente partikel deursnee word gegee: hulle voorspel binne 15 % van die gemete waardes. Hierdie werk sal n tegno-ekonomiese studie van rotsbeddens toelaat wat meer akkurate voorspellings van pompdrywing gebruik as voorheen moontlik was. Termiese toetse onder 80 °C wys dat die warmteoordrag nie baie sensitief is vir partikelvorm en -tipe nie. n Warmte-oordragskorrelasie vir lug in terme van die volume-ekwivalente deursnee is ontwikkel en met die E-NTU-metode gekombineer. Die voorspelde lug uitlaat temperatuur is binne 5 °C van die meting vir toetse by 530 °C. Dit wys dat termiese geleiding en straling redelikerwys buite rekening gelaat kan word vir n enkele laai/ontlaai siklus by massa vloeitempos van omtrent 0.2 kg/m2s. n Oorspronklike metode vir die bepaling van die optimum partikelgrootte en bedlengte word gegee: Die Biot-getal is vas, en die netto inkomste (die inkomste minus die bed omkoste) van n stoomsiklus voorsien met warmte van die bed word bereken. n Vereenvoudigde berekening wat die metode gebruik wys dat die optimum grootte en lengte ongeveer 20 mm en 6-7 m is. Afhangende van die behoueringsontwerp en koste, kan die kapitale koste n orde kleiner wees as dié van n gesmelte nitraatsout stelsel

Resistance of human pathogenic bacterial strains results in selective pressure against known antibiotic. However, plant derived compounds that possess antibacterial potential are currently being investigated for treatment of wound infections in diabetic patients as they are inexpensive and non-toxic. Hence, this dissertation was designed to evaluate two medicinal plants (Brachylaena elliptica and Brachylaena ilicifolia) traditionally used in the treatment of various diseases such as diabetes, and its secondary complications in diabetic patients. The in vitro antioxidant activity of both plants were evaluated using DPPH (1, 1-diphenylhydrazl), ferric reducing power, ABTS (2, 2’-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid), NO (nitric oxide) and H2O2 (hydrogen peroxide) techniques. The antibacterial test and Minimum inhibitory concentration (MIC) was determined by agar dilution method against 5 bacteria strains (Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pyogene, Proteus vulgaris and Proteus mirabilis) infecting wounds in diabetic patients using amoxicillin and ciprofloxacin as positive control. The phytochemical analyses were assessed using standard published methods. Identification of bioactive components in essential oils of both plants were assessed using GCMS. The aqueous and ethanol extracts of both plants were also evaluated to identify bioactive components using LC-MS. The results of the phytochemical analysis revealed the presence of phenols, tannins, flavanoids, flavanols, proanthocyanidins, saponins and alkaloids in both plants. Both plants indicated strong antioxidant activities which might be due to the presence of bioactive compounds. The aqueous and ethanol leaf extracts of both plants demonstrated appreciable broad spectrum activities against these wound pathogens with MIC ranging between 5 and 0.3 mg/ml. The GC-MS analysis of the essential oils of both plants revealed the presence of monoterpenes, oxygenated sesquiterpenes, phenolics and esters. The LC-MS analysis of the aqueous and ethanol leaf extracts of both plants showed that both plants are rich in alkaloids, terpenes, terpenoids, monoterpernoids, and flavanoids. Conclusively, this study has partially justified the ethnomedicinal use of B. elliptica and B.licifolia leaves for the treatment of various diseases, including diabetes and wound infections caused by bacteria in diabetic patients. These may be attributed to the presence of antioxidant compound such as phenols, flavanoids, saponins, tannins, alkaloids and other phytochemical compounds.

The search for cheap, non toxic and readily available antidiabetic drugs has been a challenge for researchers and the pharmaceutical industries. Diabetes mellitus is a metabolic disease characterized by defects in the synthesis of insulin and/or insensitivity to the action of insulin at the target cells. The disease has been on the increase mostly in developing countries where large proportions of the population have little access to good medical care due to either accessibility or non availability of synthetic drugs. This has led to the use of medicinal plants to treat diabetes because it is safe, cheap and with few side effects. There is little scientific evidence on the dosages, active compounds, mechanisms of action and toxicity of these traditionally used plants. Two of the most frequently used plants; Albuca setosa and Albuca bracteata were investigated in this study. The qualitative analysis of different extractions of these plants revealed the presence of phenolics, alkaloids, tannins and saponins. The antioxidant properties of aqueous, acetone and methanollic extracts of Albuca setosa and Albuca bracteata were investigated using models such as Diphenyl-1-Picrylhydrazyl (DPPH), 2, 2’-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), Ferric ion reducing antioxidant potential (FRAP), Nitric Oxide and Hydrogen Peroxide (H2O2). Both plants revealed inhibitions against DPPH in a concentration - dependent manner with Albuca setosa (0.330 mg/ml) showing higher activity than Albuca bracteata (0.647 mg/ml) determined from the IC50. The aqueous extract of Albuca setosa showed a higher inhibition against DPPH radical compared to the Albuca bracteata aqueous extract at all concentrations investigated. The isolated saponins from Albuca bracteata had a higher DPPH scavenging activity than the crude methanolic extract of the plant in a concentration - dependent manner but are significantly different from each other at 0.4, 0.6 and 1.0 mg/ml only. The IC50 of the saponins was also observed to be higher than the crude extracts and standards.The Albuca setosa aqueous extract showed a higher percentage inhibition of ABTS radicals than Albuca bracteata at all the concentrations investigated. Overall, the Albuca setosa aqueous extract (0.0809 mg/ml) showed maximum activity against ABTS radicals. The iron reducing power was significantly higher (P < 0.05) in the methanolic extract of both plants compared to the aqueous counterpart. Overall, the Albuca bracteata aqueous extract (0.344 mg/ml) showed maximum activity as indicated by the IC50. The aqueous extracts of both plants also revealed percentage inhibitions in a concentration - dependent manner against NO2. The aqueous extract of Albuca bracteata bulb was more active against nitric oxide and hydrogen peroxide inhibition. In this study, the cytotoxicity of the extracts was evaluated at a high dose of 100 μg/ml on Chang liver cells and determined using MTT, crystal violet, glucose consumption, lactate production and lactate dehydrogenase release and FRAP. The aqueous extracts of both Albuca setosa and Albuca bracteata were non-toxic on Chang liver cells at the concentrations investigated. The MTT revealed that the aqueous extract of Albuca setosa bulb had the optimum cell viability of 108.09 percent while the acetonic extract of Albuca bracteata showed the least cell viability (37.72 percent) compared with the control. The crystal violet test also revealed the acetone extract of Albuca bracteata to have the least percentage of cell viability at 31.47 percent, while the aqueous extract of Albuca setosa showed the maximum cell viability at 112.5 percent. The aqueous extracts of both plants showed higher percentage cell density on the second day of incubation from the proliferation assay. All the tested samples were observed to consume more glucose than the blank except for the methanollic and acetone extracts of Albuca bracteata bulb. The aqueous and methanolic extracts of Albuca setosa bulbs produced the highest lactate with 120.2 μg/ml and 113.7 μg/ml respectively. The acetone extracts of both Albuca setosa and Albuca bracteata revealed toxicity with a higher lactate dehydrogenase release compared to the control.

Panax ginseng C.A. Mey. (Araliaceae), which has been known in China for more than 4000 years, occupies a particular place among tonic remedies. Pharmacological investigations of the roots have shown that the basic effect of ginseng's action is its capacity to increase the nonspecific resistance of the organism to various untoward influences. In addition to ginseng, another plant of the Araliaceae family is used in a similar manner and is known as Siberian ginseng, Eleutherococcus senticosus (Rupr. et Maxim.) Maxim.). Its roots have been very extensively investigated by Russian scientists. Ginseng is reported to be shorter in duration and weaker in activity when compared to E. semicosus in respect to stimulant and tonic effects. 13 Chinese scientists have claimed that China Produced E. senticosus can exert a definite anti fatigue action. Less extensive studies have been reported on the berries of Schisandra chinensis (Turcz.) Baill. (Magnoliaceae). for its adaptogenic properties. The main objective of the work reported in the following pages was to design and test a simpler and easier animal test model whereby multiple physiologic parameters such as Tn EKG and respiratory rates could be continuously and concurrently monitored. It was desired that the test model could be used repeatedly and rapidly to serve as a screen for all potential adaptogenic plants and their derivatives and extracts.

The etiology of kwashiorkor, a form of severe acute malnutrition in children, may be linked to inflammation and oxidative stress. Biodiversity can contribute health-promoting properties that may address the inflammation and oxidative stress seen in kwashiorkor. Six medicinal plants, five leafy green vegetables (LGV), and two wild fruits were collected from Kaiti Division, Makueni County, Eastern Province, Kenya and examined for antioxidant and anti-inflammatory properties using the oxygen radical absorbance capacity (ORAC) and total phenolics assays and a TNF-α in vitro assay, respectively. All the medicinal plants and several LGV had antioxidant and anti-inflammatory activity. A. dubius, V. unguiculata ( both LGV), O. americanum, and Z. chalybeum (medicinal plants) showed the greatest anti-inflammatory activity among the plants tested and were also widely consumed and used among the children in this study. There was a wide variety of LGV and wild fruits available in the study region, which may have contributed to the high mean food variety score (FVS) of 26 for the non-breastfed children. This study demonstrates a theoretical basis for investigating a link between health-promoting properties of biodiversity, dietary diversity, and the development of kwashiorkor for improved nutrition and health outcomes in children.
L'éthologie de kwashiorkor, une forme de malnutrition severe et aigu chez les enfants, peut-etre lié a l'inflammation et le stress oxydatif. La biodiversité peux contribuer des propriétés qui favorise la santé et qui adresse l'inflammation et le stress oxydatif qui se trouve dans le kwashiorkor. Six plantes medicinal, cinq légumes à feuilles vertes et deux fruits sauvages ont été recueillis par Kaiti Division, Makueni County, Eastern Province, Kenya et examiné pour des propriétés antioxydant et anti-inflammatoire en utilisant les dosages ORAC et des phénols totaux et un dosage TNF- α in vitro, respectivement. Tous les plantes médicinales et plusieurs LGV ont eu de l'activité antioxydant et anti-inflammatoire. A. dubius, V. unguiculata (LGV), O. americanum, et Z. chalybeum (des plantes médicinales) ont montré le plus grand activité anti-inflammatoire de toutes les plantes testées et ont été également largement consommé et utilisé chez les enfants dans cette étude. Il y avait une grande variété de LGV et de fruits sauvages disponibles dans la région étudiée, ce qui peut avoir contribué à des scores élevés moyennes alimentaires divers (FVS) de 26 pour les enfants non allaités au sein. Cette étude démontre une base théorique pour enquêter sur un lien entre promotion de la santé des propriétés de la biodiversité, la diversité alimentaire, et le développement du kwashiorkor pour améliorer la nutrition et la santé chez les enfants.

Thesis MTech (Food Technology))--Cape Peninsula University of Technology, 2017.
Bambara groundnut (Vigna subterranea) an indigenous legume cultivated in Sub-Saharan Africa has been proclaimed to have medicinal properties from communities and in rural areas. However, there is not enough scientific information to validate these claims. Therefore, this study aimed to identify possible medicinal properties of Bambara groundnut (BGN), by analysing the phytochemical and antimicrobial properties of BGN seed and product extracts from Mpumalanga province within South Africa. The BGN extracts (70% methanol, 70% ethanol, milli-Q water) from seeds and products (milk and yoghurt) were screened for the presence of alkaloids, flavonoids, phenols, riboflavin and thiamine using analytical laboratory methods for basic screening, high-performance liquid chromatography (HPLC) and gas chromatography (GC) for quantification. The antimicrobial activity involved direct bioautography and minimum inhibitory concentration (MIC) against six antibiotic-resistant microorganisms, Acinetobacter baumannii ATCC 19606T, Enterococcus faecalis ATCC 29212, Klebsiella pneumoniae subsp. pneumoniae ATCC 700603, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus subsp. aureus ATCC 33591 and Candida albicans ATCC 24433. For the seed extracts, flavonoids and phenols were highly concentrated in the red and brown hulls of BGN compared to whole and dehulled BGN. Organic solvents in comparison to water yielded the highest concentration of flavonoids, whilst water yielded the highest concentration for phenols. Flavonoid compounds that were detected at the highest concentrations were rutin (24.458 ± 0.234 mg.g-1, brown hull extracted with 70% methanol), quercetin (0.070 ± 0.043 mg.g-1, red hull extracted with 70% methanol), kaempferol (0.391 ± 0.161 mg.g-1; brown hull extracted with 70% ethanol) and myricetin (1.800 ± 0.771 mg.g-1; red hull extracted with 70% methanol). For phenol compounds, gallic acid (0.009 ± 0.004 mg.g-1; brown hull extracted with milli-Q water), catechin (0.026 ± 0.041 mg.g-1; brown hull extracted with milli-Q water), methyl gallate (0.008 ± 0.013 mg.g-1; brown whole extracted with milli-Q water), chlorogenic acid (0.115 ± 0.199 mg.g-1; brown hull extracted with milli-Q water) and ellagic acid (0.105 ± 0.082 mg.g-1; red hull extracted with milli-Q water) were detected. Vitamins B1 and B2 (riboflavin and thiamine) were mostly present in milli-Q water extracts. Black-eye hull had the highest concentration of thiamine (vitamin B1) and riboflavin (vitamin B2) consisting of 0.072 mg.g-1 (extracted with milli-Q water) and 0.002 mg.g-1 (extracted with 70% ethanol and 70% methanol). Red and brown hull extracts from organic solvents (70% ethanol and 70% methanol) showed the highest antimicrobial activity, whereas the whole, dehulled and hulls (black-eye and brown-eye) extracts had no antimicrobial activity. As for BGN products extracts, flavonoid compounds that were detected at the highest concentrations were rutin (5.694 mg.g-1, whole BGN milk, milli-Q water), quercetin (0.703 mg.g-1, whole BGN yoghurt, milli-Q water) and myricetin (0.987 mg.g-1, whole BGN yoghurt, 70% ethanol).

CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior
Protium heptaphyllum March (Burseraceae) populary known as âalmÃcegaâ is a popular medicinal plant largely encountered in the Amazon region, various States of Brazil and in several South American Countries. The oily amorphous exudate obtained from this plant is widely used in skin diseases, healing of ulcers, and as an analgesic and anti-inflamatory agent. Phytochemical studies reveled the presence of several monoterpenes and pentacyclic triterpenes such as a mixture of α- e β â amyrin, maniladilol and breine. The present study aimed to investigate the general toxicity and to establish the pharmacological activity of resin and is major triterpenoid mixture, the α and β â amyrin. In toxicity tests, both the resin and triterpene mixture exhibited low toxicity to mice. Resin at doses up 5 g/kg, (p.o.) or 2 g/kg (i.p.) and triterpene mixture up to 3 g/kg, (p.o.) or 2 g/kg (i.p.) failed to induce any mortality in mice. In Artemia-lethality test, the calculated (probit analysis) CL50 values for resin and triterpenes were in the order of 42,54 Â 19,96 and 400 Â 27,85 μg/mL, respectively. In pharmacological tests, the resin was analysed for anti-inflamatory (carrageenan-induced edema, cotton pellet-induced granuloma, and vascular permeability increase induced by i.p. acetic acid) and gastroprotective (absolute ethanol and acidified ethanol) effects, whereas the triterpene mixture was examined in assays that demostrate gastroprotective (against lesions induced by absolute ethanol), antipruritus (against pruritus induced by Dextran T40 and compound 48/80), acute and visceral antinociceptive (test of subplantar and intracolonic capsaicin) and hepatoprotective (against acetaminophen- and Ga1N/LPS-induced models of hepatitis) effects. In anti-inflammatory test, the resin (200 e 400 mg/kg, p.o.) although failed to modify the carrageenan-induced acute rat paw-edema response, it caused signficant inhibitions at a dose of 400mg/kg on the formation of cotton pellet-induced granulomas and on the vascular permeability increase induced by i.p. acetic acid in mice. In addition, the (200 e 400 mg/kg) showed gastroprotective potential against absolute- and acidified ethanol- induced gastric lesions as evidenced from siginificant diminution in lesion scores, restoration of the ethanol-induced depletion of non-protein sulfhydryl content More over, the resin demonstrated an antisecretory effect on gastric acid secretion induced in 4-h pylorus ligated rats. The triterpene mixture also produced similar gastroprotection against ethanol-induced lesions in a manner similar to capsaicin, a pungent principle from hot peppers. This protection possibly involves capsaicin-sencitive primary afferents since it was abolished in mice pretreated with a neurotoxic dose of capsaicin. The α and β â amyrin mixture (100 mg/kg) manifested antipruritus effect as evidenced from suppression of scratching behaviour in the mouse model of prurits induced by s.c. injections of dextran T40 and compound 48/80. Besides, it also produced an antiedematogenic effect in model of hind paw edema induced by histamine, compound 48/80 and dextran T40 and markedly depressed the compound 48/80-elicited rat mast cell degranulation (ex vivo). An antinociceptive effect of triterpenoid mixture (3-100 mg/kg) was observed in capsaicin-evoked somatic (1.6 μg/site, suplantar) and visceral (149 μg, intracolonic) models of nociception in mice. Greater suppression of nociceptive behaviors were evidenced at a dose of 10 mg/kg α and β â amyrin mixture, which mimicked the effect produced by ruthenium red, a non-competitive capsaicin antagonist. The antinociceptive effect of triterpenoid mixture was found to be naloxone (2 mg/kg)- sensitive, suggesting an opioid mechanism. A blockade by triterpene mixture was also evidenced on the hyperthermic but not the hypothermic response of subcutaneously administered capsaicin (10 mg/kg) suggesting possible incolvement of TRPV1 receptor. In open-field and rota-rod tests, the triterpene mixture did not manifest signs of either sedation or motor abnormality in mice that could account for the observed antinociception. In the model of acetaminophen (500 mg/kg)-induced hepatotoxicity, the triterpenoid mixture (50 and 100 mg/kg) effectively reduced the elevated serum AST and ALT levels, restored the depleted GSH and markedly diminished the histopathological alterations. Potentation of pentobarbital-sleeping time was, however observed at these doses of triterpenoid, incidating a probable suppression of cytochrome P450 and thus a diminished metabolite formation that may account for reduced acetaminophen toxicity. The α- and β â amyrin mixture offered complete protection against the mortality associated with Ga1N/LPS , but caused only a moderate diminution of serum enzymes and histopathological alterations. Taken together, these findings show that the resin and α- and β â amyrin mixture possess low toxicity and have a wide therapeutic potential with anti-inflammatory, antinociceptive, antipruritus, and gastro- and hepato-protective actions. Most of the effects of triterpenoid mixture appear to involve in part the participation of primary sensory afferents in their actions.
A espÃcie Protium heptaphyllum (Aubl.) March (Burseraceae) popularmente conhecida como almÃcega, à encontrada na regiÃo AmazÃnica, em vÃrios Estados do Brasil e paÃses da AmÃrica do Sul. Esta espÃcie exsuda uma resina oleosa e amorfa, usada na medicina popular como analgÃsico, cicatrizante e expectorante. Estudos fitoquÃmicos demonstraram a presenÃa de monoterpenos e triterpenos pentacÃclicos, tais como α - amirina e β - amirina, maniladilol e breina. O presente trabalho teve como objetivo investigar os efeitos tÃxicos e farmacolÃgicos da resina e de seus constituintes majoritÃrios, a mistura de triterpenos α e β â amirina. Na avaliaÃÃo dos efeitos tÃxicos observamos a toxicidade aguda destes produtos em camundongos e Artemia sp. Analisando os efeitos sistÃmicos, avaliamos a atividade antiinflamatÃria da resina (edema de pata induzido por carragenina, granuloma induzido por âpelletsâ de algodÃo e permeabilidade vascular induzida por Ãcido acÃtico) e da mistura de α e β â amirina (edema induzido por histamina, serotonina, dextrana T40 e composto 48/80). Examinamos ainda as atividades gastroprotetora e antisecretÃria da resina (lesÃes gÃstricas induzidas pelo etanol absoluto e etanol acidificado e secreÃÃo Ãcida induzida pela ligaÃÃo pilÃrica) e as atividades gastroprotetora (lesÃes gÃstricas induzidas pelo etanol absoluto, com animais dessensibilizados por capsaicina), antipruriginosa (prurido induzido pelo dextrana T40 e composto 448/80 e desgranulaÃÃo de mastÃcitos ex vivo) antinociceptiva (nocicepÃÃo induzida pela administraÃÃo subplantar e intracolÃnica de capsaicina, resposta hipotÃrmica induzida por capsaicina) e hepatoprotetora (lesÃes hepÃticas induzidas por acetaminofeno e Ga1N/LPS) da mistura de α e β â amirinas. NÃo foi possÃvel estabelecer as DL50 da resina (atà 5 g/kg, v.o. e 1 g/kg, i.p.) e da mistura de α e β â amirina (atà 3 g/kg, v.o. e atà 2 g/kg, i.p.) em camundongos. A mistura de α e β â amirina, mas nÃo a resina, mostrou toxicidade para Artemisa sp, sendo as CL50 de 42,54  19,96 e 400  27,85 μg/mL, respectivamente. Nos modelos de permeabilidade vascular induzido por Ãcido acÃtico (camundongo) e granuloma induzido por âpelletâ de algodÃo (ratos), a resina demonstrou efeito antiinflamatÃrio significativo na dose de 400mg/kg, reduzindo a permeabilidade vascular e o peso seco do granuloma. Contudo, a reina nÃo apresentou atividade sobre edema induzido por carragenina (ratos). Adicionalmente, a resina preveniu as lesÃes gÃstricas induzidas por etanol absoluto e etanol acidificado, alÃm de impedir a depleÃÃo dos grupos sulfidrilas produzida pelo etanol absoluto nas doses de 200 e 400 mg/kg. Um efeito antisecretÃrio da resina (200 e 400mg/kg) foi observado no modelo de secreÃÃo Ãcida induzida pela ligaÃÃo pilÃrica em ratos. A mistura de α e β â amirina tambÃm exibiu atividade gastroprotetora inibindo as lesÃes gÃstricas por etanol absoluto, cujo mecanismo parece envolver os neurÃnios sensoriais primÃrios sensÃveis à capsaicina. A administraÃÃo oral dos triterpenos α e β â amirina (100 mg/kg), apresentou atividade antiedematogÃnica, nos modelos de edema de pata induzidos por histamina, composto 48/80 e dextrana T40, mas nÃo sobre o edema induzido por serotonina. A atividade antipruriginosa tambÃm foi observada com as α e β â amirina nas doses variando de 50 a 200 mg/kg, em modelos de prurido induzido por dextrana T40 e pelo composto 48/80 e na reduÃÃo (100 mg/kg) da degranulaÃÃo de mastÃcitos peritoneais ex vivo pelo composto 48/80. O efeito antinociceptivo da mistura, nas doses de 3 a 100 mg/kg, foi verificado atravÃs da inibiÃÃo dos comportamentos de nocicepÃÃo induzidos pela administraÃÃo subplantar ou intracolÃnica de capsaicina em camundongos. A antinocicepÃÃo produzida por estes triterpenos (10 mg/kg) sobre o tempo de lambedura induzido pela capsaicina (1,6 μg/20 μL) nÃo foi potencializada nem revestida pelo vermelho de rutÃnio (1,5 mg/kg), mas foi significativamente inibida pela naloxona (2 mg/kg), sugerindo mecanismo opiÃide. A participaÃÃo dos receptores α2 - adrenÃrgicos neste efeito tambÃm foi eliminada, tendo em vista que a ioimbina nÃo reverteu o efeito antinociceptivo das amirinas no modelo de nocicepÃÃo visceral induzida pela capsaicina. Estes triterpenos bloquearam ainda a hipertermia induzida pela capsaicina (10 mg/kg), mas nÃo reverteram a resposta hipotÃrmica induzida por este agente, sugerindo a participaÃÃo do receptor vanilÃide (TRPV1) no efeito antinociceptivo das amirinas. Nos modelos de hepatoxidade, a mistura de α e β â amirina (50 e 100 mg/kg) reduziu o aumento dos nÃveis sÃricos de ALT e AST e restabeleceu os nÃveis de GSH hepÃticos, diminuindo as alteraÃÃes histopatolÃgicas induzidas pelo acetaminofeno (500 mg/kg), alÃm de potencializar o tempo de sono induzido por pentobarbital sÃdico (50 mg/kg), indicando que este efeito hepatoprotetor envolve a inibiÃÃo do citocromo P â 450. A mistura ofereceu ainda completa proteÃÃo contra a mortalidade induzida por Ga1N/LPS, reduzindo as lesÃes hepÃticas em camundongos e reduzindo os nÃveis sÃricos de ALT, mas nÃo de AST ou GSH hepÃticos, sugerindo um possÃvel feito neuroimunomodulatÃrio neste modelo. Os triterpenos α e β â amirina nas doses variando de 3 a 30 mg/kg, nÃo manifestam efeitos sedativos ou incoordenaÃÃo motora em camundongos. A resina e mistura de α e β â amirina possuem baixa toxicidade e atividades antiinflamatÃria e gastroprotetora. Os triterpenos α e β â amirina exibiram atividade antipruriginosa, antinociceptiva e hepatoprotetora, cujos efeitos envolvem, pelo menos em parte, a participaÃÃo dos neurÃnios aferentes sensoriais primÃrios.

Magister Scientiae (Medical Bioscience) - MSc(MBS)
Even though Tulbaghia violacea has been used to treat and manage epilepsy in South Africa by traditional medicine practitioners, no evidence in any literature has shown any scientific scrutiny of the effectiveness of the plant species in therapy. This project was intended, therefore, to investigate the anticonvulsant effect of the leaf methanol extract of Tulbaghia violacea by studying its effect against tonic convulsion induced by either pentylenetetrazole (PTZ), bicuculline, picrotoxin, strychnine or N-methyl-DL-aspartic acid (NMDLA) in mice. Qualitative phytochemical analysis, acute toxicity and HPLC studies were also carried out on the plant species. The doses of 200 (mg/kg, i.p.) and 400 (mg/kg, i.p.) of the leaf methanol extract of T. Violacae significantly delayed the onset of PTZ (100 mg/kg, i.p.)-induced tonic convulsion in a dose dependent manner. Leaf methanol extract of the plant species (200 mg/kg, i.p.) did not affect the incidence of PTZ (100 mg/kg, i.p.)-induced tonic convulsion while 400 mg/kg (i.p.) protected only one mouse against the tonic convulsion. Leaf methanol extract of Tulbaghia violacea (100mg/kg, i.p.) did not significantly affect the onset or incidence of PTZ (100 mg/kg, i.p.)- induce tonic convulsion. Phenobarbitone (12 mg/kg, i.p.), diazepam (0.5 mg/kg, i.p.) and muscimol (2mg/kg, i.p.) significantly delayed the onset of PTZ (100 mg/kg, i.p.)-induced tonic convulsion and also significantly reduced the number of animals convulsing. Muscimol (0.2 mg/kg, i.p.) did not significantly affect the onset or incidence of PTZ (100 mg/kg, i.p.)-induced tonic convulsion. However, combined therapy of sub effective doses of the leaf methanol extract of T. Violacea (100 mg/kg, i.p.) and muscimol (0.2 mg/kg, i.p.) significantly delayed the onset of PTZ (100mg/kg, i.p.)-induced tonic convulsion and but did not significantly reduce the number of animals convulsing. The combined therapy of sub effective doses of the leaf methanol extract of T. violacea (100 mg/kg, i.p.) and muscimol (0.2 mg/kg, i.p.) protected two of the mice against the tonic convulsion. Leaf methanol extract of Tulbaghia violacea (100-400 mg/kg, i.p.) significantly and dose dependently delayed the onset of tonic convulsion produced by bicuculline (30 mg/kg, i.p.), picrotoxin (20 mg/kg, i.p.) or NMDLA (400 mg/kg, i.p.)-induced tonic convulsion but did not affect the incidence of any of the convulsions. Phenobarbitone (12 mg/kg, i.p.), diazepam (0.5 mg/kg, i.p.) or muscimol (2 mg/kg, i.p.) significantly delayed the onset of bicuculline (30 mg/kg, i.p.) or picrotoxin (20 mg/kg, i.p.)-induced tonic convulsion and also significantly reduced the number of animals convulsing. Phenobarbitone (12 mg/kg, i.p.) or diazepam (0.5 mg/kg, i.p.) did affect significantly affect the onset or incidence of NMDLA (400 mg/kg, i.p.)-induced tonic convulsion. LY233053 (5 mg/kg, i.p.) significantly delayed the onset of tonic convulsion produced by NMDLA (400 mg/kg, i.p.) and also significantly reduced the number of animals convulsing. Leaf methanol extract of Tulbaghia violacea (200 and 400 mg/kg, i.p.) significantly delayed the onset of strychnine (2 mg/kg, i.p.)-induced tonic convulsion but did not significantly affect the number of mice convulsing. The dose of 100 mg/kg (i.p.) of leaf methanol extract of T. violacea did not significantly affect the onset or incidence of strychnine (2 mg/kg, i.p.)-induced tonic convulsion. Phenobarbitone (12 mg/kg, i.p.) significantly delayed the onset of strychnine (2 mg/kg, i.p.)-induced tonic convulsion and also significantly reduced the number of animals convulsing. Diazepam (0.5 mg/kg, i.p.) did not significantly delay the onset of strychnine (2 mg/kg, i.p.)-induced tonic convulsion and also did not significantly affect the number of mice convulsing. Phenytoin (30 mg/kg, i.p.) or DMSO (0.25 ml, i.p.) did not significantly affect the onset or incidence of bicuculline (30 mg/kg, i.p.), picrotoxin, strychnine or NMDLA-induced tonic convulsion. The qualitative phytochemical analysis of the plant species showed the presence of alkaloids, saponins, cardiac glycosides, flavonoids, triterpene steroids, quinones and tannins. The LD50 value obtained following oral administration of the leaf methanol extract of Tulbaghia violacea may be greater than 4000 mg/kg. The HPLC fingerprint of the leaf methanol extract of Tulbaghia violacea showed distinct peaks at the following retention times, 2.911, 3.269, 4.010, 7.597, and 15.122 min. The results obtained in this study indicate that the leaf methanol extract of Tulbaghia violacea has anticonvulsant activity. The results obtained also indicate that GABA, glutamic acid and glycine mechanisms may probably be involved in the anticonvulsant activity of the plant extract. The relatively high LD50 obtained for the plant species, given orally, indicate that it is safe in mice.

Thesis (MScMedSc)--University of Stellenbosch, 2011.
ENGLISH ABSTRACT: Introduction: Athrixia phylicoides is an aromatic, indigenous shrub with high antioxidant content and numerous indigenous medicinal properties inferred by ingestion of an herbal brew of the plant. Commercialization of “bush tea” (derived from A. phylicoides) holds economic and developmental potential for indigenous communities provided the safety and efficacy of the herbal tea is established. Recently A. phylicoides has been shown by McGaw et al. (2007) to have similar antioxidant activity to Rooibos tea, and a unique, new flavonol (i.e. a polyphenolic antioxidant plant metabolite) 5-hydroxy-6,7,8,3′,4′,5′-hexamethoxyflavon-3-ol, unique to A. phylicoides, was isolated by Mashimbye et al. in 2006. With changes in the socio-economic climate and a new trend in merging Western lifestyle with traditional practices, new interest has been shown in herbal/natural remedies. Study Aim: The aim of this study was to firstly, determine the in vitro effect of A. phylicoides aqueous extract on glucose metabolism in cell lines that mimic the three key organs implicated in glucose homeostasis. Secondly, the study aimed to determine the potential ex vivo antioxidant and anti-inflammatory effect of the extract in pancreatic β-cells and peripheral mononuclear cells respectively. Methods: Leaves and fine twigs of A. phylicoides were processed into an aqueous extract. C2C12, Chang and 3T3-L1 cells were cultured under standard conditions and acutely exposed to increasing concentrations of extract and water vehicle, as well as 1 μM insulin and metformin as positive controls. Glucose uptake from 8 mM glucose culture media was determined using a fluorimetric oxidase method. Radioactive 14C-glucose oxidation to 14CO2 and determination of glycogen content of cells were used to assess the fate of intracellular glucose. RT-PCR was used to assess the extract effect on insulin-signalling gene expression. The antioxidative effect of A. phylicoides extract in pancreatic β-cells isolated from Wistar rats was determined by measuring nitric oxide (NO) production in response to hyperglycemic conditions. NO was labelled with diaminofluorocein diacetate and fluorescence was measured using flow cytometry. Insulin secretion of pancreatic β- cells was measured using radio-immuno assay. The anti-oxidative effect of the extract in lipopolysaccharide-stimulated peripheral mononuclear cells isolated from Wistar rats was determined by measuring the production of TNF-α using an ELISA kit. Results: C2C12 myocytes showed maximal increased glucose uptake at the 0.05 μg/μl extract concentration (228.3% ± 66.2, p<0.001). In Chang cells, A. phylicoides extract maximally increased the amount of glucose taken up at the 0.05 μg/μl concentration (134.5% ± 2.5, p<0.05). In 3T3-L1 cells, the extract maximally increased the amount of glucose taken up at the 0.025 μg/μl concentration (143.5% ± 10.3, p<0.001). An extract-induced increase in insulin receptor and glucose transporter four expression was seen in C2C12 myocytes. The oxidation of 14C-glucose to 14CO2 by C2C12 myocytes was maximally increased following acute exposure to the extract at 0.1 μg/μl (2919.3 fmol/1x10^6 cells ± 428, p<0.01). The oxidation of 14C-glucose to 14CO2 by Chang cells was maximally increased following acute exposure to extract at 0.1 μg/μl (4476.7 fmol/1x10^6 cells ± 1620, p<0.05); as seen in the C2C12 cells. A. phylicoides extract increased glycogen storage at all three concentrations tested in Chang cells, but maximally at the 0.025 μg/μl concentration (13.6 μg/1x10^6 cells ± 0.7, p<0.05). A. phylicoides extract did not have any measurable effect on the oxidative status of β-cells or the anti-inflammatory status of peripheral mononuclear cells. The extract did show an increase in first phase insulin secretion of β-cells in hyperglycemic conditions, although it was not significant. Conclusion: Athrixia phylicoides aqueous extract stimulates in vitro glucose uptake and metabolism in an insulin-mimetic manner, suggesting that this extract could potentially be beneficial to type two diabetics as an adjunct therapy.
AFRIKAANSE OPSOMMING: Inleiding: Athrixia phylicoides is 'n aromatiese, inheemse struik met 'n hoë antioksidant inhoud. Vele tradisionele medisinale eienskappe is gekoppel aan die ingestie van 'n kruie brousel van die plant, wat ook bekend as “bostee” is. Kommersialisering van “bostee” hou ekonomiese en ontwikkelings potensiaal in vir inheemse gemeenskappe mits die veiligheid en effektiwiteit van die kruietee bevestig kan word. McGaw et al. (2007) het onlangs bevind dat A. phylicoides se antioksidant aktiwiteit vergelykbaar is met die van rooibostee. 'n Unieke nuwe flavonol ('n polifenoliese antioksidant plant metaboliet) 5-hydroksie-6,7,8,3′,4′,5′-hexamethoksieflavon-3-ol, eie aan A. phylicoides, is deur Mashimbye et al. in 2006 geïsoleer. Met veranderings in die sosio-ekonomiese klimaat en 'n nuwe tendens om die westerse lewenstyl met tradisionele gebruike aan te vul word nuwe belangstelling in kruie/natuurlike rate ondervind. Studie Doelwitte: Die doelwitte van hierdie studie was eerstens om die in vitro effek van A. phylicoides waterekstrak op die glukosemetabolisme van drie sellyne wat die sleutel organe naboots wat glukosehomeostase beheer, te bepaal. Tweedens, is die potensiële ex vivo antioksidant en anti-inflammatoriese effek van die ekstrak op pankreatiese β-selle en perifere mononuklêere-selle onderskeidelik ondersoek. Metodes: n Waterige ekstrak is van die blare en fyn takkies van A. phylicoides berei. C2C12, Chang and 3T3-L1 selle is gekultuur onder standaard kondisies en akuut blootgestel aan stygende ekstrakkonsentrasies. Water het as kontrole gedien, met 1 μM insulien en metformien as positiewe kontroles. Glukose opname vanuit 8 mM glukose kultuurmedia is bepaal deur 'n fluorimetriese oksidase metode. Radioaktiewe 14C-glukose-oksidasie na 14CO2 en die bepaling van die glukogeen inhoud van selle is gebruik om die lot van intrasellulêre glukose te bepaal. RT-PKR is gebruik om die effek van die ekstrak op die insulien-seinpad geen-uitdrukking te ondersoek. Die antioksidant effek van A. phylicoides ekstrak in pankreatiese β-selle geïsoleer van Wistar rotte, is bepaal deur stikstofoksied (NO) produksie na aanleiding van hiperglukemiese kondisies. NO is met diaminofluorosien diasetaat gemerk en die fluoresensie gemeet deur vloeisitometrie. Insulien afskeiding deur die pankreatiese β-selle is deur radio-immuno metode bepaal. Die anti-oksidatiewe effek van die ekstrak op lipopolisakkaried-gestimuleerde perifere mononuklêere-selle afkomstig van Wistar rotte is bepaal deur die meting van TNF-α produksie met 'n ELISA kit. Resultate: C2C12 miosiete het 'n maksimale toename in glukoseopname by 'n 0.05 μg/μl ekstrakkonsentrasie (228.3% ± 66.2, p<0.001) gehad. Dieselfde ekstrakkonsentrasie het maksimale toename in glukoseopname in Chang selle (134.5% ± 2.5, p<0.05 getoon. In 3T3-L1 selle is maksimale toename in die glukoseopname by 'n konsentrasie van 0.025 μg/μl (143.5% ± 10.3, p<0.001) bereik. 'n Ekstrak-geinduseerde verhoging in die insulienreseptor en glukosetransporter vier ekspressie is in C2C12 miosiete waargeneem. Die oksidasie van 14C-glukose na 14CO2 deur C2C12 miosiete is maksimaal verhoog deur akute blootstelling aan die ekstrak by 'n konsentrasie van 0.1 μg/μl (2919.3 fmol/1x10^6 cells ± 428, p<0.01). Die oksidasie van 14C-glukose na 14CO2 deur Chang selle was maksimaal verhoog deur akute blootstelling aan die ekstrak by 'n konsentrasie van 0.1 μg/μl (4476.7 fmol/1x10^6 cells ± 1620, p<0.05) soos gevind in die C2C12 selle. Die ekstrak het glukogeenstoring verhoog teen al drie die konsentrasies waarteen getoets is in Chang selle, maar 'n maksimale effek is gevind by 'n konsentrasie van 0.025 (13.6 μg/1x10^6 cells ± 0.7, p<0.05). A. phylicoides ekstrak het nie 'n meetbare effek op die oksidatiewe status van β-selle of die anti-inflammatoriese status van perifere mononuklêere-selle gehad nie. Die ekstrak het wel 'n verhoging in die eerstefase insuliensekresie van β-selle in hyperglukemiese kondisies gehad, alhoewel die verhoging nie statisties betekenisvol was nie. Afleiding: Athrixia phylicoides waterekstrak stimuleer in vitro glukoseopname en metabolisme in 'n insulin-mimetiese manier, wat beteken dat die ekstrak potensiëel voordele vir tipe twee diabete kan inhou as aanvullingsterapie.

Thesis (M.Sc.(Soil Science)) -- University of Limpopo, 2015
Winery solid waste materials namely, wine filter materials (FM), grape marc (berry stalks, skins and seeds) and chopped grapevine pruning canes were composted in heaps through a thermophilic process. The filter materials were mixed with the grape marc and grapevine prunings at five rates (10%, 25%, 50%, 75% and 100%) to produce five composts herein designated as C10FM, C25FM, C50FM, C75FM and C100FM, respectively. A laboratory incubation study was thereafter carried out to determine the nutrient release potential of the composts using two soil types with varying textural characteristics. Each compost was mixed with soil at a rate equivalent to 200 kg N ha-1 and the mineral N, available P and exchangeable K content determined over 42 days incubation period. Results revealed that the composts possess high C content and low C:N ratios; and released significantly higher NH4-N and K concentration relative to un-amended control. The differences in the amount of P mineralised among the five compost treatments were not significant while significantly higher amount of K was mineralised at higher FM mix rates. The composts were applied to maize cv. SNK2147 on sandy soil in a greenhouse pot study at five rates (5, 10, 20, 40 and 80 t ha-1) to determine their effects on crop growth and yield as well as on selected soil chemical properties. An un-fertilised control and NPK fertiliser treatments were included for comparison. The pots were arranged in a completely randomized design, with each treatment replicated four times. The C50FM, C75FM and C100FM treatments applied at 80 t ha-1 gave significantly higher maize dry matter yield than the NPK fertiliser treatment. Quantitative estimates of the optimum compost rate for dry matter production ranged from 450 to 1842 g pot-1. Application of these composts significantly increased dry matter yield, plant height, stem diameter and the number of functional leaves per plant compared to the un-fertilised control. The K content of shoot from composts treatments exceeded the critical nutritional level of 3.3%. Plant tissue Zn content from C10FM, C25FM and C50FM treatments exceeded the critical nutritional level of 15 mg kg-1 while the residual soil K, Na and Zn contents after crop harvest were significantly increased following compost application. Similarly, the residual P was significantly increased in C25FM, C75FM and C100FM treatments after harvest. In conclusion, application of these composts exerted beneficial effects on maize performance and soil. Field studies under variable conditions are recommended to validate these findings. Keywords: wine, compost, nutrient release potential, maize, soil chemical properties