Academic literature on the topic 'Alkaloidal extracts'
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Journal articles on the topic "Alkaloidal extracts"
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Opletal, Lubomír, Miroslav Ločárek, Adéla Fraňková, et al. "Antimicrobial Activity of Extracts and Isoquinoline Alkaloids of Selected Papaveraceae Plants." Natural Product Communications 9, no. 12 (2014): 1934578X1400901. http://dx.doi.org/10.1177/1934578x1400901211.
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Alkaloidal extracts of seven selected plants of the family Papaveraceae were studied with respect to their activity against six strains of pathogenic bacteria and their alkaloidal fingerprint. Twenty-four alkaloids were determined by GC/MS, and twenty of them identified from their mass spectra, retention times and retention indexes. In the antibacterial assay, three Gram-positive ( Enterorococcus faecalis, Staphylococcus aureus and S. hyicus), and three Gram-negative ( Escherichia coli, Proteus mirabilis and Pseudomonas aeruginosa) strains were used. The most promising antimicrobial activity was shown by the alkaloidal extract of Macleaya cordata with MIC values of 16 μg/mL for Staphylococcus aureus, 32 μg/mL for Enterococcus faecalis and 64 μg/mL for Staphylococcus hyicus and Escherichia coli. All the tested pure isoquinoline alkaloids were considered inactive within the tested concentrations.
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Cruz-Chacón, Iván De la, Alma Rosa González-Esquinca, Patricia Guevara Fefer, and Luis Felipe Jímenez Garcia. "Liriodenine, Early Antimicrobial Defence in Annona diversifolia." Zeitschrift für Naturforschung C 66, no. 7-8 (2011): 377–84. http://dx.doi.org/10.1515/znc-2011-7-809.
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Annonaceae aporphine alkaloids, of which liriodenine is the most abundant, have not been extensively studied from a biological standpoint. The goal of this study was to investigate the role of liriodenine in antimicrobial defense during early developmental stages in Annona diversifolia. The fungi Rhizopus stolonifer and Aspergillus glaucus, which are responsible for seed deterioration, were isolated during imbibition, and their antifungal activity was determined by diffusion, macrodilution, and metabolic inhibition assays using purified liriodenine and alkaloid extracts obtained from embryos, radicles, and roots at early developmental stages. The presence of liriodenine in extracts was quantified by high-performance liquid chromatography. Purified liriodenine and alkaloidal extracts inhibited both fungi, and there was a positive relationship between extract activity and amount of liriodenine contained therein. The quantity of liriodenine present in extracts suggests its importance in controlling other phytopathogens.
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El-Shazly, A., A. M. Ateya, L. Witte, and M. Wink. "Quinolizidine Alkaloid Profiles of Retama raetam, R. sphaerocarpa and R. monosperma." Zeitschrift für Naturforschung C 51, no. 5-6 (1996): 301–8. http://dx.doi.org/10.1515/znc-1996-5-607.
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Abstract About 28 quinolizidine alkaloids and the dipiperidine alkaloids am modendrine, dehydroammodendrine and N -formylammodendrine were identified in the alkaloidal extracts of Retama raetam, Retama sphaerocarpa and Retama monosperma by capillary GLC and GLCMS. Alkaloid profiles of the three Retama species with a Mediterranean distribution are more similar than alkaloid patterns of different organs of the same plant. Whereas sparteine and retamine are the major components of stems, lupanine, retam ine, N-methylcytisine and cytisine dominate in flowers and pods, and cytisine in seeds indicating a high degree of organ specificity of alkaloid storage.
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Bakr, Riham O., Mohammed F. El-Behairy, Ahmed M. Elissawy, Hanan Elimam, and Marwa A. A. Fayed. "New Adenosine Derivatives from Aizoon canariense L.: In Vitro Anticholinesterase, Antimicrobial, and Cytotoxic Evaluation of Its Extracts." Molecules 26, no. 5 (2021): 1198. http://dx.doi.org/10.3390/molecules26051198.
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Aizoaceae is a large succulent family characterized by many psychoactive species. Aizoon canariense L., a wild neglected plant traditionally used in gastrointestinal ailments, has been the subject of a limited number of phytochemical and biological studies. Therefore, herein, we investigated the in vitro cytotoxic, antimicrobial, and anticholinesteraseactivity of the aerial parts of A. canariense L. and analyzed the phytochemical compositions of the lipoidal and alkaloidal fractions. Petroleum ether extract showed the presence of behenic and tricosylic acid, while an in-depth investigation of the alkaloidal fraction revealed the identification of new adenine based alkaloids (1–5), which were isolated and identified for the first time from Aizoon canariense L. Their structures were elucidated based on extensive spectroscopic analyses. The alkaloidal extract showed a powerful cytotoxic effect (IC50 14–28 μg/mL), with the best effect against colon carcinoma, followed by liver and breast carcinomas. The alkaloidal extract also had a potent effect against Candida albicans and Escherichia coli, with minimum inhibitory concentrations (MIC) values of 312.5 and 625 µg/mL. The in vitro anticholinesterase activity was potent, with IC50 < 200 ng/mL for the tested extracts compared with 27.29 ± 0.49 ng/mL for tacrine.
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Ločárek, Miroslav, Jitka Nováková, Pavel Klouček, et al. "Antifungal and Antibacterial Activity of Extracts and Alkaloids of Selected Amaryllidaceae Species." Natural Product Communications 10, no. 9 (2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000912.
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Alkaloidal extracts of six selected species of Amaryllidaceae were studied with respect to their antibacterial and anti-yeast activity and their alkaloidal fingerprint. Twenty-five alkaloids were determined by GC/MS, and sixteen of them identified from their mass spectra, retention times and retention indexes. In the antimicrobial assay, Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus were used, along with isolates of the human pathogenic yeasts Candida albicans, C. glabrata, C. dubliniensis and Lodderomyces elongiosporus. The six extracts, together with 19 Amaryllidaceae alkaloids isolated in our laboratory, showed almost no inhibitory activity against the bacteria tested. However, promising anti-yeast properties were detected; the most potent activity was shown by lycorine, which inhibited C. dubliniensis with a MIC of 32 μg/mL, C. albicans and L. elongiosporus, both with MICs of 64 μg/mL, followed by caranine inhibiting C. dubliniensis with a MIC of 128 μg/mL. Among the alkaloidal extracts, Narcissus jonquilla cv. Baby Moon showed the most potent anti-yeast activity, with minimal and average MIC values of 128 and 192 μg/mL, respectively, followed by Leucojum aestivum, Narcissus poeticus var. recurvus and N. canaliculatus (average MICs 256, 267 and 299 μg/mL, respectively). The lowest MIC value among extracts was obtained for N. canaliculatus against L. elongiosporus (MIC 64 μg/mL).
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Yang, Zhong Duo, Jin Ren, and Zong Mei Shu. "Monoamine Oxidase Inhibitory Activity of the Total Alkaloid and Organic Acid from Chinese Herbal Medicines." Advanced Materials Research 781-784 (September 2013): 899–902. http://dx.doi.org/10.4028/www.scientific.net/amr.781-784.899.
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The aim of this study was to search for potential monoamine oxidase (MAO) inhibitors from Chinese herbal medicine. The organic acid extracts of 34 and the total alkaloidal extracts of 30 traditional Chinese medicines were tested for their MAO inhibitory activities. The results showed that the organic acid extracts of Liquidambar formosana, Pharbitis nil, Punica granatum and alkaloid extracts of Coptis chinensis exhibited the most potent inhibition on MAO and their concentration that inhibited 50% of MAO activity (IC50) values less than 10 μg/mL.
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El-Shazly, Assem, Abdel-Monem M. Ateya, and Michael Wink. "Quinolizidine Alkaloid Profiles of Lupinus varius orientalis, L. albus albus, L. hartwegii, and L. densiflorus." Zeitschrift für Naturforschung C 56, no. 1-2 (2001): 21–30. http://dx.doi.org/10.1515/znc-2001-1-204.
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Abstract Alkaloid profiles of two Lupinus species growing naturally in Egypt (L. albus albus [synonym L. term is], L. varius orientalis) in addition to two New World species (L. hartwegii, L. densiflorus) which were cultivated in Egypt were studied by capillary GLC and GLC-mass spectrometry with respect to quinolizidine alkaloids. Altogether 44 quinolizidine, bipiperidyl and proto-indole alkaloids were identified; 29 in L. albus, 13 in L. varius orientalis, 15 in L. hartwegii, 6 in L. densiflorus. Some of these alkaloids were identified for the first time in these plants. The alkaloidal patterns of various plant organs (leaves, flowers, stems, roots, pods and seeds) are documented. Screening for antimicrobial activity of these plant extracts demonstrated substantial activity against Candida albicans, A spergillus flavus and Bacillus subtilis.
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Bonagiri Sreedevi, Vijaya Kuchana, and Shobharani S. "Comparative evaluation of anti-diabetic action and pancreatic histopathology of rats treated with two alkaloidal plant extracts." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (2020): 1841–46. http://dx.doi.org/10.26452/ijrps.v11ispl4.4387.
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This study aimed to understand Strychnosnuxvomica and Holarrhena pubescens Stem bark extract action towards M3 receptor in controlling blood glucose levels. Strychnos nux vomica and Holarrhena pubescens are both alkaloidal drugs can help in controlling Hyperglycemic level. This will be useful in the formulation of a new herbal drug molecule for treating diabetes. Chloroform and ethanolic extracts of selected alkaloidal plants were extracted using the soxhlet apparatus and obtained quotes were tested for acute toxicity studies and carried out anti-diabetic action on Wister albino rats for 21 days. Results obtained from Blood glucose levels and histopathological study of test groups are compared with blood glucose levels of standard group, and highly significant action was identified by the chloroform extract of Strychnos nux vomica and Holarrhena pubescens group. Moderate anti-diabetic action was observed remaining two groups of ethanolic extracts. Strychnos nux vomica and Holarrhena pubescens ethanolic extract groups are acting on M3 receptors and controlling Hyperglycemic levels.
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Gacemi, Safia, Khedidja Benarous, Santiago Imperial, and Mohamed Yousfi. "Lepidine B & E as New Target Inhibitors from Lepidium Sativum Seeds Against Four Enzymes of the Pathogen Candida albicans: In Vitro and In Silico Studies." Endocrine, Metabolic & Immune Disorders - Drug Targets 20, no. 1 (2020): 127–38. http://dx.doi.org/10.2174/1871530319666190415141520.
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Background and Objective: The present paper aims to study the inhibition of Candida albicans growth as candidiasis treatment, using seeds of Lepidium sativum as source. Methods: In vitro assays were carried out on the antifungal activity of three kinds of extracts from L. sativum seeds against four strains of C. albicans, then testing the same phytochemicals on the inhibition of Lipase (LCR). A new in silico study was achieved using molecular docking, with Autodock vina program, to find binding affinity of two important and major lepidine alkaloids (lepidine E and B) towards the four enzymes secreted by C. albicans as target drugs, responsible of vitality and virulence of this yeast cells: Lipase, Serine/threonine phosphatase, Phosphomannose isomerase and Sterol 14-alpha demethylase (CYP51). Results: The results of the microdillution assay show that the hexanic and alkaloidal extracts have an antifungal activity with MICs: 2.25 mg/ml and 4.5mg/ml, respectively. However, Candida rugosa lipase assay gives a remarkable IC50 values for the hexanic extract (1.42± 0.04 mg/ml) followed by 1.7± 0.1 and 2.29 ± 0.09 mg/ml of ethyl acetate and alkaloidal extracts respectively. The molecular docking confirms a significant correlation between C. albicans growth and inhibition of crucial enzymes involved in the invasion mechanism and cellular metabolisms, for the first time there were an interesting and new positive results on binding modes of lepidine E and B on the four studied enzymes. Conclusion: Through this work, we propose Lepidine B & E as potent antifungal drugs.
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Sarikaya, Buket Bozkurt, Strahil Berkov, Jaume Bastida, Gulen Irem Kaya, Mustafa Ali Onur, and Nehir Unver Somer. "GC-MS Investigation of Amaryllidaceae Alkaloids in Galanthus xvalentinei nothosubsp. subplicatus." Natural Product Communications 8, no. 3 (2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800312.
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A GC-MS analysis of alkaloids in the aerial parts and bulbs of Galanthus x valentinei nothosubsp. subplicatus was performed for the first time. Totally, twenty-six alkaloids were identified, of which tazettine and galanthindole were the major ones. Acetylcholinesterase inhibitory activity of the alkaloidal extracts was determined using modified in vitro Ellman's method. Significant anticholinesterase activity was observed in the tested samples (bulbs: IC50 = 21.3 μg/mL, aerial parts: IC50 = 16.3 μg/mL).
Dissertations / Theses on the topic "Alkaloidal extracts"
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Wilkinson, Celeste T. "Quantitative Analysis of Tobacco-Specific Nitrosamines and their Precursor Alkaloids in Tobacco Extracts." VCU Scholars Compass, 2017. https://scholarscompass.vcu.edu/etd/5172.
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Tobacco-specific nitrosamines (TSNA) are carcinogenic constituents derived from alkaloids in tobacco. Researchers are actively exploring several avenues to reduce TSNA levels in tobacco products like moist snuff tobacco. The focus of the research presented within is the quantitative analysis of TSNA in tobacco, specifically N’-nitrosonornicotine (NNN), 4-(methylnitrosamino)-1(3-pyridyl)-1-butanone (NNK), N’-nitrosoanatabine (NAT), and N’-nitrosoanabasine (NAB).
Tobacco alkaloids and nitrosamines in tobacco are currently analyzed by different instrumentation due to orders of magnitude difference in their concentrations, chromatographic separation challenges due to structural similarities, and similar mass fragmentation patterns. An analytical column using silica and 1,2-bis(siloxy)ethane hybrid particles of 1.7 µm size is the foundation of a chromatographic separation of NNN, NNK, NAT, NAB, nicotine, nornicotine, anatabine, and anabasine. This is the first rapid and robust quantitative method for the TSNA and their alkaloid precursors using high pH mobile phase conditions with ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). The suitability of the method is demonstrated by its application to the analysis of reference tobacco materials for cigarettes and moist snuff. In addition, a novel TSNA analytical method was developed using TSNA-specific molecularly imprinted polymers (MIP) as the selective extraction element from tobacco extract. The affinity mechanisms between MIP and TSNA were found to have extensive cross-reactivity to structurally similar alkaloids present in tobacco extract. TSNA-specific MIP was demonstrated to have stronger retention for the alkaloids than for the TSNA substrate. The MIP-TSNA interaction was optimized to create the first analytical method to quantify underivatized NNN and NNK from tobacco extracts by HPLC-UV.
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Saidin, Nor Aini. "Cytotoxicity of extract of Malaysian Mitragyna speciosa Korth and its dominant alkaloid mitragynine." Thesis, Imperial College London, 2008. http://hdl.handle.net/10044/1/4263.
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Mitragyna speciosa Korth (Kratom), a herb of the Rubiaceae family is indigenous in southeast Asia mainly in Malaysia and Thailand. It is used as an opium substitute and has been increasingly abused by drug addicts in Malaysia. Recently, the potent analgesic effect of plant extract and its dominant alkaloid mitragynine (MIT) were confirmed in vivo and in vitro. MIT acted primarily on μ- and δ-opioid receptors, suggesting that MIT or similar compounds could be promising alternatives for future pain management treatments. However the potential cytotoxicity of this plant is unknown. Therefore, the cytotoxicity of methanol-chloroform extract (MSE) and MIT on human cell lines (HepG2, HEK 293, MCL-5, cHol and SH-SY5Y cells) has been examined. MSE appeared to exhibit dose-dependant inhibition of cell proliferation in all cell lines examined, at concentration > 100 μg/ml with substantial cell death at 1000 μg/ml. SH-SY5Y was the most sensitive cell line examined. MIT showed a similar response. Clonogenicity assay was performed to assess the longer-term effects of MSE and MIT. The colony forming ability of HEK 293 and SH-SY5Y cells was inhibited in a dose-dependant manner. Involvement of metabolism in cytotoxicity was further assessed by clonogenicity assay using rat liver S9 (induced by Arochlor 1254); toxicity increased 10-fold in both cell lines. To determine if cytotoxicity was accompanied by DNA damage, the Mouse lymphoma tk gene mutation assay was used. The results were negative for both MSE and MIT. Studies on the involvement of metabolism in cytotoxicity of MSE and MIT were performed using MCL-5 and it appeared that CYP 2E1 is involved in activation of cytotoxicity. Studies with opioid antagonists were performed using SH-SY5Y cells treated with MSE and MIT. Naloxone (μ and δ receptor antagonists), naltrindole (δ receptor antagonist) and cyprodime hydrobromide (μ receptor antagonist) confirmed that MSE cytotoxicity was associated with μ and δ receptor while MIT mainly acted on μ receptor. Studies on mechanism of MSE and MIT cytotoxicity showed that cell death observed at high dose was preceded by cell cycle arrest, however MSE cell arrest was independent of p53 and p21 while MIT showed opposite result. Studies have been undertaken to examine the nature of this cell death. Morphological examinations showed that cell death induced by MSE was cell type dependant, in which SH-SY5Y cells appeared to die via apoptosis-like cell death while HEK 293 and MCL-5 cells predominantly via necrosis. Biochemical assessments confirmed that MSE induced cell death independent of p53 or caspases pathway while MIT cell death appeared to be associated with p53 and caspases pathway. The involvement of reactive oxygen species (ROS) generation in MSE and MIT mediating cell death was performed using SH-SY5Y cells. The results appeared negative for both MSE and MIT treated cells. Collectively, the findings of these studies suggest that MSE and its dominant alkaloid MIT produced cytotoxicity effects at high dose. Thus, the consumption of Mitragyna speciosa Korth leaves may pose harmful effects to users if taken at high dose and the evidence for involvement of CYP 2E1 in increasing the MSE cytotoxicity suggests that caution may be required if the leaves are to be taken with CYP 2E1 inducers.
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Chow, Yit Lai. "Caenorhabditis elegans as a whole organism screening system for isoquinoline alkaloid bioactivities." 京都大学 (Kyoto University), 2014. http://hdl.handle.net/2433/188834.
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Jia, Yang. "INTERACTION OF ISOFLAVONES AND ENDOPHYTE-INFECTED TALL FESCUE SEED EXTRACT ON VASOACTIVITY OF BOVINE MESENTERIC VASCULATURE." UKnowledge, 2014. http://uknowledge.uky.edu/animalsci_etds/41.
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Endophyte-infected tall fescue produces many ergot alkaloids, which have been shown to be vasoconstrictive in various vessel types of bovine. On the other hand, substantial evidence has been reported on the vasodilative effects of formononetin and biochanin A in different vessel types in humans and rats. So, a study was conducted using mesenteric vasculature collected from heifers shortly after slaughter. After 2-h incubation with formononetin (F), biochanin A (B), or an ergovaline-containing tall fescue seed extract (EXT) and their combinations, vessels were mounted in a multi-myograph to determine their ergotamine-induced contractility. Results indicated that F and B at 1 × 10-6 M and their combination did not impact the contractile response to ergotamine in mesenteric vasculature. The pre-myograph incubation of mesenteric vasculature with EXT altered the contractile response manner to ergotamine. However, at higher concentration, F and B may alleviate the reduction of vasoconstriction caused by prior exposure to EXT. To our knowledge, this study was the first to investigate the interaction of ergot alkaloids and isoflavones on in vitro bovine mesenteric vasculature. However, further investigations are necessary to understand the mechanism behind the interaction of ergot alkaloids and isoflavones on vasoactivity.
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Abubakar, Ibrahim Babangida. "In vitro investigation on synergistic anticancer effects between vitamin E isomers, pure compounds and crude alkaloid plant extracts on human cancerous cells." Thesis, University of Nottingham, 2017. http://eprints.nottingham.ac.uk/35974/.
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Anticancer chemotherapeutic treatment using single dose has been limited due to drug resistance and potential metabolic degradation. For instance, high-dose tocotrienols undergo metabolic degradation that limits the availability of therapeutic dose thereby limiting the potency in vivo. Combined treatment of tocotrienols at low dosage has been suggested as alternative to circumventing this limitation. This study was designed to investigate the cytotoxic effects and subsequently the apoptotic mechanisms of individual doses and combined treatments at lower dosages of tocotrienols (delta and gamma), jerantinines (A and B) and extracts (ethanol and alkaloid crude) from leaves and bark of Ficus hispida, Ficus fistulosa and Ficus schwarzii on lung (A549), brain (U87MG) and colon (HT-29) cancer cell lines. Neutral red uptake assay was conducted to evaluate the antiproliferative effect of individual and combined treatments. Staining techniques (histochemical and fluorescence), COMET assay flow cytometric analysis and immunofluorescence were conducted to evaluate cell morphology, DNA damage, cell cycle arrest pattern and antimicrotubule effects. Finally cell and molecular based assays were conducted to investigate the pathways for induction of apoptosis. Cell viability study revealed that alkaloid crude extracts of leaves and bark of F. fistulosa demonstrated the highest potency with IC50 range of 0.96 – 46.81 µg/ml compared to F. schwarzii (8.79 – 107.9 µg/ml) and F. hispida (15.14 – 49.58 µg/ml) on A549, U87MG and HT-29 cells. Both delta- and gamma-tocotrienols induced antiproliferative effects on A549, U87MG and HT-29 cells with IC50 values of 3.12 - 12.40 µg/ml and 3.17 – 16.36 µg/ml, respectively. Potent antiproliferative effects were also evident for jerantinine A (IC50 0.62 – 1.74 µg/ml), jerantinine B (IC50 0.58 – 1.48 µg/ml) and vinblastine (IC50 0.03 – 0.71 µg/ml). However, similar toxic effects on these three compounds were also evident on non-cancerous lung fibroblast (MRC5) cells. The leaf and bark alkaloid crude extracts of F. fistulosa and F. schwarzii were selected for combined treatments. The combined treatment of IC20 doses of F. fistulosa with both delta- and gamma-tocotrienols induced synergistic antiproliferative effects (combination index (CI) < 1) on U87MG and HT-29 with up to 34.7-fold and 4-fold dose reductions for tocotrienols and F. fistulosa extracts, respectively. In contrast, additive (CI = 0.98) or antagonistic effects (CI > 1) were observed for IC20 doses of F. schwarzii extracts combined with delta- and gamma-tocotrienols on HT-29 cells. On the other hand, combined treatments of tocotrienols (delta and gamma) with IC20 doses of jerantinines (A and B) induced synergistic effects (CI < 1) on A549, U87MG and HT-29 cells causing up to 4.48-fold dose reduction of tocotrienols thus reducing toxicity towards MRC5 cells compared to cancer cells. Further morphological and DNA damage assessment focusing on tocotrienols (delta and gamma), jerantinines (A and B) and combined low-dose treatments revealed anticancer features including cell shrinkage, nuclear chromatin condensation and fragmentation, membrane blebbing, apoptotic bodies and induction of predominantly double stranded DNA breaks. Cell cycle analysis demonstrated the induction of G0/G1 and G2/M cell cycle arrests by tocotrienols (delta and gamma) and jerantinines (A and B), respectively on U87MG, A549 and HT-29 cells. Meanwhile, G2/M (A549) and G0/G1 (U87MG and HT-29) cell cycle arrests were evident for combined low-dose treatments of tocotrienols (delta and gamma) with IC20 doses of jerantinines (A and B). Jerantinines A and B and combined low-dose treatments with tocotrienols (delta and gamma) caused disruption of microtubule networks and induction of caspase 8-, 9- and 3-mediated apoptosis with caspase-independent growth inhibition evidenced in the presence of caspase inhibitors on U87MG, A549 and HT-29 cells. In contrast, although treatments of tocotrienols (delta and gamma) alone caused similar apoptotic features as those of combined, disruption of microtubule networks were not characterized on these three cancer cell lines. Further mechanistic study on U87MG cells revealed that the apoptosis triggered by individual doses of tocotrienols (delta and gamma) involved the activation of TRAIL and Bid as well as the release of cytochrome C, thus confirming the recruitment of the death receptor and mitochondria-mediated pathways. On the other hand, individual doses of jerantinines (A and B) and combined low-dose treatments with tocotrienols resulted in the activation of TRAIL, FAS, p53 and Bid, as well as the release of cytochrome C. The activation of both death receptors, p53 and microtubule disruption by combined low-dose treatments demonstrates an improved mechanism of action comparing to individual doses of tocotrienols and jerantinines. In addition, the combined low-dose treatments also caused a reduction of required potent doses thereby minimizing the toxicity of jerantinines (A and B) towards the non-cancerous MRC5 cells. In conclusion, this research has presented valuable combined treatment candidates which are warranted for further investigations as future chemotherapeutic agents against cancers.
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Nascimento, Viviane do. "Caracterização eletroforética e espectrométrica de extratos de Cinchona de uso fitoterápico e cosmético." Universidade de São Paulo, 2010. http://www.teses.usp.br/teses/disponiveis/46/46133/tde-26042010-100610/.
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A cada ano a malária mata cerca de um milhão de pessoas. Segundo a OMS, 3,3 bilhões de pessoas, metade da população mundial, estão expostas à doença, principalmente em países subdesenvolvidos. Os fármacos utilizados no tratamento da malária incluem: cloroquina, primaquina, quinina, mefloquina, doxiclina, clindamicina e artemisina. A extensa resistência do parasita Plasmodium falciparum ao medicamento sintético cloroquina re-estabeleceu a quinina, um alcalóide encontrado na planta do gênero Cinchona, como droga antimalarial. A quinidina, o diastereoisômero da quinina, é usada como droga antiarrítmica e no tratamento de fibrilação arterial. Os estereoisômeros, cinchonina e cinchonidina, não são usados como medicamentos, embora mostrem efeitos similares àqueles da quinina e da quinidina. Os efeitos cardíacos da quinidina impossibilita seu uso como antimalarial. Outro alcalóide presente na espécie Cinchona é a hidroquinidina, que assim como a quinidina também apresenta atividade antiarrítmica. Os extratos vegetais são base para a produção de fitoterápicos, porém sem padronização o produto perde qualidade e a indústria não pode garantir a eficácia apregoada já que desconhece a concentração do princípio ativo no produto à venda. A portaria RDC 48/04 de 16.03.04 da Agência Nacional de Vigilância Sanitária (ANVISA) estabeleceu uma legislação específica, que se baseia na “garantia da qualidade”, exigindo a reprodutibilidade dos fitoterápicos produzidos, que só pode ser garantida com a utilização de extratos padronizados. De acordo com essa tendência, o objetivo do presente trabalho é o desenvolvimento de métodos de análise para os principais alcalóides da Cinchona por eletroforese capilar, podendo ser usada em caracterização de drogas vegetais, no controle de qualidade de extratos, bem como em possíveis adulterações. As determinações dos cinco principais alcalóides da Cinchona foram realizadas por eletroforese capilar de zona (CZE), utilizando como eletrólito TEA (1,1% v/v) com pH ajustado para 2,5 com ácido fosfórico e 20 mmol L-1 de α-ciclodextrina, com tempo total de análise inferior a 12 minutos. A otimização das condições de análise foi realizada através da realização de experimentos de planejamento fatorial 32+1, sendo as variáveis do estudo a concentração de TEA e de α-ciclodextrina. Com o uso de seletores quirais também foi desenvolvido um método para análise confirmatória dos alcalóides através do acoplamento de eletroforese capilar à espectrometria de massas, utilizando a estratégia de “partial filling”. Com objetivo de verificar o efeito do solvente na separação dos presentes alcalóides foi realizado um estudo do mecanismo de separação modulada por solvente em meio micelar (MEKC) e em meio não-aquoso (NACE).<br>Every year, malaria kills about one million people. According to OMS, 3.3 billion people, half of the world population, are exposed to the disease, mostly in underdeveloped countries. The pharmaceuticals used in the treatment of malaria include: chloroquine, primaquine, quinine, mefloquine, doxyclyne, clindamicina and artemisin. The increased resistance of the parasite Plasmodium falciparum to the synthetic pharmaceutical chloroquine reestablished quinine, an alkaloid found in the genus Cinchona, as antimalarial drug. Quinidine, the diasteroisomer of quinine, is used as antiarrhythmic drug in the treatment of arterial fibrillation. The diastereoisomers cinchonine and cinchonidine are not employed as pharmaceuticals although present similar effects to quinine and quinidine. The cardiac effects of quinidine hinders its use as antimalarial. Another alkaloid found in Cinchona is hydroquinidine, which similarly to quinidine also presents antiarrhythmic activity. Herbal extracts are the basis of phytotherapic production, however, with no standardization, the product lacks quality and the industry cannot guarantee its alleged efficacy, since there is no knowledge of the active principle concentration in the product put to sale. The ANVISA protocol (RDC 48/04 published on March16, 2004) established a specific legislation based on the “guarantee of quality”, which demands the reprodutibility of the produced phytotherapic, only achievable with standardized extracts. Following this tendency, the aim of this work was to develop methods of analysis for the main alkaloids of Cinchona using capillary electrophoresis, to apply in the characterization of herbal drugs, in the quality control of extracts as well as in the searching of possible adulterations. The determinations of five main alkaloids of Cinchona were carried out by capillary zone electrophoresis (CZE) using an electrolyte composed of 1.1% (v,v) TEA adjusted to pH 2.5 with phosphoric acid containing 20 mmol L-1 α-cyclodextrin, providing a less than 12 min total analysis time. The optimization of analytical conditions was conducted experimentally by a 32+1 factorial design where the studied variables were TEA and α-cyclodextrin concentrations. With the use of chiral selectors a confirmatory analytical method for alkaloids was also developed with the coupling of capillary electrophoresis and mass spectrometry employing a strategy called “partial filling”. With the purpose of verifying solvent effects on the separation of the alkaloids under investigation, studies of the separation mechanism as modulated by solvent in micelar medium (MEKC), and non aqueous medium (NACE) were conducted.
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Denny, Carina. "Atividade anticancer de extratos e principios ativos obtidos de Virola sebifera (Myristicaceae)." [s.n.], 2006. http://repositorio.unicamp.br/jspui/handle/REPOSIP/289321.
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Previous issue date: 2006<br>Resumo: Modelos de avaliação da citotoxicidade têm proporcionado a obtenção de importantes dados preliminares, ajudando a selecionar extratos de plantas com propriedade antitumoral para estudos futuros. Como parte de um programa de screening de plantas medicinais brasileiras e produtos naturais com propriedades anticâncer, o presente trabalho apresenta a atividade da Virola sebifera (Myristicaceae), uma árvore endêmica do Cerrado brasileiro. O objetivo geral desse trabalho foi avaliar as propriedades in vitro e in vivo de amostras da V. sebifera. além de isolar e identificar seus compostos ativos. O primeiro estudo descreve a atividade antiproliferativa em cultura de células tumorais humanas de duas lignanas e dois policetídeos isolados das folhas da V. sebifera. Assim, reportamos o isolamento e elucidação estrutural de um novo policetídeo 3,5-diidro-2-(l'-oxo-3'-hexadecenil)-2-ciclohexano-l-ona com alta atividade antiproliferativa contra 8 linhagens de células tumorais humanas. No segundo estudo, purificamos a fração ativa (FR4) a partir do extrato bruto diclorometânico, com atividade in vitro (IC50- 5,19-10,57 (xg/mL - ensaio do SRB) pãrã âs mesmas linhagens celulares. Pãrã ãvãliãr ã atividade in vivo da fração ativa utilizamos o ensaio da hollow fiber. Assim, foram estabelecidas as condições de crescimento para as linhagens celulares MCF-7, NCI-ADR e OVCAR03 em fibras (hollow fibers) implantadas no abdômen (i.p.) e no dorso (s.c.) de camundongos imunocompetentes. Os animais foram tratados com FR4 (500mg/kg), doxorubicina (6mg/kg) ou veículo intraperitonealmente. Após 14 dias de tratamento, as fibras foram retiradas, seguindo-se a coloração do MTT para determinação da densidade de células viáveis. A fração FR4 demonstrou efeito significante contra células de mama (MCF-7) e ovário (OVCAR03). A confirmação das propriedades anticâncer in vitro e in vivo da Virola sebifera apresentadas nesse estudo, nos permite avançar em pesquisas futuras, orientando a seleção de outros modelos e estudos de mecanismo de ação<br>Abstract: Cytotoxicity screening models provide important preliminary data to help select plant extracts with potential antitumor properties for future work. As part of a screen program searching for Brazilian medicinal plants and natural products with anticancer properties, the present investigation reports the anticancer activity the Virola sebifera (Myristicaceae), an endemic tree from the Brazilian Cerrado. The overall aim of this work was the evaluation of in vitro and in vivo properties of samples from V. sebifera, there for the isolation and identification of the active compounds. The first study describes the antiproliferative properties against human cell lines of two lignans and two polyketides isolated from leaves of V. sebifera. Herein we report the isolation and structure elucidation of a novel polyketide 3,5-dihydro-2-(r-oxo-3J-hexadecenyl)-2-cyclohexen-l-one with high antiproliferative activity against 8 human cancer cell lines. In the second study, we purified the active fraction (FR4) from the crude dichloromethanic extract with in vitro activity (IC5ri=5.19 - 10.57 pg/mL - SRB assay) against the same cell lines. In addition, the hollow fiber assay was used to study the effect in vivo of the active fraction (FR4). Using this model, we have established growth conditions for MCF-7, NCI-ADR and OVCAR03 cells implanted at the intraperitoneal (i.p.) and subcutaneous (s.c.) compartments of immunocompetent mice. Then, the animals were treated with FR4 (500 mg/kg). doxorubicin (6mg/kg) or vehicle only intraperitoneally. After 14 days the fibers were retrieved, followed by determination of living cell density by MTT staining. FR4 showed significant effect against breast (MCF-7) and ovarian (OVCAR03) tumor cells. The anticancer properties of Virola sebifera in vitro and in vivo was confirmed in this study. These findings may guide future studies in other models and detailed studies on the mechanisms of action<br>Doutorado<br>Farmacologia, Anestesiologia e Terapeutica<br>Doutor em Odontologia
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Merlugo, Liara. "Análise cromatográfica, constituição química em alcaloides e avaliação do potencial hipotensor de extratos vegetais obtidos de espécies de Erythrina." Universidade Federal do Pampa, 2015. http://dspace.unipampa.edu.br:8080/xmlui/handle/riu/282.
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Previous issue date: 2015-03-12<br>O gênero Erythrina está presente mundialmente nas regiões tropicais e subtropicais. Estudos fitoquímicos utilizando vários órgãos dessas plantas, demostraram a presença de alcaloides, flavonoides, pterocarpanos e triterpenóides. Várias espécies são encontradas no Brasil, dentre elas Erythrina falcata e Erythrina crista-galli, conhecidas popularmente como “corticeira” e utilizadas medicinalmente devido à ação sedativa, ansiolítica, anti-inflamatória e antihipertensiva. Este trabalho objetivou estudar a composição química de extratos vegetais obtidos de folhas de E. falcata e E. crista-galli e ainda, avaliar o potencial hipotensor in vivo de extratos de E. falcata. Inicialmente, após coleta do material, as folhas foram selecionadas, submetidas à secagem e trituradas. Então, foram submetidas à extração por maceração exaustiva utilizando etanol 40% (v/v) e por infusão utilizando água a 100 °C. Para a caracterização em termos de fenólicos totais e conteúdo de flavonoides, os extratos foram quantificados por espectrofotometria. Para o ensaio cromatográfico, os extratos foram analisados por CLAE em sistema de fase reversa, com fase móvel consistindo de acetonitrila:água em eluição por gradiente e fluxo de 1,0 mL/min. Para a análise por CLUEESI- MS, a fase móvel foi composta de mistura de acetonitrila:metanol (4:1) e ácido fórmico pH 3,0, com eluição por gradiente e fluxo de 0,2 mL/min. A detecção por espectrometria de massas foi conduzida a partir das seguintes condições: N2 como nebulizante; energia de colição 4.0 eV; temperatura da fonte do eletrospray e do gás de solvatação 100°C e 120°C, respectivamente; voltagem do capilar 3000V; voltagem do cone 40V. Os espectros de massas foram obtidos na faixa de m/z 200-800. A avaliação dos efeitos hemodinâmicos foi realizadaem ratos wistar normotensos, anestesiados com uretana (1,4 mg/Kg), via canulação da artéria carótida (para a verificação da PAS, PAD e FC) e veia jugular (para administração do extratose drogas). A avaliação do potencial hipotensor da E. falcata foi investigada através da realização de uma curva crescente de administração dos extratos e os possíveis mecanismos de ação envolvidos foram analisados através da administração de diferentes drogas sendo elas: L-NAME (30 mg/kg); losartana (10 mg/Kg); hexametônio (20mg/Kg) e propranolol (5mg/kg). Os teores de fenólicos totais para E. falcata e E. crista-galli estiveram na faixa de 1,3193 – 1,4989 mgEAG/mL para os extratos obtidos por maceração e de 0,8771 – 0,9506 mgEAG/mL para as infusões. Em flavonoides totais, os conteúdos estiveram na faixa de 7,7829 – 8,1976 ER mg/g para os extratos obtidos por maceração e 9,3471 – 10,4765 ER mg/g para as infusões. Na determinação por CLUE-MS, os dados de íon molecular e fragmentos de massa indicaram a composição predominante em alcaloides, sugerindo-se os componentes erythristemine, 11β-methoxyglucoerysodine, erysothiopine, 11β- hydroxyerysodine–glicose e 11-hydroxyerysotinone-ramnosídeo. O extrato aquoso da E. falcata mostrou-se um potente hipotensor dose-dependente, causando uma queda na PAS de 23 a 35% e na PAD de 32 a 49% para ambos os extratos estudados, sem influenciar a FC, podendo este efeito estar relacionado com a via dos receptores β-adrenérgicos.<br>The genus Erythrina is present worldwide in tropical and subtropical regions. Phytochemical studies using various organs of these plants demonstrated the presence of alkaloids, flavonoids, pterocarpans and triterpenoids. Several species are found in Brazil, among them Erythrina falcata and Erythrina crista-galli, which are popularly known as “corticeira” and. used medicinally due to it action as sedative, anxiolytic, anti-inflammatory and antihypertensive. The present study aimed to investigate the chemical composition of extracts obtained from leaves of E. falcata and E. crista-galli, and still, to evaluate the hypotensive potential in vivo of E. falcata extracts. Initially, after collection of material plant, the leaves were selected, submitted to dryness and powdered. Then, submitted to extration by exhaustive maceration using ethanol 40% (v/v) and by infusion using water at 100 °C. For characterization in terms of phenolics and flavonoid content, the extracts were quantified by spectrophotometry. For chromatographic assay, the extracts were analysed by HPLC in reversed phase system, with a mobile phase consisting of acetonitrile:water in gradient elution and flow rate of 1.0 mL/min. For analysis by UPLC-ESI-MS, the mobile phase consisted in a mixture of acetonitrile:methanol (4:1) and 0.1% formic acid pH 3.0, with a elution by gradient and flow rate of 0.2 mL/min. The MS detection was performed following the conditions: N2
as nebulizing; collision energy 4.0 eV; temperature of electrospray source and desolvation gas 100°C and 120°C, respectively; capillary voltage 3000V; sample cone 40V. Mass spectra were recorded in the range of m/z 200-800. The evaluation of the hemodynamic effects was performed in normotensive Wistar rats, anesthetized with urethane (1.4 mg/kg) by cannulation of the carotid artery (for verification of SBP, DBP and HR) and jugular vein (for administration of the extracts and drugs). The hypotensive potential of E. falcata was investigated by conducting a growing curve administration of the extracts and the possible mechanisms involved were analyzed by administering different drugs such as: L-NAME (30 mg/kg); losartan (10 mg/kg); hexamethonium (20 mg/kg) and propranolol (5 mg/kg). The total phenolics content for E. falcata and E. crista-galli was from 1.3193 to 1.4989 mgGAE/mL for maceration and 0.8771 to 0.9506 mgGAE/mL for infusions. In total flavonoid, the content was from 7.7829 to 8.1976 mg RE/g for maceration and 9.3471 to 10.4765 RE mg/g for infusions. The molecular ions and mass fragments obtained by UPLCMS indicated the predominant composition in alkaloids, suggesting the components erythristemine, 11β-methoxyglucoerysodine, erysothiopine, 11β-hydroxyerysodine-glucose and 11-hydroxyerysotinone-rhamnoside. The aqueous extract of E. falcata showed to be a potent dose-dependent hypotensive, decreasing the SBP in 23 to 35% and DBP in 32 to 49% for both extracts, without influence in HR, and this effect may be due to the route of β- adrenergic receptors.
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Yamaguchi, Klenicy Kazumy de Lima. "Estudos biológicos dos extratos e composição química dos óleos essenciais de espécies da família Lauraceae." Universidade Federal do Amazonas, 2011. http://tede.ufam.edu.br/handle/tede/3338.
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Previous issue date: 2011-08-02<br>Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>The family Lauraceae is one of the most important families in the Amazon rainforest featuring an significant number of species with different uses due to the quality of products natural.The species this family are Chemically characterized by the presence of alkaloids, neolignans, flavonoids, terpenes and phenylpropanoids. This study contributes to the analysis of the chemical profile of the three genera Endlicheria, Ocotea and Rhodostemonodaphne about directing the investigations on the chemical composition of extracts and essential oils, contributing to the screening of promising genera and species. This work was carried out prospecting phytochemical , alkaloid profile analysis by thin layer chromatography (TLC) and mass spectrometry of the ethanol extracts, identification of the essential oil and analysis of activities: anticholinesterase, antioxidant and cytotoxic of ethanolic extracts of E. citriodora, E. sericea, O. minor, O. ceanothifolia, O. leucoxylon, R. recurva and R. crenaticupula. The species were collected in Reserva Ducke, in Manaus. The material was separated to obtain essential oils and ethanolic extracts. These were analyzed for chemical / biological activities and subjected to acid-base partition to obtain enriched fractions of alkaloids. The alkaloid profile was analyzed by mass spectrometry and TLC with revealing specific. The essential oils were analyzed by GC-FID and GC-MS. It was confirmed the high presence of alkaloids in the genus Ocotea and low in species Endlicheria and Rhodostemonodaphne. In mass spectrometry the peaks m/z 300 and 330 were present in most fractions and may correspond to the type alkaloids Benzylisoquinolines and Aporphines. The yields of essential oils obtained by hydrodistillation in Clevenger modified ranged from 0.02% to 4.29%. The specie Endlicheria citriodora was the highest yield, 2.5% in the branches and 4.3% in the leaves. The Methyl geranate was the major constituent, (above 93%), elucidated by GC-FID, GC-MS RMN1H and RMN 13C. The essential oils from other species showed less than 1% yield and caryophyllene and its oxide were the major constituents. The antioxidant activity was assessed by sequestering ability of the stable radical 2,2-diphenyl-1-picrylhydrazyl (DPPH ), using quercetin as external standard, expressed as effective concentration values (EC50). The extracts of Ocotea minor presented the best antioxidant potential (EC50 = 7.31 ± 0.32 μg / mL). Qualitative analysis of anticholinesterase activity was performed according to the method of Ellman (modified), with negative results for inhibiting the enzyme acetylcholinesterase. The branches of the three species of Ocotea were positive. The antitumor activity was evaluated against four cell lines (leukemia, breast, colon and glioblastoma) by the method of Mossman. None of the extracts tested showed pronounced cytotoxic activity.<br>A família Lauraceae é uma das famílias mais importantes na floresta amazônica apresentando um número expressivo de espécies com diversas utilizações devido a qualidade dos seus produtos naturais. Quimicamente as espécies desta família caracterizam-se pela presença de alcalóides, neolignanas, flavonóides, terpenos e fenilpropanóides. Este estudo contribui para a análise do perfil químico dos três gêneros Endlicheria, Ocotea e Rhodostemonodaphne através da varredura dos extratos brutos auxiliando no direcionamento das investigações químicas sobre a composição dos extratos e óleos essenciais, contribuindo para a triagem de gêneros e das espécies promissoras. Neste trabalho foi realizado prospecção fitoquímica, análise do perfil alcaloídico por cromatografia em camada delgada (CCD) e espectrometria de massa (EM) dos extratos etanólicos, identificação dos constituintes do óleo essencial e verificação das atividades anticolinesterásica, antioxidante e citotóxica dos extratos etanólicos das espécies E. citriodora, E. sericea, O. minor, O. ceanothifolia, O. leucoxylon, R. recurva e R. crenaticupula. As espécies foram coletadas na Reserva Ducke, em Manaus e separadas para obtenção de óleos essenciais e extratos etanólicos. Estes foram analisados quanto as atividades química/biológicas e submetidos a partições ácido-base para obtenção de frações enriquecidas de alcalóides. O perfil alcaloídico foi analisado por CCD utilizando reveladores específicos e por EM. Os óleos essenciais foram analisados por CG-DIC e CG-EM. Confirmou-se que a pronunciada presença de alcalóides no gênero Ocotea e em baixas concentrações nas espécies de Endlicheria e Rhodostemonodaphne. Na espectrometria de massa os picos m/z de 300 e 330 estiveram presentes na maioria das frações e podem corresponder a alcalóides do tipo benzilisoquinolínicos e aporfínicos. Os rendimentos dos óleos essenciais obtidos por hidrodestilação em clevenger modificado variaram de 0,02% a 4,29%, sendo Endlicheria citriodora a espécie que apresentou maior rendimento, 2,5% nos galhos e 4,3% nas folhas, tendo como constituinte majoritário, o geranato de metila (acima de 93%), elucidado por CG-DIC, CG-EM, RMN1H e RMN 13C. Os óleos essenciais das outras espécies apresentaram rendimento inferior a 1% e como constituinte majoritário o cariofileno e seu óxido. A atividade antioxidante foi avaliada através da capacidade seqüestrante do radical estável 2,2-difenil-1-picrilhidrazil (DPPH ), utilizando quercetina como padrão externo, expressos como valores de concentração eficiente (CE50).Os extratos de Ocotea minor foram os que apresentaram maior potencial antioxidante (CE50=7,31 ± 0,32 μg/mL). A análise qualitativa da atividade anticolinesterase foi realizada de acordo com o método de Ellman (modificado), com resultados negativos para inibição da enzima acetilcolinesterase. Os galhos das três espécies de Ocotea apresentaram resultado positivo. A atividade antitumoral foi avaliada contra quatro linhagens de células (leucemia, mama, cólon e glioblastoma) segundo o método de Mossman.Nenhum dos extratos testados apresentou atividade citotóxica pronunciada.
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Montrucchio, Deise Prehs. "Avaliação da atividade antinociceptiva do extrato e do alcaloide s-(+)-dicentrina extraído de frutos de Ocotea puberula (lauraceae)." Universidade Federal de Santa Maria, 2012. http://repositorio.ufsm.br/handle/1/3840.
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Ocotea puberula (Lauraceae) is a brazilian native tree, known in the South regions as canela guaicá or canela amarela. Its phytochemical composition includes several alkaloids of aporphinic type, some of them with biological activities already reported. Fruits collected in
Curitiba, state of Paraná, were submitted to extraction and fractioning processes, allowing the isolation of an alkaloid identified as dicentrine, present as the majoritarian substance. In the present work we investigated the antinociceptive potential of the organic fractions
obtained from O. puberula fruits extract and dicentrine (DCTN) isolated from the chloroform fraction (CF). Both CF and DCTN, given by oral route, were able to reduce the nociception induced by formalin and acetic acid with similar ID50, suggesting that the CF effect is due to
the presence of DCTN. Hexanic (HF) or ethyl acetate (EAF) fractions had no antinociceptive effect. DCTN also presented antinociceptive effects in chronic models such as inflammatory (induced by intraplantar injection of Freund s complete adjuvant) and neuropathic (induced by partial sciatic nerve ligation), being able to reduce mechanical and cold hypersensitivity,with no changes in the response to heat. When evaluated against the thermo-receptors
activation, DCTN administered either systemically (by oral route) or locally (by intraplantar route) reduced the nociception induced by cinnamaldehyde, a TRPA1 activator, but did not alter the response induced by capsaicin, a TRPV1 activator. The antinociceptive effect of DCTN was not affected by the pretreatment with antagonists of opioid, adrenergic or cannabinoid receptors, and neither by the pretreatment with an inhibitor of serotonin synthesis, suggesting that these descending mechanisms of pain control are not involved in the DCTN mechanism of action. On the other hand, DCTN was able to prevent the hypersensitivity induced by cAMP/PKA pathway activators, forskolin and PGE2, and it also reduced PKA activation, demonstrated by western blotting analysis, suggesting that DCTN may act by interaction with this signaling pathway. On the other hand, DCTN presented few or none action on the hypersensitivity induced by bradikinin or PMA, respectively, suggesting
that the PLC/PKC pathway is not involved in DCTN antinociceptive action. Additionally, DCTN did not cause any sedative effect, neither alterations on motor activity or body temperature, and although daily treatment caused a slight increase in liver relative weight, alterations on AST, ALT or γ-GT levels were not observed. Together, these results demonstrate that DCTN has an important antinociceptive effect in acute and chronic models
of pain, mainly of inflammatory origin, and its mechanism of action seems to involve an interaction with TRPA1 channels and the cAMP/PKA signaling pathway. In this way, DCTN
may be considered a potential candidate to further pre-clinical and even clinical investigations for development of analgesic drugs.<br>A Ocotea puberula (Lauraceae) é uma árvore nativa brasileira, conhecida nos estados da região sul por canela guaicá ou canela amarela, cuja composição fitoquímica inclui diversos alcaloides do tipo aporfínicos, alguns dos quais com atividades biológicas já demonstradas. Frutos coletados na região de Curitiba, Paraná, foram submetidos a processos de extração e fracionamento, permitindo isolar um alcaloide identificado como dicentrina, presente como componente majoritário. Neste trabalho, foi investigado o potencial antinociceptivo das frações orgânicas obtidas a partir do extrato dos frutos de O. puberula e da dicentrina (DCTN) isolada da fração clorofórmica (FC). Tanto a FC quanto a DCTN, administradas por via oral, foram capazes de reduzir a nocicepção induzida pela formalina e pelo ácido acético,
com DI50 semelhantes, sugerindo que o efeito de FC seja devido à presença da DCTN. As frações hexânica (FH) e acetato de etila (FAE), por sua vez, não apresentaram efeito antinociceptivo. A DCTN também apresentou efeito antinociceptivo em modelos crônicos, tanto inflamatório (injeção intraplantar de Adjuvante Completo de Freund) quanto neuropático (ligadura parcial do nervo ciático), sendo capaz de reduzir a hipersensibilidade
mecânica e ao frio, porém sem alterar a resposta ao calor. Quando avaliada frente à ativação de termo-receptores, a DCTN administrada tanto por via sistêmica (via oral) quanto
local (via intraplantar) reduziu a nocicepção induzida pelo cinamaldeído, um ativador de canais TRPA1, mas não alterou a resposta induzida pela capsaicina, um ativador de canais
TRPV1. O efeito antinociceptivo da DCTN não foi revertido pelo pré-tratamento com antagonistas de receptores opióides, adrenérgicos ou canabinóides e nem pelo prétratamento
com um inibidor da síntese de serotonina, sugerindo que estes sistemas descendentes de controle da dor não estão envolvidos no mecanismo de ação da DCTN. Por outro lado, a DCTN foi capaz de prevenir a hipersensibilidade induzida pelos ativadores
da via AMPc/PKA, forscolina e PGE2, e também foi capaz de reduzir a ativação da PKA, demonstrada por análise de western blotting, sugerindo que a DCTN possa agir por interação com essa via de sinalização. Por outro lado, a DCTN apresentou pouca ou
nenhuma ação frente à hipersensibilidade mecânica induzida pela bradicinina ou pelo PMA, respectivamente, o que sugere que a via PLC/PKC não está envolvida no seu efeito antinociceptivo. A DCTN não causou efeitos sedativos, alteração motora ou alteração na temperatura corporal dos animais e, embora o tratamento diário durante 14 dias tenha aumentado o peso relativo do fígado, não foram observadas alterações nos níveis
sanguíneos de AST, ALT ou γ-GT. Coletivamente, os dados deste trabalho demonstram que a DCTN apresenta um importante efeito antinociceptivo em modelos de dor agudos e crônicos, principalmente de cunho inflamatório, e seu mecanismo de ação parece envolver interação com canais TRPA1 e com a via de sinalização AMPc/PKA. Desta forma, a DCTN constitui-se como uma potencial candidata para a continuidade de estudos pré-clínicos aprofundados, e futuramente clínicos, visando o desenvolvimento de fármacos analgésicos.
Book chapters on the topic "Alkaloidal extracts"
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Heinig, Uwe, and Asaph Aharoni. "Analysis of Steroidal Alkaloids and Saponins in Solanaceae Plant Extracts Using UPLC-qTOF Mass Spectrometry." In Methods in Molecular Biology. Springer New York, 2014. http://dx.doi.org/10.1007/978-1-4939-0606-2_12.
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Djellali, Souad, Hana Ferkous, Rachid Sahraoui, and Sara Meharga. "Efficiency of Alkaloids Crude Extract of Cinnamomum Zeylanicum as Corrosion Inhibitor of Mild Steel in Sulfuric Acid Solution." In Recent Advances in Environmental Science from the Euro-Mediterranean and Surrounding Regions (2nd Edition). Springer International Publishing, 2021. http://dx.doi.org/10.1007/978-3-030-51210-1_219.
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Mustafa, Kiran, Javaria Kanwal, Samia Khakwani, and Sara Musaddiq. "Cognitive Enhancement and Neuroprotective Abilities of Plants." In Advanced Pharmacological Uses of Medicinal Plants and Natural Products. IGI Global, 2020. http://dx.doi.org/10.4018/978-1-7998-2094-9.ch007.
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Extensive research suggests that a number of plant-derived chemicals and traditional Oriental herbal remedies possess cognition-enhancing properties. Widely used current treatments for dementia include extracts of Ginkgo biloba and several alkaloidal, and therefore toxic, plant-derived cholinergic agents. Several non-toxic, European herbal species have pan-cultural traditions as treatments for cognitive deficits, including those associated with aging. Acute administration has also been found to reliably improve mnemonic performance in healthy young and elderly cohorts, whilst a chronic regime has been shown to attenuate cognitive declines in sufferers from Alzheimer's disease. The present chapter looks at the ethnobotanical and pharmacological importance of various plants cognitive enhancing and other neuroprotective abilities.
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Morrow, Gary W. "Biosynthesis of Alkaloids and Related Compounds." In Bioorganic Synthesis. Oxford University Press, 2016. http://dx.doi.org/10.1093/oso/9780199860531.003.0010.
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Though definitions may vary from source to source, the term alkaloid generally refers to members of a large set of naturally occurring, slightly basic (i.e., alkaline) nitrogen-containing organic compounds. Generally excluded from this group are amino acids, peptides, proteins, N-containing carbohydrates, and nitrogenous bases used in the construction of nucleotides. Though a small number are produced by animals or microorganisms, the vast majority of alkaloids are plant-produced compounds possessing a remarkably diverse range of structural features, from simple cycloaliphatic amines to highly complex polycyclic N-heterocycles. Some representative alkaloids are shown in Fig. 7.1. Alkaloid-containing plants and their extracts have been used by humans for thousands of years, mainly on the basis of their stimulant, therapeutic, or poisonous properties. References to plants containing compounds such as morphine (from opium poppies), strychnine (from seeds of the Strychnos nux-vomica tree), ephedrine (from the plant Ephedra chinensis), and coniine (from the poison hemlock plant) may be found in some of our earliest known writings. Today, it has been estimated that the health care of over 5 billion people worldwide benefits from the use of plant-based medicinal agents, many of which are alkaloids. With that in mind, it is worth noting concerns that deforestation, environmental damage, large-scale development, and unregulated harvesting programs may ultimately lead to the extinction of hundreds of known medicinal plants and perhaps even more whose medicinal properties have yet to be discovered, thereby endangering the prospects for future discoveries of new curative agents for the benefit of all humankind. As a scientific field, alkaloid chemistry itself dates back to the early 1800s with the first isolation of pure crystalline morphine from opium. This milestone achievement allowed the delivery of accurate, therapeutic doses of a drug that was immensely valuable for the relief of pain but which could also lead to fatal overdoses when administered from simple extracts of variable composition and strength. The subsequent rapid development of increasingly sophisticated techniques for the isolation and purification of the active components (often alkaloids) from many other medicinal plants essentially spawned the field of organic chemistry.
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Yokote, K., and M. Takemoto. "Plant Extracts and Alkaloids." In Bioactive Food as Dietary Interventions for Diabetes. Elsevier, 2013. http://dx.doi.org/10.1016/b978-0-12-397153-1.00023-8.
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Omujal, Francis. "Phytochemistry and Ethnopharmacology of Vebris nobilis Delile (Rutaceae)." In Pharmacognosy - Medicinal Plants [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.96809.
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Vepris nobilis Mziray (formerly Teclea noblis Delile) is an ever-green plant in the tropical climate. The different parts (leaves, stem bark, roots and fruits) of this plant are popular for treatment of various diseases including; malaria, rheumatism, arthritis, pneumonia, cough, fever, measles, asthma, common cold, headache, join and chest pains and as antithelmintic. Several phytochemical compounds including quinoline and furoquinoline alkaloids, terpenoids and flavonoids have been isolated from the different plant. Pharmacological investigations on the different crude extracts and isolated compounds covering antipyretic, analgesic, anti-inflammatory, antimicrobial, antimalarial, antileishmanial and ant-trypanosomal have been conducted.
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Sansi, Manish Singh, Daraksha Iram, Kapil Singh Narayan, Sandeep Kumar, Om Prakash, and Dipanjan Misra. "Antidiabetic Activity (Anti-Hyperglycemic Activity, Anti-Hyperlipidemic Activity)/Agents From Medicinal Plants." In Advanced Pharmacological Uses of Medicinal Plants and Natural Products. IGI Global, 2020. http://dx.doi.org/10.4018/978-1-7998-2094-9.ch002.
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Diabetes mellitus (DM) is a chronic disease caused by inherited or acquired deficiency in insulin secretion and by decreased insulin secretion by the organ. Insulin deficiency causes the DM. Synthetic drugs are widely used in the treatment of diabetes, but they have some side effects. The antihyperglycemic and antihyperlipedemic effects of the plants are related to their ability to maintain pancreatic function. Medicinal plants constituents such as glycosides, alkaloids, terpenoids, and flavonoids mitigate DM. B. ciliata inhibits the α-glucosidase and α-amylase. Cinnamon extracts improve insulin receptor function by activating insulin receptor kinase and inhibiting insulin receptor phosphatase, which lead to an increase in insulin sensitivity. Morinda lucida also had the highest antioxidant activity, and it also inhibited the α-glucosidase. Many plants have also been shown to antihyperlipedemic effects. Finally, it can be concluded that medicinal plants have that ability to treat or prevent DM.
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Fotsing Yannick Stéphane, Fongang, Bankeu Kezetas Jean Jules, Gaber El-Saber Batiha, Iftikhar Ali, and Lenta Ndjakou Bruno. "Extraction of Bioactive Compounds from Medicinal Plants and Herbs." In Pharmacognosy - Medicinal Plants [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.98602.
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Human beings have relied on herbs and medicinal plants as sources of food and remedy from time immemorial. Bioactive compounds from plants are currently the subject of much research interest, but their extraction as part of phytochemical and/or biological investigations present specific challenges. Herbalists or scientists have developed many protocols of extraction of bioactive ingredients to ensure the effectiveness and the efficacy of crude drugs that were used to get relief from sickness. With the advent of new leads from plants such as morphine, quinine, taxol, artemisinin, and alkaloids from Voacanga species, a lot of attention is paid to the mode of extraction of active phytochemicals to limit the cost linked to the synthesis and isolation. Thus, the extraction of active compounds from plants needs appropriate extraction methods and techniques that provide bioactive ingredients-rich extracts and fractions. The extraction procedures, therefore, play a critical role in the yield, the nature of phytochemical content, etc. This chapter aims to present, describe, and compare extraction procedures of bioactive compounds from herbs and medicinal plants.
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Kumar, Brijesh, Sunil Kumar, Vikas Bajpai, and K. P. Madhusudanan. "Structural Characterization of Monoterpene Indole Alkaloids in Ethanolic Extracts of Rauvolfia Species by LC-QTOF-MS." In Phytochemistry of Plants of Genus Rauvolfia. CRC Press, 2020. http://dx.doi.org/10.1201/9781003014843-2.
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Payal, R. "Green Corrosion Inhibitors for Coatings." In Sustainable Corrosion Inhibitors. Materials Research Forum LLC, 2021. http://dx.doi.org/10.21741/9781644901496-7.
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Corrosion is emerging as a potential hazard which abolishes metals and their structures and hence become an imperative menace. It is an omnipotent and omnipresent process which is present in every environment, i.e., air, soil, water. Green chemistry is one of the notable branches of chemistry that focuses on the protection of environment and human well–being in an economically viable approach allowing dodging of toxins and reducing hazards due to corrosion. Green chemistry exploited well–known strategy namely green inhibitors to prevent, control or impede the growth of corrosion. Green inhibitors are eco–friendly, cost–effective, renewable natural products which are favourable over toxic synthetic corrosion inhibitors. Extracts of natural products contain natural products containing alkaloids, carboxylic acids, nicotine, polyphenols, quinine, terpenes, and other functional groups possessing elements like C, N, O, S, etc., prompting adsorption via forming a thin layer (coating) on the metallic surface to shield the surface and encumber corrosion. In the field of economical loop, this approach develops various potential applications in manufacturing areas other than ‘Trash to treasure’. Even though a bunch of experiments have been performed and several research articles have been in print, however, the area of green inhibitors is still demanding more investigation on this open issue. More and more interest in the area extended the research, consequentially to a large variety of tried molecules. Nevertheless, the most accepted protocols are classical and, therefore, are incompetent to completely portray the probable worth of inhibitors. Hence all above stated features should be the objective of the contemporary research so that productive analysis to emphasize the weak areas of the green inhibitors field and tackle the prospect research in the field that still requires validation.
Conference papers on the topic "Alkaloidal extracts"
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Zielińska, S., A. Junka, M. Wójciak-Kosior, et al. "The relevance of alkaloid proportions in Chelidonium maius extracts." In 67th International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA) in cooperation with the French Society of Pharmacognosy AFERP. © Georg Thieme Verlag KG, 2019. http://dx.doi.org/10.1055/s-0039-3400100.
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Iskandarova, S. F., and N. A. Dzhabbarov. "THE AMOUNT OF TOTAL ALKALOIDS IN SOPHORA JAPONICA EXTRACT." In VI International Youth Conference "Perspectives of Science and Education". Premier Publishing s.r.o., 2019. http://dx.doi.org/10.29013/vi-conf-usa-6-19-20.
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Agustina, R., A. H. Cahyana, and R. R. Tjandrawinata. "Abrine (N-methyltryptophan), an alkaloid from Abrus precatorius Linn. leaves extract." In PROCEEDINGS OF THE 5TH INTERNATIONAL SYMPOSIUM ON CURRENT PROGRESS IN MATHEMATICS AND SCIENCES (ISCPMS2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0007888.
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Wei Qiao, Lu Li, Jingshu Liu, Yi Yang, and Liyan Ren. "Antidepressant-like effect of total alkaloids extracted from Semen Zizyphi Sponosae." In 2011 International Conference on Remote Sensing, Environment and Transportation Engineering (RSETE). IEEE, 2011. http://dx.doi.org/10.1109/rsete.2011.5964024.
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Maiza-Benabdesselam, F., and N. Bribi. "Antibacterial activity against multi resistant bacteria strains of alkaloid extracts of two Algerian FUMARIA species." In MICROBES IN APPLIED RESEARCH - Current Advances and Challenges. WORLD SCIENTIFIC, 2012. http://dx.doi.org/10.1142/9789814405041_0094.
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Schenk, A., B. Siewert, S. Toff, and J. Drewe. "Determination of 34 pyrrolizidine alkaloids (PA) as contaminants in various plant extracts using UHPLC-ToF-HRMS." In GA 2017 – Book of Abstracts. Georg Thieme Verlag KG, 2017. http://dx.doi.org/10.1055/s-0037-1608497.
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Silitonga, Hendrika Andriana, Gontar Alamsyah Siregar, Rosita Juwita Sembiring, and Marline Nainggolan. "Effect of Chayote (Sechium Edule Jacq. Swartz) Extract on Level of Interleukin-8 in Wistar Rats with Aspirin-Induced Gastritis." In The 7th International Conference on Public Health 2020. Masters Program in Public Health, Universitas Sebelas Maret, 2020. http://dx.doi.org/10.26911/the7thicph.05.35.
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ABSTRACT Background: Recent studies showed that Interleukin-8 (IL-8), activated cytokine immune response which plays an important role in the development of acute and chronic gastritis. Harmless anti-inflammatory therapeutic alternatives have been proposed, for example, the consumption of Sechium Edule Jacq. Swartz (chayote). Antioxidant (flavonoid) and cell regeneration (alkaloid) agents were found in chayote. This study aimed to determine the effect of chayote Sechium Edule Jacq. Swartz extracts on the level of IL-8 in Wistar rats with aspirin- induced gastritis. Subjects and Method: This was a randomized controlled trial (RCT) conducted at the laboratory of Mathematics and Natural Science, Universitas Sumatra Utara from January to February 2020. A total of 35 male Wistar rats was selected for this study and randomly allocated into 7 groups: (1) Negative control; (2) Positive control; (3) 100 mg/ kg BW chayote ethanol extract ; (4) 200 mg/kg BW chayote ethanol extract; (5) 100 mg/ kg BW chayote ethyl acetate fraction; (6) 200 mg/kg BW chayote ethyl acetate fraction; and (7) 20 mg omeprazole. The rats in positive control and treatment groups were induced with aspirin (200mg/ kg BW). The negative control group received no intervention. The dependent variable was level of IL-8 measured by ELISA. The independent variables were treatment status. The data were analyzed by One Way Anova and post hoc test. Results: The mean differences of IL-8 level were not statistically significant between study groups (p= 0.327). Mean of IL-8 level was higher in positive control group (Mean= 160.80; SD= 6.90) than in negative control group (Mean= 141.20; SD= 10.98). The lowest IL-8 level was in 100mg/ kg BW chayote ethanol extract group (Mean= 149.94; SD= 40.4), followed by 200mg/ kg BW (Mean= 152.4; SD= 30.73) and 100mg/ kg BW (Mean= 164.60; SD= 25.04) chayote ethyl acetate fraction groups, 20 mg omeprazole group (Mean= 170.60; SD= 21.58), and 200 mg/ kg BW chayote ethanol extract group (Mean= 176.80; SD= 10.98). Conclusion: The low dose (100mg/ kg BW) chayote ethanol extract has the most potential antiinflammation effect on in vitro gastritis with the lowest IL-8 level of all doses of chayote ethanol extract, chayote ethyl acetate fraction, and omeprazole. Keywords: antiinflammation, IL-8, chayote ethanol extract, ethyl acetate fraction, omeprazole, aspirin induced gastritis Correspondence: Hendrika Andriana Silitonga. Department of Histology, Faculty of Medicine, Universitas Methodist Indonesia. Email: andr38482@gmail.com. Mobile: +6281361430688. DOI: https://doi.org/10.26911/the7thicph.05.35
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Chaingam, J., T. Juengwatanatrakul, G. Yusakul, T. Kanchanapoom, and W. Putalun. "Simultaneous determination of three canthin-6-one alkaloids in different extracts of Eurycoma longifolia and Eurycoma harmandiana using HPLC-UV." In 67th International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA) in cooperation with the French Society of Pharmacognosy AFERP. © Georg Thieme Verlag KG, 2019. http://dx.doi.org/10.1055/s-0039-3399775.
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Montana, Fajar Daniswara, Yuni Setyaningsih, and Fajriati Zulfa. "Effectiveness of Cocoa (Theobroma Cacao L.) Seed Extract on the Growth of in Vitro Malassezia Furfur." In The 7th International Conference on Public Health 2020. Masters Program in Public Health, Universitas Sebelas Maret, 2020. http://dx.doi.org/10.26911/the7thicph.05.01.
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ABSTRACT Background: Pityriasis versicolor or Tinea versicolor is a skin disease caused by the Malassezia furfur which is often found in Indonesia. People can use anti-fungal drugs to treat this disease. However, long-term use of anti-fungal drugs is relatively more expensive and can have side effects for its users. Cocoa bean husk contains flavonoids, saponins, and alkaloids which have anti-fungal effects. This study aimed to determine the antifungal effectiveness of the cocoa bean husk extract on the growth of M. furfur. Subjects and Methods: This was an experimental study using cocoa bean husk extract with a concentration variance of 25%, 50%, 75%, 100%, with a positive control for ketoconazole 2% and a negative control using distilled water. The test was carried out by the well diffusion method using Sabouraud Dextrose Agar media. The inhibition of fungal growth was calculated by looking at the clear zone formed after 48 hours. Data were analyzed using Kruskal-Wallis and Post hoc Mann Whitney statistical tests. Results: The mean diameter of the inhibition zone at a concentration of 25%, 50%, 75% and 100% was 3.42 mm, 4.07 mm, 4.9 mm, and 7.3 mm, respectively, and it was statistically significant (p = 0.001). Conclusion: Cocoa bean husk extract has weak anti-fungal effectiveness at concentrations of 25%, 50%, and 75%, while at 100% it has moderate effectiveness. Keywords: antifungal, Pityriasis versicolor, cocoa bean shell, well diffusion, Malassezia furfur Correspondence: Yuni Setyaningsih. Department of Parasitology, Faculty of Medicine, Universitas Pembangunan Nasional “Veteran” Jakarta. DOI: https://doi.org/10.26911/the7thicph.05.01
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Nakamori, S., N. Miyajima, S. Hyuga, et al. "Therapeutic and analgesic effects of ephedrine alkaloids-free Ephedra Herb extract on complete Freud’s adjuvant-induced arthritis model mouse." In 67th International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA) in cooperation with the French Society of Pharmacognosy AFERP. © Georg Thieme Verlag KG, 2019. http://dx.doi.org/10.1055/s-0039-3399686.
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