To see the other types of publications on this topic, follow the link: Bioactive compounds – Testing.
Journal articles on the topic 'Bioactive compounds – Testing'
Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles
Consult the top 50 journal articles for your research on the topic 'Bioactive compounds – Testing.'
Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.
You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.
Browse journal articles on a wide variety of disciplines and organise your bibliography correctly.
1
Suryaningtyas, Indyaswan Tegar. "SENYAWA BIOAKTIF MIKROALGA DAN PROSPEKNYA DI MASA DEPAN." OSEANA 44, no. 1 (April 30, 2019): 15–25. http://dx.doi.org/10.14203/oseana.2019.vol.44no.1.28.
Full textAbstract:
BIOACTIVE COMPOUND FROM MICROALGAE AND ITS FUTURE PROSPECT. Microalgae biomass is potential to be used in various fields, one of which is as a producer of bioactive compounds. Bioactive compounds from microalgae can be used extensively in the pharmaceutical industry, cosmetic’s raw materials, food flavouring substances, and functional food ingredients. In terms of health, the bioactive compounds have the potential as antioxidants, antiviral, antibacterial, anti-fungal, anti-inflammatory, anti-tumor, and prevent the effects of malaria, but the potential for microalgae’s bioactive compound has not been explored well if compared to the production of terrestrial plants. Some examples of the bioactive compounds that have been used are carotenoid groups such as lutein, β-carotene, astaxanthin and fucoxanthin; fatty acid groups such as EPA and DHA; and also some toxin compounds such as domoic acid. To obtain the optimum yield of bioactive compounds, it requires the right method in biomass production, compound extraction, compounds isolation and compounds identification. While testing the activities, it is necessary to do some assays such as antioxidan, antibiotic, antiviral and anticancer assay. The development of the technology can improve the potential use of microalgae to synthesis its bioactive compounds.
2
Vettorazzi, Ariane, Adela López de Cerain, Julen Sanz-Serrano, Ana G. Gil, and Amaya Azqueta. "European Regulatory Framework and Safety Assessment of Food-Related Bioactive Compounds." Nutrients 12, no. 3 (February 26, 2020): 613. http://dx.doi.org/10.3390/nu12030613.
Full textAbstract:
A great variety of functional foods, nutraceuticals, or foods with bioactive compounds are provided nowadays to consumers. Aware of the importance of the safety aspects, the food industry has to comply with different legal requirements around the world. In this review, the European regulatory framework for food-related bioactive compounds is summarized. The term ‘bioactive compound’ is not defined in the European regulations, however, since they can be part of food supplements, fortified foods, or novel food, they are included within the legal requirements of those corresponding types of foods or supplements. Lists of authorized compounds/foods appear in the correspondent regulations, however, when a new compound/food is going to be launched into the market, its safety assessment is essential. Although the responsibility for the safety of these compounds/foods lies with the food business operator placing the product on the market, the European Food Safety Authority (EFSA) carries out scientific evaluations to assess the risks for human health. To facilitate this procedure, different guidelines exist at the European level to explain the tier toxicity testing approach to be considered. This approach divides the evaluation into four areas: (a) toxicokinetics; (b) genotoxicity; (c) subchronic and chronic toxicity and carcinogenicity; and (d) reproductive and developmental toxicity.
3
Sandomenico, Annamaria, Andrea Caporale, Nunzianna Doti, Simon Cross, Gabriele Cruciani, Angela Chambery, Sandro De Falco, and Menotti Ruvo. "Synthetic Peptide Libraries: From Random Mixtures to In Vivo Testing." Current Medicinal Chemistry 27, no. 6 (March 16, 2020): 997–1016. http://dx.doi.org/10.2174/0929867325666180716110833.
Full textAbstract:
Combinatorially generated molecular repertoires have been largely used to identify novel bioactive compounds. Ever more sophisticated technological solutions have been proposed to simplify and speed up such process, expanding the chemical diversity space and increasing the prospect to select new molecular entities with specific and potent activities against targets of therapeutic relevance. In this context, random mixtures of oligomeric peptides were originally used and since 25 years they represent a continuous source of bioactive molecules with potencies ranging from the sub-nM to microM concentration. Synthetic peptide libraries are still employed as starting “synthetic broths” of structurally and chemically diversified molecular fragments from which lead compounds can be extracted and further modified. Thousands of studies have been reported describing the application of combinatorial mixtures of synthetic peptides with different complexity and engrafted on diverse structural scaffolds for the identification of new compounds which have been further developed and also tested in in vivo models of relevant diseases. We briefly review some of the most used methodologies for library preparation and screening and the most recent case studies appeared in the literature where compounds have reached at least in vivo testing in animal or similar models. Recent technological advancements in biotechnology, engineering and computer science have suggested new options to facilitate the discovery of new bioactive peptides. In this instance, we anticipate here a new approach for the design of simple but focused tripeptide libraries against druggable cavities of therapeutic targets and its complementation with existing approaches.
4
Tung, Nguyen Huu, Le Quoc Hung, Ha Van Oanh, Duong Thi Ly Huong, Phuong Thien Thuong, Dinh Doan Long, and Nguyen Thanh Hai. "Bioactive Phenolic Compounds from the Roots of Danshen (Salvia miltiorrhiza)." Natural Product Communications 13, no. 10 (October 2018): 1934578X1801301. http://dx.doi.org/10.1177/1934578x1801301018.
Full textAbstract:
Danshen ( Salvia miltiorrhiza Bunge) is one of the most used medicinal plants in the Oriental medicine and has been well studied for application in modern medicine. In our continuing study on chemical constituents of danshen cultivated in Vietnam, using chromatography separation resulted in the isolation of six phenolic compounds including a benzophenone, iriflophenone 2- O- α-L-rhamnopyranoside (1), and five phenolic acids including rosmarinic acid (2), rosmarinic acid methyl ester (3), rosmarinic acid ethyl ester (4), salvianolic acid A methyl ester (5) and salvianolic acid A ethyl ester (6) from the butanol portion of the danshen crude extract. Beside the typically main phenolic acid components, to our knowledge, iriflophenone 2- O- α-L-rhamnopyranoside (1) was first isolated from salvia sp. On biological testing, compound 1 showed strong antiproliferative activity on HL-60 leukemia cells with the IC50 of 8.9 μM; compounds 1 and 3–6 inhibited markedly nitric oxide production in lipopolysaccharide-treated RAW 264.7 cells.
5
Octarya, Zona, Fitri Refelita, and Novia Rahim. "Antimicrobial Activities of Bioactive Compounds from Jatropha curcas." Indonesian Journal of Chemical Science and Technology (IJCST) 2, no. 1 (January 7, 2020): 66. http://dx.doi.org/10.24114/ijcst.v2i1.12366.
Full textAbstract:
Jatropha curcas L is widely planted in people's homes. Jatropha has many bioactive compounds, including flavonoids, saponins, tannins, and alkaloids. In this research, phytochemical tests and antimicrobial activities of sap and water extraction of Jatropha curcas L leaves on Candida albicans, Aspergillus, and Pseudomonas aeruginosa were carried out. The results of the phytochemical test of sap and water extraction of leaves showed positive results in the test of flavonoids, saponins, alkaloids and tannins. While steroid testing showed negative results. The antimicrobial capabilities of sap and water extraction of leaves to Aspergillus were 10.5 mm and 11 mm and to Pseudomonas Aeruginosa were 15 mm and 11 mm. Whereas the antimicrobial ability of sap and water extraction of leaf to Candida albicans was negative. In this case, it means that Pseudomonas aeruginosa is including microbes that are sensitive to antimicrobial origin of plants.
6
Qiu, Shi, Shabana I. Khan, Mei Wang, Jianping Zhao, Siyu Ren, Ikhlas A. Khan, Amy Steffek, William P. Pfund, and Xing-Cong Li. "Chemometrics-Assisted Identification of Anti-Inflammatory Compounds from the Green Alga Klebsormidium flaccidum var. zivo." Molecules 25, no. 5 (February 26, 2020): 1048. http://dx.doi.org/10.3390/molecules25051048.
Full textAbstract:
The green alga Klebsormidium flaccidum var. zivo is a rich source of proteins, polyphenols, and bioactive small-molecule compounds. An approach involving chromatographic fractionation, anti-inflammatory activity testing, ultrahigh performance liquid chromatography-mass spectrometry profiling, chemometric analysis, and subsequent MS-oriented isolation was employed to rapidly identify its small-molecule anti-inflammatory compounds including hydroxylated fatty acids, chlorophyll-derived pheophorbides, carotenoids, and glycoglycerolipids. Pheophorbide a, which decreased intracellular nitric oxide production by inhibiting inducible nitric oxide synthase, was the most potent compound identified with an IC50 value of 0.24 µM in lipopolysaccharides-induced macrophages. It also inhibited nuclear factor kappaB activation with an IC50 value of 32.1 µM in phorbol 12-myristate 13-acetate-induced chondrocytes. Compared to conventional bioassay-guided fractionation, this approach is more efficient for rapid identification of multiple chemical classes of bioactive compounds from a complex natural product mixture.
7
D’Urso, Gilda, Jurriaan J. Mes, Paola Montoro, Robert D. Hall, and Ric C. H. de Vos. "Identification of Bioactive Phytochemicals in Mulberries." Metabolites 10, no. 1 (December 20, 2019): 7. http://dx.doi.org/10.3390/metabo10010007.
Full textAbstract:
Mulberries are consumed either freshly or as processed fruits and are traditionally used to tackle several diseases, especially type II diabetes. Here, we investigated the metabolite compositions of ripe fruits of both white (Morus alba) and black (Morus nigra) mulberries, using reversed-phase HPLC coupled to high resolution mass spectrometry (LC-MS), and related these to their in vitro antioxidant and α-glucosidase inhibitory activities. Based on accurate masses, fragmentation data, UV/Vis light absorbance spectra and retention times, 35 metabolites, mainly comprising phenolic compounds and amino sugar acids, were identified. While the antioxidant activity was highest in M. nigra, the α-glucosidase inhibitory activities were similar between species. Both bioactivities were mostly resistant to in vitro gastrointestinal digestion. To identify the bioactive compounds, we combined LC-MS with 96-well-format fractionation followed by testing the individual fractions for α-glucosidase inhibition, while compounds responsible for the antioxidant activity were identified using HPLC with an online antioxidant detection system. We thus determined iminosugars and phenolic compounds in both M. alba and M. nigra, and anthocyanins in M. nigra as being the key α-glucosidase inhibitors, while anthocyanins in M. nigra and both phenylpropanoids and flavonols in M. alba were identified as key antioxidants in their ripe berries.
8
Boustie, Joël, and Martin Grube. "Lichens—a promising source of bioactive secondary metabolites." Plant Genetic Resources 3, no. 2 (August 2005): 273–87. http://dx.doi.org/10.1079/pgr200572.
Full textAbstract:
Lichen-forming fungi are unique organisms, producing biologically active metabolites with a great variety of effects, including antibiotic, antimycobacterial, antiviral, anti-inflammatory, analgesic, antipyretic, antiproliferative and cytotoxic activities. However, only very limited numbers of lichen substances have been screened for their biological activities and their therapeutic potential in medicine. This is certainly due to the difficulties encountered in identification of the species, collection of bulk quantities, and the isolation of pure substances for structure determination and testing activity. Recently, possibilities for bypassing some of these former difficulties have arisen by the introduction of new techniques. This includes axenic cultivation for production of the genuine compounds or new ones, extraction of focused compounds, or synthesis of natural products or their derivatives for testing. Utilizing these new opportunities, the discovery of novel active metabolites, which could serve as lead compounds, is significantly facilitated. At the same time, the evolution of secondary metabolite patterns is studied using phylogenetic approaches. Yet, the genetic background of the complex chemical patterns is poorly understood. The scattered occurrence of some compounds suggests that their production evolved either in parallel or that ancient biosynthetic pathways are abandoned in many lineages. At least, studies on polyketide synthase genes from different lichen groups suggest a high level of gene paralogy. In this context, clades of orthologous polyketide synthase genes, which are often shared with distantly related non-lichenized fungi, can roughly be identified by their sequence similarity and their similar patterns of substitution rates. The functional assignment of paralogs is nevertheless difficult and reasonable only in a few cases. A global approach of the lichen metabolomic features appears to be essential in developing new and viable biotechnological processes which could afford suitable amounts of unique lichen compounds.
9
Hummell, Nicholas A., and Natalia V. Kirienko. "Repurposing bioactive compounds for treating multidrug-resistant pathogens." Journal of Medical Microbiology 69, no. 6 (June 1, 2020): 881–94. http://dx.doi.org/10.1099/jmm.0.001172.
Full textAbstract:
Introduction. Antimicrobial development is being outpaced by the rising rate of antimicrobial resistance in the developing and industrialized world. Drug repurposing, where novel antibacterial functions can be found for known molecular entities, reduces drug development costs, reduces regulatory hurdles, and increases rate of success. Aim. We sought to characterize the antimicrobial properties of five known bioactives (DMAQ-B1, carboplatin, oxaliplatin, CD437 and PSB-069) that were discovered in a high-throughput phenotypic screen for hits that extend Caenorhabditis elegans survival during exposure to Pseudomonas aeruginosa PA14. Methodology. c.f.u. assays, biofilm staining and fluorescence microscopy were used to assay the compounds' effect on various virulence determinants. Checkerboard assays were used to assess synergy between compounds and conventional antimicrobials. C. elegans-based assays were used to test whether the compounds could also rescue against Enterococcus faecalis and Staphyloccus aureus. Finally, toxicity was assessed in C. elegans and mammalian cells. Results. Four of the compounds rescued C. elegans from a second bacterial pathogen and two of them (DMAQ-B1, a naturally occurring insulin mimetic, and CD437, an agonist of the retinoic acid receptor) rescued against all three. The platinum complexes displayed increased antimicrobial activity against P. aeruginosa . Of the molecules tested, only CD437 showed slight synergy with ampicillin. The two most effective compounds, DMAQ-B1 and CD437, showed toxicity to mammalian cells. Conclusion. Although these compounds' potential for repurposing is limited by their toxicity, our results contribute to this growing field and provide a simple road map for using C. elegans for preliminary testing of known bioactive compounds with predicted antimicrobial activity.
10
VIRGANITA, JENNY, DINAR SARI CAHYANINGRUM WAHYUNI, and ESTU RETNANINGTYAS NUGRAHENI. "Antibacterial activity of bioactive compounds from radish (Raphanus sativus) leaves against Escherichia coli and its chemical compounds." Biofarmasi Journal of Natural Product Biochemistry 7, no. 2 (August 17, 2009): 94–98. http://dx.doi.org/10.13057/biofar/f070205.
Full textAbstract:
Virganita J, Wahyuni DSC, Nugraheni ER. 2009. Antibacterial activity of bioactive compounds from radish (Raphanus sativus) leaves against Escherichia coli and its chemical compounds. Biofarmasi 7: 94-98. Indonesia has many kinds of plants, some of them are medicinal plants that were used to cure various diseases. One of medicinal plants is radish (Raphanus sativus L.), known as vegetable. That is the reason conducting the research to find out the bioactive compounds from plants, which can be used as raw materials of drug. Other reasons are expensive drug prices in the market, the death case due to microbial infection, and the increasing of bacterial resistance because of ineffectiveness usage of antibiotic. This study aimed to determine the antibacterial effect of bioactive compounds from radish leaves against Escherichia coli. Bioactive compounds were found by extraction dan partition using centrifugation. Dry powder from radish leaves was extracted with chloroform and methanol. After the antibacterial testing, methanol extract resulted in an antibacterial effect was separated in a partition by ethyl acetate into soluble and insoluble parts. The soluble part of ethyl acetate resulted in an antibacterial effect on the concentration of 30-50% was shown by a clear zone (average 10 mm). It was separated again into soluble and insoluble fractions with dichloromethane. Dichloromethane soluble fraction formed a clear zone about 8.30 mm on 10% concentration and 8.42 mm on 20% concentration. Furthermore, the chemical constituent profile of the most active fraction was monitored using KLT method and detected with spray chemicals. The results indicated that radish leaves had bioactive compounds from phenolic group. It was proved by ammonia detection which giving a yellow color, and dark blue with FeCl3 detection.
11
Martínez-Ballesta, MCarment, Ángel Gil-Izquierdo, Cristina García-Viguera, and Raúl Domínguez-Perles. "Nanoparticles and Controlled Delivery for Bioactive Compounds: Outlining Challenges for New “Smart-Foods” for Health." Foods 7, no. 5 (May 7, 2018): 72. http://dx.doi.org/10.3390/foods7050072.
Full textAbstract:
Nanotechnology is a field of research that has been stressed as a very valuable approach for the prevention and treatment of different human health disorders. This has been stressed as a delivery system for the therapeutic fight against an array of pathophysiological situations. Actually, industry has applied this technology in the search for new oral delivery alternatives obtained upon the modification of the solubility properties of bioactive compounds. Significant works have been made in the last years for testing the input that nanomaterials and nanoparticles provide for an array of pathophysiological situations. In this frame, this review addresses general questions concerning the extent to which nanoparticles offer alternatives that improve therapeutic value, while avoid toxicity, by releasing bioactive compounds specifically to target tissues affected by specific chemical and pathophysiological settings. In this regard, to date, the contribution of nanoparticles to protect encapsulated bioactive compounds from degradation as a result of gastrointestinal digestion and cellular metabolism, to enable their release in a controlled manner, enhancing biodistribution of bioactive compounds, and to allow them to target those tissues affected by biological disturbances has been demonstrated.
12
González-Montelongo, Rafaela, M. Gloria Lobo, and Mónica González. "Antioxidant activity in banana peel extracts: Testing extraction conditions and related bioactive compounds." Food Chemistry 119, no. 3 (April 1, 2010): 1030–39. http://dx.doi.org/10.1016/j.foodchem.2009.08.012.
Full text
13
Nuryani, Shinta Ayu, Shanti Dwita Lestari, and Ace Baehaki. "Uji Fitokimia dan Aktivitas Antioksidan Teh Daun Daruju (Acanthus illicifolius)." Jurnal FishtecH 7, no. 1 (August 23, 2018): 27–35. http://dx.doi.org/10.36706/fishtech.v7i1.5977.
Full textAbstract:
The purposes of the research were to compare the method of makes daruju (Acanthus illicifolius) leaves the tea to determine the bioactive compounds. The research was conducted from June 2016 until December 2016. This research uses laboratory experimental methods and data analysis was done descriptively. The parameters observed testing phytochemical compounds flavonoids, alkaloids, tannins, saponins, phenols and steroids and analysis of antioxidant with DPPH and reducing power. The result showed that the crude extract daruju leaves tea has a bioactive compound acts as an antioxidant compound. The result of antioxidant activity DPPH methods was medium in the methanol extract with IC50 values of 101.4 ppm and boiled extract (217.5 ppm) and a very weak activity in the brewed extract (294.9 ppm) while the reducing power method shown good results in the methanol extract instead of boiled extract and brewed extract. From the results of the antioxidant activity of these three methods, the use of extraction are best is methanol. While the comparing from the method of makes daruju leaves the are best is boiled extract than brewed extract.
14
Arifin, Adani Fatahilal, Irvina Nurrachmi, and Efriyeldi Efriyeldi. "TOXICITY TO Artemia salina AND PHYTOCHEMICAL COMPONENTS OF Thalassia Hemprichii SEAGRASS ON NIRWANA BEACH PADANG CITY WEST SUMATERA PROVINCE." Jurnal Perikanan dan Kelautan 25, no. 3 (November 23, 2020): 163. http://dx.doi.org/10.31258/jpk.25.3.163-171.
Full textAbstract:
Many of marine ecotourism activities on Nirwana Beach has had a negative impact to the development of seagrass ecosystems. Pressure that occurs on the coastal ecosystem becomes a trigger factor seagrasses to adapt with produce certain compounds for maintain immunity, the name is bioactive compounds. This research was aimed to know toxicity to Artemia salina and phytochemical component of Thalassia hemprichii seagrass from Nirwana Beach by using experimental method. Two seagrass extracts with different solvents have been made in the Marine Chemistry Laboratories for use in toxicity and phytochemical tests. The results of the test are displayed in tabular or graphical form and analyzed descriptively. The results of toxicity testing showed that seagrass had a toxicity level of 446.872 ppm (n-hexane solvent) and 218.183 ppm (methanol solvents), both of extract are toxic to the Artemia salina. Phytochemical testing shows tannin compounds founded in extracts with n-hexane and methanol solvent, alkaloids and triterpenoids compound contained in extracts with methanol solvent.
15
Zhang, Siqi, Danielle Hagstrom, Patrick Hayes, Aaron Graham, and Eva-Maria S. Collins. "Multi-Behavioral Endpoint Testing of an 87-Chemical Compound Library in Freshwater Planarians." Toxicological Sciences 167, no. 1 (June 8, 2018): 26–44. http://dx.doi.org/10.1093/toxsci/kfy145.
Full textAbstract:
Abstract There is an increased recognition in the field of toxicology of the value of medium-to-high-throughput screening methods using in vitro and alternative animal models. We have previously introduced the asexual freshwater planarian Dugesia japonica as a new alternative animal model and proposed that it is particularly well-suited for the study of developmental neurotoxicology. In this article, we discuss how we have expanded and automated our screening methodology to allow for fast screening of multiple behavioral endpoints, developmental toxicity, and mortality. Using an 87-compound library provided by the National Toxicology Program, consisting of known and suspected neurotoxicants, including drugs, flame retardants, industrial chemicals, polycyclic aromatic hydrocarbons (PAHs), pesticides, and presumptive negative controls, we further evaluate the benefits and limitations of the system for medium-throughput screening, focusing on the technical aspects of the system. We show that, in the context of this library, planarians are the most sensitive to pesticides with 16/16 compounds causing toxicity and the least sensitive to PAHs, with only 5/17 causing toxicity. Furthermore, while none of the presumptive negative controls were bioactive in adult planarians, 2/5, acetaminophen and acetylsalicylic acid, were bioactive in regenerating worms. Notably, these compounds were previously reported as developmentally toxic in mammalian studies. Through parallel screening of adults and developing animals, planarians are thus a useful model to detect such developmental-specific effects, which was observed for 13 chemicals in this library. We use the data and experience gained from this screen to propose guidelines for best practices when using planarians for toxicology screens.
16
Kilungga, Apianus, Linus Y. Chrystomo, and Puguh Sujarta. "Skrining Senyawa Kimia dan Uji Aktivitas Sitotoksik Ekstrak Etanol Teripang Kridou Bintik (Bohadschia argus Jeager) Asal Pantai Harlem Kabupaten Jayapura, Papua." JURNAL BIOLOGI PAPUA 11, no. 1 (May 29, 2019): 12–17. http://dx.doi.org/10.31957/jbp.633.
Full textAbstract:
The Bohadschia argus Jeager contains bioactive compounds that have the potential as antibiotics, antibacterial, antitumor, anticoagulants and anesthetics and alleviate cancer. This study aims to determine the content of chemical compounds group and to test the cytotoxic activity of ethanol extract of Bohadschia argus Jeager. The method for determining the group of chemical compounds was used the color reaction and precipitation using chemical reagents. The method for testing cytotoxic activity using the Brine Shimp Lethality Test (BSLT), this method commonly was used to test the safety of the use of natural ingredients as traditional medicine. The results of screening of the chemical compound group of Bohadschia argus Jeager extract showed that the extract contained a lot of alkaloids secondary metabolites and few saponins. The results of testing of cytotoxic activity showed LC50 value of 878.22 ppm. Base on the results of this study it can be concluded that the ethanol extract of Bohadschia argus Jeager has significant cytotoxic activity against Artemia salina Leach, so it can be considered as a chemotherapeutic agent. Key words: Screening, chemical compounds, ethanol extract, B. argus, BSLT.
17
Ikhtiarudin, Ihsan, Nesa Agistia, Neni Frimayanti, Tria Harlianti, and Jasril Jasril. "Microwave-assisted synthesis of 1-(4-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one and its activities as an antioxidant, sunscreen, and antibacterial." Jurnal Kimia Sains dan Aplikasi 23, no. 2 (February 24, 2020): 51–60. http://dx.doi.org/10.14710/jksa.23.2.51-60.
Full textAbstract:
Chalcone analogs have been reported to have a variety of exciting biological activities, such as anticancer, anti-inflammatory, antioxidant, photoprotective, antibacterial, and antidiabetic activities. Therefore, analogs of these compounds have been widely synthesized as intermediate compounds or target molecules in the discovery of bioactive compounds to be applied in the pharmaceutical field. The purpose of this study is to synthesize chalcone analog compounds (E)-1-(4-hydroxyphenyl)-3-(4-methoxyphenyl) prop-2-en-1-on with the microwave irradiation method and explore some of the biological activities of these compounds, including testing the antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method, in vitro sunscreen activity by microplate method, and antibacterial activity by disk diffusion method. DPPH test results indicate that the compound has weak antioxidant activity, with an IC50 value of 300.43 µg/mL. However, the compound showed excellent potential as a UV B and UV A filter at a concentration of 150 µg/mL with a value of %Te of 0.73±0.10% (sunblock), %Tp of 0.07±0.00% (sunblock), SPF value of 21.10±1.46 (ultra-protection) and potentially better than benzophenone-3 as a standard sunscreen. Then, disk diffusion testing showed that the compound had weak antibacterial activity against Staphylococcus aureus and did not show antibacterial activity against Escherichia coli bacteria at test concentrations of 30, 60, and 120 µg/disk.
18
Wangchuk, Phurpa, Paul A. Keller, Stephen G. Pyne, Malai Taweechotipatr, and Sumalee Kamchonwongpaisan. "GC/GC-MS Analysis, Isolation and Identification of Bioactive Essential Oil Components from the Bhutanese Medicinal Plant, Pleurospermum Amabile." Natural Product Communications 8, no. 9 (September 2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800930.
Full textAbstract:
We have hydrodistilled the essential oil (EO) from the aerial parts of the Bhutanese medicinal plant, Pleurospermum amabile using a Clevenger apparatus and evaluated this EO by GC/GC-MS and NMR analysis followed by testing for bioactivity. The GC-MS analysis identified 52 compounds with ( E)-isomyristicin as a major component (32.2%). Repeated purification yielded four compounds; ( E)-isomyristicin (1), ( E)-isoapiol (2), methyl eugenol (3) and ( E)-isoelemicin (4). Compound 2 and the mother EO showed the best antiplasmodial activity against the Plasmodium falciparum strains, TM4/8.2 (chloroquine and antifolate sensitive) and K1CB1 (multidrug resistant). They exhibited mild antibacterial activity against Bacillus subtilis. None of the test samples showed cytotoxicity.
19
Santos Oliveira, Ana Júlia de Morais, Ricardo Dias de Castro, Hilzeth de Luna Freire Pessôa, Abdul Wadood, and Damião Pergentino de Sousa. "Amides Derived from Vanillic Acid: Coupling Reactions, Antimicrobial Evaluation, and Molecular Docking." BioMed Research International 2019 (April 15, 2019): 1–11. http://dx.doi.org/10.1155/2019/9209676.
Full textAbstract:
A series of amides derived from vanillic acid were obtained by coupling reactions using PyBOP ((Benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate) and DCC (Dicyclohexylcarbodiimide) coupling reagents. These were submitted to biological evaluation for species of Candida, Staphylococcus, and Pseudomonas. The microdilution method in broth was used for the antimicrobial testing to determine the Minimum Inhibitory Concentration (MIC) and to verify the likely mechanism of action for antifungal activity. The ten amides were obtained with yields ranging from 28.81 to 86.44%, and three compounds were novel. In the antibacterial evaluation, the amides (in their greatest concentrations) were bioactive against Staphylococcus aureus strain ATCC 25925. Meanwhile, all of the tested amides presented antifungal activity against at least one strain. The amide with best antifungal profile was compound 7, which featured an MIC of 0.46 μmol/mL, and a mechanism of action involving the plasma membrane and fungal cell wall. The presence of a methyl group in the para position of the aromatic ring is suggested which enhances the activity of the compound against fungi. Docking studies of the ten compounds using the protein 14α-demethylase as a biological target were also performed. The biological results presented good correlation with molecular docking studies demonstrating that a possible site of antifungal action for bioactive amides is the enzyme 14α-demethylase.
20
Tharrun Daniel Paul L, Roshan Kumar Sah, and Thirunavukkarasu Palaniyandi. "Molecular docking studies of pancreatic cancer expressed proteins with Psidium guajava (guava) derived bioactive compounds." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 21, 2020): 3176–83. http://dx.doi.org/10.26452/ijrps.v11ispl4.4664.
Full textAbstract:
The current study evaluates the binding affinities (kcal/mol) of different proteins expressed in pancreatic cancer with Psidium guajava derived bioactive compounds by performing molecular docking through auto dock vina. Auto dock vina was used to perform molecular docking between the proteins expressed in pancreatic cancer and P. guajava derived bioactive compounds. Nine proteins and nine ligands were chosen for molecular docking. Among the nine ligands, gemcitabine which is a commercial first-line drug used to treat pancreatic cancer, was selected. The docking output was visualized using the Biovia Discovery Studio visualizer. From the docking results, we found that, out of the nine ligands, quercetin had a better binding affinity than the other ligands and the commercial drug (gemcitabine). SNAI1 docked with quercetin had a binding affinity of -9.6 kcal/mol, which was found to be the highest. In conclusion, it can be said that the compound quercetin derived from the ethanolic extract of the P. guajava has the highest binding affinity, so it can be used for the treatment of pancreatic cancer after modification to its properties so that it has good efficacy and pharmacokinetic properties. Further studies will be based on the in-vitro testing of the extract and gene and protein expression analysis using RT-PCR and MALDI-TOF, respectively.
21
Brkljača, Robert, and Sylvia Urban. "Rapid Dereplication and Identification of the Bioactive Constituents from the Fungus, Leucocoprinus birnbaumii." Natural Product Communications 10, no. 1 (January 2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000124.
Full textAbstract:
A series of fatty acids were rapidly dereplicated and partially identified from the flowerpot fungus, Leucocoprinus birnbaumii using HPLC-NMR and HPLC-MS. Subsequent off-line isolation unequivocally established the structures, and anti-microbial testing concluded that the fatty acids displayed moderate but selective anti-microbial activity. This represents the first report of these compounds occurring in this particular terrestrial fungus.
22
Suhendar, Usep, Muhammad Fathurrahman, and Sogandi Sogandi. "Antibacterial Activity and Mechanism of Action of Methanol Extract from Kasturi Mango Fruit (Mangifera casturi) on Caries-Causing Bacterium Streptococcus mutans." Jurnal Kimia Sains dan Aplikasi 22, no. 6 (October 16, 2019): 235–41. http://dx.doi.org/10.14710/jksa.22.6.235-241.
Full textAbstract:
One of the problems frequently found in the oral cavity is dental caries caused by Streptococcus mutans. Thus far, dental caries is treated using antibiotics. However, the bacterium is known to be resistant to many antibiotics; hence, another alternative is needed. An alternative option is found in the Kasturi mango (Mangifera casturi). This study aims to identify the bioactive compounds of Kasturi mango and find out the mechanism of its action in inhibiting the growth of Streptococcus mutans. Kasturi mangoes were macerated using 96% methanol, then the phytochemical compounds were identified qualitatively. Antibacterial activity testing was carried out using the agar diffusion method, and bioactive compounds were identified using GCMS. The results showed that the methanol extract of Kasturi mango contains alkaloids, flavonoids, phenolics, terpenoids, and saponins. In 1 gr/mL of the methanol extract of Kasturi mango fruit has an inhibitory activity against the growth of Streptococcus mutans with a zone of inhibition of ± 10 mm and MIC (minimum inhibitory concentration) value of 25% extract. The inhibitory action is suspected to be through a mechanism where holes in the bacterial cell membrane are made. This can be seen from the results of SEM (scanning electron microscope) images showing that cell leakage or lysis has occurred. This research also, for the first time, revealed the types of bioactive compounds from the methanol extracts of Kasturi mango (Mangifera casturi) consisting of 18 compounds with the most abundance is 5-Hydroxymethylfurfural compounds, Octadecenoic acid, n-Hexadecanoic acid, Phenyl 4-methyl-1-piperidine carboxylate, and Methyl linolenate.
23
Hernández-Hernández, Cristian, Cristóbal Noé Aguilar, Adriana Carolina Flores-Gallegos, Leonardo Sepúlveda, Raúl Rodríguez-Herrera, Jesús Morlett-Chávez, Mayela Govea-Salas, and Juan Ascacio-Valdés. "Preliminary Testing of Ultrasound/Microwave-Assisted Extraction (U/M-AE) for the Isolation of Geraniin from Nephelium lappaceum L. (Mexican Variety) Peel." Processes 8, no. 5 (May 12, 2020): 572. http://dx.doi.org/10.3390/pr8050572.
Full textAbstract:
The rambutan peel (RP) is a relevant source of bioactive molecules, which could be used for application in cosmetics, food, and pharmaceutical areas. Total soluble polyphenol content was extracted from Mexican variety rambutan peels using an emergent ultrasound/microwave-assisted extraction (U/M-AE) technology. Five extractions were performed using different mass/volume and ethanol/water ratios; 1:16-0; 1:16-70; 1:8-0; 1:8-70; 1:12-30. Condition 1:16-0 was defined as the best extraction condition with 0% ethanol percentage (only water). The content of total soluble polyphenols was 307.57 mg/g. The total bound polyphenol content was 26.53 mg/g. Besides, two separation processes were made with the soluble fraction; the first one was performed using Amberlite XAD-16 (Sigma-Aldrich, Saint Louis, MO, USA), and seven polyphenolic compounds were obtained. The second one was performed using a preparative HPLC (Varian, Palo Alto, CA, USA) equipment obtained fraction where three compounds were obtained: geraniin (main compound), ellagic acid, and ellagic acid pentoside. The major compound isolated in the two separations was geraniin, according to HPLC/ESI/MS (High Performance Liquid Chromatography/ElectroSpray Ionization/Mass) analysis.
24
Luo, Yu-Syuan, Kyle C. Ferguson, Ivan Rusyn, and Weihsueh A. Chiu. "In Vitro Bioavailability of the Hydrocarbon Fractions of Dimethyl Sulfoxide Extracts of Petroleum Substances." Toxicological Sciences 174, no. 2 (February 10, 2020): 168–77. http://dx.doi.org/10.1093/toxsci/kfaa007.
Full textAbstract:
Abstract Determining the in vitro bioavailable concentration is a critical, yet unmet need to refine in vitro-to-in vivo extrapolation for unknown or variable composition, complex reaction product or biological material (UVCB) substances. UVCBs such as petroleum substances are commonly subjected to dimethyl sulfoxide (DMSO) extraction in order to retrieve the bioactive polycyclic aromatic compound (PAC) portion for in vitro testing. In addition to DMSO extraction, protein binding in cell culture media and dilution can all influence in vitro bioavailable concentrations of aliphatic and aromatic compounds in petroleum substances. However, these in vitro factors have not been fully characterized. In this study, we aimed to fill in these data gaps by characterizing the effects of these processes using both a defined mixture of analytical standards containing aliphatic and aromatic hydrocarbons, as well as 4 refined petroleum products as prototypical examples of UVCBs. Each substance was extracted with DMSO, and the protein binding in cell culture media was measured by using solid-phase microextraction. Semiquantitative analysis for aliphatic and aromatic compounds was achieved via gas chromatography-mass spectrometry. Our results showed that DMSO selectively extracted PACs from test substances, and that chemical profiles of PACs across molecular classes remained consistent after extraction. With respect to protein binding, chemical profiles were retained at a lower dilution (higher concentration), but a greater dilution factor (ie, lower concentration) resulted in higher protein binding in cell medium, which in turn altered the ultimate chemical profile of bioavailable PACs. Overall, this case study demonstrates that extraction procedures, protein binding in cell culture media, and dilution factors prior to in vitro testing can all contribute to determining the final bioavailable concentrations of bioactive constituents of UVCBs in vitro. Thus, in vitro-to-in vivo extrapolation for UVCBs may require greater attention to the concentration-dependent and compound-specific differences in recovery and bioavailability.
25
Klevenhusen, F., K. Deckardt, Ö. Sizmaz, S. Wimmer, A. Muro-Reyes, R. Khiaosa-ard, R. Chizzola, and Q. Zebeli. "Effects of black seed oil and Ferula elaeochytris supplementation on ruminal fermentation as tested in vitro with the rumen simulation technique (Rusitec)." Animal Production Science 55, no. 6 (2015): 736. http://dx.doi.org/10.1071/an13332.
Full textAbstract:
Plant bioactive compounds are currently viewed as possible feed additives in terms of methane mitigation and improvement of ruminal fermentation. A range of analyses, including the botanical characterisation, chemical composition and in vitro efficiency, have to be conducted before testing the compounds in vivo. Therefore, the aims of this study were (1) to identify the main bioactive components of black seed (Nigella sativa) oil (BO) and of the root powder of Ferula elaeochytris (FE), and (2) to investigate their effects on ruminal fermentation in vitro, when supplemented in different dosages to a diet (1 : 1, forage : concentrate), using the rumen simulation technique (Rusitec). Main compounds of BO were thymoquinone and p-cymene and α-pinene in FE. Supplementation of the diet with BO and FE did not affect concentration of volatile fatty acids but ammonia concentrations decreased with both supplements (P < 0.001). No effects of supplements on protozoal counts were detected but in vitro disappearance of DM and organic matter tended to increase with 50 mg/L FE (P < 0.1), compared with the control.
26
Tsekouras, Vasileios, and Spyridon Kintzios. "Biotechnology of Viscum Album L. and Cancer Treatment: A Review." Current Bioactive Compounds 16, no. 6 (October 2, 2020): 738–46. http://dx.doi.org/10.2174/1573407215666190410151958.
Full textAbstract:
Background: This review aims to highlight biotechnological techniques applied for the identification, isolation and propagation of mistletoe-derived bioactive compounds and the preclinical evaluation of their anticancer properties. Methods: We undertook a structured search of bibliographic databases to identify and evaluate the literature, regarding biotechnology of mistletoe and malignancy treatment. The selected articles were classified into five modules according to the study design. Results: Firstly, we have provided an overview of the role of biotechnology in plant-derived pharmaceuticals, by reviewing twelve articles. Then, V. album L. botany and a retrospection of the plant pharmaceutical applications are presented from a set of ten articles. Subsequently, mistletoe derived compounds and their anticancer properties are highlighted, throughout sixty-two articles, which emphasized the mechanisms of antitumor action. The next module is referred to as the biosynthesis of mistletoe bioactive compounds, covering nine cases of ‘in vitro’ propagation and genetic manipulation. Finally, fourteen assays regarding mistletoe preparations and preclinical testing for chemosensitivity are presented. Conclusion: Biotechnology provides essential tools for the identification, production and evaluation of anticancer compounds derived from Viscum album L. The preclinical studies indicate the potential use of V. album preparations in chemotherapy but further research is essential for standardizing the therapeutic benefits of mistletoe compounds in the treatment of malignancies.
27
Seukep, Armel Jackson, Minxia Fan, Satyajit Dey Sarker, Victor Kuete, and Ming-Quan Guo. "Plukenetia huayllabambana Fruits: Analysis of Bioactive Compounds, Antibacterial Activity and Relative Action Mechanisms." Plants 9, no. 9 (August 28, 2020): 1111. http://dx.doi.org/10.3390/plants9091111.
Full textAbstract:
Plukenetia huayllabambana is an edible plant traditionally used to cure wounds and various infections. The present work assessed, for the first time, the antibacterial efficacy of solvent fractions from P. huayllabambana fruits. The crude methanol extract was obtained applying ultrasound-assisted extraction, followed by partitioning through successive depletion among solvents of increasing polarity to yield fractions (n-hexane, dichloromethane, ethyl acetate, and n-butanol). The minimal inhibitory concentration (MIC) was determined following antibacterial testing, using the broth microdilution technique against a panel of drug-resistant Gram-negative and Gram-positive bacteria. Possible modes of action of the most active fraction were also investigated. Gas chromatography–mass spectrometry (GC–MS) was used to identify phytocompounds that may account for the recorded activities. Methanol, n-hexane (PH-n-Hex), and ethyl acetate extracts inhibited 100% of studied bacteria, with the recorded MIC ranging from 0.125–1 mg/mL. PH-n-Hex appeared as the most active partition, exerting a bacteriostatic effect. PH-n-Hex probably acts by interfering with bacterial biofilm formation, proton pumps, and bacterial cell membrane integrity. The GC–MS analysis of PH-n-Hex led to the identification of 11 potentially bioactive components, including fatty acids, phytosterol, and diterpene alcohol as major ones. P. huayllabambana can be considered as a plant of pharmacological value—a source of potent anti-infective drug entities.
28
Marrelli, Mariangela, Filomena Conforti, Daniela Rigano, Carmen Formisano, Maurizio Bruno, Felice Senatore, and Francesco Menichini. "Cytotoxic Properties of Marrubium globosum ssp. libanoticum and its Bioactive Components." Natural Product Communications 8, no. 5 (May 2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800503.
Full textAbstract:
Marrubium globosum Montbr. et Auch. ex Benth. ssp. libanoticum Boiss. (Lamiaceae) is a medicinal plant used in Lebanon for the treatment of inflammatory diseases, asthma, coughs and other pulmonary and urinary problems. The goal of our study was to assess the biological activity of M. globosum by testing different extracts of the aerial parts for their antiproliferative activity against human melanoma cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The chloroform fraction showed the greatest activity. The compounds isolated from the extracts were also tested: the mixture of (13 S)-9α,13α-epoxylabda-6β(19),16(15)-diol dilactone and (13 R)-9α,13α-epoxylabda-6β(19),16(15)-diol dilactone was the most active fraction, with an IC50 value of 29.2 ± 0.06 μg/mL.
29
McCallum, Megan M., Premchendar Nandhikonda, Jonathan J. Temmer, Charles Eyermann, Anton Simeonov, Ajit Jadhav, Adam Yasgar, David Maloney, and Alexander (Leggy) Arnold. "High-Throughput Identification of Promiscuous Inhibitors from Screening Libraries with the Use of a Thiol-Containing Fluorescent Probe." Journal of Biomolecular Screening 18, no. 6 (February 27, 2013): 705–13. http://dx.doi.org/10.1177/1087057113476090.
Full textAbstract:
Testing small molecules for their ability to modify cysteine residues of proteins in the early stages of drug discovery is expected to accelerate our ability to develop more selective drugs with lesser side effects. In addition, this approach also enables the rapid evaluation of the mode of binding of new drug candidates with respect to thiol reactivity and metabolism by glutathione. Herein, we describe the development of a fluorescence-based high-throughput assay that allows the identification of thiol-reactive compounds. A thiol-containing fluorescent probe, MSTI, was synthesized and used to evaluate small molecules from the Library of Pharmacologically Active Compounds (LOPAC) collection of bioactive molecules. LOPAC compounds that are known to react with sulfur nucleophiles were identified with this assay, for example, irreversible protease inhibitors, nitric oxide–releasing compounds, and proton-pump inhibitors. The results confirm that both electrophilic and redox reactive compounds can be quickly identified in a high-throughput manner, enabling the assessment of screening libraries with respect to thiol-reactive compounds.
30
Celano, Rita, Teresa Docimo, Anna Lisa Piccinelli, Patrizia Gazzerro, Marina Tucci, Rosa Di Sanzo, Sonia Carabetta, Luca Campone, Mariateresa Russo, and Luca Rastrelli. "Onion Peel: Turning a Food Waste into a Resource." Antioxidants 10, no. 2 (February 16, 2021): 304. http://dx.doi.org/10.3390/antiox10020304.
Full textAbstract:
Food waste is a serious problem for food processing industries, especially when it represents a loss of a valuable source of nutrients and phytochemicals. Increasing consumer demand for processed food poses the problem of minimizing waste by conversion into useful products. In this regard, onion (Allium cepa) waste consisting mainly of onion skin is rich in bioactive phenolic compounds. Here, we characterized the flavonoid profiles and biological activities of onion skin wastes of two traditional varieties with protected geographical indication (PGI), the red “Rossa di Tropea” and the coppery “Ramata di Montoro”, typically cultivated in a niche area in southern Italy. The phytochemical profiles of exhaustive extracts, characterized by ultra-high-performance liquid chromatography coupled with ultraviolet (UV) detection and high-resolution mass spectrometry, revealed that flavonols and anthocyanins were the characteristic metabolite classes of onion skins. Quercetin, quercetin glucosides and their dimer and trimer derivatives, and, among anthocyanins, cyanidin 3-glucoside, were the most abundant bioactive compounds. The potential of onion skins was evaluated by testing several biological activities: ABTS/oxygen radical absorbance capacity (ORAC) and in vitro alpha-glucosidase assays were performed to evaluate the antioxidant and anti-diabetic properties of the extracts and of their main compounds, respectively, and proliferative activity was evaluated by MTT assay on human fibroblasts. In the present study, by observing various biological properties of “Rossa di Tropea” and “Ramata di Montoro” onion-dried skins, we clearly indicated that this agricultural waste can provide bioactive molecules for multiple applications, from industrial to nutraceutical and cosmetical sectors.
31
Tejman-Yarden, Noa, Yukiko Miyamoto, David Leitsch, Jennifer Santini, Anjan Debnath, Jiri Gut, James H. McKerrow, Sharon L. Reed, and Lars Eckmann. "A Reprofiled Drug, Auranofin, Is Effective against Metronidazole-Resistant Giardia lamblia." Antimicrobial Agents and Chemotherapy 57, no. 5 (February 12, 2013): 2029–35. http://dx.doi.org/10.1128/aac.01675-12.
Full textAbstract:
ABSTRACTGiardiasis is one of the most common causes of diarrheal disease worldwide. Treatment is primarily with 5-nitro antimicrobials, particularly metronidazole. Resistance to metronidazole has been described, and treatment failures can occur in up to 20% of cases, making development of alternative antigiardials an important goal. To this end, we have screened a chemical library of 746 approved human drugs and 164 additional bioactive compounds for activity againstGiardia lamblia. We identified 56 compounds that caused significant inhibition ofG. lambliagrowth and attachment. Of these, 15 were previously reported to have antigiardial activity, 20 were bioactive but not approved for human use, and 21 were drugs approved for human use for other indications. One notable compound of the last group was the antirheumatic drug auranofin. Further testing revealed that auranofin was active in the low (4 to 6)-micromolar range against a range of divergentG. lambliaisolates representing both human-pathogenic assemblages A and B. Most importantly, auranofin was active against multiple metronidazole-resistant strains. Mechanistically, auranofin blocked the activity of giardial thioredoxin oxidoreductase, a critical enzyme involved in maintaining normal protein function and combating oxidative damage, suggesting that this inhibition contributes to the antigiardial activity. Furthermore, auranofin was efficaciousin vivo, as it eradicated infection with differentG. lambliaisolates in different rodent models. These results indicate that the approved human drug auranofin could be developed as a novel agent in the armamentarium of antigiardial drugs, particularly against metronidazole-resistant strains.
32
Br Karo, Reh Malem, Putranto Manalu, and Jhon Patar Sinurat. "Antibacterial Activity of Flavonoid-Rich Fractions Of Citrus Maxima Peel Extract." Stannum : Jurnal Sains dan Terapan Kimia 2, no. 2 (October 31, 2020): 16–21. http://dx.doi.org/10.33019/jstk.v2i2.1977.
Full textAbstract:
Natural products can be used as an alternative in the treatment of various diseases such as infectious diseases due to the bioactive compounds contained therein. Moreover nowdays, there are many antibiotic resistance in the treatment of infectious diseases. Citrus maxima is one of the natural products. Citrus maxima have been used for many diseases in traditional medicine.The aim of this study was to investigate the antibacterial activity of flavonoid-rich fractions of citrus maxima peel extract. The bioactive compounds contained in Citrus maxima peel were extracted by maceration method using 96% ethanol solvent. Fractionation was conducted using liquid-liquid extraction using a solvent of water and ethyl acetate obtained ethyl acetate fraction. In this fraction, the TLC test was carried out to confirm the presence of phenolic and flavonoid compounds. The antibacterial activity testing for ethyl acetate fraction against S.aureus and E.coli was determined by disk diffusion method with concentration of 25 ppm, 50 ppm, 75 ppm and 100 ppm. The ciprofloxacin and distilled water were used as positive and negative control, respectively. The result of this study showed that ethyl acetate fraction ( flavonoid-rich fractions) Of Citrus Maxima has potential as antibacterial for bacterial S.aureus and E.coli with medium inhibitory ability in all of concentration ranges. The highest inhibition zone for S.aureus was found at a concentration of 100 ppm while for E.coli was at a concentration of 75 ppm.
33
Klöppel, Anne, Franz Brümmer, Denise Schwabe, and Gertrud Morlock. "Detection of Bioactive Compounds in the Mucus Nets ofDendropoma maxima, Sowerby 1825 (Prosobranch Gastropod Vermetidae, Mollusca)." Journal of Marine Biology 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/283506.
Full textAbstract:
The sessile suspension-feeding wormsnailDendropoma maxima, Sowerby 1825 (Vermetidae) secretes a mucus net to capture planktonic prey. The nets are spread out over the corals and often have remarkable deleterious effects on them like changes in growth form and pigmentation shifts not uncommonly resulting in tissue necrosis. Until now, there is no explanation for this phenomenon although the indication as well as theories about its genesis is mentioned in several publications. Vermetids are well studied concerning the intraspecific competition with neighboring individuals but not in their interaction with other taxa like corals or fish. We did extensivein situvideo recording and observed that fish avoided the plankton-load nets although several specialized taxa are known to be molluscivores, mucivores, and/or feed on plankton. As many molluscs use chemical weapons to combat feeding pressure and to defend themselves against predators, we screened empty and plankton-load mucus nets for potential bioactive metabolites. Bioactivity testing was performed with a recently developed system based on a chromatographic separation (high-performance thin-layer chromatography (HPTLC)) and a bioassay with luminescent bacteriaVibrio fischeri. Thus, we found at least two active compounds exclusively accumulated by the wormsnails themselves. This is the first record of bioactive properties in the whole family of Vermetidae.
34
Henning, Susanne, Jeraldine Guzman, Jason Li, Gail Thames, Jenny Kim, and Zhaoping Li. "Protocol for Pilot Study Testing the Effect of Avocado Consumption on Skin Aging." Current Developments in Nutrition 5, Supplement_2 (June 2021): 1279. http://dx.doi.org/10.1093/cdn/nzab057_009.
Full textAbstract:
Abstract Objectives Avocados are an excellent source of bioactive compounds such as monounsaturated fatty acids, sterols, polyhydroxylated fatty alcohols and carotenoids. A common cause of photoaging is exposure to UV light, as the radiation generates oxidative stress, which leads to inflammation and erythema of the skin. Studies have demonstrated that topical application of bioactive compounds from avocado reduce UVB-induced photoaging. Ultraviolet-B (UVB) protection by oral avocado consumption has not been clinically investigated in humans. Therefore, it is the objective of this pilot study to determine if the consumption of one avocado daily for 16 weeks can increase resistance to UVB radiation and reduce skin aging in healthy women. Methods This study is a randomized, two arm, parallel group comparison of daily avocado consumption vs. habitual diet. Eligible participants are females, at least 25 years of age, Fitzpatrick Skin type II-IV, in good health with an increased waist circumference of 35 cm. Participants will be excluded if they are habitually eating 2 avocados per month, allergic to avocado and any unstable medical conditions. At screening, informed consent and HIPAA authorization will be reviewed and signed. In addition, Fitzpatrick Skin type and response to UVB will be assessed. Subjects will consume 1 avocado a day (Hass Avocado) or maintain habitual diet (up to 2 avocados/month) daily for 16 weeks. Skin will be assessed at weeks 0, 8 and 16. Minimal erythema dose (MED) will be determined by exposing the inner arm covered by a sleeve with 6 cut out windows with an increasing dose of UVB using the Dermalight 90. Facial melanin index, hydration and sebum will be determined using the mexameter MA18, corneometer CM825 and sebumeter SM815 probes attached to the Cutometer dual MPA 580 (Courage&Khazaka electronic GmbH, Koeln, Germany). 22 participants will be enrolled in each group considering a 10%dropout rate. Results Primary outcome will be the effect of daily avocado consumption on MED assessed by UVB exposure compared to habitual diet. Secondary outcomes will be the effect of daily avocado consumption on facial skin elasticity, sebum, melanin and hydration status as assessed by cutometer compared to habitual diet. Conclusions This study is currently recruiting participants. Funding Sources Hass Avocado Board.
35
Hwang, Seung Hwan, Zhiqiang Wang, Yanymee N. Guillen Quispe, Soon Sung Lim, and Jae Myung Yu. "Evaluation of Aldose Reductase, Protein Glycation, and Antioxidant Inhibitory Activities of Bioactive Flavonoids in Matricaria recutita L. and Their Structure-Activity Relationship." Journal of Diabetes Research 2018 (2018): 1–11. http://dx.doi.org/10.1155/2018/3276162.
Full textAbstract:
The inhibitory activities of Matricaria recutita L. 70% methanol extract were evaluated by isolating and testing 10 of its compounds on rat lens aldose reductase (RLAR), advanced glycation end products (AGEs), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging. Among these compounds, apigenin-7-O-β-D-glucoside, luteolin-7-O-β-D-glucoside, apigenin-7-O-β-D-glucuronide, luteolin-7-O-β-D-glucuronide, 3,5-O-di-caffeoylquinic acid, apigenin, and luteolin showed potent inhibition, and their IC50 values in RLAR were 4.25, 1.12, 1.16, 0.85, 0.72, 1.72, and 1.42 μM, respectively. Furthermore, these compounds suppressed sorbitol accumulation in rat lens under high-glucose conditions, demonstrating their potential to prevent sorbitol accumulation ex vivo. Notably, luteolin-7-O-β-D-glucuronide and luteolin showed antioxidative as well as AGE-inhibitory activities (IC50 values of these compounds in AGEs were 3.39 and 6.01 μM). These results suggest that the M. recutita extract and its constituents may be promising agents for use in the prevention or treatment of diabetic complications.
36
Sami, F. J., N. H. Soekamto, Firdaus, and J. Latip. "Bioactivity profile of three types of seaweed as an antioxidant, UV-protection as sunscreen and their correlation activity." Food Research 5, no. 1 (February 13, 2021): 441–47. http://dx.doi.org/10.26656/fr.2017.5(1).389.
Full textAbstract:
Seaweed is one of the marine algae that have antioxidant sources because it contains bioactive compounds such as carotenoids, phenol compounds and their derivatives, polysaccharide sulfate, and vitamins. Algae consist of three major groups namely brown algae (phaeophyta), red algae (rhodophyta), and green algae (chlorophyta). The purpose of this study was to determine the bioactivity profile of seaweed extract Eucheuma cottoni, Sargassum polycystum and Caulerpa racemosa so that it could be developed as a cosmetic raw material. The three types of seaweed were extracted by maceration and bioactivity testing was carried out as an antioxidant using the ABTS radical reduction method and bioactivity testing as UV-protection with the parameters of the percentage transmission of erythema, pigmentation and Sun Protective Factor (SPF). The results showed that C. racemosa extract provided a very strong antioxidant activity and was able to protect the skin from UV exposure with an SPF value that was categorized as ultra-protection. Antioxidant activity of the three types of seaweed is positively correlated to the protective effect based on the SPF value.
37
Buciński, A., H. Zieliński, and H. Kozłowska. "Prediction of the kind of sprouts of Cruciferae family based on artificial neural network analysis." Czech Journal of Food Sciences 25, No. 4 (January 7, 2008): 189–94. http://dx.doi.org/10.17221/734-cjfs.
Full textAbstract:
The aim of this work was to show that artificial neural networks (ANNs) are a convenient tool for predicting the kind of sprouts originated from <i>Cruciferae<i> family. For this purpose, the known contents of bioactive compounds of small radish, radish, white mustard, and rapeseed seeds and sprouts were used for the prediction of the kind of a specific sprout. The input data reflected the contents of the following compounds in cruciferous seeds in the course of germination: soluble proteins (SP), ascorbic acid (AH<sub>2</sub>), total glucosinolates (GLS), reduced glutathione (GSH), and tocopherols (α-T, β-T, γ-T, δ-T), expressed in their biological activity. The ANN used was trained on the learning set. The ability of the utilised ANN to generalise the gained knowledge based on the learning set was verified by the validating and testing sets. The trained and validated ANN was able to classify, with complete accuracy, the kind of sprouts out of the four kinds used. It can be concluded that ANN can be used as a useful tool for determining the identity of cruciferous seeds and sprouts based on the determined levels of their bioactive components.
38
Guerrini, Alessandra, Gianni Sacchetti, Alessandro Grandini, Antonella Spagnoletti, Mercedes Asanza, and Laura Scalvenzi. "Cytotoxic Effect and TLC Bioautography-Guided Approach to Detect Health Properties of AmazonianHedyosmum spruceiEssential Oil." Evidence-Based Complementary and Alternative Medicine 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/1638342.
Full textAbstract:
Bioautography has been used as rapid and easy strategy to detect and identify bioactive fractions/molecules in the never before investigatedHedyosmum spruceiSolms (Chloranthaceae) essential oil (EO). The antioxidant activity, performed through DPPH bioautographic assay and spectrophotometric evaluations (IC50= 230 ± 10 µg/mL), seemed to be mainly due toα-cadinol andα-muurolol. (HP)TLC bioautography, focused on antimicrobial capacities, pointed outα-cadinol,α-muurolol,τ-muurolol, caryophyllene oxide, and methyleugenol as the most effective compounds againstStaphylococcus aureus, considered as testing strain. Moreover, the microdilution method, assessed among a wide panel of microorganisms, revealedListeria grayiandStaphylococcus aureusas the most sensitive among human tested strains andClavibacter michiganensisamong phytopathogens. GC-MS chemical profile showed that bioactive molecules represented only a small quantity of the whole EO: germacrene D (23.16%),β-caryophyllene (15.53%),δ-cadinene (5.50%),α-copaene (5.08%), andα-phellandrene (3.48%) were the main compounds, highlighting an uncommon composition among the genusHedyosmum. Finally,H. spruceiEO was checked for cytotoxic potential against A549 (lung cancer) and MCF-7 (breast cancer) cell lines showing promising cytotoxic effects against both cell lines after 48 h (IC50A549 = 44.05 ± 2.35 µg/mL; IC50MCF-7 = 32.76 ± 4.92 µg/mL) and 72 h (IC50A549 = 43.55 ± 2.80 µg/mL; IC50MCF-7 = 33.64 ± 0.43 µg/mL).
39
Yahya, Galal, Asmaa Ebada, Eman M. Khalaf, Basem Mansour, Nehal A. Nouh, Rasha A. Mosbah, Sameh Saber, et al. "Soil-Associated Bacillus Species: A Reservoir of Bioactive Compounds with Potential Therapeutic Activity against Human Pathogens." Microorganisms 9, no. 6 (May 24, 2021): 1131. http://dx.doi.org/10.3390/microorganisms9061131.
Full textAbstract:
Soil hosts myriads of living organisms with the extensive potential to produce bioactive compounds. Bacteria are the major soil inhabitants that represent a rich reservoir for antibiotic production along with their role in recycling nutrients and maintenance of the soil ecosystem. Here, from 55 tested soil samples, we isolated and identified a novel antibiotic-producing bacterial strain with a phylogenetically closest match to Bacillus subtilis sp. based on BLASTN search of GenBank for the 16S rRNA gene sequence. We characterized this novel strain through microscopic, biochemical, and molecular techniques, combined with testing its potential antimicrobial activity. Chemical studies revealed that the antibiotic produced by this strain is a glycopeptide. It exhibited profound activity against both methicillin-resistant Staphylococcus aureus (MRSA) and Candida albicans. The antibiotic is optimally produced at 37 °C after 28 h of growth. The biocompatibility of the extracted antibiotic was tested over a wide range of factors including temperature, pH, surfactants, and metal salts. To confirm its therapeutic potential, a sterile solution of the antibiotic was tested in vivo against bacteria-induced keratitis in rats where significant healing activity was recorded. Hence, this soil Bacillus strain may lead to the development of novel antibiotics for the treatment of human pathogens.
40
Fahdi, Firdaus, Harwitavia Harwitavia, and Herviani Sari. "UJI AKTIVITAS ANTIBAKTERI DARI EKSTRAK ETANOL DAUN PERIA LAUT (Colubrina Asiatica L.) TERHADAP BAKTERI STAPHYLOCOCCUS AUREUS DAN ESCHERICHIA COLI." Jurnal Penelitian Farmasi & Herbal 2, no. 1 (November 4, 2019): 14–18. http://dx.doi.org/10.36656/jpfh.v2i1.201.
Full textAbstract:
The discovery of new antibiotic drugs is getting more and more reactive. The plant of the peria laut leaf is one of the drugs that is often used as a traditional medicine and contains bioactive compounds of polyphenols, flavonoids, and saponins, which can inhibit antibacterial growth. Purpose of this study was to determine the antibacterial activity of ethanol extract of peria laut leaves (Colubrina asiatica L.) against Staphylococcus aureus and Escherichia coli bacteria. Method the experimental, of the sample used was concentrated marine peria laut leaf extract of 25mg/ml, 50mg/ml, 75mg/ml, 100mg/ml, 200mg/ml, 300mg/ml, 400mg/ml, and 500mg/ml, positive control of amoxicillin tablet 500 mg, negative control of dimethylsulfoxide with the method of disc diffusion testing using media Nutrient Agar. Results the showed thet the peria laut leaf extract positively contained bioactive alkaloid compounds, flavonoids, saponins, steroids, and tannins, and had inhibitory effects on Staphylococcus aureus and Escgerichia coli bacteria with various concentrations which had been tested on the average area of the highest inhibition zone of 18,6 mm in Staphylococcus aureus bacteria, and 10,2 mm in Escherichia coli bacteria. Conclusion peria laut leaf extract (Colubrina asiatica L.) has antibacterial activity against Staphylococcus aureus and Escherichia coli bacteria in the most inhibitory zone at a concentration of 500mg/ml with a diameter of 18,6 in Staphylococcus aureus bacteria and 10,2 in Escherichia coli.
41
Fahdi, Firdaus, Harwitavia Harwitavia, and Herviani Sari. "UJI AKTIVITAS ANTIBAKTERI DARI EKSTRAK ETANOL DAUN PERIA LAUT (Colubrina Asiatica L.) TERHADAP BAKTERI STAPHYLOCOCCUS AUREUS DAN ESCHERICHIA COLI." Jurnal Penelitian Farmasi & Herbal 2, no. 1 (October 30, 2019): 19–23. http://dx.doi.org/10.36656/jpfh.v2i1.77.
Full textAbstract:
The discovery of new antibiotic drugs is getting more and more reactive. The plant of the peria laut leaf is one of the drugs that is often used as a traditional medicine and contains bioactive compounds of polyphenols, flavonoids, and saponins, which can inhibit antibacterial growth. Purpose of this study was to determine the antibacterial activity of ethanol extract of peria laut leaves (Colubrina asiatica L.) against Staphylococcus aureus and Escherichia coli bacteria. Method the experimental, of the sample used was concentrated marine peria laut leaf extract of 25mg/ml, 50mg/ml, 75mg/ml, 100mg/ml, 200mg/ml, 300mg/ml, 400mg/ml, and 500mg/ml, positive control of amoxicillin tablet 500 mg, negative control of dimethylsulfoxide with the method of disc diffusion testing using media Nutrient Agar. Results the showed thet the peria laut leaf extract positively contained bioactive alkaloid compounds, flavonoids, saponins, steroids, and tannins, and had inhibitory effects on Staphylococcus aureus and Escgerichia coli bacteria with various concentrations which had been tested on the average area of the highest inhibition zone of 18,6 mm in Staphylococcus aureus bacteria, and 10,2 mm in Escherichia coli bacteria. Conclusion peria laut leaf extract (Colubrina asiatica L.) has antibacterial activity against Staphylococcus aureus and Escherichia coli bacteria in the most inhibitory zone at a concentration of 500mg/ml with a diameter of 18,6 in Staphylococcus aureus bacteria and 10,2 in Escherichia coli.
42
Kumar, P. Shamsher, E. Radha Krishna, P. Sujatha, and B. Veerendra Kumar. "Screening and Isolation of Associated Bioactive Microorganisms fromFasciospongia cavernosafrom of Visakhapatnam Coast, Bay of Bengal." E-Journal of Chemistry 9, no. 4 (2012): 2166–76. http://dx.doi.org/10.1155/2012/873203.
Full textAbstract:
Nature, especially the marine environment, provides the most effective drugs used in human therapy. Among the metazoans, the marine sponges produce the most potent and highly selective bioactive secondary metabolites. These animals (or their associated symbiotic microorganisms) synthesize secondary metabolites whose activity and selectivity has developed during their long evolutionary history. During the course of exploitation of these resources two marine sponges,Fasciospongia cavernosa doc var.brown (dark brown) Fasciospongia cavernosa doc var.yellow (yellow)collected from the visakhapatnam coast of Bay of Bengal were investigated in order to assess the potential of these microorganisms for the production of antimicrobial compounds. The aqueous and organic extracts of both the sponges showed broad spectrum antibiotic activity. In this study a total of 178 microorganisms were isolated from different parts of two sponges and most of them from middle part of the sponge. The isolates were investigated in order to assess the potential of these microorganisms for the production of antimicrobial compounds. Testing for antimicrobial activities were performed against Gram-positive (Staphylococcus aureus, Bacillus subtilis, Bacillus cereus) Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli, Proteus vulgaris), fungi (Candida albicans, Aspergillus niger) and 10 pathogenic organisms. Resulting mean diameter of inhibition zones revealed isolates B4 & B6 were the most potent of all the isolates. The present study has revealed the presence of high numbers of diverse culturable microorganisms associated with the marine sponges from Visakhapatnam Coast of Bay of Bengal as well as their potential to produce bioactive metabolites.
43
Yang, Shih-Chun, Ching-Yun Hsu, Wei-Ling Chou, Jia-You Fang, and Shih-Yi Chuang. "Bioactive Agent Discovery from the Natural Compounds for the Treatment of Type 2 Diabetes Rat Model." Molecules 25, no. 23 (December 3, 2020): 5713. http://dx.doi.org/10.3390/molecules25235713.
Full textAbstract:
Diabetes mellitus is a well-known chronic metabolic disease that poses a long-term threat to human health and is characterized by a relative or absolute lack of insulin, resulting in hyperglycemia. Type 2 diabetes mellitus (T2DM) typically affects many metabolic pathways, resulting in β-cell dysfunction, insulin resistance, abnormal blood glucose levels, inflammatory processes, excessive oxidative reactions, and impaired lipid metabolism. It also leads to diabetes-related complications in many organ systems. Antidiabetic drugs have been approved for the treatment of hyperglycemia in T2DM; these are beneficial for glucose metabolism and promote weight loss, but have the risk of side effects, such as nausea or an upset stomach. A wide range of active components, derived from medicinal plants, such as alkaloids, flavonoids, polyphenol, quinones, and terpenoids may act as alternative sources of antidiabetic agents. They are usually attributed to improvements in pancreatic function by increasing insulin secretions or by reducing the intestinal absorption of glucose. Ease of availability, low cost, least undesirable side effects, and powerful pharmacological actions make plant-based preparations the key player of all available treatments. Based on the study of therapeutic reagents in the pathogenesis of humans, we use the appropriate animal models of T2DM to evaluate medicinal plant treatments. Many of the rat models have characteristics similar to those in humans and have the advantages of ease of genetic manipulation, a short breeding span, and access to physiological and invasive testing. In this review, we summarize the pathophysiological status of T2DM rat models and focus on several bioactive compounds from herbal medicine with different functional groups that exhibit therapeutic potential in the T2DM rat models, in turn, may guide future approach in treating diabetes with natural drugs.
44
Freile-Pelegrín, Yolanda, and Deniz Tasdemir. "Seaweeds to the rescue of forgotten diseases: a review." Botanica Marina 62, no. 3 (June 26, 2019): 211–26. http://dx.doi.org/10.1515/bot-2018-0071.
Full textAbstract:
Abstract Neglected tropical diseases (NTDs) are a group of diseases that are predominant in the poorest parts of the world affecting 1.4 billion people. The development of new drugs is urgently needed in order to combat these forgotten diseases. Natural products from marine organisms have been widely explored as a source of new bioactive molecules. However, despite their enormous potential in drug discovery, not even one seaweed-based molecule has entered pre-clinical testing for NTDs. This review gives an overview of the current status of algal natural products against NTDs. The list of compounds is by no means exhaustive, but covers the most important classes of active substances in marine algae against the most studied NTDs.
45
Nishimura, Moe, Hiroyuki Fuchino, Kaoru Takayanagi, Hitomi Kawakami, Hiroko Nakayama, Nobuo Kawahara, and Yasuhito Shimada. "Toxicity of Jegosaponins A and B from Styrax japonica Siebold et al. Zuccarini in Prostate Cancer Cells and Zebrafish Embryos Resulting from Increased Membrane Permeability." International Journal of Molecular Sciences 22, no. 12 (June 14, 2021): 6354. http://dx.doi.org/10.3390/ijms22126354.
Full textAbstract:
(1) Background: Screening of medicinal herbs is one of the most powerful approaches to identifying novel therapeutic molecules against many human diseases. To avoid potential harmful effects during medicinal use, toxicity testing is necessary in the early stages of drug discovery. The objective of this study was to identify the cytotoxic mechanisms of jegosaponin A and B from Styrax japonica Siebold et al. Zuccarini; (2) Methods: We screened Japanese medicinal herb extracts using PC-3 prostate cancer cells and found that a methanol extract isolated from the unripe fruit of Styrax japonica Siebold et al. Zuccarini (SJSZ) had an inhibitory effect on cell viability. We further performed fractionation assays with PC-3 cells and identified the bioactive compounds using LC/MS and NMR analysis. We clarified the toxic mechanisms of these compounds using PC-3 cells and zebrafish embryos; (3) Results: We identified two active molecules, jegosaponin A and jegosaponin B, in the inhibitory fractions of the methanol extract. These jegosaponins are toxic to zebrafish embryos during the early developmental stage. Jegosaponin A and B showed strong haemolytic activity in sheep defibrinated blood (EC50 = 2.1 μM, and 20.2 μM, respectively) and increased the cell membrane permeability in PC-3 cells and zebrafish embryos, which were identified using a membrane non-permeable DRAQ7, a fluorescent nucleus staining dye; (4) We identified the cytotoxic compounds jegosaponin A and B from SJSZ, which we showed to exhibit cell membrane disruptive properties using cell- and zebrafish-based testing.
46
Sülsen, Valeria P., Fernanda M. Frank, Silvia I. Cazorla, Claudia A. Anesini, Emilio L. Malchiodi, Blanca Freixa, Roser Vila, Liliana V. Muschietti, and Virginia S. Martino. "Trypanocidal and Leishmanicidal Activities of Sesquiterpene Lactones from Ambrosia tenuifolia Sprengel (Asteraceae)." Antimicrobial Agents and Chemotherapy 52, no. 7 (April 28, 2008): 2415–19. http://dx.doi.org/10.1128/aac.01630-07.
Full textAbstract:
ABSTRACT Bioassay-guided fractionation of the organic extract of Ambrosia tenuifolia Sprengel (Asteraceae) led to the isolation of two bioactive sesquiterpene lactones with significant trypanocidal and leishmanicidal activities. By spectroscopic methods (1H- and 13C-nuclear magnetic resonance, distortionless enhancement by polarization transfer, correlated spectroscopy, heteronuclear multiple-quantum coherence, electron impact-mass spectrometry, and infrared spectroscopy), these compounds were identified as psilostachyin and peruvin. Both compounds showed a marked in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes with 50% inhibitory concentration (IC50) values of less than 2 μg/ml. Psilostachyin exerted a significant in vitro activity against the trypomastigote forms of T. cruzi (IC50, 0.76 μg/ml) and was selected for in vivo testing. Psilostachyin-treated mice had a survival of 100% and lower parasitemia values than control mice. Both compounds were also tested on Leishmania sp. promastigotes: psilostachyin (IC50, 0.12 μg/ml) and peruvin (IC50, 0.39 μg/ml) exerted significant leishmanicidal activities. This is the first time that the trypanocidal and leishmanicidal activities of these compounds have been reported. The selectivity index (SI) was employed to evaluate the cytotoxic effect of lactones on T lymphocytes. Although the SIs of both compounds were high for T. cruzi epimastigotes, psilostachyin was more selective against trypomastigotes (SI, 33.8) while peruvin showed no specificity for this parasite. Both compounds presented high selectivity for Leishmania spp. The results shown herein suggest that psilostachyin and peruvin could be considered potential candidates for the development of new antiprotozoal agents against Chagas' disease and leishmaniasis.
47
Akhmetova, Vnira R., Nail S. Akhmadiev, Radik A. Zainullin, Veronika R. Khayrullina, Ekaterina S. Mescheryakova, and Natalia A. Glushkova. "Synthesis, in vitro and in silico studies of inhibitory activity towards α-amylase of bis-azole scaffolds linked by an alkylsulfanyl chain." Canadian Journal of Chemistry 98, no. 11 (November 2020): 725–35. http://dx.doi.org/10.1139/cjc-2019-0186.
Full textAbstract:
Twelve new α,ω-bis[(3,5-dimethylpyrazol-4-yl)methylsulfanyl]alkanes linked by alkyl, diethyl sulfide, and triethyl dioxide spacers were prepared by the multicomponent reaction of acetylacetone, formaldehyde, α,ω-dithiols, and monosubstituted hydrazines. Testing of these products for inhibition of α-amylase enzyme in vitro showed that bis(N-methylpyrazolylmethylsulfanyl)ethane 4a inhibits the enzyme by the competitive mechanism. Meanwhile, the water-soluble adduct of bis(isoxazolylmethylsulfanyl)ethane 2 with HCl (2·HCl) is a noncompetitive inhibitor. The molecular docking results attest to high complementarity between the test molecules and the enzymes such as α-amylases from Aspergillus niger and human pancreas. Bis-pyrazole compounds 1, 1·HCl, and 4a and bis-isoxazole compounds 2 and 2·HCl positioned in the active site of both α-amylases form two closely spaced clusters. For all cases, the bioactive conformations of the modeled ligands were identified, demonstrating high affinity of the bis-azoles (1, 1·HCl, 2, 2·HCl, 4a) to the enzymes. Hydrogen bonds stabilizing their position in both α-amylases active sites were identified.
48
SESTRAS, Radu E. "Introduction Pages." Notulae Scientia Biologicae 10, no. 1 (March 27, 2018): I—VI. http://dx.doi.org/10.15835/nsb10110272.
Full textAbstract:
Notulae Scientia Biologicae (http://www.notulaebiologicae.ro), Issue 1, Volume 10, 2018: The papers published in this issue (http://www.notulaebiologicae.ro/index.php/nsb/issue/current) represent interesting novelties in different topics of life science. Among the exciting researches, we invite you to find news about enhancing the resistance of watermelon; biodiversity within Mt. Hamiguitan Range Wildlife Sanctuary; bioactive compounds investigated in several species (Litsea glutinosa, Senna alata, etc.); new approaches for technical aspects for improving crops of interest (mass production of Spirulina, gamma radiation treatments on potato and sesame, testing banana peel as substrate); cytogenetic, forestry and carbon sequestration; reproductive behavior with significant embryological data. Notulae Scientia Biologicae journal has moved to online-only publication at the start of 2017. At the same time, we maintain our standard publication, as printed form, with 'classic' style - volume, issue, pagination.
49
Ortiz-Andrade, Rolffy, Jesús Alfredo Araujo-León, Amanda Sánchez-Recillas, Gabriel Navarrete-Vazquez, Avel Adolfo González-Sánchez, Sergio Hidalgo-Figueroa, Ángel Josabad Alonso-Castro, et al. "Toxicological Screening of Four Bioactive Citroflavonoids: In Vitro, In Vivo, and In Silico Approaches." Molecules 25, no. 24 (December 16, 2020): 5959. http://dx.doi.org/10.3390/molecules25245959.
Full textAbstract:
Many studies describe different pharmacological effects of flavonoids on experimental animals and humans. Nevertheless, few ones are confirming the safety of these compounds for therapeutic purposes. This study aimed to investigate the preclinical safety of naringenin, naringin, hesperidin, and quercetin by in vivo, in vitro, and in silico approaches. For this, an MTT-based cytotoxicity assay in VERO and MDCK cell lines was performed. In addition, acute toxicity was evaluated on Wistar rats by OECD Guidelines for the Testing of Chemicals (Test No. 423: Acute Oral Toxicity-Class Method). Furthermore, we used the ACD/Tox Suite to predict toxicological parameters such as hERG channel blockade, CYP450 inhibition, and acute toxicity in animals. The results showed that quercetin was slightly more cytotoxic on cell lines (IC50 of 219.44 ± 7.22 mM and 465.41 ± 7.44 mM, respectively) than the other citroflavonoids. All flavonoids exhibited an LD50 value > 2000 mg/kg, which classifies them as low-risk substances as OECD guidelines established. Similarly, predicted LD50 was LD50 > 300 to 2000 mg/kg for all flavonoids as acute toxicity assay estimated. Data suggests that all these flavonoids did not show significant toxicological effects, and they were classified as low-risk, useful substances for drug development.
50
Fredotović, Željana, Barbara Soldo, Matilda Šprung, Zvonimir Marijanović, Igor Jerković, and Jasna Puizina. "Comparison of Organosulfur and Amino Acid Composition between Triploid Onion Allium cornutum Clementi ex Visiani, 1842, and Common Onion Allium cepa L., and Evidences for Antiproliferative Activity of Their Extracts." Plants 9, no. 1 (January 13, 2020): 98. http://dx.doi.org/10.3390/plants9010098.
Full textAbstract:
Species that belong to the genus Allium have been widely used for human food and traditional medicine. Their beneficial health effects, as well as the specific aroma, are associated with their bioactive chemical compounds, such as sulfur compounds and flavonoids. Gas chromatography and mass spectrometry (GC–MS) and reverse-phase high-performance liquid chromatography (reverse-phase HPLC) were used to identify organosulfur and amino acid content of triploid hybrid onion, Allium cornutum Clement ex Visiani, 1842, and common onion, Allium cepa L. Allium extracts were tested for their antiproliferative activity in three human cancer cell lines (HeLa, HCT116, and U2OS). DNA fragmentation and DAPI staining analysis were performed on HeLa cells to evaluate the effect of extracts on DNA damage and cell morphology. The mRNA expression of p53, Bax, and Caspase-3 genes involved in apoptosis were analyzed by real-time PCR. Using GC–MS, 27 compounds were found in two Allium species headspaces. Differences were noted among the main compound abundance in the headspace (although the major thiols and disulfides were qualitatively identic in both Allium species) and dipropyl disulfide, diisopropyl trisulfide, and (Z)-prop-1-enyl propyl trisulfide were predominant sulfides. Identification of amino acids and their quantities were determined by reverse-phase HPLC. Most abundant amino acids in both onions were arginine (Arg) and glutamic acid (Glu). The results of cytotoxicity testing confirmed antiproliferative effects of both species. The DNA fragmentation assay, DAPI staining and real time PCR analysis confirmed that A. cornutum and A. cepa extracts induced apoptosis in HeLa cells. This study presents the evidence for possible therapeutic use of A. cornutum and A. cepa extracts against human cervical carcinoma cell line.