scholarly journals Microbial Transformation of Prenylquercetins by Mucor hiemalis

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 528 ◽  
Author(s):  
Fubo Han ◽  
Yina Xiao ◽  
Ik-Soo Lee
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Microbial Transformation ◽  
Mass Spectrometric ◽  
Microbial Metabolites ◽  
Mucor Hiemalis ◽  
Chemical Structures ◽  
Polar Metabolites ◽  
Anti Inflammatory ◽  
Derivatives Of

Quercetin, one of the most widely distributed flavonoids, has been found to show various biological activities including antioxidant, anticancer, and anti-inflammatory effects. It has been reported that bioactivity enhancement of flavonoids has often been closely associated with nuclear prenylation, as shown in 8-prenylquercetin and 5′-prenylquercetin. It has also been revealed in many studies that the biological activities of flavonoids could be improved after glucosylation. Three prenylated quercetins were prepared in this study, and microbial transformation was carried out in order to identify derivatives of prenylquercetins with increased water solubility and improved bioavailability. The fungus M. hiemalis was proved to be capable of converting prenylquercetins into more polar metabolites and was selected for preparative fermentation. Six novel glucosylated metabolites were obtained and their chemical structures were elucidated by NMR and mass spectrometric analyses. All the microbial metabolites showed improvement in water solubility.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

scholarly journals Competitive Biological Activities of Chitosan and Its Derivatives: Antimicrobial, Antioxidant, Anticancer, and Anti-Inflammatory Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Suyeon Kim
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Biological Properties ◽  
Biomedical Science ◽  
Amino Groups ◽  
Chitosan Oligosaccharides ◽  
Primary Amino ◽  
Anti Inflammatory ◽  
Key Functional Groups ◽  
Application Fields

Chitosan is obtained from alkaline deacetylation of chitin, and acetamide groups are transformed into primary amino groups during the deacetylation. The diverse biological activities of chitosan and its derivatives are extensively studied that allows to widening the application fields in various sectors especially in biomedical science. The biological properties of chitosan are strongly depending on the solubility in water and other solvents. Deacetylation degree (DDA) and molecular weight (MW) are the most decisive parameters on the bioactivities since the primary amino groups are the key functional groups of chitosan where permits to interact with other molecules. Higher DDA and lower MW of chitosan and chitosan derivatives demonstrated higher antimicrobial, antioxidant, and anticancer capacities. Therefore, the chitosan oligosaccharides (COS) with a low polymerization degree are receiving a great attention in medical and pharmaceutical applications as they have higher water solubility and lower viscosity than chitosan. In this review articles, the antimicrobial, antioxidant, anticancer, anti-inflammatory activities of chitosan and its derivatives are highlighted. The influences of physicochemical parameters of chitosan like DDA and MW on bioactivities are also described.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

A rapid solid supported synthesis of 4-amino-5-(pyridin-4-YL)-4H-1,2,4-triazol-3-thiol and its derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Solid State ◽  
Microwave Irradiation ◽  
Future Study ◽  
Biological Activities ◽  
Uv Visible ◽  
Anti Inflammatory ◽  
Derivatives Of

1,2,4-triazoles and its substituted derivatives were synthesized since these compounds are known for their excellent antibacterial, antifungal, anti-tubercular, antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant and anxiolytic activities. 1,2,4-triazole and substituted derivatives of 1,2,4-triazole were synthesized using solid state microwave irradiation technique and synthesized compounds were characterized by UV-Visible, FTIR and GC-MS techniques and in future study the biological activities of synthesized compounds will be studied.

scholarly journals Anti-glycation, Carbonyl Trapping and Anti-inflammatory Activities of Chrysin Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1752 ◽  
Author(s):  
Seung Hwang ◽  
Hyun Kim ◽  
Guanglei Zuo ◽  
Zhiqiang Wang ◽  
Jae-Yong Lee ◽  
...  
Keyword(s):  
Water Solubility ◽  
Aldol Condensation ◽  
Inhibitory Effect ◽  
Food Ingredient ◽  
Inflammatory Agent ◽  
Glycation End Products ◽  
Anti Inflammatory ◽  
Applicable Knowledge ◽  
Derivatives Of ◽  
Anti Inflammation

The aim of this study was searching anti-glycation, carbonyl trapping and anti-inflammatory activities of chrysin derivatives. The inhibitory effect of chrysin on advanced glycation end-products (AGEs) was investigated by trapping methylglyoxal (MGO), and MGO-conjugated adducts of chrysin were analyzed using LC-MS/MS. The mono- or di-MGO-conjugated adducts of chrysin were present at 63.86 and 29.69% upon 48 h of incubation at a chrysin:MGO ratio of 1:10. The MGO adducted positions on chrysin were at carbon 6 or 6 & 8 in the A ring by classic aldol condensation. To provide applicable knowledge for developing chrysin derivatives as AGE inhibitors, we synthesized several O-alkyl or ester derivatives of chrysin and compared their AGE formation inhibitory, anti-inflammatory, and water solubility characteristics. The results showed that 5,7-di-O-acetylchrysin possessed higher AGE inhibitory and water solubility qualities than original chrysin, and retained the anti-inflammation activity. These results suggested that 5,7-di-O-acetylchrysin could be a potent functional food ingredient as an AGE inhibitor and anti-inflammatory agent, and promotes the development of the use of chrysin in functional foods.

scholarly journals Resveratrol Oligomers for the Prevention and Treatment of Cancers

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
You-Qiu Xue ◽  
Jin-Ming Di ◽  
Yun Luo ◽  
Ke-Jun Cheng ◽  
Xing Wei ◽  
...  
Keyword(s):  
Research And Development ◽  
Human Health ◽  
Drug Research ◽  
Biological Activities ◽  
Anticancer Properties ◽  
Prevention And Treatment ◽  
Significant Interest ◽  
Anti Inflammatory ◽  
Derivatives Of

Resveratrol (3,4′,5-trihydroxystilbene) is a naturally derived phytoalexin stilbene isolated from grapes and other plants, playing an important role in human health and is well known for its extensive bioactivities, such as antioxidation, anti-inflammatory, anticancer. In addition to resveratrol, scientists also pay attention to resveratrol oligomers, derivatives of resveratrol, which are characterized by the polymerization of two to eight, or even more resveratrol units, and are the largest group of oligomeric stilbenes. Resveratrol oligomers have multiple beneficial properties, of which some are superior in activity, stability, and selectivity compared with resveratrol. The complicated structures and diverse biological activities are of significant interest for drug research and development and may provide promising prospects as cancer preventive and therapeutical agents. This review presents an overview on preventive or anticancer properties of resveratrol oligomers.

scholarly journals One new compound from Borreria alata (Aubl.) DC (Rubiaceae) in Vietnam

2016 ◽  
Vol 19 (1) ◽  
pp. 19-25
Author(s):  
Loan Cam To ◽  
Tuyen Nguyen Kim Pham ◽  
Phung Kim Phi Nguyen
Keyword(s):  
Spectroscopic Data ◽  
Biological Activities ◽  
2D Nmr ◽  
Chemical Structures ◽  
Anti Inflammatory ◽  
First Time

Borreria is a genus of Rubiaceae widespread in tropical and subtropical America, Africa, Asia, and Europe. Studies have confirmed that extracts as well as some isolated compounds of species of Borreria genus possess diverse biological activities, including anti-inflammatory, antitumor, antimicrobial, antioxidant, anti-ulcer… In this paper, we present the chemical structures of four compounds isolated from Borreria alata, collected at Di Linh district, Lam Dong province, Vietnam. 3β, 6β, 23-trihydroxyurs- 12-en-28-oic acid (1), sodium deacetylasperulosidate (2), 7β-hydroxy-11-methylforsythide (3) and sodium loganate (4). Among them, three compounds (1), (2), (3) were known for the first time in Borreria genus to our best knowledge and (4) is a new compound. The chemical structures of these compounds wereelucidated by analysis of 1D and 2D NMR and HR-MS spectroscopic data, as well as by comparison with those reported in the literature.

scholarly journals COUMARINS: A UNIQUE SCAFFOLD WITH VERSATILE BIOLOGICAL BEHAVIOR

2019 ◽  
pp. 27-38 ◽  
Author(s):  
MANDEEP KUMAR GUPTA ◽  
SUSHIL KUMAR ◽  
SACHIN CHAUDHARY
Keyword(s):  
Pharmacological Activity ◽  
Biological Activities ◽  
Biological Behavior ◽  
Pharmacokinetic Studies ◽  
Coumarin Derivatives ◽  
Toxicological Studies ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Anti Hiv

Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study.

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

scholarly journals Plectranthus ecklonii Benth: A Comprehensive Review Into its Phytochemistry and Exerted Biological Activities

2021 ◽  
Vol 12 ◽  
Author(s):  
Ana Ribeirinha Antão ◽  
Gabrielle Bangay ◽  
Eva María Domínguez-Martín ◽  
Ana María Díaz-Lanza ◽  
Patrícia Ríjo
Keyword(s):  
Biological Activities ◽  
Eligibility Criteria ◽  
Database Retrieval ◽  
Pharmaceutical Ingredients ◽  
Chemical Structures ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Pharmaceutical Uses

Ethnopharmacological Relevance:Plectranthus genus (Lamiaceae family) contain several species with acknowledged ethnopharmacological uses, such as, for gastrointestinal and respiratory-related problems, due to their anti-inflammatory, antibacterial and antifungal properties. The bioactivity of isolated medicinal compounds from this genus justifies the increased interest in recent times for species of Plectranthus, placing them in the spotlight for natural product drug development.Aim of the study: To the best of our knowledge, this is the first review on the biological activities of Plectranthus ecklonii Benth. As such, the aim of this review was three-fold: 1) to summarize the chemical compounds isolated from P. ecklonii; 2) to collate the biological activities and mechanisms of action of these compounds from in vitro studies; and 3) to evaluate the documented uses and potential applications of this species, in order to postulate on the direction of pharmaceutical uses of this species.Materials and methods: An extensive database retrieval was performed using the electronic databases Web of Science, PubMed, Google Scholar and ScienceDirect. The search criteria consisted of the keywords “Plectranthus ecklonii”, “Plectranthus ecklonii + review”, “Plectranthus ecklonii + diterpenes” or “Plectranthus ecklonii + abietanes”, “ecklonii + parviflorone D”, searched individually and as combinations. Eligibility criteria were set out and titles in English, Portuguese and Spanish were reviewed, with all references included dating from 1970 to 2021. A total of 169 papers were selected and included. Chemical structures were drawn using ChemDraw 20.0, CID numbers were searched in PubChem and the PRISMA diagram was created using PowerPoint 2012.Results: To date, a total of 28 compounds have been isolated from P. ecklonii, including diterpenes, triterpenes, flavonoids, and hydroxycinnamic acids. Most focused on the antimicrobial action of its constituents, although compounds have demonstrated other bioactivities, namely antioxidant, anti-inflammatory and antitumor. The most recent studies emphasize the diterpenoids, particularly parviflorone D, with the help of nanotechnology.Conclusions: The widespread ethnobotanical and traditional uses of P. ecklonii can be scientifically justified by a range of biological activities, demonstrated by isolated secondary metabolites. These bioactivities showcase the potential of this species in the development of economically important active pharmaceutical ingredients, particularly in anticancer therapy.

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