Inhibitory potential.
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Lichens, formed by the symbiosis of fungi and algae or cyanobacteria, are increasingly recognized for their potential medicinal properties, including their potential to treat type 2 diabetes. Many studies have shown that the bioactive metabolites of lichens originate from their fungal partners. This study isolated the mycobiont from a Graphis lichen sample and investigated the antioxidant and α-glucosidase inhibitory activity of its ethyl acetate extract.
10p visergeyne 18-06-2024 2 0 Download
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The winged-helix domain within the N-terminus of human MUS81 has been considered as potential target for drug development since the inhibition of this protein might significantly enhance the sensitivity of various cancer cells towards anticancer drugs. Nine cytotoxic triterpenoids previously purified from Helicteres hirsuta and Pterospermum truncatolobatum were selected for the docking experiment.
6p dianmotminh02 03-05-2024 1 1 Download
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This study would like to point out the potential compounds as inflammatory agents. Herein, we displayed the isolation and structural identification of thirteen compounds including ten flavonoids, one tannin, one triterpenoid, and one derivative of benzoic acid from the methanolic extract. Furthermore, all of them were evaluated the anti-inflammatory activity.
12p dianmotminh02 03-05-2024 3 1 Download
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The synthesized compounds' enzyme inhibition potential was tested against a-glucosidase, AChE, and BChE enzymes. As illustrated from the results of IC50, these compounds are observed as the active inhibitory potential for these enzymes. The cytotoxic activity by hemolytic Assay revealed that these compounds have mild exposure to cytotoxicity on RBCs.
10p visergey 02-04-2024 0 0 Download
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Speckle-type POZ protein(SPOP), a substrate adaptor of Cul3 ubiquitin ligase, plays crucial roles in solid neoplasms by promoting the ubiquitination and degradation of substrates.
11p vileonardodavinci 23-12-2023 5 2 Download
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Unsaturated ketone derivatives are known as monoamine oxidase B (MAO-B) inhibitors, a potential drug target for Parkinson’s disease. Here, molecular modeling studies, including 2D-QSAR, ADMET prediction, molecular docking, and MD simulation, were performed on a new series of MAO-B inhibitors. The objective is to identify new MAO-B inhibitors with high inhibitory efficacy. The developed 2D-QSAR model was based on the descriptors of MOE software.
21p lyhuyenthu 31-01-2023 4 2 Download
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This study aims to provide an in vitro evidence for the potential antibacterial activity of the ethanolic and aqueous extracts from fruiting bodies of the Pycnoporus sanguineus (L.: Fr.) Murrill mushroom via agar well diffusion method (concentration of extracts 250 mg/mL) and determination of the antibacterial activity and minimum inhibitory concentrations (MIC) of ethanolic and aqueous extracts from the fruiting bodies of this mushroom by agar dilution method (concentration range of 25; 12.5; 6.25; 3.125 and 1.5625 mg/mL).
8p viporsche 28-10-2022 6 2 Download
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Bladder cancer (BCa) shows its potential immunogenity in current immune-checkpoint inhibitor-related immunotherapies. However, its therapeutic effects are improvable and could be affected by tumor immune microenvironment. Hence it is interesting to find some more prognostic indicators for BCa patients concerning immunotherapies.
11p visusanwojcicki 28-06-2022 12 2 Download
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Sevoflurane potently enhances glycine receptor currents and more modestly decreases NMDA receptor currents, each of which may contribute to immobility. This modest NMDA receptor antagonism by sevoflurane at a minimum alveolar concentration (MAC) could be reciprocally related to large potentiation of other inhibitory ion channels.
7p viisaacnewton 26-04-2022 12 1 Download
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14α-Demethylase (CYP51) inhibitors have been widely used in the treatment of fungal infections. In this study, a series of imidazole derivatives with CYP51 inhibitory activity were subjected to a molecular docking study followed by quantitative structure–activity relationship (QSAR) analyses in search of the ideal physicochemical characteristics of potential CYP51 inhibitors. Desired imidazoles were built using the HyperChem program, and conformational studies were performed through a semiempirical method followed by the PM3 method.
15p langthannam 29-12-2021 14 0 Download
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The aim of the present study was to synthesize and characterize benzothiazine derivatives prepared by using 2-aminothiophenol and saccharine and in vitro screen their enzyme inhibition and antioxidant potential. Nine different derivatives were prepared and their structures were confirmed by spectral studies (EIMS, 1H and 13 C NMR). Enzyme inhibition potential of the synthesized compounds was evaluated by Ellman’s method, while antioxidant activity was determined by DPPH and FRAP assays.
9p langthannam 29-12-2021 12 0 Download
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The essential oil, obtained from the aerial parts of the plant, exhibited high AChE inhibitory activity, consisting of mainly 1,8-cineol (58.89%). The antioxidant activity according to 6 complementary tests and anticholinesterase potential of the methanol extracts and triterpenoids α-amyryltetracosanoate, oleanolic acid, ursolic acid, and sitosterol acetate were also investigated, and methanol extract exhibited the highest antioxidant and anticholinesterase activity, surpassing the other tested extracts and pure compounds.
14p langthannam 29-12-2021 14 1 Download
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The new compounds 7a–k, 8a–k, and 9a–k were synthesized from flavonones 4–6, which can be considered new precursors for quinoline synthesis through a one-step reaction. All the target compounds (7a–k, 8a–k, and 9a–k) were evaluated for their in vitro antimicrobial activity against nine test microorganisms. They showed the most activity against Mycobacterium smegmatis with minimum inhibitory concentrations (MIC) of 62.5–500 µg/mL, indicating their potential uses as antituberculosis agents. Among them 8a–k (m-fluoride) were the most active compounds against M. smegmatis (MIC, 62.5–125 µg/mL).
17p langthannam 29-12-2021 11 0 Download
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This study also observed that supplements like minimal essential medium amino acids and B complex vitamins individually has further enhanced the bacteriocin activity by 13% (total 33%), biomass by 43%, total protein and activity by 17% and 22% respectively. However, addition of some common growth supplements like multivitamins with trace elements, CaCl2 and MgSO4 had shown inhibitory effect on bacteriocin activity.
5p mudbound 10-12-2021 12 1 Download
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The aim of this study was to evaluate the antimicrobial activity of three commercial GSE (Grapefruit Seed Extract) products against six bacterial and one fungal strain, through the agar well diffusion method, determination of minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and minimum fungicidal concentration (MFC). Obtained results indicate strong antimicrobial effects of investigated extracts, with different microbial susceptibility, including the multidrug-resistant (MDR) bacteria.
4p mudbound 10-12-2021 11 1 Download
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As part of the ongoing efforts to exploit the pharmaceutical potential of domestic cyanobacteria, six strains belonging to the Nostocales order have been isolated from several sampling sites in Hanoi as prerequisite material. The cytotoxic activity evaluation based on the MTT test resulted in four extracts of two strains (HK7 and NK1111) exhibiting the inhibitory activity against HeLa cells, with IC50 values ranging from 84.6 µg/mL to 257.3 µg/mL.
11p guitaracoustic02 08-12-2021 9 1 Download
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Finding novel cholinesterase inhibitors that would be able to cross the blood–brain barrier, have favorable pharmacokinetic parameters, and reduce hepatotoxicity along with other side effects has been the main focus of investigations dealing with Alzheimer disease. In this study we evaluated cholinesterase inhibitory and antioxidant activity of seven oxazole derivatives. These compounds have been efficiently and sustainably prepared by photochemical electrocyclization reaction.
7p tudichquannguyet 29-11-2021 10 2 Download
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Laggera tomentosa Sch. Bip. ex Oliv. et Hiern (Asteraceae), an endemic Ethiopian medicinal plant, is traditionally used to treat various ailments. Previously, the chemical constituents of the essential oil (EO) of its leaves and inflorescence were documented. However, no data about the chemical compositions of other parts of the EOs of the plant have been reported to date. Moreover, there are no previous biological activity reports on any parts of the EOs of this plant.
10p tudichquannguyet 29-11-2021 13 1 Download
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N-(1-(4-Methoxyphenyl)-3-oxo-3-((4-(N-(substituted)sulfamoyl)phenyl)amino)prop-1-en-1-yl)benzamides 3a – g were designed since sulfonamide and benzamide pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies. Structure elucidation of the compounds was carried out by 1 H NMR, 13C NMR, and HRMS spectra.
28p tudichquannguyet 29-11-2021 13 1 Download
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In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a–g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a–g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II.
14p tudichquannguyet 29-11-2021 6 1 Download