In the current study, metronidazole derivatives containing 1-1,2,3-triazole and carboxylate moieties were evaluated and by computational methods for their anti-diabetic potential to insight into their medicinal use for the management of type II diabetes mellitus. Interestingly all 14 compounds displayed high to significant inhibitory capability against the key carbohydrate's digestive enzyme α-glucosidase with IC values in range of 9.73-56.39 μM, as compared to marketed drug acarbose (IC = 873.34 ± 1.67 μM). Compounds and exhibited the highest inhibition, therefore, these two compounds were further evaluated for their mechanistic studies to explore its type of inhibition. Compounds and both displayed a concentration-dependent (competitive type of inhibition) with values 7.14 ± 0.01, 6.15 ± 0.02 μM, respectively, which conclude their favourable interactions with the active site residues of the α-glucosidase. Interestingly all compounds are non-cytotoxic against BJ cell line. To further validate our findings, approaches like molecular docking, and molecular dynamic simulations were applied to investigate the mode of bindings of compounds with the enzyme and identifies their inhibition mechanism, which strongly complements our experimental findings.Communicated by Ramaswamy H. Sarma.
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http://dx.doi.org/10.1080/07391102.2024.2322622 | DOI Listing |
Glob Chang Biol
January 2025
Key Laboratory of National Forestry and Grassland Administration on Forest Ecosystem Protection and Restoration of Poyang Lake Watershed, College of Forestry, Jiangxi Agricultural University, Nanchang, China.
Leaf photosynthesis and respiration are two of the largest carbon fluxes between the atmosphere and biosphere. Although experiments examining the warming effects on photosynthetic and respiratory thermal acclimation have been widely conducted, the sensitivity of various ecosystem and vegetation types to warming remains uncertain. Here we conducted a meta-analysis on experimental observations of thermal acclimation worldwide.
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January 2025
Institute of Horticultural Production Systems, Fruit Science Section, Leibniz University Hannover, Herrenhäuser Straße 2, 30419, Hannover, Germany.
The mango cultivar 'Apple' is commercially important in Kenya but highly susceptible to russeting. Russeting refers to an area of fruit skin where the primary (epidermal) surface has been replaced by a secondary (peridermal) surface. The objective was to establish histologies, gene expressions and chemical compositions of a natural periderm, a wound-induced periderm and of cuticles of an un-russeted skin.
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January 2025
Department of Food Toxicology and Contaminant, National Research Centre, Dokki, Giza, Egypt.
This study evaluates the potential of ozonated corn starch (OCS) and ultrasonicated ozonated corn starch (USOCS) as adsorbents for patulin removal in buffer solutions. The results indicated that dual modification significantly altered the starch's structure, introducing functional groups such as carbonyl and carboxyl groups, and increasing its surface area. These modifications led to enhanced patulin adsorption capacity.
View Article and Find Full Text PDFNat Struct Mol Biol
January 2025
Zhejiang Provincial Key Laboratory of Pancreatic Disease, Department of Gastroenterology, The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.
Thymidine kinase 1 (TK1), a crucial enzyme in DNA synthesis, is highly expressed in various cancers. However, the mechanisms underlying its elevated expression and the implications for tumor metabolism remain unclear. Here we demonstrate that activation of growth factor receptors enhances TK1 expression.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Key Laboratory of Colloid and Interface Chemistry of the Ministry of Education, School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.
We report the assembly of poly(ethylene glycol) nanoparticles (PEG NPs) and optimize their surface chemistry to minimize the formation of protein coronas and immunogenicity for improved biodistribution. PEG NPs cross-linked with disulfide bonds are synthesized utilizing zeolitic imidazolate framework-8 NPs as the templates, which are subsequently modified with PEG molecules with different end groups (carboxyl, methoxy, or amino) to vary the surface chemistry. Among the modifications, the amino and residual carboxyl groups form a pair of zwitterionic structures on the surface of PEG NPs, which minimize the adsorption of proteins (e.
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