Benzimidazoles are antiparasitic drugs having an extensive application field like agriculture, medicine, and especially in veterinary medicine. In this study, we report the effect of some benzimidazole drugs such as ricobendazole (RBZ), thiabendazole (TBZ), albendazole (ALBA) and oxfendazole (OFZ) on glutathione s-transferase (GST) enzyme activity. The kinetics studies, IC and Ki values of the tested drugs on GSTs enzyme activity were investigated. The obtained ranking of IC values were found to be approximately RBZ (53.31 μM, r 0.9778) < OFZ (57.75 μM, r 0.9630) < ALBA (63.00 μM, r 0.9443) < TBZ (69.30 μM, r 0.9491). And the obtained ranking of Ki values of the tested drugs (RBZ, TBZ, ALBA, and OFZ) for GSTs enzyme activity was found to be approximately 26.37 ± 2.96, 44.01 ± 5.74, 39.82 ± 3.98 and 30.14 ± 3.03 μM, respectively. Experimental results showed that tested the benzimidazoles drugs have some significant inhibitory effect on GSTs enzyme activity. And also, it was determined that RBZ, ALBA, OFZ are competitive inhibition, but TBZ is non-competitive inhibitors on GSTs enzyme activity. RBZ drug showed the best inhibitory effect with the lowest Ki value.
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http://dx.doi.org/10.1016/j.jpba.2019.113048 | DOI Listing |
Biomacromolecules
January 2025
School of Physics and Astronomy, University of Leeds, Leeds LS2 9JT, U.K.
Enzymes are attractive as catalysts due to their specificity and biocompatibility; however, their use in industrial and biomedical applications is limited by stability. Here, we present a facile approach for enzyme immobilization within "all-enzyme" hydrogels by forming photochemical covalent cross-links between the enzyme glucose oxidase. We demonstrate that the mechanical properties of the enzyme hydrogel can be tuned with enzyme concentration and the data suggests that the dimeric nature of glucose oxidase results in unusual gel formation behavior which suggests a degree of forced induced dimer dissociation and unfolding.
View Article and Find Full Text PDFUnlabelled: One of the principles of prevention and non-drug treatment of liver diseases, including hepatitis of various etiologies, is the normalization of the diet, including the use of daily diet foods with physiologically active ingredients, in particular betulin, which helps to reduce metabolic and oxidative processes within liver cells. The aim of the work was to evaluate the in vivo effect of triterpene alcohol betulin Roth isolated from the bark of birch Betula pendula Roth. added to fat-containing products (for example, mayonnaise) on the biochemical parameters of blood and the morphological structure of the liver of rats with initiated acute toxic hepatitis.
View Article and Find Full Text PDFIntroduction: The developed domestic retrodipeptide analogue of cholecystokinin tetrapeptide (CCK) (N-(6-phenylhexanoyl)-glycyltryptophan amide, or compound GB-115) with antagonistic properties in relation to CCK1 receptors has anxiolytic activity previously shown in preclinical and clinical studies. The aim of the study was to evaluate the anxiolytic effect of GB-115 as a tablet form with subchronic oral administration in comparison with phenazepam in nonhuman primates.
Materials And Methods: The study was conducted on four male rhesus monkeys (Macaca mulatta) aged 5.
Vet Res Commun
January 2025
Department of Veterinary Medicine and Animal Sciences, University of Milan, Lodi, 26900, Italy.
South American camelids (SACs), particularly llamas (Lama glama) and alpacas (Vicugna pacos) are gaining popularity in Europe. Initially valued for their fiber and land management capabilities, these animals are now also kept for animal therapy, outdoor activities, and as companion animals. Despite their close interactions with humans and other animals, there is limited research on the transmission of microbes or antimicrobial resistance genes from SACs.
View Article and Find Full Text PDFJ Mater Chem B
January 2025
Departamento de Química Inorgánica, Orgánica y Bioquímica, Facultad de Ciencias y Tecnologías Químicas, Universidad de Castilla-La Mancha, 13071 Ciudad Real, Spain.
Diabetes remains one of the most prevalent chronic diseases globally, significantly impacting mortality ratetables. The development of effective treatments for controlling glucose level in blood is critical to improve the quality of life of patients with diabetes. In this sense, smart optical sensors using hydrogels, responsive to external stimuli, have emerged as a revolutionary approach to diabetes care.
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