More studies are needed to develop new drugs for problems associated with drug resistance and unfavorable side effects. The natural flavonoid of quercetin revealed a wide range of biological activities by the modulation of various targets and signaling pathways. However, quercetin's low solubility and poor bioavailability have restricted its applicability; as a result, researchers have attempted to design and synthesize numerous novel quercetin derivatives using various methodologies in order to modify quercetin's constraints; the physico-chemical properties of quercetin's molecular scaffold make it appealing for drug development; low molecular mass and chemical groups are two of these characteristics. Therefore, the biological activities of quercetin derivatives, as well as the relationship between activity and chemical structure and their mechanism of action, were investigated. These quercetin-based molecules could be valuable in the creation and discovery of medications for a number of diseases.
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http://dx.doi.org/10.1016/j.ejmech.2021.114068 | DOI Listing |
Onderstepoort J Vet Res
December 2024
Department of Pharmacology and Therapeutics, Faculty of Medicine, Sefako Makgatho Health Sciences University, Pretoria.
Plant foliages used as feed additives pose a health risk due to high oxidant concentrations. Oxidants cause oxidative stress and high rate of morbidities and mortalities. Hence, the aim of the study was to validate the methods to quantify gallic acid (GA) and quercetin (Q) as putative antioxidants, and to evaluate antioxidant activities in feed (F), Hyperacanthus amoenus (HA) and Carissa bispinosa (CB) extracts.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Vinča Institute of Nuclear Sciences, National Institute of the Republic of Serbia, University of Belgrade, P.O. Box 522, 11000 Belgrade, Serbia.
Quercetin, a well-known flavonoid with significant medicinal potential, was derivatized at the C8 position with a tetrahydroisoquinoline (THIQ) moiety, and physicochemical and pharmacological properties, inhibition potential, antioxidant activity, and cytotoxicity of new compounds were evaluated. Physicochemical and pharmacological properties, including lipophilicity, membrane permeability, and P-glycoprotein substrate affinity, were assessed theoretically using the SwissADME software. The metal-chelating ability of the new compounds was evaluated on metal ions Fe, Zn, and Cu, whose homeostasis disruption is linked to the development of Alzheimer's disease.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Centre for Systems Biology, Biodiversity and Bioresources, Department of Molecular Biology and Biotechnology, Faculty of Biology and Geology, Babes-Bolyai University, 5-7 Clinicilor Street, 400006 Cluj-Napoca, Romania.
Despite the growing interest in using natural compounds for disease prevention and treatment, (wild garlic), known for its therapeutic properties, has not been extensively studied for its chemical composition and biological activities. Therefore, this study aims to explore the in vitro antioxidant, antibacterial, and antitumor activities of extracts according to their functional phytochemical profile, while assessing whether ultrasound-assisted extraction (UAE) enhances bioactive properties in comparison to conventional maceration (CM). Both extracts were characterized by spectrophotometric methods and LC-ESI+-MS.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Faculdade de Ciências, Universidade Estadual Paulista (UNESP), Bauru 17033-360, SP, Brazil.
This study evaluates how the polarity of the medium affects the binding efficiency of hydrophobic ligands with human serum albumin (HSA). The polarity of the aqueous medium was changed by adding 1,4-dioxane in concentrations of 0%, 10%, and 20% /, resulting in solvent mixtures with decreasing dielectric constants (ε = 80, 72, and 63). The addition of 1,4-dioxane did not affect the integrity of the protein, as confirmed by Far-UV-CD, Rayleigh scattering, and time-resolved fluorescence experiments.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
A.N. Bach Institute of Biochemistry, Research Center of Biotechnology of the Russian Academy of Sciences, Leninsky Ave. 33/2, Moscow 119071, Russia.
Polyphenols are powerful natural antioxidants with numerous biological activities. They change cell membrane permeability, interact with receptors, intracellular enzymes, and cell membrane transporters, and quench reactive oxygen species (ROS). yeast, being similar to mammalian cells, can be used as a model to study their survival ability upon long-lasting cultivation, assaying the effect of dihydroquercetin polyphenol (DHQ).
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