519 Design of a new molecule proven to be safe and effective for topical depigmenting and antiaging method
نویسندگان
چکیده
Skin hyperpigmentation is a biological process that results in an excess production of melanin. Tyrosinase inhibition effective approach to this condition, although inhibitors reported the literature lack clinical efficacy or show toxic effects. Chalcone derivatives are well known tyrosinase but insoluble aqueous phase limiting its use final product formulations. The aim study develop new chalcone-related molecule safe and as skin depigmenting antiaging agent. Homology modelling was used build tridimensional structure human tyrosinase, virtual docking predict molecule-enzyme binding modes. designed synthesised compounds evaluated vitro. activity assessed spectrophotometrically, water solubility determined by HPLC. Cell assays were performed determine melanin content, toxicity, antiglycation, antioxidation autophagy efficacy. Chromatin accessibility miRNA levels also quantified. Two chalcone-based molecules with affinity for synthesised. Their tested resulting one molecule, 5-[(E)-3-(4-hydroxyphenyl)acryl]-2-hydroxybencensulfonic acid, increased 2-fold reference more than 80 times. Moreover, it demonstrated be non-cytotoxic non-irritant inhibited 51% content. Epigenetic effects overexpressing miR-137 miR-218 related melanogenesis. showing antioxidant (TXNRD1 FTH1 increment reversion oxidant molecule), antiglycation (reduction 29%) Results lead us conclude ideal candidate agent suitable properties introduced formulations such dermatology cosmetics.
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ژورنال
عنوان ژورنال: Journal of Investigative Dermatology
سال: 2022
ISSN: ['1523-1747', '0022-202X']
DOI: https://doi.org/10.1016/j.jid.2022.09.534