Molecular modeling and phenoloxidase inhibitory activity of arbutin and arbutin undecylenic acid ester
نویسندگان
چکیده
Excessive melanin formation has been linked to various skin disorders such as hyperpigmentation and cancer. Tyrosinase is the most prominent target for inhibitors of production. In this study, we investigated whether arbutin its prodrug, undecylenic acid ester, might inhibit phenoloxidase (PO), a tyrosinase-like enzyme. Molecular docking simulation results suggested that ester can bind substrate-binding pocket PO. Arbutin with an IC50 6.34 mM was effective PO compared (IC50 29.42 mM). addition, showed low cytotoxicity in Drosophila S2 cells compound inhibited melanization reaction. Therefore, study have demonstrated potential inhibitor We successfully designed new platform utilizing melanogaster Bombyx mori animal models propounding fast, cheap, high effectiveness method screen tyrosinase inhibitors.
منابع مشابه
Syntheses of arbutin-alpha-glycosides and a comparison of their inhibitory effects with those of alpha-arbutin and arbutin on human tyrosinase.
The effects of 4-hydroxyphenyl alpha-glucopyranoside (alpha-arbutin) and 4-hydroxyphenyl beta-glucopyranoside (arbutin) on the activity of tyrosinase from human malignant melanoma cells were examined. The inhibitory effect of alpha-arbutin on human tyrosinase was stronger than that of arbutin. The K(i) value for alpha-arbutin was calculated to be 1/20 that for arbutin. We then synthesized arbut...
متن کاملHypoglycemic activity of Pyrus biossieriana Buhse leaf extract and arbutin: Inhibitory effects on alpha amylase and alpha glucosidase
Background: The mechanism of hypoglycemic and hypolipidemic activities of Pyrus biossieriana Buhse leaf extract (PbBLE) and its phytochemical component arbutin, have not been well determined. The present study was performed to understand the hypoglycemic activity mechanisms of pbBLE and arbutin more clearly.Methods: In vitro enzymatic carbohydrate digestion with PbBLE and arbutin was assessed u...
متن کاملMolecular Profiling of A375 Human Malignant Melanoma Cells Treated with Kojic Acid and Arbutin
متن کامل
Flavonoids and arbutin from Turnera diffusa.
The infusion of the aerial parts of Turnera diffusa was phytochemically examined. Chromatographic procedures led to the isolation of a new flavone glycoside, five known flavonoids and p-arbutin. Structures were determined by 1D- and 2D NMR experiments, as well as ES-MS and UV spectra.
متن کاملHypoglycemic activity of Pyrus biossieriana Buhse leaf extract and arbutin: Inhibitory effects on alpha amylase and alpha glucosidase.
BACKGROUND The mechanism of hypoglycemic and hypolipidemic activities of Pyrus biossieriana Buhse leaf extract (PbBLE) and its phytochemical component arbutin, have not been well determined. The present study was performed to understand the hypoglycemic activity mechanisms of pbBLE and arbutin more clearly. METHODS In vitro enzymatic carbohydrate digestion with PbBLE and arbutin was assessed ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Biochemical and Biophysical Research Communications
سال: 2021
ISSN: ['0006-291X', '1090-2104']
DOI: https://doi.org/10.1016/j.bbrc.2021.02.006