In vitro and in silico insights into tyrosinase inhibitors with (E)-benzylidene-1-indanone derivatives.

ABSTRACT: Tyrosinase is a key enzyme responsible for melanin biosynthesis and is effective in protecting skin damage caused by ultraviolet radiation. As part of ongoing efforts to discover potent tyrosinase inhibitors, we systematically designed and synthesized thirteen (E)-benzylidene-1-indanone derivatives (BID1-13) and determined their inhibitory activities against tyrosinase. Among the compounds evaluated, BID3 was the most potent inhibitor of mushroom tyrosinase (IC₅₀ = 0.034 µM, monophenolase activity; IC₅₀ = 1.39 µM, diphenolase activity). Kinetic studies revealed that BID3 demonstrated a mixed type of tyrosinase inhibition with K _i value of 2.4 µM using l-DOPA as a substrate. In silico molecular docking simulat

SUBMITTER: Jung HJ 

PROVIDER: S-EPMC6944710 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature