Chemical Constituents from Apios americana and Their Inhibitory Activity on Tyrosinase

美洲大叶芹的化学成分及其对酪氨酸酶的抑制活性

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作者:Jang Hoon Kim, Hyo Young Kim, Si Yong Kang, Jin-Baek Kim, Young Ho Kim, Chang Hyun Jin

Abstract

The goal of this study was to identify phytochemicals with inhibitory activity against tyrosinase. Nine compounds 1-9 were isolated from the tubers of Apios americana. This is the first report of aromadendrin 5-methyl ether (1) being isolated from the Apios species. Among them, compounds 2 and 8 showed inhibitory activity toward tyrosinase. Based on a Dixon plot, the potential Ki values of competitive inhibitors 2 and 8 were calculated as 10.3 ± 0.8 µM and 44.2 ± 1.7 µM, respectively. An IC50 value of 13.2 ± 1.0 µM was calculated for the slow-binding inhibitor 2 after preincubation with tyrosinase. Additionally, the predicted binding sites between the receptor and ligand, as well as secondary structure changes, in the presence of 2 were examined by molecular simulation.

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