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.
Highlights
Tyrosinase (EC 1.14.18.1) is a copper-containing bifunctional enzyme found in plants, insects, and humans [1]
Dried tubers of A. americana were extracted with methanol at room temperature
To gain insight on the receptor–ligand complex, we performed enzyme kinetics and molecular simulations. The former indicated that the two compounds act as competitive inhibitors, with Ki values of 10.3 ± 0.8 μM and 44.2 ± 1.7 μM, respectively
Summary
Tyrosinase (EC 1.14.18.1) is a copper-containing bifunctional enzyme found in plants, insects, and humans [1]. Melanin protects human skin by absorbing UV radiation from sunlight, and it is responsible for the browning of fruits, vegetables, and mushrooms [1,3]. This causes adverse effects, such as melisma, freckles and ephelis in skin [1,3]. Tyrosinase has been regarded as an enzyme target to attenuate these phenomena Representative tyrosinase inhibitors, such as kojic acid and arbutin, have been developed for skin whiting from natural sources [4]. Many studies has been performed to develop new tyrosinase inhibitor from natural plants [6,7,8]
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