Sesquiterpenoids and 2-(2-phenylethyl)chromones respectively acting as ?-glucosidase and tyrosinase inhibitors from agarwood of an Aquilaria plant.

ABSTRACT: The ethyl ether extract of agarwood from an Aquilaria plant afforded six new sesquiterpenoids, Agarozizanol A?-?F (1-6), together with four known sesquiterpenoids and six known 2-(2-phenylethyl)chromones. Their structures were elucidated via detailed spectroscopic analysis, X-ray diffraction, and comparisons with the published data. All the isolates were evaluated for the ?-glucosidase and tyrosinase inhibitory activities in vitro. Compounds 5, 7, 8, and 10 showed significant inhibition of ?-glucosidase with IC50 values ranging between 112.3?±?4.5 and 524.5?±?2.7?µM (acarbose, 743. 4?±?3.3?µM). Compounds 13 and 14 exhibited tyrosinase inhibitory effect with IC50 values of 89.0?±?1.7 and 51.5?±?0.6?µM, respectively (kojic acid, 46.1?±?1.3). In the kinetic studies, compounds 5 and 14 were found to be uncompetitive inhibitors for ?-glucosidase and mixed type inhibitors for tyrosinase, respectively. Furthermore, molecular docking simulations revealed the binding sites and interactions of the most active compounds with ?-glucosidase and tyrosinase.

SUBMITTER: Yang L 

PROVIDER: S-EPMC6495113 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature