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

文献类型： 外文期刊

作者： Yang, Li 1 ; Yang, Yi-Ling 1 ; Dong, Wen-Hua 1 ; Li, Wei 1 ; Wang, Pei 1 ; Cao, Xue 1 ; Yuan, Jing-Zhe 1 ; Chen, Hui-Qin; 1 ;

作者机构： 1.Minist Agr, Inst Trop Biosci & Biotechnol, Key Lab Biol & Genet Resources Trop Crops, Chinese Acad Trop Agr Sci, Haikou 571101, Hainan, Peoples R China

2.Hainan Key Lab Res & Dev Nat Prod Li Folk Med, Haikou, Hainan, Peoples R China

3.Hainan Engn Res Ctr Agarwood, Haikou, Hainan, Peoples R China

关键词： Agarwood; aquilaria plant; sesquiterpenoid; 2-(2-phenylethyl)chromone; alpha-glucosidase inhibition; tyrosinase inhibition

期刊名称：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY （ 影响因子：5.051； 五年影响因子：4.598 ）

ISSN： 1475-6366

年卷期： 2019 年 34 卷 1 期

页码：

收录情况： SCI

摘要： 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 alpha-glucosidase and tyrosinase inhibitory activities in vitro. Compounds 5, 7, 8, and 10 showed significant inhibition of alpha-glucosidase with IC50 values ranging between 112.3 +/- 4.5 and 524.5 +/- 2.7 mu M (acarbose, 743. 4 +/- 3.3 mu M). Compounds 13 and 14 exhibited tyrosinase inhibitory effect with IC50 values of 89.0 +/- 1.7 and 51.5 +/- 0.6 mu M, respectively (kojic acid, 46.1 +/- 1.3). In the kinetic studies, compounds 5 and 14 were found to be uncompetitive inhibitors for alpha-glucosidase and mixed type inhibitors for tyrosinase, respectively. Furthermore, molecular docking simulations revealed the binding sites and interactions of the most active compounds with alpha-glucosidase and tyrosinase.

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