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Triterpenoids as bivalent and dual inhibitors of acetylcholinesterase/butyrylcholinesterase from the fruiting bodies of Inonotus obliquus

文献类型： 外文期刊

作者： Wei, Yan-Mei 1 ; Yang, Li 1 ; Wang, Hao 1 ; Cai, Cai-Hong 1 ; Chen, Zhi-Bao 3 ; Chen, Hui-Qin 1 ; Mei, Wen-Li 1 ; Dai, Hao-Fu 1 ;

作者机构： 1.Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Key Lab Nat Prod Res & Dev Li Folk Med Hainan Pro, Haikou 571101, Hainan, Peoples R China

2.Hainan Acad Trop Agr Resources, Key Lab Conservat & Utilizat Trop Agrobioresource, Haikou 571101, Hainan, Peoples R China

3.Guangdong Ocean Univ, Coll Agron, Zhanjiang 524088, Peoples R China

关键词： Inonotus obliquus; Hymenochaetaceae; Triterpenoids; Acetylcholinesterase inhibitors; Butyrylcholinesterase inhibitors

期刊名称：PHYTOCHEMISTRY （ 影响因子：4.004； 五年影响因子：4.129 ）

ISSN： 0031-9422

年卷期： 2022 年 200 卷

页码：

收录情况： SCI

摘要： Inonotus obliquus, an edible and medicinal mushroom parasitic on birches, has been used in human diet and for traditional therapies in the high latitude regions of Europe and Asia for a long time. Our phytochemical study of this fungus led to the identification of fourteen triterpenoids including four undescribed ones, and two pairs of undescribed phenolic enantiomers. The undescribed compounds were elucidated by extensive spectroscopic analysis including 1D and 2D NMR and HRESIMS, quantum chemical NMR and ECD calculations, as well as single-crystal X-ray diffraction analysis. Bioassays revealed that eight compounds showed dual inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values ranging from 2.40 +/- 0.05 to 28.72 +/- 0.46 mu M, while 3 beta-hydroxy-lanosra-8,24-dien-21-al and trametenolic acid only presented BuChE inhibitory activities with IC50 values of 22.21 +/- 1.01 and 7.68 +/- 0.13 mu M, respectively. In the kinetic studies, the most active three compounds acted as non-competitive inhibitors for both cholinesterases. Furthermore, molecular docking simulations revealed that three compounds demonstrated dual-sites bounding to AChE/BuChE. These triterpenoids emerged as bivalent and dual inhibitors of AChE/BuChE and could be effective drug candidates to prevent and treat Alzheimer's disease in the future.

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