Drechmerin H, a novel 1(2), 2(18)-diseco indole diterpenoid from the fungus Drechmeria sp as a natural agonist of human pregnane X receptor
文献类型： 外文期刊
作者： Zhao, Jian-Chao 1 ; Luan, Zhi-Lin 1 ; Liang, Jia-Hao 1 ; Cheng, Zhong-Bin 3 ; Sun, Cheng-Peng 1 ; Wang, Ya-Li 2 ; Zhan 1 ;
作者机构： 1.Dalian Med Univ, Adv Inst Med Sci, Coll Med Lab, Coll Pharm,Coll Inst Integrat Med, Dalian 116044, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Wenhua Rd 103, Shenyang 110016, Liaoning, Peoples R China
3.Henan Univ, Pharmaceut Coll, Kaifeng 475004, Peoples R China
4.Wenshan Univ, Wenshan Sanqi Res Inst, Wenshan 663000, Peoples R China
5.Yunnan Acad Agr Sci, Inst Med Plants, Kunming 650200, Yunnan, Peoples R China
关键词： Drechmeria sp.; Indole diterpenoid; Agonistic effect; Pregnane X receptor; Molecular docking
期刊名称：BIOORGANIC CHEMISTRY （ 影响因子：5.275； 五年影响因子：5.252 ）
ISSN： 0045-2068
年卷期： 2018 年 79 卷
页码：
收录情况： SCI
摘要： A novel 1(2), 2(18)-diseco indole diterpenoid, drechmerin H (1), was isolated from the fermentation broth of Drechmeria sp. together with a new indole diterpenoid, 2 '-epi terpendole A (3), and a known analogue, terpendole A (2). Their structures were determined by HRESIMS, 1D and 2D NMR, ECD, and X-ray single crystal diffraction analyses as well as quantum chemical calculation. The abosulte configuration of terpendole A (2) was determined for the first time. Compound 1 displayed the significant agonistic effect on pregnane X receptor (PXR) with EC50 value of 134.91 +/- 2.01 nM, and its interaction with PXR was investigated by molecular docking. Meantime, a plausible biosynthetic pathway for compounds 1-3 is also discussed in the present work.
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