1. 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.
- Author
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Zhao JC, Luan ZL, Liang JH, Cheng ZB, Sun CP, Wang YL, Zhang MY, Zhang TY, Wang Y, Yang TM, Wu YY, Zhang YX, Zhao XY, and Ma XC
- Subjects
- Biological Products chemistry, Biological Products isolation & purification, Diterpenes chemistry, Diterpenes isolation & purification, Dose-Response Relationship, Drug, Hep G2 Cells, Humans, Indoles chemistry, Indoles isolation & purification, Molecular Structure, Structure-Activity Relationship, Biological Products pharmacology, Diterpenes pharmacology, Hypocreales chemistry, Indoles pharmacology, Pregnane X Receptor agonists
- Abstract
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 EC
50 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., (Copyright © 2018 Elsevier Inc. All rights reserved.)- Published
- 2018
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