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

作者：Zhao, Jian-Chao; Luan, Zhi-Lin; Liang, Jia-Hao; Cheng, Zhong-Bin; Sun, Cheng-Peng^*; Wang, Ya-Li; Zhang, Meng-Yue; Zhang, Tian-Yuan; Wang, Yong; Yang, Tian-Mei; Wu, Ying-Ying; Zhang, Yi-Xuan^*; Zhao, Xin-Yu; Ma, Xiao-Chi^*

来源：Bioorganic Chemistry, 2018, 79: 250-256.

DOI：10.1016/j.bioorg.2018.05.001

• Drechmeria sp.
• Indole diterpenoid
• Agonistic effect
• Pregnane X receptor
• Molecular docking

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.

• 出版日期2018-9
• 单位沈阳药科大学; 云南省农业科学院; 文山学院; 河南大学; 河北医科大学; 大连医科大学