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Updated: Jan 28, 2026

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
Published on: October 4, 2019
Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities
Jianbin Wang1, Menghua Wu2, Chun Gao3
1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Science, Peking University, Beijing 100191, China; Guangdong-Macau Traditional Chinese Medicine Technology Industrial Park Development Co., Ltd., Zhuhai 519000, China; Research Center for Traditional Chinese Medicine of Lingnan (Southern China), College of Pharmacy, Jian University, Guangzhou 510632, China.
Abstract:
Kirenol is one of the biologically active diterpenoids from Siegesbeckia pubescens. In terms of the high content and typical structure, many ent-diterpenoids separated from S. pubescens were presumed to be biologically related to kirenol. Among them, epoxy-pimarane diterpenoids are belonging to a special family of naturally occurring compounds that attracted our attentions on their putative biosynthesis pathway and biological activities. Here, we designed and synthesized two known 14,16-epoxy-pimarane diterpenoids (2 and 3) and five 8,15-epoxy-pimarane diterpenoids (4-8) from kirenol. Their absolute structures were determined by 1D and 2D NMR data and the absolute configurations of 4 were confirmed by X-ray crystallographic data. Their inhibition effects on factor Xa (FXa) were evaluated to assess the potentiality of epoxy-pimarane diterpenoids as FXa inhibitor agents.
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