Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities |
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Authors: | Jianbin Wang Menghua Wu Chun Gao Hongzheng Fu |
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Institution: | 1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Science, Peking University, Beijing 100191, China;2. Guangdong-Macau Traditional Chinese Medicine Technology Industrial Park Development Co., Ltd., Zhuhai 519000, China;3. Research Center for Traditional Chinese Medicine of Lingnan (Southern China), College of Pharmacy, Jian University, Guangzhou 510632, China |
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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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Keywords: | Kirenol Epoxy-pimarane diterpenoids X-ray crystallographic data Factor Xa |
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