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从传统中药川西獐牙菜中提取的抗乙肝病毒活性内酯。

Anti-hepatitis B virus active lactones from the traditional Chinese herb: Swertia mileensis.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, P R China.

出版信息

Chemistry. 2011 Mar 28;17(14):3893-903. doi: 10.1002/chem.201003180. Epub 2011 Mar 1.

Abstract

Swerilactones H-K (1-4), which are four novel lactones with an unprecedented C29 skeleton, were isolated from Swertia mileensis (Qing-Ye-Dan), an endemic Chinese herb used for treating viral hepatitis. Their structures were determined by extensive spectroscopic and X-ray crystallographic diffraction analyses. Swerilactones H-K exhibit potent anti-hepatitis B virus activity against HBV DNA replication with IC(50) values ranging from 1.53 to 5.34 μM. For the first time, a plausible biogenetic pathway for swerilactones H-K, together with the previously reported swerilactones A-D is proposed. From a biogenetic point of view, swerilactones A-D are ascribed as secoiridoid dimers, and swerilactones H-K as secoiridoid trimers.

摘要

Swerilactones H-K(1-4)是从中国特有的治疗病毒性肝炎的草药青叶胆(Swertia mileensis)中分离得到的四种具有全新 C29 骨架的新型内酯。通过广泛的光谱和 X 射线晶体衍射分析确定了它们的结构。Swerilactones H-K 对 HBV DNA 复制具有很强的抗乙型肝炎病毒活性,IC50 值范围为 1.53-5.34 μM。首次提出了 Swerilactones H-K 与其之前报道的 Swerilactones A-D 的合理生物合成途径。从生物发生学的角度来看,Swerilactones A-D 被归为裂环环烯醚萜二聚体,而 Swerilactones H-K 则为裂环环烯醚萜三聚体。

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