瑞香狼毒中的瑞香烷型二萜糖苷。

Tigliane-type diterpenoid glycosides from Euphorbia fischeriana.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany , Chinese Academy of Sciences, Kunming 650204, People's Republic of China.

出版信息

J Nat Prod. 2011 Jun 24;74(6):1508-12. doi: 10.1021/np200058c. Epub 2011 May 2.

DOI:10.1021/np200058c

PMID:21534540

Abstract

Investigation of whole plants of Euphorbia fischeriana afforded three new tigliane-diterpenoid glycosides, fischerosides A-C (1-3), together with 11 known diterpenoids. Fischerosides A-C (1-3) are the first tigliane-type diterpenoid glucosides. Their structures were determined by a combination of 1D and 2D NMR, MS, and acid hydrolysis. Inhibitory activity against HIV-1 was assessed for compounds 1-5. The new compound 3 showed an EC₅₀ value of 0.02 μM and a therapeutic index (TI) of 17.50, while prostratin (4) and 12-deoxyphorbol-13,20-diacetate (5) showed significantly greater anti-HIV-1 activity.

摘要

对飞扬草全草进行研究得到了三种新的瑞香烷二萜糖苷，即 Fischerosides A-C（1-3），以及 11 种已知的二萜类化合物。Fischerosides A-C（1-3）是第一类瑞香烷型二萜葡萄糖苷。通过 1D 和 2D NMR、MS 和酸水解的组合，确定了它们的结构。对化合物 1-5 进行了抗 HIV-1 的活性评估。新化合物 3 的 EC₅₀ 值为 0.02 μM，治疗指数（TI）为 17.50，而 prostratin（4）和 12-脱氧佛波醇-13,20-二乙酸酯（5）表现出更强的抗 HIV-1 活性。