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甘肃大戟中具有独特葎草烯-间苯三酚骨架的细胞毒倍半萜糖苷化合物大戟苷 A。

Euphorboside A, a cytotoxic meroterpenoid glycoside with an unusual humulene-phloroglucinol skeleton from Euphorbia kansuensis.

机构信息

School of Pharmacy, Guizhou Medical University, Guian New District 550025, Guizhou, China.

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.

出版信息

Fitoterapia. 2021 Sep;153:104966. doi: 10.1016/j.fitote.2021.104966. Epub 2021 Jun 15.

Abstract

Euphorboside A (1), an unusual meroterpenoid glycoside featuring the incorporation of an acylphloroglucinol moiety into a humulene skeleton to form a 6/6/11 ring system, was isolated from the roots of Euphorbia kansuensis. Its structure was elucidated by extensive spectroscopic analysis, chemical methods, and ECD calculations. Compound 1 was screened for the cytotoxicity against nine cancer cell lines, and 1 showed marked inhibitory activities against human colon cancer RKO and human breast cancer MDA-MB-231 cell lines with IC values of 3.70 and 4.15 μM, respectively.

摘要

大戟苷 A(1)是一种罕见的倍半萜苷类化合物,其特征在于将酰基间苯三酚部分并入到葎草烯骨架中,形成 6/6/11 环系统,从甘肃大戟的根部分离得到。通过广泛的光谱分析、化学方法和 ECD 计算阐明了其结构。对化合物 1 进行了对 9 种癌细胞系的细胞毒性筛选,化合物 1 对人结肠癌 RKO 和人乳腺癌 MDA-MB-231 细胞系表现出显著的抑制活性,IC 值分别为 3.70 和 4.15 μM。

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