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从秘鲁桐种子中分离得到具有细胞毒性的强心苷。

Cardiac glycosides with cytotoxic activity from the seeds of Thevetia peruviana.

机构信息

Guangdong Provincial Key Laboratory of Research and Development of Natural Drugs, School of Pharmacy, Guangdong Medical University, Dongguan 523808, PR China.

GuangDong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, Key Lab of Zhanjiang for R&D Marine Microbial Resources in the Beibu Gulf Rim and School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, PR China.

出版信息

Fitoterapia. 2024 Sep;177:106126. doi: 10.1016/j.fitote.2024.106126. Epub 2024 Jul 15.

Abstract

Phytochemical investigation on the extract of the seeds of Thevetia peruviana resulted in the isolation of six new cardiac glycosides, namely theveperosides A-F (1-6), including a rare 19-nor-cardenolide (1), together with seven known analogues (7-13). The chemical structures of these compounds were determined based on detailed spectroscopic analysis. The cytotoxic activities of 1-13 were evaluated against MCF-7, HCT-116, HeLa, and HepG2 cancer cell lines, and their structure-activity relationships (SARs) were investigated. Compound 3 exhibited the significant cytotoxic effects with IC values ranging from 0.032 to 0.055 μΜ, which could induce HepG2 cells apoptosis in a dose-dependent manner.

摘要

从假鹰爪属植物的种子提取物中进行植物化学研究,分离得到了六种新的强心苷,分别为 theveperosides A-F(1-6),包括一种罕见的 19-去甲强心甾内酯(1),以及七种已知类似物(7-13)。这些化合物的化学结构是基于详细的光谱分析确定的。评估了 1-13 对 MCF-7、HCT-116、HeLa 和 HepG2 癌细胞系的细胞毒性活性,并研究了它们的结构-活性关系(SAR)。化合物 3 表现出显著的细胞毒性作用,IC 值范围为 0.032 至 0.055 μΜ,可呈剂量依赖性诱导 HepG2 细胞凋亡。

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