Cytotoxic cardenolides from Calotropis gigantea
Cytotoxic cardenolides from Calotropis gigantea
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来自牛角豆的细胞毒性强心内酯
DOI：
10.1016/j.phytochem.2021.112951
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发表时间：
2021-09-24
期刊：
影响因子：
3.8
通讯作者：
Gao, Kun
中科院分区：
文献类型：
--
作者：
He, Yi-Lin;Yang, Hong-Ying;Gao, Kun
本文报道了从马蹄莲（Calotropis acutea（L.）光谱数据和电子圆二色性（ECD）分析用于确定其结构。Caloclavin C是第一个天然存在的在环A中含有7元内酯的Cardenlavin的例子。评价了这些化合物对A172、U251、AGS、PANC-1、HepG 2、HCT 116和NCI-H226细胞系的细胞毒活性。其中四个对一组人癌细胞系表现出最有效的生长抑制活性，包括A172，U251，AGS，PANC-1和HCT 116。值得注意的是，uscharidin和calotropin在低纳摩尔浓度下对A172和U251细胞显示出明显的细胞毒性，并且可能的细胞死亡机制研究表明，这两种化合物诱导G2/M细胞周期阻滞，这显示出有希望的抗癌潜力。
Sixteen cardiac glycosides, including five previously undescribed compounds, were extracted and purified from whole plants of Calotropis gigantea (L.). Spectroscopic data and electronic circular dichroism (ECD) analyses were used to determine their structures. Calogiganin C is the first naturally occurring example of a cardenolide containing a 7-membered lactone in ring A. The cytotoxic activities of these compounds against A172, U251, AGS, PANC-1, HepG2, HCT116 and NCI-H226 cell lines were evaluated. Four of them exhibited the most potent growth inhibitory activity against a panel of human cancer cell lines, including A172, U251, AGS, PANC-1 and HCT116. Notably, uscharidin and calotropin showed pronounced cytotoxicities at low nanomolar concentrations against A172 and U251 cells, and possible cell death mechanism studies manifested that these two compounds induced G2/M cell cycle arrest, which demonstrated promising anticancer potential.