Abstract:

This study aims to investigate the cardiac glycoside components in the methanol extract of Calotropis gigantea (L.) W.T.Aiton and their inhibitory effect on cancer cells.Various column chromatography techniques and preparative HPLC were used to separate and purify the methanol extract of C.gigantea.The structures of the isolated compounds were identified by NMR,MS techniques.The anti-tumor effects of these compounds on human cervical cancer cells HeLa,human non-small cell lung cancer cells A549 and human hepatocellular carcinoma cells HepG2 were studied.Eventually,six compounds were isolated and identified as coroglaucigenin (1),uzarigenine (2),3-O-β-allopyranosyluzarigenin (3),frugoside (4),calotropin (5),and glucocoroglaucigenin (6).Compounds 1-6 had inhibitory effects on HeLa,A549 and HepG2 cells.Compound 5 could induce intracellular oxidative stress in human cervical cancer cells HeLa,inhibit the activity of thioredoxin reductase 1(TrxR1) and promote apoptosis.

Key words:

Calotropis gigantea, cardiac glycosides, anti-tumor activity