New anti-proliferative triterpenes from hydrolyzate of total Gynostemma pentaphyllum saponins induces cell cycle arrest and apoptosis in human breast cancer cells

Abstract

• Three undescribed triterpenes were obtained from hydrolyzate of G. pentaphyllum . • All the isolated compounds exhibited significant cytotoxic activity. • Gypensapogenin II possessed good anti-proliferative selectivity against Bcap37 cells. • It significantly inhibited proliferation and migration led to G1 cells cycle arrest. • It also induced apoptosis in Bcap37 cells through mitochondrial pathway. Phytochemical investigation of the hydrolysate in total Gynostemma pentaphyllum saponins led to the isolation of three previously undescribed triterpenes, Gypensapogenin II ( 1 ), Gypensapogenin III ( 2 ), and Gypensapogenin IV ( 3 ), together with five known compounds. Their structures were mainly identified by NMR and HR-ESI-MS data. All isolated compounds were evaluated in Bcap37, A549, Hela, and HepG-2 cells and showed significant anti-cancer activities, while having a much weaker effect on the growth of normal human breast cells (MCF-10a) and lung fibroblast cells (MRC5). Among the compounds, compound 1 possessed good anti-proliferative selectivity against Bcap37 cells (IC 50 value of 6.13 ± 0.86 μM). Furthermore, basic mechanism studies revealed that compound 1 significantly decreased survival and inhibited proliferation and migration leading to G1 cell cycle arrest and apoptosis in Bcap37 cells through mitochondrial pathway. Taken together, these results indicated compound 1 exerted promising anti-proliferative activity, and inhibited the migration and promoted the apoptosis of Bcap37 cells.