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The aim of the study was to investigate the anti-proliferation and apoptosis-inducing effects of S1, a novel tetrandrine derivative, in human gastric cancer BGC-823 cells and explore the possible mechanism of action. The anti-proliferative activity was determined by MTT assay; the induction of cell cycle arrest and apoptosis were detected by flow cytometry. Quantitative real time RT-PCR and Western blotting were used to evaluate the m RNA and protein expression levels in mitochondrial pathway. S1 significantly reduced cell viability and induced a G2/M phase arrest and apoptosis in dose- and time-dependent manner. Further studies showed that S1 increased m RNA and protein expression of Bax and the Bax/Bcl-2 ratio. Moreover, S1 decreased the protein expression of procaspase-9 and procaspase-3, suggesting that the induction of apoptosis may be related to the alteration of the ratio of Bax/Bcl-2 and the activation of caspases. These findings suggested that S1 merits further investigation as a novel therapeutic agent for the treatment of human gastric cancer.
The aim of the study was to investigate the anti-proliferation and apoptosis-inducing effects of S1, a novel tetrandrine derivative, in human gastric cancer BGC-823 cells and explore the possible mechanism of action. The anti-proliferative activity was determined by MTT assay; the induction of cell cycle arrest and apoptosis were detected by flow cytometry. Quantitative real time RT-PCR and Western blotting were used to evaluate the m RNA and protein expression levels in mitochondrial pathway. S1 significant reduced cell viability and induced a G2 / M phase arrest and apoptosis in dose- and time-dependent manner. Further studies showed that S1 increased the mRNA and protein expression of Bax and the Bax / Bcl-2 ratio. Moreover, S1 decreased the protein expression of procaspase-9 and procaspase- 3, suggesting that the induction of apoptosis may be related to the alteration of the ratio of Bax / Bcl-2 and the activation of caspases. These findings suggested that S1 merits further investigation a s a novel therapeutic agent for the treatment of human gastric cancer.