title: Anti-proliferative and apoptotic effects of S1, a tetrandrine derivative, in human gastric cancer BGC-823 cells.
abstract: 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 mRNA 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 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 as a novel therapeutic agent for the treatment of human gastric cancer.
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors: Rong-Rong
authors: RR
authors: Lei
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China; Sinopharm Health Industry Research Co., Ltd., Shanghai 200040, China.
authors: Hai-Feng
authors: HF
authors: Hu
authors: The Kochi Prefectural Makino Botanical Garden, Kochi 4200-6, Japan.
authors: Fan
authors: F
authors: Bai
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China; Sinopharm Health Industry Research Co., Ltd., Shanghai 200040, China.
authors: Ying
authors: Y
authors: Liu
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China; Sinopharm Health Industry Research Co., Ltd., Shanghai 200040, China. Electronic address: czw1962@126.com.
authors: Chun-Zhen
authors: CZ
authors: Wu
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors: Xiao-Xing
authors: XX
authors: Huang
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors: Li-Ping
authors: LP
authors: Xie
authors: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors: You-Jia
authors: YJ
authors: Hu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D044182:Benzylisoquinolines / Q000737:chemistry / Q000494:pharmacology*; D053148:Caspase 3 / Q000235:genetics / Q000378:metabolism; D053453:Caspase 9 / Q000235:genetics / Q000378:metabolism; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics / Q000378:metabolism; D013274:Stomach Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000235:genetics / Q000503:physiopathology*; D051028:bcl-2-Associated X Protein / Q000235:genetics / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D044182:Benzylisoquinolines; D019253:Proto-Oncogene Proteins c-bcl-2; D051028:bcl-2-Associated X Protein; C009438:tetrandrine; D053148:Caspase 3; D053453:Caspase 9
keywords: Apoptosis; BGC-823 cells; G2/M phase arrest; Tetrandrine derivative