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机构地区:[1]湖南师范大学医学院,湖南长沙410006 [2]南华大学药物药理研究所,湖南衡阳421001
出 处:《中国药理学通报》2008年第10期1370-1373,共4页Chinese Pharmacological Bulletin
基 金:湖南省自然科学基金资助项目(No03JJY5009)
摘 要:目的观察8-溴-7-甲氧基白杨素(8-bromo-7-methoxy-chrysin,BrMChR)诱导人胃癌(SGC-7901)细胞凋亡作用。方法体外培养SGC-7901细胞,MTT法测定细胞存活率;PI染色流式细胞术(FCM)分析细胞凋亡率;DNA琼脂糖凝胶电泳观察梯形条带。结果MTT测定结果显示,BrMChR明显抑制SGC-7901细胞增殖,呈浓度依赖性,其IC50为2.6μmol·L-1,BrMChR的效价强度约是白杨素(ChR,IC50为16.5μmol·L-1)的8倍,约为氟尿嘧啶(5-FU,IC50为7.7μmol·L-1)的3倍。PI染色FCM分析发现BrMChR(1.25、5.00、20.00μmol·L-1)作用SGC-7901细胞48h的细胞凋亡率分别是19.8%±0.2%,36.8%±1.9%,45.5%±3.5%,BrMChR(1.25μmol·L-1)处理的细胞凋亡率较ChR(20.00μmol·L-1)的凋亡率(12.9%±1.5%)高;DNA琼脂糖凝胶电泳观察BrMChR(20.00μmol·L-1)作用24h和48h后SGC-7901细胞的基因DNA呈现典型梯形条带,且能被PPARγ阻断剂GW9662(10.00μmol·L-1)预孵育减弱。结论BrMChR可能部分通过活化PPARγ诱导SGC-7901细胞凋亡。Aim To investigate the effect of 8-bromo-7- methoxychrysin(BrMChR) on apoptosis of human gastric carcinoma SGC-7901 cell line. Methods SGC-7901 cells were cultured and the inhibitory effect of BrMChR on the proliferation of SGC-7901 cell line was measured by MTT assay . The apoptosis of SGC-7901 cells induced by BrMChR was analyzed using flow cytometry (FCM) with PI staining. DNA ladder bands were observed by DNA agarose gel electrophoresis. Resuits MTT assay suggested that BrMChR markedly inhibited the proliferation of SGC-7901 cells in a concentration-dependent manner, its IC50 was 2.6 μmol · L^-1, the potency of BrMChR was 8 times more than that of lead compound, chrysin ( ChR, IC50 was 16.5 μmol · L^-1 ), and was 3 times more than that of 5-fluorouracil (5-FU,IC50 was 7.7 μmol · L^-1 ). FCM with PI staining indicated the apoptotic rate of SGC-7901 cell line treated with BrMChR ( 1.25,5.00, 20. 00 μmol ·L^-1) for 48 h was (19.8% ± 0.2%),(36. 8% ± 1.9% ) and (45.5% ±3.5% ) respectively and the rate treated with BrMChR (1.25 μmol · L^-1) was higher than that treated with ChR (20.00 μmol · L^-1,12.9% ± 1.5% ). DNA agarose gel eleetrophoresis showed that when treated with BrMChR (20. 00 μmol · L^-1) for 48 h,the gene DNA of SGC- 7901 cells presented typical DNA ladder bands which could attenuated by the effect of pre-incubation of GW9662( 10.00 μmol · L^-1 ) , a blocker of PPARγ. Conclusion BrMChR might induce apoptosis of SGC- 7901 cell line partially by activating PPARγ.
关 键 词:胃肿瘤 白杨素 8-溴-7-甲氧基白杨素 凋亡
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