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机构地区:[1]江苏省人民医院肿瘤科 [2]江苏省人民医院心胸外科
出 处:《中国临床药理学与治疗学》2010年第8期851-855,共5页Chinese Journal of Clinical Pharmacology and Therapeutics
摘 要:目的:观察连翘中分离所得两种三萜类化合物:达玛-24-烯-3β-乙酰氧基-20s-醇[20(s)-dammar-24-ene-3β,20-diol-3β-acetate,DM]和五环齐墩果烷型三萜类化合物安博立酸(ambrolicacid,AA)对5种人消化道肿瘤细胞的抑制作用,以及AA对人胃癌细胞株SGC-7901的凋亡诱导作用。方法:MTT法观察AA和DM对5株人消化道肿瘤细胞株MKN-45、MKN-28、SGC-7901、PNAC-1、HepG-2的生长抑制作用,Annex-in-V/PI染色流式细胞术测定SGC-7901细胞的凋亡率,Western blotting检测相关凋亡蛋白表达。结果:两种三萜类化合物对人消化道肿瘤细胞有较好的抑制作用,其作用呈剂量依赖性;AA作用细胞72h后可以明显诱导细胞凋亡,而DM对细胞未有凋亡诱导作用;AA可下调pro-caspase3、6、8、9蛋白和Bcl-2蛋白表达水平,同时可上调Bax蛋白水平。结论:AA和DM对5株人消化道肿瘤细胞有明显抑制作用,AA诱导SGC-7901细胞凋亡的主要途径可能为调节凋亡相关蛋白的表达。AIM:To explore the inhibitory effects of ambrolic acid(AA)and 20(s)-dammar-24-ene-3β,20-diol-3β-acetate(DM)on five human digestive cancer cell lines and the mechanism of apoptotic induction effect of AA on human gastric cancer cell line SGC-7901.METHODS:MTT assay was used to observe the anti-proliferation effect of AA and DM on MKN-45,MKN-28,SGC-7901,PNAC-1 and HepG-2 cancer cell lines.The apoptosis rates of SGC-7901 treated by AA or DM were determined by flow cytometry(FCM).With western blotting,the levels of apoptotic-pathway related proteins were determined.RESULTS:AA and DM inhibited the proliferation of cancer cells in a dose-dependent manner.FCM analysis showed that cells co-incubated with AA were induced apoptosis dose-dependently,while DM had no ability to induce apoptosis.AA could down-regulate the levels of pro-caspase 3,6,8,9 and Bcl-2 proteins and up-regulate the levels of Bax proteins.CONCLUSION:AA and DM have significant inhibitory activities in 5 human digestive cancer cell lines.The potential mechanism of apoptosis-induction effect caused by AA on SGC-7901 may due to its ability to regulate the levels of apoptotic-related proteins.
关 键 词:连翘 安博立酸 达玛-24-烯-3β-乙酰氧基-20s-醇 胃癌 凋亡
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