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长梗秦艽酮体外抗肿瘤活性及其作用机制探讨
引用本文:章漳,段朝辉,丁侃,王峥涛.长梗秦艽酮体外抗肿瘤活性及其作用机制探讨[J].中国药学杂志,2010,45(4):259-263.
作者姓名:章漳  段朝辉  丁侃  王峥涛
作者单位:上海中医药大学中药研究所中药标准化教育部重点实验室;中国科学院上海药物所糖生物学及糖化学实验室;
基金项目:国家自然科学基金资助项目(30770484)
摘    要: 目的 研究长梗秦艽酮体外抗肿瘤活性,探讨其部分作用机制。方法 采用噻唑蓝(MTT)法观察长梗秦艽酮对BEL-7402,HeLa,BXPC-3,PANC-1细胞增殖的影响,流式细胞术分析其对BEL-7402细胞周期的影响,Western blot法检测其对ERK1/2蛋白激酶磷酸化的作用,RT-PCR法检测其对p53和乙酰肝素酶(heparanase)的mRNA表达水平的影响。 结果 长梗秦艽酮能够显著抑制4种肿瘤细胞的生长。长梗秦艽酮作用于BEL-7402细胞后能够引起S期细胞周期阻滞,激活ERK1/2磷酸化而对p38磷酸化没有影响,上调p53的mRNA表达水平,抑制乙酰肝素酶的mRNA表达。结论 长梗秦艽酮具有显著的抗肿瘤活性,其作用机制可能与激活ERK1/2信号通路及上调p53基因从而诱导细胞周期阻滞和抑制乙酰肝素酶的表达有关。

关 键 词:长梗秦艽酮  肿瘤  细胞周期  ERK1/2  p53  乙酰肝素酶
收稿时间:2012-01-01;

Bioactivity and Mechanism Study of Waltonitone on Tumor Cells Growth in vitro
ZHANG Zhang,DUAN Chao-hui,DING Kan,WANG Zheng-tao.Bioactivity and Mechanism Study of Waltonitone on Tumor Cells Growth in vitro[J].Chinese Pharmaceutical Journal,2010,45(4):259-263.
Authors:ZHANG Zhang    DUAN Chao-hui  DING Kan  WANG Zheng-tao
Institution:ZHANG Zhang1,2,DUAN Chao-hui1,DING Kan2,WANG Zheng-tao1(1.Key Laboratory of St,ardization of Chinese Medicines of Ministry of Education,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China,2.Glycobiology , Glycochemistry Laboratory,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,China)
Abstract:OBJECTIVE To investigate inhibitory effects of waltonitone(WT),a new ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill,on several human tumor cells growth in vitro and to understand the possible mechanisms.METHODS The potential effect of WT on the cell viability was examined using MTT assay.The cell cycle distribution of BEL7402 cells treated with WT was analyzed by flow cytometry.Phosphorylation of ERK1/2 and p38 MAPK were detected by Western blot,while the mRNA expression of p53 an...
Keywords:waltonitone  tumor  cell cycle  ERK1/2  p53  heparanase  
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