【摘要】 目的　研究经筛选出的法尼基转移酶抑制剂 (farnesyltransferaseinhibitors ,FTIs)CA 7的抗肿瘤作用。方法　用放射标记沉淀法筛选FTIs,结合MTT和SRB实验方法 ,对化合物CA 7进行研究 ,以生长曲线和集落形成试验研究其对不同类型细胞作用的特点 ,动物移植瘤实验观察CA 7的体内抑瘤作用。结果　在初筛的 6 0多个化合物中CA 7对法尼基转移酶 (farne syltransferase ,FTase)抑制作用最强 ,IC50 为 7.5× 10 -8mol·L-1。CA 7对几种被选瘤株表现出一定的选择性抑制作用 ,对小鼠实体型肝癌H2 2及Lewis肺癌有一定的治疗作用。结论　CA 7是一种作用于法尼基转移酶的潜在的抗肿瘤药物。更多还原

【Abstract】 OBJECTIVE To study the anti-tumor action of farnesyltransferase inhibitor(FTI) CA-7,which is screened by our experiments.METHODS FTIs were screened by radio-labeled precipitation method,MTT and SRB respectively.The effects of CA-7 on the different kinds of cancer cell lines were investigated by cell growth curve and clonogenicity tests.The antitumor action in vivo was monitored by transplantable tumor experiment.RESULTS CA-7 was the strongest inhibitor on the FTase among the supplied compounds,with IC 50 of 7.5×10 -8 mol·L -1 ,and exhibited selective inhibition on the examined cell lines.It inhibited the Lewis lung carcinoma and hepatoma H22 transplantable tumors.CONCLUSION CA-7 appeared to be a potential anti-tumor drug by acting on farnesyltransferase.更多还原