【摘要】 目的 观察国内合成的抗肿瘤化合物CA4P对体外培养的人癌细胞和荷瘤动物的抗肿瘤作用，为抗癌新药的研究和开发提供实验依据。 方法 体外实验采用MTT法测定CA4P对培养的人癌细胞的半数生长抑制浓度(IC 50 );体内实验观察CA4P对荷瘤动物肿瘤生长的抑制率。 结果 CA4P对5株人癌细胞(乳腺癌A457、肝癌Bel-7402、口腔癌KB、结肠癌HT-29、胃癌SGC-7901)的IC 50 值分别为:0.26、1.14、1.94、9.90、40.67μg/ml。CA4P对荷瘤小鼠肝癌(H22)、肉瘤(S180)、和肺癌(LLC)的抑瘤率分别为:66.7%、81.5%和57.8%;对大鼠肉瘤W256的抑瘤率为69.2%;对荷瘤裸鼠人结肠癌(HT-29)的抑瘤率为76.7%。 结论 CA4P具有明显的体内外抗肿瘤作用。

    关键词 Compretastatin(CA4P) 抗肿瘤作用

    Studies on the anticancer effect of compretastatin(CA4P)in vitro and in vivo

    Fang Jiachun，Wang Naiqin，Liu Tong，et al.

    Department of Clinical Pharmacology，The School of Oncology，Peking University，Beijing100034.

    【Abstract】 Objective To investigate the antitumor action of compretastatin(CA4P)in vitro and in vivo.Methods In the cytotoxic test on human cancer cell lines of culture in vitro seek to obtain IC50of CA4P.In the an-titumor test on transplantable solid tumor in mice and rats seek to obtain inhibitory tumor rate of CA4P.Results The IC50of CA4P on5human cancer cell lines were0.26μg/ml(breast cancer);1.14μg/ml(liver cancer);1.94μg/ml(oral cavity cancer);9.90μg/ml(colon cancer)and40.67μg/ml(stomach cancer) ......