【摘要】 目的研究17-烯丙氨基格尔德霉素的体内外抗肿瘤作用。方法 MTT法评价17-烯丙氨基格尔德霉素对人肿瘤细胞株的体外抑制作用;荷瘤小鼠静脉注射20,40,80 mg/kg剂量的17-烯丙氨基格尔德霉素,观察小鼠对异种移植实体瘤、腹水瘤及P388白血病的抗肿瘤作用。结果 17-烯丙氨基格尔德霉素对人小细胞肺癌细胞、BEL-7402肝癌细胞、MCF7乳腺癌细胞均有明显抑制作用,可明显抑制皮下移植的S180肉瘤、Lewis肺癌、B16黑色素瘤的生长,并明显延长EAC腹水瘤、H22肝癌腹水瘤、P388白血病小鼠的生存时间。结论 17-烯丙氨基格尔德霉素具有显著的体内外抗肿瘤作用。更多还原

【Abstract】 Objective To study the in vivo and in vitro antitumor activity of 17-allylamino-17-demethoxygeldanamycin.Methods The in vitro cytotoxicity of 17-allylamino-17-demethoxygeldanamycin on a panel of human tumor cell lines was evaluated by MTT assay.The tumor-bearing mice were given 20,40 and 80 mg/kg of 17-allylamino-17-demethoxygeldanamycin intravenously,respectively,and the in vivo antitumor activities of 17-allylamino-17-demethoxygeldanamycin on solid tumor,ascites tumor and P388 leukemia in mice were evaluated.Results 17-Allylamino-17-demethoxygeldanamycin displayed obvious cytotoxic activities against small lung cancer cell,BEL-7402 cell and MCF-7 cell,and obviously inhibited the growth of S180 sarcoma,Lewis lung tumor and B16 melanoma.The survival times of mice inoculated with EAC cells,H22 cells and P-388 cells were obviously prolonged.Conclusion 17-Allylamino-17-demethoxygeldanamycin has signif icant antitumor activity in vivo and in vitro.更多还原