【摘要】 目的检测长春氟宁对微管聚集的作用,并研究长春氟宁体外和体内的抗肿瘤作用。方法用浊度实验检测长春氟宁对微管聚集的抑制作用,并以多株肿瘤细胞和荷瘤小鼠分别研究长春氟宁体外、体内的抗肿瘤作用。结果长春氟宁抑制猪脑中提取的微管的聚集,IC50为2.0μmol·L-1;体外试验,长春氟宁抑制多株瘤细胞的IC50在0.05～2.2μmol·L-1之间;体内试验,长春氟宁剂量依赖性地抑制小鼠不同类型移植肿瘤的生长。长春氟宁体外和体内的药物作用比阳性对照药物长春瑞宾弱,但从最大药物疗效来看,长春氟宁对体内肿瘤生长的抑制率比长春瑞宾大。结论长春氟宁能够抑制微管的聚集,在体外体内均有明显的抗肿瘤作用。更多还原

【Abstract】 Aim To evaluate inhibitory effects of vinflunine on cellular microtubule assembly,and antitumor effects of vinflunine in vitro and in vivo. Methods Turbidity experiment was conducted to analyze the effects of vinflunine on microtubule assembly. Various tumor cell lines and mice implanted with different tumors were used to study anti-tumor effects of vinflunine in vitro and in vivo, respectively. Results Vinflunine inhibited microtubule assembly with an IC₅0 value of 2.0 μmol·L-1. In vitro, vinflunine exhibited significant cytotoxicity on various tumor cell lines with IC₅0 values ranging from 0.05～2.2 μmol·L-1. In vivo vinflunine dose-dependently inhibited different tumor growth in mice. The potency of vinflunine was lower than that of vinorelbine in vitro and in vivo. However, at the dose of the strongest efficacy, vinflunine had more significant activity compared with vinorelbine. Conclusion Vinflunine inhibits cellular microtubule assembly and shows significant antitumor effects both in vivo and in vitro.更多还原