摘要目的 探讨鬼臼毒素纳米制剂的理化性质,通过实验评价其抗人胶质瘤U251细胞的作用.方法 通过透析法制备鬼臼毒素载药聚合物胶团,应用细胞毒性实验、肿瘤细胞摄取实验、6-二脒基-2-苯基吲哚(DAPI)染色观察细胞凋亡效应评价其疗效.结果 鬼臼毒素聚合物胶团的半数抑制浓度(IC50)值在24、48、72 h时分别为(7.18±0.82)、(5.71±0.18)、(2.57±0.12) μg/ml,明显低于游离鬼臼毒素,细胞摄取率约为游离鬼臼毒素的2倍,鬼臼毒素聚合物胶团作用后的U251细胞有明显的细胞凋亡的形态学改变.结论 鬼臼毒素纳米制剂能够有效抑制人胶质瘤U251细胞的增殖.

abstractsObjective To study the physiochemical characteristics of the stearic acid-grafted chitosan oligosaccharide polymeric micelles loading podophyllotoxin (CSO-SA/PPT),and evaluate the ability of CSO-SA/PPT to inhibit the human U251 glioma cells growth.Methods CSO-SA/PPT were prepared by a dialysis method.The ability of CSO-SA/PPT to inhibit cell proliferation and its uptake in the glioma cells,and morphology of nclear of human U251 glioma cells were observed.Results 50％ inhibitory concentration (IC50) values of CSO-SA/PPT were (7.18 ± 0.82),(5.71 ± 0.18),(2.57 ±0.12) μg/ml respectively after 24,48,72 h and were lower than that of podophyllotoxin.Cellular uptake percentage of CSO-SA/PPT was almost two times as much as podophyllotoxin.4',6-Diamidino-2-phenylindole dihydrochloride (DAPI) staining showed typical apoptosis morphologyical characteristics of U251 cells after uptake CSO-SA/PPT.Conclusion CSO-SA/PPT can inhibit human U251 glioma cells proliferation,and provide a promising approach for chemotherapy of gliomas.