7-乙基-10-羟基喜树碱脂质体的抗肿瘤作用  

Investigation on the anti-tumor activity of SN-38 Liposome

作　　者：徐珊[1] 李增强[1] 齐欢[1] 钟飞[1] 王淑君[2] 吴英良[1] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2015年第3期218-222,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的探索7-乙基-10-羟基喜树碱(7-ethyl-10-hydroxy camptothecin,SN-38)脂质体的体内外抗肿瘤作用。方法体外实验采用噻唑蓝[3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide,M TT]法检测SN-38脂质体对9种人源肿瘤细胞的抑制作用;体内实验利用A549非小细胞肺癌和SKOV-3卵巢癌荷瘤裸鼠模型,以伊立替康为阳性对照药,统计裸鼠体质量、瘤体积、抑瘤率、相对肿瘤增殖率等指标,考察不同剂量的SN-38脂质体对肿瘤的生长抑制作用。结果体外实验表明SN-38脂质体能抑制多种肿瘤细胞增殖;体内实验表明SN-38脂质体高、中、低剂量(4、2、1 mg·kg-1)对A549荷瘤裸鼠的抑瘤率分别为69.75%、52.08%和29.78%,SN-38脂质体高、中、低剂量(8、4、2 mg·kg-1)对SKOV-3荷瘤裸鼠的抑瘤率分别为54.19%、38.91%、23.71%。结论 SN-38脂质体体外对多种肿瘤细胞有较好的抗增殖作用,体内对A549非小细胞肺癌及SKOV-3卵巢癌荷瘤裸鼠有较好的治疗作用。Objective To investigate the anti-tumor activity of 7-ethyl-10-hydroxy camptothecin （ SN-38 ） liposome by in vitro and in vivo tests. Methods In the in vitro experiment, MTT assay was applied to detect the inhibitory effect of SN-38 liposome on the growth of nine anthropogenic tumor cells. In the in vivo experiment, the BALB/c-nu mice models of A549 solid tumor and SKOV-3 solid tumor were established to evaluate the anti-tumor effect of different concentration of SN-38 liposome. Taking irinotecan as the positive drug, the influence of SN-38 liposome on nude mice body weight, tumor volume, tumor inhibition rate, rela- tive tumor proliferation rate were studied. Results SN-38 liposome could inhibit multiple tumor cells proliferation in vitro. SN-38 liposome （4,2,1 mg· kg -1 ）could inhibit the tumor expansion with the tumor inhibition rates of 69.75%, 52. 08% and 29. 78% on A549 tumor-bearing nude mice, and SN-38 liposome （ 8,4, 2 mg-kg-1）could inhibit the tumor expansion with the tumor inhibition rates of 54. 19% ,38.91% and 23.71% on SKOV-3 tumor-bearing nude mice in vivo. Conclusions SN-38 liposome possesses excellent an- ti-proliferative activities against multiple tumor cell lines in vitro and it has prominent therapeutical effect on A549 and SKOV-3 tumor-bearing nude mice in vivo.

关 键 词：7-乙基-10-羟基喜树碱 脂质体 抗肿瘤 非小细胞肺癌A549 卵巢癌SKOV-3 

分 类 号：R96[医药卫生—药理学]