In vitro and in vivo antitumor efficacy of CLA-PTX on B16-F10 melanoma cells  

CLA-PTX对黑色素瘤B16-F10的体内外抗肿瘤作用(英文)

作　　者：李捷思[1] 杨科[1] 柯曦宇[1] 杜若[1] 张烜[1] 张强[1,2] 

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]北京大学医学部天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2014年第1期46-53,共8页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.81172992);the National Basic Research Program of China(973 Program,Grant No.2009CB930300);Innovation Team of Ministry of Education(Grant No.BMU20110263)

摘　　要：The purpose of this study was to investigate the potential antitumor efficacy of conjugated linoleic acid-paclitaxel （CLA-PTX） on B16-F10 melanoma cell line in vitro and in vivo. The in vitro cytotoxicity, apoptosis and cell cycle of CLA-PTX were investigated. The in vitro cellular uptake of CLA-PTX in B16-F10 cells was also analyzed. The antitumor activity of CLA-PTX was also evaluated in B16-F10 tumor-bearing C57BL6/N mice in vivo. The in vitro cytotoxicity results showed that the IC50 of the CLA-PTX is （4.25±0.43） μM, compared with that of （6.70±0.80） μM in PTX treatment group （P〈0.01）. CLA-PTX increased the percentage of total apoptotic cells compared with that of control and PTX treatment groups （P〈0.01）. Compared with untreated cells, CLA-PTX arrested cell cycle progression at the S phase, whereas PTX caused accumulation of cell at GE-M phase both along with the reduction of the cellular fraction arrested at the G1 phase. The amount of cellular uptake of CLA-PTX was significantly higher than that of PTX （P〈0.01）. The in vivo antitumor activity of CLA-PTX was significantly higher than that of control and PTX treatment groups （P〈0.01 or P〈0.05）. In conclusion, our study demonstrated that CLA-PTX has significant antitumor activity in B 16-F 10 cell line.本研究旨在探索CLA-PTX对黑色素瘤B16-F10细胞的体内外抗肿瘤作用。选择鼠源B16-F10细胞系作为研究模型。研究CLA-PTX体外细胞毒,细胞凋亡,细胞周期作用,以及CLA-PTX体外细胞摄取作用。用荷瘤C57BL6/N小鼠研究CLA-PTX的体内抗肿瘤作用。体外细胞毒研究结果表明:CLA-PTX的IC50为(4.25±0.43)μM,优于紫杉醇(6.70±0.80)μM(P<0.01)。与空白组和紫杉醇组相比,CLA-PTX可使细胞总凋亡比例增加(P<0.01)。与空白对照组相比,CLA-PTX将细胞周期阻滞于S期,而紫杉醇则使细胞在G2‐M期蓄积。CLA-PTX的细胞摄取量显著高于紫杉醇(P<0.01)。体内抗肿瘤药效显示,CLA-PTX抗肿瘤活性显著高于空白对照组和紫杉醇组(P<0.01或P<0.05)。上述结果表明,CLA-PTX对B16-F10细胞有显著体内外抗肿瘤作用。

关 键 词：CLA-PTX APOPTOSIS Cell cycle Cellular uptake Antitumor efficacy 

分 类 号：R739.5[医药卫生—肿瘤]