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Journal of Chinese Pharmaceutical Sciences ›› 2014, Vol. 23 ›› Issue (1): 46-53.DOI: 10.5246/jcps.2014.01.007

• Original articles • Previous Articles     Next Articles

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

Jiesi Li, KeYang, Xiyu Ke, Ruo Du, Xuan Zhang*, Qiang Zhang   

  1. 1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2013-03-26 Revised:2013-05-07 Online:2014-01-23 Published:2014-01-22
  • Contact: Xuan Zhang*
  • About author:*Corresponding author. Tel./Fax: +86-10-82802683; E-mail: xuanzhang@bjmu.edu.cn
  • Supported by:
    National Natural Science Foundation of China (Grant No. 81172992) and the National Basic Research Program of China (973 Program, Grant No. 2009CB930300) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

Abstract:

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 G2-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 B16-F10 cell line.

Key words: CLA-PTX, Apoptosis, Cell cycle, Cellular uptake, Antitumor efficacy

CLC Number: 

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