학술논문
Reversal Effect of Apatinib on P-gp-mediated Multidrug Resistance of Human Breast Cancer and Its Mechanisms
Document Type
article
Author
Source
Zhongliu Fangzhi Yanjiu, Vol 45, Iss 4, Pp 210-214 (2018)
Subject
Language
Chinese
ISSN
1000-8578
Abstract
Objective To investigate the reversal effect of apatinib on the multidrug resistance of human breast cancer and the underlying mechanisms. Methods MCF-7 and MCF-7/ADR cells were treated with different concentrations of apatinib for 48h. Cell proliferation was measured by MTT assay. The reversal effect of apatinib on the multidrug resistance of MCF-7/ADR cells to paclitaxel and adriamycin were investigated by MTT assay. The effects of apatinib on the accumulation of rhodamine 123 in MCF-7 and MCF-7/ADR cells were investigated by flow cytometry. The effect of apatinib on ATPase activity of P-gp was investigated by Pgp-GloTM Assay Systems. The effects of apatinib on the expression of P-gp, AKT and p-AKT were investigated by Western blot. Results Apatinib could reverse the multidrug resistance of MCF-7/ADR cells to paclitaxel and adriamycin, increase the accumulation of rhodamine 123 in MCF-7/ADR cells and the ATPase activity of P-gp in a concentration-dependent manner (P < 0.05). Apatinib had no effect on the expression of P-gp or the phosphorylation of AKT. Conclusion Apatinib could reverse the P-gp-mediated multidrug resistance of human breast cancer cell line MCF-7/ADR by inhibiting the efflux function of P-gp.