肿瘤药学Issue(1)：26-31,6.DOI:10.3969/j.issn.2095-1264.2014.005
两种新型西地那非同系物对 MCF-7/ADR 细胞对阿霉素耐药的影响
Effects of Two Novel Compounds on the Drug Resistance of MCF-7/ADR cell to Doxorubicin
摘要
Abstract
Objective To explore the reversal effects of XDNF1-0425 and XDNF8-0113 on Doxorubicin resistance in human breast cancer cell line MCF-7/ADR in vitro. Methods GENMED phosphodiesterase5 (PDE5) activity assay kit was used to detect the inhibition of two kinds of sildenafil homologues to PDE5. MTT assay was used to determine the cell growth inhibiting ratio of human breast cancer cell line MCF-7 and MCF-7/ADR cells after treated by Sildenafil, XDNF1-0425, XDNF8-0113, Doxorubici (DOX) or Doxorubici (DOX) plus Sildenafil homologues. Further more, figured out each inhibi-tive concentration 50 (IC50) of DOX. The expression of P-gp was determined with Western blot. Results It showed that the two kinds of homologues (XDNF1-0425 and XDNF1-0113) have weaker inhibitory activity of PDE5 than the sildenafil. The sensitivity of MCF-7/ADR to DOX was significantly increased by XDNF1-0425 and XDNF1-0113 in a dose-dependent manner (P<0.05). The sensitivity of MCF-7/ADR to DOX was significantly increased with a reversal fold of 6.36/5.58 by 10 μmol·L-1 XDNF1-0425/XDNF1-0113, and even increased with a reversal fold of 11.83/13.47 by 20 μmol·L-1 XDNF1-0425/XDNF1-0113. Western blot results showed that both homologues had no effect on the expression of protein. Conclusion The two Sildenafil homologues have a weaker inhibitory activity. Certain concentration of Sildenafil homologues could effectively reverse Doxorubicin resistance in human breast cancer cell line MCF-7/ADR in vitro.关键词
西地那非/阿霉素/逆转/肿瘤多药耐药Key words
Sildenafil/Doxorubicin/Reverse/Multidrug resistance分类
医药卫生引用本文复制引用
黄海波,陈思东,季恒,葛如意,吴冰,梁英杰,周俊立,李晓华,林海逢,汪保国..两种新型西地那非同系物对 MCF-7/ADR 细胞对阿霉素耐药的影响[J].肿瘤药学,2014,(1):26-31,6.基金项目
广东省高等学校大学生创新实验项目（10573120033）；广州市国际区域科技合作项目（2011J5200017）。 （）
