Hang Zhang, Shaopan Bian, Zhihao Xu, Ming Gao, Han Wang, Junwei Zhang, Mingkun Zhang, Yu Ke, Weijia Wang, Zhe-Sheng Chen, Haiwei Xu
Encequidar, a gut-specific P-glycoprotein (P-gp) inhibitor, makes oral paclitaxel possible, and has been used in clinical treatment of metastatic breast cancer, however, its pharmacological effect and mechanism of reversal of drug resistance in drug-resistant colon cancer cells SW620/AD300 are still unknown. Herein, we first synthesized encequidar and demonstrated that it could inhibit the transport activity of P-gp, reduced doxorubicin (DOX) efflux, enhanced DOX cytotoxicity and promoted tumor-apoptosis in SW620/AD300 cells...
September 27, 2022: Biochemical Pharmacology