【摘 要】
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Previously,we reported that Y6,a new epigallocatechin gallate derivative,is efficacious in reversing doxorubicin (DOX)-mediated resistance in hepatocellular car
【机 构】
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Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St.John’s University
论文部分内容阅读
Previously,we reported that Y6,a new epigallocatechin gallate derivative,is efficacious in reversing doxorubicin (DOX)-mediated resistance in hepatocellular carcinoma BEL-7404/DOX cells.In this study,we evaluated the efficacy of Y6 in reversing drug resistance both in vitro and in vivo by determining its effect on the adenosine triphosphate-binding cassette protein B1 transporter (ABCB1 or P-glycoprotein,P-gp).Our results showed that Y6 significantly sensitized cells overexpressing the ABCB1 transporter to anticancer drugs that are ABCB1 substrates.Y6 significantly stimulated the adenosine triphosphatase activity of ABCB1.Furthermore,Y6 exhibited a higher docking score as compared with epigallocatechin gallate inside the transmembrane domain of ABCB1.In addition,in the nude mouse tumor xenograft model,Y6 (110mg/kg,intragastric administration),in combination with doxorubicin (2 mg/kg,intraperitoneal injection),significantly inhibited the growth of BEL-7404/DOX cell xenograft tumors,compared to equivalent epigallocatechin gallate.In conclusion,Y6 significantly reversed ABCB1-mediated multidrug resistance and its mechanisms of action may result from its competitive inhibition of the ABCB1 drug efflux function.
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