【摘 要】
：
Multidrug resistance (MDR) is one of the major obstacles in cancer chemotherapy.Our previous study has shown that icariin could reverse MDR in MG-63 doxorubicin-resistant (MG-63/DOX) cells.It is reported that icariin is usually metabolized to icariside Ⅱ
【机 构】
：
State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmace
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Multidrug resistance (MDR) is one of the major obstacles in cancer chemotherapy.Our previous study has shown that icariin could reverse MDR in MG-63 doxorubicin-resistant (MG-63/DOX) cells.It is reported that icariin is usually metabolized to icariside Ⅱ and icaritin.Herein,we investigated the effects of icariin,icariside Ⅱ,and icaritin (ICT) on reversing MDR in MG-63/DOX cells.Among these compounds,ICT exhibited strongest effect and showed no obvious cytotoxicity effect on both MG-63 and MG-63/DOX cells ranging from 1 to 10 μrnol·L-1.Furthermore,ICT increased accumulation of rhodamine 123 and 6-carboxyfluorescein diacetate and enhanced DOX-induced apoptosis in MG-63/DOX cells in a dose-dependent manner.Further studies demonstrated that ICT decreased the mRNA and protein levels of multidrug resistance protein 1 (MDR1) and multidrug resistance-associated protein 1 (MRP1).We also verified that blockade of STAT3 phosphorylation was involved in the reversal effect of multidrug resistance in MG-63/DOX cells.Taken together,these results indicated that ICT may be a potential candidate in chemotherapy for osteosarcoma.
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