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Abstract
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 icaris-ide
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 μmol·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.
Author and article information
Journal
Title:
Chinese Journal of Natural Medicines
Abbreviated Title:
Chinese Journal of Natural Medicines