ABSTRACT
OBJECTIVE: To investigate berberine's potential to enhance the sensitivity of doxorubicin-resistant human leukemia cell lines (K562/DOX) to doxorubicin in vitro. METHODS: MTT assay was performed to determine the effect of berberine on the sensitivity of K562/DOX cells to doxorubicin. Doxorubicin accumulation assay was performed by Arrary Scan VTI HCS600 High-Contents. The effect of berberine on doxorubicin-induced cell apoptosis was tested by PI/Hoechst 33342 assay. The efflux activity of P-gp was investigated by measuring the accumulation of the rhodamine 123 after treatment with berberine. RESULTS: μmol · L-1 of berberine, as a wild dose, reduced IC50 of doxorubicin to K562/DOX cells by 1.5 times. 1 μmol · L-1 of berberine showed the enhancement effect on doxorubicin-induced apoptosis. The increase of doxorubicin and rhodamine 123 accumulation was observed in K562/ DOX cells treated with 1 μmol · L-1 of berberine which indicated the inhibition of the activity of P-gp. CONCLUSION: Berberine is shown to effectively enhance chemosensitivity of K562/DOX cells to Dox by inhibiting the efflux activity of P-gp.