Reversal of P-glycoprotein-mediated MDR by 5,7,3′,4′,5′-pentamethoxyflavone and SAR
Copyright policy )Reversal of P-glycoprotein-mediated MDR by 5,7,3′,4′,5′-pentamethoxyflavone and SAR
During screening for the flavonoid chemosensitizers, it was found that 5,7,3',4',5'-pentamethoxyflavone (PMF) was equipotent to verapamil in vitro with respect to the chemosensitizing effect. PMF appears to have a chemosensitizing effect not only by increasing the intracellular accumulation of the drugs without competition in a binding site of azidopine but also by interfering with the substrate-stimulated ATPase activity. Structure-activity relationship suggests that methoxylated substitution and its numbers or sites of the rings are more important than its hydroxylated counterparts in chemosensitization. Overall, PMF is anticipated to be a novel and highly potent second-generation flavonoid chemosensitizer because PMF has significant advantages of having a high therapeutic index, of being a non-transportable inhibitor, and of having a low possibility of drug interactions at the azidopine-binding site of Pgp.
- Chosun University Korea (Republic of)
Adenosine Triphosphatases, Flavonoids, Dose-Response Relationship, Drug, Cell Survival, Daunorubicin, Drug Resistance, Multiple, Enzyme Activation, Leukemia, Myeloid, Acute, Structure-Activity Relationship, Vincristine, Cell Line, Tumor, Humans, ATP Binding Cassette Transporter, Subfamily B, Member 1
Adenosine Triphosphatases, Flavonoids, Dose-Response Relationship, Drug, Cell Survival, Daunorubicin, Drug Resistance, Multiple, Enzyme Activation, Leukemia, Myeloid, Acute, Structure-Activity Relationship, Vincristine, Cell Line, Tumor, Humans, ATP Binding Cassette Transporter, Subfamily B, Member 1
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