Cytochrome P450(CYP) Inhibition Study by (Thiolated) Polymers

摘要

The aim of this study was to investigate novelpotential inhibitors of cytochrome P450 mediatedmetabolism. 7-Benzyloxy-4-(trifluoromethyl)-coumarin(BFC) was used as fluorescent substrate for thedetermination of catalytic activity of CYP3A4 whilefluorescence emitted by 7-hydroxycoumarin wasmeasured in alkaline condition for CYP2A6 catalyticactivity. Several thiolated polymers along with other testsubstances were screened for CYP3A4 and CYP2A6inhibitory activity and their IC50 values were determined.Thiolated polymers were found to be potent inhibitors ofboth CYP3A4 and CYP2A6 catalytic activity. Thiolationprocess greatly improves the inhibitory properties of thepolymers. Myrj-52 and brij-35 along with verapamil werealso identified as potent CYP P450 inhibitors.