Simultaneos determination of taxol and its metabolits in microsomal samples by a simple thin-layer chromatography radioactivity assay - inhibitory effect of NK-104, a new inhibitor of HMG-CoA reductase

摘要

The inhibitory effect of NK-104, a potent inhibitor of HMG-CoA reductase, ontaxol metabolism was examined using radio-TLC. This method is described for in vitro measurement of taxol metabolites as an alternative to the commonly used HPLC assay. After incubationof ~(14)C-taxol with humanliver microsomes, the supernatants were developed using a solvent system consisting of toluene-acetone-formic acid (60:39:1, v/v) and quantified with a bioimaging analyzer. The described method provides a valuable tool for the simultaneous determinationof unchanged taxol and its major metabolites. There was no inhibitory effect of NK-104 on CYP-mediated metabolism of taxol inhuman liver microsomes.