CHARACTERIZATION OF METABOLITES OF ELLIPTICINE IN RAT BILE

Abstract

The 2 major metabolites of ellipticine (NSC 71795) [an antineoplastic drug] were isolated from rat bile by a combination of solvent extraction, partition column chromatography and reverse phase high-performance liquid chromatography. Purification and structural elucidation of the bile products were aided by administration of the drug with a dual label (14C and 2H). The 2 metabolites were the sulfate and glucuronide conjugates of 9-hydroxyellipticine by chemical, enzymatic and mass-spectral fragmentation comparison with synthetic and enzymatically prepared reference compounds.