HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC ASSAY FOR THE SEPARATION AND CHARACTERIZATION OF METABOLITES OF THE POTENTIAL CYTOSTATIC DRUG ORACINE

Oracine (I), a potential cytostatic drug, is enzymically converted to a number of metabolites whose formation has been studied in vitro and in vivo. The metabolites were separated by reversed-phase HPLC and cha racterized by UV spectra. Preparative TLC served for the isolation of the individual metabolites to allow their identification. Two metaboli tes were identified by Fourier transform NMR as 11-dihydrooracine (II) and a phenolic product (III). Two further metabolites (IV,V) were cha racterized. Some minor, presumably 11-dihydro metabolites and an 11-ox o metabolite produced in vitro and in vivo were revealed.