HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY STUDY OF STEREOSPECIFIC MICROSOMAL-ENZYMES CATALYZING THE REDUCTION OF A POTENTIAL CYTOSTATIC DRUG, ORACIN - INTERSPECIES COMPARISON
V. Wsol et al., HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY STUDY OF STEREOSPECIFIC MICROSOMAL-ENZYMES CATALYZING THE REDUCTION OF A POTENTIAL CYTOSTATIC DRUG, ORACIN - INTERSPECIES COMPARISON, Journal of chromatography, 797(1-2), 1998, pp. 197-201
Citations number
9
Categorie Soggetti
Chemistry Analytical","Biochemical Research Methods
One of the main metabolites of oracin (I) -dioxo-5,6-dihydro-11H-inden
o[1,2-c]isoquinoline}, a potential cytostatic drug, is 11-dihydrooraci
n (II) ydroxy-5,6-dihydro-11H-indeno[1,2-c]isoquinoline}, a metabolite
formed by the reduction of oracin's pro-chiral centre on C 11. This m
etabolite has been found in all laboratory species in vitro and in viv
o and it constitutes the main metabolite in man. The stereospecificity
of reducing enzymes participating in the oracin biotransformation pat
hway was investigated using microsomal preparations from standard labo
ratory animals. Enzyme stereospecificity has been defined as preferent
ial formation by the enzyme of the (+) or (-) stereoisomer of II. Sign
ificant interspecies differences were observed in the stereospecificit
y of the respective biotransformation enzymes. HPLC quantitative deter
minations of both enantiomers were performed using a Chiralcel OD-R co
lumn as chiral stationary phase with excellent resolution and stabilit
y. (C) 1998 Elsevier Science B.V.