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KMID : 0617219980090010071
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Duksung Bulletin Phamaceutical Sciences
1998 Volume.9 No. 1 p.71 ~ p.87
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Identification of cytochrome P450 isoforms for formation of lisofylline to lisofylline 4,5-diol
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Abstract
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Lisofylline is a drug being developed to prevent the complications of high dose chemotheraphy. Conversion of lisofylline to llisofylline 4,5-diol, one of two principal metabolites in human liver microsomes, by cytochrome P450 isoforms was investigated. Lisofylline 4,5-diol formation in microsomes prepared from human livers was two enzyme kinetics. Through identify the individual cytochrome P450 isoforms experiments with selective chemical inhibitors, CYP3A4 was implicated as the low and high K_m enzyme and CYP2A6 was implicated as the high K_m enzyme. The formation of lisofylline 4,5-diol by these enzymes was confirmed with cDNA expressed human CYP3A4 and CYP2A6.
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