Impact of CYP2C9 Polymorphism Found in the Chinese Population on the Metabolism of Propofol in Vitro

Impact of CYP2C9 Polymorphism Found in the Chinese Population on the Metabolism of Propofol in Vitro

The microsomal CYP2C9 alleles involved in the biotransformation of propofol, a widely used anesthetic agent, were investigated in vitro. To examine the enzymatic activity of the CYP2C9 alleles, kinetic parameters for propofol 4-hydroxylation were determined in recombinant human P450s CYP2C9 microsom...

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Veröffentlicht in:Biological & pharmaceutical bulletin 2015/04/01, Vol.38(4), pp.531-535
Hauptverfasser: Lian, Qing-Quan, Pan, Pei-Pei, Li, Jun-Wei, Lin, Han, Hu, Guo-Xin, Zuo, Ming-Zhang, Cai, Jian-Ping
Format: Artikel
Sprache:eng
Schlagworte:
Alleles
allelic variant
Anesthetics - metabolism
Animals
Asian Continental Ancestry Group - genetics
catalytic character
Cell Line
CYP2C9
Cytochrome P-450 CYP2C9 - genetics
Cytochrome P-450 CYP2C9 - metabolism
Humans
Hydroxylation
Insecta
metabolism
microsome
Microsomes - metabolism
Mutation
Polymorphism, Genetic
propofol
Propofol - metabolism
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Zusammenfassung:The microsomal CYP2C9 alleles involved in the biotransformation of propofol, a widely used anesthetic agent, were investigated in vitro. To examine the enzymatic activity of the CYP2C9 alleles, kinetic parameters for propofol 4-hydroxylation were determined in recombinant human P450s CYP2C9 microsomes from Sf21 insects cells carrying CYP2C9*1 and other variants. Some of the variants showed decreased enzyme activity compared with the wild type, as previously reported. Two variants (CYP2C9*36 and *56) were found substantially to increase intrinsic clearance relative to the wild type variant. Most variants significantly (p
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.b14-00671