The inhibition of CYP2C9 isoenzyme in Cunninghamella blakesleeana AS 3. 910 / 药学学报
Acta Pharmaceutica Sinica
;
(12): 967-972, 2006.
Article
in Chinese
| WPRIM
| ID: wpr-294904
ABSTRACT
<p><b>AIM</b>To investigate the variation of CYP2C9 isoenzyme activity in the microbial model in response to inhibitors of CYP2C9.</p><p><b>METHODS</b>Using C. blakesleeana AS 3. 910 as a model strain, the impact of CYP2C9 inhibitors on the metabolites yields of CYP2C9 substrates was determined and the drug-drug interactions among CYP2C9 substrates were evaluated. Liquid chromatography-mass spectrometry was used to analyze biotransformation products.</p><p><b>RESULTS</b>Benzbromarone decreased the yield of 4'-hydroxytolbutamide from 100% to 14.5%; sulfaphenazole decreased the yield of O-demethylindomethacin from 75.2% to 9.9%; valproic acid decreased the yield of 4'-hydroxydiclofenac from 98.6% to 2.7%, separately. Tolbutamide, indomethacin and diclofenac interacted with each other, resulting in the decreased formation of metabolites catalyzed by CYP2C9.</p><p><b>CONCLUSION</b>Three CYP2C9 inhibitors inhibit the activity of CYP2C9 isoenzyme in C. blakesleeana AS 3. 910 differently, and there are drug-drug interactions among CYP2C9 substrates.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Substrate Specificity
/
Sulfaphenazole
/
Tolbutamide
/
Benzbromarone
/
Fungal Proteins
/
Aryl Hydrocarbon Hydroxylases
/
Biotransformation
/
Catalysis
/
Diclofenac
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2006
Type:
Article
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