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Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo.
MedLine Citation:
PMID:  22375877     Owner:  NLM     Status:  In-Data-Review    
Capsaicin and dihydrocapsaicin, the two most abundant members of capsaicinoids in chili peppers, are widely used as food additives and for other purposes. In this study, we examined the inhibitory potentials of capsaicin and dihydrocapsaicin against CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4/5 activities in human liver microsomes. The effects of these two capsaicinoids on CYP450 enzymes were also evaluated in vivo in rats. The results demonstrated that capsaicin and dihydrocapsaicin moderately inhibited five isozymes (IC(50) values ranging from 4.4 to 61.8 μM), with the exception of CYP2E1 (IC(50)>200 μM). Both capsaicinoids exhibited competitive, mixed, and noncompetitive inhibition on these isozymes (K (i) = 3.1 ± 0.5 - 78.6 ± 8.4 μM). Time-dependent inhibition of CYP3A4/5 by capsaicin was found. After multiple administrations of capsaicin and dihydrocapsaicin (1, 4, and 10 mg/kg) to rats, chlorzoxazone 6-hydroxylase activity and the expression of CYP2E1 were increased in liver microsomes. Our findings indicated that the possibility of food-drug interactions mediated by capsaicin and dihydrocapsaicin could not be excluded, and provided the useful information for evaluating the anticarcinogenic potentials of these two capsaicinoids.
Qing-Hao Zhang; Jin-Ping Hu; Bao-Lian Wang; Yan Li
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of Asian natural products research     Volume:  14     ISSN:  1477-2213     ISO Abbreviation:  J Asian Nat Prod Res     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-03-01     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100888334     Medline TA:  J Asian Nat Prod Res     Country:  England    
Other Details:
Languages:  eng     Pagination:  382-95     Citation Subset:  IM    
a Chinese Academy of Medical Sciences & Peking Union Medical College, Institute of Materia Medica , Beijing , 100050 , China.
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