Document Detail

Tanshinone I increases CYP1A2 protein expression and enzyme activity in primary rat hepatocytes.
MedLine Citation:
PMID:  21899995     Owner:  NLM     Status:  MEDLINE    
This study investigated the effects of Danshen and its active ingredients on the protein expression and enzymatic activity of CYP1A2 in primary rat hepatocytes. The ethanolic extract of Danshen roots (containing mainly tanshinones) inhibited CYP1A2-catalyzed phenacetin O-deethylation (IC(50)=24.6 μg/ml) in primary rat hepatocytes while the water extract containing mainly salvianolic acid B and danshenshu had no effect. Individual tanshinones such as cryptotanshinone, dihydrotanshinone, tanshinone IIA inhibited the CYP1A2-mediated metabolism with IC(50) values at 12.9, 17.4 and 31.9 μM, respectively. After 4-day treatment of the rat hepatocytes, the ethanolic extract of Danshen and tanshinone I increased rat CYP1A2 activity by 6.8- and 5.2-fold, respectively, with a concomitant up-regulation of CYP1A2 protein level by 13.5- and 6.5-fold, respectively. CYP1A2 induction correlated with the up-regulation of mRNA level of aryl hydrocarbon receptor (AhR), which suggested a positive feedback mechanism of tanshinone I-mediated CYP1A2 induction. A formulated Danshen pill (containing mainly danshensu and salvianolic acid B and the tanshinones) up-regulated CYP1A2 protein expression and enzyme activity, but danshensu and salvianolic acid B, when used individually, did not affect CYP1A2 activity. This study was the first report on the Janus action of the tanshinones on rat CYP1A2 activity.
Wayne Y W Lee; Xuelin Zhou; Penelope M Y Or; Yiu Wa Kwan; John H K Yeung
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-09-06
Journal Detail:
Title:  Phytomedicine : international journal of phytotherapy and phytopharmacology     Volume:  19     ISSN:  1618-095X     ISO Abbreviation:  Phytomedicine     Publication Date:  2012 Jan 
Date Detail:
Created Date:  2011-12-19     Completed Date:  2012-04-13     Revised Date:  2014-01-10    
Medline Journal Info:
Nlm Unique ID:  9438794     Medline TA:  Phytomedicine     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  169-76     Citation Subset:  IM    
Copyright Information:
Copyright © 2011 Elsevier GmbH. All rights reserved.
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MeSH Terms
Benzofurans / pharmacology
Cell Survival
Cytochromes / genetics,  metabolism*
Diterpenes, Abietane / pharmacology*
Drugs, Chinese Herbal / pharmacology
Enzyme Activation
Enzyme Induction
Ethanol / metabolism
Hepatocytes / cytology,  drug effects*,  enzymology
Phenacetin / metabolism
Phenanthrenes / pharmacology
Phenanthrolines / pharmacology
Primary Cell Culture
RNA, Messenger / genetics,  metabolism
Rats, Sprague-Dawley
Receptors, Aryl Hydrocarbon
Tacrine / pharmacology
Reg. No./Substance:
0/Benzofurans; 0/Cytochromes; 0/Diterpenes, Abietane; 0/Drugs, Chinese Herbal; 0/Phenanthrenes; 0/Phenanthrolines; 0/RNA, Messenger; 0/Receptors, Aryl Hydrocarbon; 115939-25-8/salvianolic acid B; 35825-57-1/cryptotanshinone; 3K9958V90M/Ethanol; 4VX7YNB537/Tacrine; 568-73-0/tanshinone; 79483-68-4/dan-shen root extract; EC protein, rat; ER0CTH01H9/Phenacetin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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