Document Detail


Tanshinone I increases CYP1A2 protein expression and enzyme activity in primary rat hepatocytes.
MedLine Citation:
PMID:  21899995     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Wayne Y W Lee; Xuelin Zhou; Penelope M Y Or; Yiu Wa Kwan; John H K Yeung
Related Documents :
12385785 - Individual response profiles of male wistar rats in animal models for anxiety and depre...
21781845 - Modulating effects of thyroid state on the induction of biotransformation enzymes by 2,...
2858075 - Benzodiazepines and the developing rat: a critical review.
2926335 - Influence of long-term sensitization on long-term habituation of the acoustic startle r...
6263215 - Malignant fibrous histiocytoma. an unusual neoplasm of soft-tissue origin in the rat th...
19483715 - Proliferation and phenotypic changes of stromal cells in response to varying estrogen/a...
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.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Animals
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
Male
Phenacetin / metabolism
Phenanthrenes / pharmacology
Phenanthrolines / pharmacology
Primary Cell Culture
RNA, Messenger / genetics,  metabolism
Rats
Rats, Sprague-Dawley
Receptors, Aryl Hydrocarbon
Tacrine / pharmacology
Chemical
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 1.14.14.1/Cyp1a2 protein, rat; ER0CTH01H9/Phenacetin

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


Previous Document:  Danshen-Gegen decoction protects against hypoxia/reoxygenation-induced apoptosis by inhibiting mitoc...
Next Document:  In vitro anti-influenza virus activity of a cardiotonic glycoside from Adenium obesum (Forssk.).