In vitro inhibition of five traditional Chinese medicine injections on rat liver microsomal CYP3A / 中国中药杂志
China Journal of Chinese Materia Medica
;
(24): 492-495, 2011.
Article
in Chinese
| WPRIM
| ID: wpr-247449
ABSTRACT
<p><b>OBJECTIVE</b>Qingkailing injection (QKLI), Jinnaduo injection (JNDI), Shuxuetong injection (SXTI), Shenmai injection (SMI) and Kangai injection (KAI) are widely used in China. To predict the herb-drug interactions in clinical application, they were evaluated for their in vitro inhibition effect on CYP3A in rat liver microsomes.</p><p><b>METHOD</b>The rat liver microsomes were incubated with different doses of 5 kinds of traditional Chinese medicine injections (TCMIs) in the present of testosterone, a specific substrate of CYP3A. 6beta-hydroxytestosterone, the metabolite of testosterone, was monitored by HPLC to compare the inhibition effect of 5 TCMIs on CYP3A in rat liver microsomes. Ketoconazole was used as a positive control.</p><p><b>RESULT</b>10% QKLI reduced the formation of 6beta-hydroxytestosterone by approximately 93.0%, which is more significant than other four TCMIs. The half maximal inhibitory concentration (IC50) and the enzyme-inhibitor constant K(i) were 1.0% and 0.7% respectively.</p><p><b>CONCLUSION</b>QKLI showed much stronger inhibition activity against CYP3A, comparing to other 4 TCMIs. The results revealed that QKLI may be involved in herb-drug interactions by inhibition of CYP3A.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Microsomes, Liver
/
Rats, Sprague-Dawley
/
Cytochrome P-450 CYP3A Inhibitors
/
Injections
/
Medicine, Chinese Traditional
Type of study:
Diagnostic study
Limits:
Animals
Language:
Chinese
Journal:
China Journal of Chinese Materia Medica
Year:
2011
Type:
Article
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