[In vitro effects of Genkwa Flos chloroform extract on activity of human liver microsomes UGTs and UGT1A1].

Autor:	Chen N; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Miao PP; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Guo CE; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Chen HY; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Ma PK; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Li HP; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Zhu HY; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Gao X; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China., Zhang YJ; School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
Jazyk:	čínština
Zdroj:	Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica [Zhongguo Zhong Yao Za Zhi] 2016 Sep; Vol. 41 (17), pp. 3296-3302.
DOI:	10.4268/cjcmm20161729
Abstrakt:	To predict the mechanism of liver injury induced by Genkwa Flos, we investigated the effect of chloroform extract on UGTs and UGT1A1 activities of the liver microsomes in rat and human. In the present study, 4-nitrophenol(4-NP) and β-estradiol were elected as substrates to determine activities of UGTs and UGT1A1 by UV and HPLC. The results showed that there were 1.00% of apigenin, 6.40% of hydroxygenkwanin and 18.38% of genkwanin in chloroform extract; and total diterpene mass fraction was 31.40%. Compared with the control group, chloroform extract could significantly inhibit the activity of UGTs in rat liver microsomes(RLM) system, while the inhibitory effect was not obvious in human liver microsomes(HLM) system. UGT1A1 activity was inhibited by chloroform extract in rat liver microsomes and human liver microsomes (based on genkwanin, IC₅₀=8.76, 10.36 μmol•L⁻¹). The inhibition types were non-competitive inhibition(RLM) and uncompetitive inhibition(HLM). In conclusion, the results indicated that chloroform extract showed different inhibitory effects on UGTs and UGT1A1 activity, which may be one of the mechanisms of liver injury induced by Genkwa Flos. Competing Interests: The authors of this article and the planning committee members and staff have no relevant financial relationships with commercial interests to disclose. (Copyright© by the Chinese Pharmaceutical Association.)
Databáze:	MEDLINE
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