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Molecules 2016, 21(6), 738; doi:10.3390/molecules21060738

Effects of Flavonoids in Lysimachia clethroides Duby on the Activities of Cytochrome P450 CYP2E1 and CYP3A4 in Rat Liver Microsomes

1
Institute of Chinese Materia Medica, Henan University, Kaifeng 475004, China
2
Kaifeng Key Laboratory of Functional Components in Health Food, Kaifeng 475004, China
3
Minsheng College, Henan University, Kaifeng 475004, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Isabel C. F. R. Ferreira
Received: 3 May 2016 / Revised: 27 May 2016 / Accepted: 1 June 2016 / Published: 14 June 2016
(This article belongs to the Collection Bioactive Compounds)
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Abstract

Incubation systems were established to investigate the effects of quercetin, kaempferol, isoquercitrin and astragalin in Lysimachia clethroides Duby on the activities of CYP2E1 and CYP3A4 in rat liver microsomes in vitro. Probe substrates of 4-nitrophenol and testosterone as well as flavonoids at different concentrations were added to the incubation systems. After incubation, a validated high performance liquid chromatography (HPLC) method was applied to separate and determine the relevant metabolites. The results suggested that kaempferol exhibited a weak inhibition of CYP2E1 activity with an IC50 of 60.26 ± 2.54 μM, while quercetin and kaempferol caused a moderate inhibition of CYP3A4 activity with IC50 values of 18.77 ± 1.69 μM and 32.65 ± 1.32 μM, respectively. Isoquercitrin and astragalin had no effects on the activities of either CYP2E1 or CYP3A4. It could be speculated from these results that the inhibitory effects of quercetin and kaempferol on the activities of CYP2E1 and CYP3A4 could be the mechanisms underlying the hepatoprotective effects of L. clethroides. View Full-Text
Keywords: Lysimachia clethroides Duby; flavonoids; HPLC; CYP2E1; CYP3A4; liver microsomes Lysimachia clethroides Duby; flavonoids; HPLC; CYP2E1; CYP3A4; liver microsomes
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Zhang, Z.-J.; Xia, Z.-Y.; Wang, J.-M.; Song, X.-T.; Wei, J.-F.; Kang, W.-Y. Effects of Flavonoids in Lysimachia clethroides Duby on the Activities of Cytochrome P450 CYP2E1 and CYP3A4 in Rat Liver Microsomes. Molecules 2016, 21, 738.

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