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

Molecules

Zhi-Juan Zhang¹  Jin-Feng Wei¹  Zhao-Yang Xia¹  Jin-Mei Wang¹  Wen-Yi Kang¹  Xue-Ting Song² 

[1] Institute of Chinese Materia Medica, Henan University, Kaifeng 475004, China;Minsheng College, Henan University, Kaifeng 475004, China;

关键词: Lysimachia clethroides Duby;    flavonoids;    HPLC;    CYP2E1;    CYP3A4;    liver microsomes;   

DOI  :  10.3390/molecules21060738

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown