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.
Highlights
Lysimachia clethroides Duby (L. clethroides), belonging to the family Primulaceae, is found in mild regions of northeast China, the southwest and other eastern provinces [1]
The results of this study showed that flavoneThis glycosides and astragalin) had had no effect on the activities of CYP2E1the andtwo might be(isoquercitrin due to the reason that there is no aeffect on quantitative the activitiesstructure-activity of CYP2E1 and CYP3A4
Researchers have used CYP2E1 knockout mice to evaluate the effect of CYP2E1 on ethanol-induced chronic liver injury, and the results showed that the fatty liver production and ethanol-induced oxidative stress of wild-type mice were significantly higher than those in CYP2E1 knockout mice [30], showing that CYP2E1 is involved in the oxidative stress of the body, increasing the severity of liver damage
Summary
Lysimachia clethroides Duby (L. clethroides), belonging to the family Primulaceae, is found in mild regions of northeast China, the southwest and other eastern provinces [1]. Phytochemical research has showed that flavonoids and glycosides, triterpenes and organic acids are the main compounds in. Pharmacological investigation showed that L. clethroides possesses antitumor [6,7], antioxidant [8], hypoglycemic [9] and hepatoprotective [10] effects. The flavonoids are a group of the most important active compounds in L. clethroides. Glutamic pyruvic transaminase (GPT) and glutamic oxaloacetic transaminase (GOT) are the main non-specific functional enzymes in the liver [11,12], their activities reflect the degree of hepatocyte damage to a certain extent. Our previous pharmacodynamic studies showed that the levels of both GOT and GPT in serum in response to carbon tetrachloride (CCl4 )-induced acute liver injury in mice were significantly decreased by intragastric administration of extracts of
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