Journal of Cellular and Molecular Medicine | |
Genistein as a potential inducer of the anti‐atherogenic enzyme paraoxonase‐1: studies in cultured hepatocytes in vitro and in rat liver in vivo | |
Charlotte Schrader1  Insa M. A. Ernst1  Heike Sinnecker1  Sebastian T. Soukup2  Sabine E. Kulling2  | |
[1] Institute of Human Nutrition and Food Science, Christian-Albrechts-University of Kiel, Kiel, Germany;Department of Safety and Quality of Fruit and Vegetables, Max Rubner-Institut, Federal Research Institute of Nutrition and Food, Karlsruhe, Germany | |
关键词: aryl hydrocarbon receptor; oestrogen receptor; flavonoids; genistein; genistein metabolites; oxidized LDL; paraoxonase 1; | |
DOI : 10.1111/j.1582-4934.2012.01542.x | |
来源: Wiley | |
【 摘 要 】
A number of cardioprotective effects, including the reduced oxidation of the low-density lipoprotein (LDL) particles, have been attributed to dietary soy isoflavones. Paraoxonase 1 (PON1), an enzyme mainly synthesized in the liver, may exhibit anti-atherogenic activity by protecting LDL from oxidation. Thus, dietary and pharmacological inducers of PON1 may decrease cardiovascular disease risk. Using a luciferase reporter gene assay we screened different flavonoids for their ability to induce PON1 in Huh7 hepatocytes in culture. Genistein was the most potent flavonoid with regard to its PON1-inducing activity, followed by daidzein, luteolin, isorhamnetin and quercetin. Other flavonoids such as naringenin, cyanidin, malvidin and catechin showed only little or no PON1-inducing activity. Genistein-mediated PON1 transactivation was partly inhibited by the oestrogen-receptor antagonist fulvestrant as well as by the aryl hydrocarbon receptor antagonist 7-ketocholesterol. In contrast to genistein, the conjugated genistein metabolites genistein-7-glucuronide, genistein-7-sulfate and genistein-7,4′-disulfate were only weak inducers of PON1 transactivation. Accordingly, dietary genistein supplementation (2 g/kg diet over three weeks) in growing rats did not increase hepatic PON1 mRNA and protein levels as well as plasma PON1 activity. Thus, genistein may be a PON1 inducer in cultured hepatocytes in vitro, but not in rats in vivo.Abstract
【 授权许可】
Unknown
© 2012 The Authors Journal of Cellular and Molecular Medicine © 2012 Foundation for Cellular and Molecular Medicine/Blackwell Publishing Ltd
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