Sex hormone modulation of both induction and inhibition of CYP1A by genistein in HepG2/C3A cells

Liu, Yitong; Santillo, Michael F.; Flynn, Tom; Ferguson, Martine

doi:10.1007/s11626-014-9848-9

Cited by 8 publications

(4 citation statements)

References 28 publications

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“…15) product inhibited CYP1A2 and CYP2C9. The isoflavone-based product contained isoflavones derived from soybean and red clover, such as genistein and biochanin A, which reportedly inhibit CYP1A2 [18, 19]. In contrast, few reports are available on P450 inhibition by vitamins in vitamin-based products, although lipid-soluble vitamins, such as vitamin A and vitamin D, have been reported to induce CYPs [20, 21].…”

Section: Discussionmentioning

confidence: 99%

Effect of health foods on cytochrome P450-mediated drug metabolism

Sasaki

Sato

Kumagai

et al. 2017

J Pharm Health Care Sci

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BackgroundHealth foods have been widely sold and consumed in Japan. There has been an increase in reports of adverse effects in association with the expanding health food market. While health food-drug interactions are a particular concern from the viewpoint of safe and effective use of health foods, information regarding such interactions is limited owing to the lack of established methods to assess the effects of health food products on drug metabolism. We therefore developed cells that mimicked the activities of cytochrome P450 1A2 (CYP1A2), CYP2C9, CYP2C19, CYP2D6, and CYP3A4, which strongly contribute to drug metabolism in human hepatocytes, and established a system to assess the inhibitory activity of health foods toward P450-mediated metabolism.MethodsWe simultaneously infected HepG2 cells with five P450-expressing adenoviruses (Ad-CYP1A2, Ad-CYP2C9, Ad-CYP2C19, Ad-CYP2D6, and Ad-CYP3A4) to mimic the activity levels of these P450s in human hepatocytes, and named them Ad-P450 cells. The activity levels of P450s in Ad-P450 cells and human hepatocytes were calculated via simultaneous liquid chromatography/tandem mass spectrometry analysis utilizing a P450 substrate cocktail.ResultsWe established Ad-P450 cells mimicking the activity levels of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 in human hepatocytes. We determined the Km values of P450 substrates and IC50 values of P450 inhibitors in Ad-P450 cells. These values were approximately equivalent to those obtained in previous studies. We investigated the inhibitory effects of 172 health foods that were recently in circulation in Japan on P450-mediated metabolism using Ad-P450 cells. Of the 172 health foods, five products (two products having dietary effects, one turmeric-based product, one collagen-based product, and one propolis-containing product) simultaneously inhibited the five P450s by more than 50%. Another 29 products were also confirmed to inhibit one or more P450s.ConclusionsWe established a comprehensive assessment system to elucidate the effects of health foods on P450-mediated metabolism and identified the inhibitory activity of 34 of 172 health foods toward the drug-metabolizing P450s. Our results may provide useful information to predict health food-drug interactions.

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Section: Discussionmentioning

confidence: 99%

Effect of health foods on cytochrome P450-mediated drug metabolism

Sasaki

Sato

Kumagai

et al. 2017

J Pharm Health Care Sci

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“…і передбачають застосування препаратів вісмуту, інгібіторів протонної помпи та комбінації 2-3 антибактеріальних препаратів (амоксицилін, кларитроміцин, метронідазол, тетрациклін, левофлоксацин, рифабутин або фуразолідон) [7,8]. Особливу загрозу становить проведення комбінованої противиразкової терапії у хворих на тлі супутнього гепатиту або цирозу печінки, адже майже всі лікарські засоби підлягають біотрансформації в печінці, а особливу небезпеку становлять препарати з власне гепатотоксичною дією [9,10,12]. Токсичну дію метаболітів лікарських засобів можна викласти в наступній послідовності: І фаза -метаболізм препарату, ІІ фаза -біотрансформація його метаболітів і ІІІ фазаекскреція продуктів біотрансформації із жовчю і сечею [7,13,14].…”

Section: вступunclassified

The influence of hormonal status on the hepatotropic effect and metronidazole in chronic liver damage and the administration of placenta cryoextract

Кошурба

Hladkykh

Chyzh

2023

GASTRO

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Background. Liver diseases occupy an important place in the structure of gastrointestinal pathology and remain an important medical and social problem throughout the world. Almost half of patients with manifest disorders of the hepatobiliary system have a polymorbid status or a high risk of developing concomitant pathology. One of the variants of the combined pathology in the clinic of gastroenterology is peptic ulcer on the background of liver disorders. As a potential anti-ulcer biotechnological agent with a hepatoprotective effect, cryocell — placenta cryoextract, a domestic drug, attracted attention. The purpose was to determine the gender aspects of the hepatotropic effect of placenta cryoextract in tetrachloromethane hepatitis with background ethanol-induced liver cirrhosis and liver damage by antiulcer agents. Materials and methods. Hepatotropic effects were studied at different levels of sex hormones in 112 male and female rats weighing 200–220 g, divided into 4 groups of 28 animals each. Tetrachloromethane hepatitis with background ethanol-induced liver cirrhosis was simulated by administration of an oily solution of tetrachloromethane in combination with a 5.0% ethanol solution for 45 days. Modulation of the content of sex hormones was achieved by surgical ovariectomy or orchiectomy. The activity of γ-glutamyl-transpeptidase was determined by the spectrophotometric method according to G. Szasz.

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“…In HepG2/C3A cells, genistein can cause both long-term (72 h) stimulation and short-term downregulation of CYP1A activity. In male hormone cells, various enzyme activities and CYP1A gene expressions were encouraged to a greater extent rather than in female hormone cells [127,128].…”

Section: Gastrointestinal Cancersmentioning

confidence: 99%

Genistein: An Integrative Overview of Its Mode of Action, Pharmacological Properties, and Health Benefits

Sharifi‐Rad

Quispe

Imran

et al. 2021

Oxidative Medicine and Cellular Longevity

179

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Genistein is an isoflavone first isolated from the brooming plant Dyer’s Genista tinctoria L. and is widely distributed in the Fabaceae family. As an isoflavone, mammalian genistein exerts estrogen-like functions. Several biological effects of genistein have been reported in preclinical studies, such as the antioxidant, anti-inflammatory, antibacterial, and antiviral activities, the effects of angiogenesis and estrogen, and the pharmacological activities on diabetes and lipid metabolism. The purpose of this review is to provide up-to-date evidence of preclinical pharmacological activities with mechanisms of action, bioavailability, and clinical evidence of genistein. The literature was researched using the most important keyword “genistein” from the PubMed, Science, and Google Scholar databases, and the taxonomy was validated using The Plant List. Data were also collected from specialized books and other online resources. The main positive effects of genistein refer to the protection against cardiovascular diseases and to the decrease of the incidence of some types of cancer, especially breast cancer. Although the mechanism of protection against cancer involves several aspects of genistein metabolism, the researchers attribute this effect to the similarity between the structure of soy genistein and that of estrogen. This structural similarity allows genistein to displace estrogen from cellular receptors, thus blocking their hormonal activity. The pharmacological activities resulting from the experimental studies of this review support the traditional uses of genistein, but in the future, further investigations are needed on the efficacy, safety, and use of nanotechnologies to increase bioavailability and therapeutic efficacy.

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Sex hormone modulation of both induction and inhibition of CYP1A by genistein in HepG2/C3A cells

Cited by 8 publications

References 28 publications

Effect of health foods on cytochrome P450-mediated drug metabolism

Effect of health foods on cytochrome P450-mediated drug metabolism

The influence of hormonal status on the hepatotropic effect and metronidazole in chronic liver damage and the administration of placenta cryoextract

Genistein: An Integrative Overview of Its Mode of Action, Pharmacological Properties, and Health Benefits

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