Bisphenol-A glucuronidation in human liver and breast: identification of UDP-glucuronosyltransferases (UGTs) and influence of genetic polymorphisms

Street, Christina M.; Zhu, Zhaohui; Finel, Moshe; Court, Michael H.

doi:10.3109/00498254.2016.1156784

Cited by 22 publications

(19 citation statements)

References 37 publications

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“…Only a few studies have evaluated UDP-glucuronosyltransferases (UGTs) presence in breast tissue. Expression of UGT2B10, UGT2B11, UGT2B15 and UGT2B UGT1A10 and UGT2B7, and UGT2B11 enzymes have been proven in humans, and the results of Street et al confirm the capability of glucuronidation of BPA in human breast tissue, although with glucuronidation activities that are much lower (by more than 100,000-fold) compared with those seen in the liver 22 . There are currently no (to the best of our knowledge) known studies that have evaluated the presence of UDP-glucuronosyltransferases in the ewe mammary gland, although it seems reasonable to assume that the mammary glands of all mammals are equipped with comparable detoxifying mechanisms.…”

Section: Discussionmentioning

confidence: 93%

Preliminary toxicokinetic study of BPA in lactating dairy sheep after repeated dietary and subcutaneous administration

Šturm

Grabnar

Škibin

et al. 2020

Sci Rep

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Dietary intake is the predominant route of human exposure to bisphenol A and one of the important food commodities is milk. the aim of our study was to preliminarily evaluate the bisphenol A exposure and disposition in sheep milk after repeated dietary and subcutaneous administration of a relatively low dose (100 µg/kg of b. w./day) of bisphenol A to a sheep. on the basis of blood plasma sampling, milk sampling and HpLc analysis, we developed the toxicokinetic model. With the toxicokinetic model we showed that most likely only free bisphenol A passes into the mammary gland and is subsequently conjugated there. the percentage of the dose eliminated with milk was less than 0.1%, regardless of the route of bisphenol A administration. It is proven that the bisphenol A is eliminated through the milk of lactating sheep. However, the amounts excreted in the milk that were detected in this study are minimal.Since the start of the commercial production of bisphenol A (BPA) in the 1950s until the present, the global production and consumption of this substance, regardless of the suspected negative health effects, has continued to rise 1 . With both the wide use of BPA and its leaching from many products and materials 2 , it is known to be one of the ubiquitous environmental contaminants 3 . The main route of human BPA exposure is thought to be oral ingestion (up to 83% of the total estimated exposure), and in 2013 canned products accounted for about 50% of the dietary exposure to BPA. Thus, cans and packaging are believed to be the main source of contamination in foods 4 . Current migration limit of BPA from varnishes or coatings applied to materials and articles is 0.05 mg/kg BPA of food 5 . However, the products from farm animals, being directly exposed to human pollution, could still be, in some cases, an additional risk factor for human exposure 6 .It is believed that BPA causes endocrine disrupting effects by the interaction with various receptors, such as thyroid hormone receptor, androgen receptor and oestrogen receptor. Thus, BPA health hazards for reproductive system, nervous system, metabolic function, immune function, the growth and development of offspring were raised 4,7 . The European Food Safety Authority (EFSA) decreased the tolerable daily intake (TDI) from the 50 μg/ kg of b. w./day to 4 μg/kg of b. w./day as a response to a refined risk assessment of BPA 7 .A food commodity important in our daily diet is milk. The quality and safety of milk depends considerably on the environment and human activity in its production. A broad range of environmental contaminants can enter the milk chain in the beginning via application of contaminated material on the soil such as industrial waste and sewage sludge, and atmospheric deposition from industrial activities 6 . It is also true that chemicals can enter milk during the collection and preparation processes of dairy products 8 . For instance, BPA may be introduced during milking from plastic parts of the milking machines, or also transferred from bulk milk to plasti...

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Section: Discussionmentioning

confidence: 93%

Preliminary toxicokinetic study of BPA in lactating dairy sheep after repeated dietary and subcutaneous administration

Šturm

Grabnar

Škibin

et al. 2020

Sci Rep

View full text Add to dashboard Cite

show abstract

“…Only a few studies have evaluated UDP-glucuronosyltransferases (UGTs) presence in breast tissue. Expression of UGT2B10, UGT2B11, UGT2B15 and UGT2B UGT1A10 and UGT2B7, and UGT2B11 enzymes have been proven in humans, and the results of Street et al confirm the capability of glucuronidation of BPA in human breast tissue, although with glucuronidation activities that are much lower (by more than 100,000-fold) compared with those seen in the liver [14]. There are currently no (to the best of our knowledge) known studies that have evaluated the presence of UDP-glucuronosyltransferases in the ewe mammary gland, although it seems reasonable to assume that the mammary glands of all mammals are equipped with similar detoxifying mechanisms.…”

Section: Discussionmentioning

confidence: 94%

Industrial chemical bisphenol A and raw milk: a toxicokinetic study in lactating dairy sheep after repeated dietary and subcutaneous administration

Šturm

Škibin

Grabnar

et al. 2019

Preprint

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• Background: Dietary intake is the predominant route for human exposure to bisphenol A and one of the food items important for humans is milk, and BPA-polluted animal feed and environments may thus affect human exposure. The aim of our study was to evaluate the BPA exposure and disposition in sheep milk after repeated dietary and subcutaneous administration of a relatively low dose (100 µg/kg of body weight per day) of BPA to a sheep. • Results: With our toxicokinetic model, we showed that most likely only free BPA passes into the mammary gland and is subsequently conjugated there. The percentage of the dose eliminated with milk was less than 0.1%, regardless of the route of BPA administration. • Conclusions: It is proven that the BPA is eliminated through the milk of lactating sheep. However, the amounts excreted in the milk that were detected in this study are minimal.

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“…Metabolism of cholecalciferol was decreased by genistein in women [ 15 ]. In further research, it was found that genistein had noncompetitive inhibition on CYP2C9 and CYP3A4 [ 16 ]. Knowledge on the contribution of genistein with celecoxib in metabolic progress is urgent, and it may lead to dose adjustment aimed at effective therapeutic depth.…”

Section: Discussionmentioning

confidence: 99%

“…Based on the in vitro experiment, genistein inhibited the metabolic progress of celecoxib on RLM and HLM. From previous research, the IC50 on CYP2C9∗1 was ∼30 µM [ 16 ]. It was different with ∼11 µM.…”

Section: Discussionmentioning

confidence: 99%

“…Most Asians like to eat soy products as a part of daily necessary [ 13 , 14 ]. Studies by Burnett et al and Kopecna-Zapletalova et al showed that genistein noncompetitively inhibited cytochrome P450 (CYP450) 2C9 and 3A4 [ 15 , 16 ]. So, we deduce that genistein is a possible origin of many drug interactions by interfering with CYP450.…”

Section: Introductionmentioning

confidence: 99%

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Genistein Exposure Interferes with Pharmacokinetics of Celecoxib in SD Male Rats by UPLC-MS/MS

Xiang

Wen

Liu

et al. 2017

Biochemistry Research International

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Objective To discuss the effects of genistein on the metabolism of celecoxib in vitro and in vivo. Method In vitro, the effects of genistein on the metabolism of celecoxib were studied using rat and human liver microsomes. In vivo, pharmacokinetics of celecoxib was evaluated in rats with or without genistein. Fifteen Sprague-Dawley (SD) rats were randomized into three groups: celecoxib (A group), celecoxib and 50 mg/kg genistein (B group), and celecoxib and 100 mg/kg genistein (C group). Single dose of 33.3 mg/kg celecoxib was orally administered 30 min after genistein ig. At 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 h after celecoxib administration, 300–400 µl blood samples were collected and the concentration of celecoxib was analyzed by ultrahigh-performance liquid chromatography-tandem mass spectrometry system. Result Genistein showed notable inhibitory effects on three microsomes. It affected pharmacokinetics of celecoxib in vivo experiments. Genistein had dramatically ability to suppress CYP2C9∗1 and ∗3. After pretreatment with genistein, AUC and Cmax of the C group were higher than B group. CLz/F of C group was lower than the B group. Conclusion Genistein inhibits the conversion of celecoxib in vitro and in vivo. So, the dosage of celecoxib should be adjusted if it was used associated with genistein.

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Bisphenol-A glucuronidation in human liver and breast: identification of UDP-glucuronosyltransferases (UGTs) and influence of genetic polymorphisms

Cited by 22 publications

References 37 publications

Preliminary toxicokinetic study of BPA in lactating dairy sheep after repeated dietary and subcutaneous administration

Preliminary toxicokinetic study of BPA in lactating dairy sheep after repeated dietary and subcutaneous administration

Industrial chemical bisphenol A and raw milk: a toxicokinetic study in lactating dairy sheep after repeated dietary and subcutaneous administration

Genistein Exposure Interferes with Pharmacokinetics of Celecoxib in SD Male Rats by UPLC-MS/MS

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