Background: A large amount of evidence has demonstrated that phenolic phytochemicals possess bioactivity and health benefits, including antioxidant and hepatoprotective effects. Paracetamol is the most frequently used analgesic and antipyretic drug and can induce oxidative stress-mediated hepatotoxicity at high doses1. Our purpose is to provide an overview of the pros and cons of the association between antioxidant nutraceuticals and paracetamol2. Methods: A full provisional analysis of literature with particular reference to paracetamol pharmacokinetics, hepatotoxicity and its interactions with nutraceuticals in vivo has been made2. Results: Paracetamol metabolism occurs mainly in the liver through sulfation and glucuronidation. CYP metabolism is important in high-doses induced hepatotoxicity. The metabolic activation of paracetamol produces reactive oxygen species and the N-acetyl-p-benzoquinone imine (NAPQI) that reacts readily with the nucleophilic sulfhydryl groups and depletes GSH and forms mitochondrial protein adducts, increasing the production of superoxide radicals. This can react with nitric oxide to produce the potent oxidant peroxynitrite, causing hepatotoxicity3. The interactions between paracetamol and antioxidants in vivo models4,5 showed an evident protective effects of plant extracts against paracetamol hepatotoxicity, in terms of decreases in interleukin (IL)-86 and tumor necrosis factor (TNF)-α7. However, in certain cases, nutraceuticals had opposite effects depending on time of administration. In humans, both nutraceuticals and the consumption of fruit and vegetable diet, known to affect phase I and/or phase II metabolism systems, alter paracetamol pharmacokinetics8. Pharmacogenetic profiles have been suggested to have a role in the inter-individual differences in paracetamol metabolism, the related differences in susceptibility to toxicity and the efficacy of paracetamol in therapeutics. Conclusions: We can say with certainty that there are interactions between paracetamol and nutraceuticals or plant foods. Next goal could be the human study, particularly, gene-diet interactions and ethnic variability, as a result of interaction between antioxidant nutraceuticals and paracetamol2.

Association of antioxidant nutraceuticals and acetaminophen (paracetamol): Friend or foe? / Minosi, Paola; Aiello, Paola; Peluso and Maura Palmery, Ilaria. - (2019). (Intervento presentato al convegno 2nd Conference on Innovations in Food Science & Human Nutrition(IFHN-2019) tenutosi a Londra).

Association of antioxidant nutraceuticals and acetaminophen (paracetamol): Friend or foe?

Paola Minosi;Paola Aiello;
2019

Abstract

Background: A large amount of evidence has demonstrated that phenolic phytochemicals possess bioactivity and health benefits, including antioxidant and hepatoprotective effects. Paracetamol is the most frequently used analgesic and antipyretic drug and can induce oxidative stress-mediated hepatotoxicity at high doses1. Our purpose is to provide an overview of the pros and cons of the association between antioxidant nutraceuticals and paracetamol2. Methods: A full provisional analysis of literature with particular reference to paracetamol pharmacokinetics, hepatotoxicity and its interactions with nutraceuticals in vivo has been made2. Results: Paracetamol metabolism occurs mainly in the liver through sulfation and glucuronidation. CYP metabolism is important in high-doses induced hepatotoxicity. The metabolic activation of paracetamol produces reactive oxygen species and the N-acetyl-p-benzoquinone imine (NAPQI) that reacts readily with the nucleophilic sulfhydryl groups and depletes GSH and forms mitochondrial protein adducts, increasing the production of superoxide radicals. This can react with nitric oxide to produce the potent oxidant peroxynitrite, causing hepatotoxicity3. The interactions between paracetamol and antioxidants in vivo models4,5 showed an evident protective effects of plant extracts against paracetamol hepatotoxicity, in terms of decreases in interleukin (IL)-86 and tumor necrosis factor (TNF)-α7. However, in certain cases, nutraceuticals had opposite effects depending on time of administration. In humans, both nutraceuticals and the consumption of fruit and vegetable diet, known to affect phase I and/or phase II metabolism systems, alter paracetamol pharmacokinetics8. Pharmacogenetic profiles have been suggested to have a role in the inter-individual differences in paracetamol metabolism, the related differences in susceptibility to toxicity and the efficacy of paracetamol in therapeutics. Conclusions: We can say with certainty that there are interactions between paracetamol and nutraceuticals or plant foods. Next goal could be the human study, particularly, gene-diet interactions and ethnic variability, as a result of interaction between antioxidant nutraceuticals and paracetamol2.
2019
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1317287
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