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Biotransformation of Piceatannol, a Dietary Resveratrol Derivative: Promises to Human Health
Author(s) -
Dai Yu,
Lim Jin Xuan,
Yeo Samuel Chao Ming,
Xiang Xiaoqiang,
Tan Kai Soo,
Fu Jia Hui,
Huang Lizhen,
Lin HaiShu
Publication year - 2020
Publication title -
molecular nutrition and food research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.495
H-Index - 131
eISSN - 1613-4133
pISSN - 1613-4125
DOI - 10.1002/mnfr.201900905
Subject(s) - biotransformation , piceatannol , glucuronidation , microsome , chemistry , pharmacology , resveratrol , metabolite , metabolism , sulfation , pharmacokinetics , bioavailability , biochemistry , in vivo , oral administration , enzyme , biology , microbiology and biotechnology
Scope To evaluate the health‐promoting potentials of piceatannol (PIC), a dietary resveratrol derivative, its biotransformation is examined. Methods and results The biotransformation is tested in human/rat hepatic microsomes and cytosols; its pharmacokinetic profiles are assessed in rats. Although limited phase I metabolism exists in microsomes, PIC is rapidly converted to two pharmacologically active metabolites, namely rhapontigenin (RHA) and isorhapontigenin (ISO) in cytosols. Such biotransformation is completely blocked by entacapone, a well‐known catechol‐ O ‐methyltransferase (COMT) inhibitor, demonstrating that the O ‐methylation is mediated by COMT. Moreover, PIC is identified as a substrate inhibitor of COMT, suggesting its potential benefits in Alzheimer's disease. Due to extensive phase II metabolism including glucuronidation, sulfation, and O ‐methylation, PIC displays rapid clearance and at least 4.02% ± 0.61% and 17.70% ± 0.91% of PIC is converted to RHA and ISO, respectively, in rats after intravenous administration. Similarly, PIC serves as an effective precursor of ISO upon oral administration. Conclusion Since PIC and its metabolites possess pleiotropic health‐promoting activities, it has emerged as a promising nutraceutical candidate for further development. This study also reinforces the importance of in vivo testing in nutritional researches as the active metabolite(s) may be absent from the in vitro system.