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China Journal of Chinese Materia Medica ; (24): 524-528, 2012.
Artigo em Chinês | WPRIM | ID: wpr-274311

RESUMO

<p><b>OBJECTIVE</b>To study major human UGT isoforms involved in trans-resveratrol (TR) phase II metabolism.</p><p><b>METHOD</b>trans-resveratrol and 12 major human UGT isoforms were incubated in vitro and then glucuronic acid metabolites were determined by HPLC-MS, in order to preliminarily analyze the structure and observe the effect of different UGT isoforms on the generation rate of glucuronic acid metabolites.</p><p><b>RESULT</b>In in vitro metabolic system, two metabolites-4'-O-monoglucuronide resveratrol (M-1) and 3-0-monoglucuronide resveratrol (M-2)-were generated from trans-resveratrol after being catalyzed by UGT. During the cause, generation of M-1 and M-2 were catalyzed by UGT1A1, UGT1A3, 1A8, 1A9 andlA10, whereas only UGT1A6 and 1A7 contributed to the forma-tion of M-2. Both the formation rate of M-1 and M-2 catalyzed by UGT1A1, 1A10 and the formation of M-2 catalyzed by UGT1A8 slowed down with the increasing concentration of substrates, causing the phenomenon of "substrate inhibition".</p><p><b>CONCLUSION</b>UGT1A1, 1A8, 1A9, 1A10 get involved in the formation of M-1, and of them UGTIA9 is the most important contributor. UGT1A3 also makes small contribution to the formation of M-1 and M-2, while other UGT isoforms show hardly any reaction with the trans-resveratrol phase II metabolites.</p>


Assuntos
Humanos , Ácido Glucurônico , Metabolismo , Glucuronosiltransferase , Metabolismo , Isoenzimas , Metabolismo , Cinética , Estilbenos , Química , Metabolismo
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