Sass J O, Tzimas G, Nau H
Institut für Toxikologie und Embryopharmakologie, Freie Universität Berlin, Germany.
Life Sci. 1994;54(6):PL69-74. doi: 10.1016/0024-3205(94)00703-9.
The in vivo metabolism of 9-cis-retinoic acid (9-c-RA), an endogenous ligand of retinoid X receptors (RXRs), which can also bind to retinoic acid receptors (RARs), was examined in pregnant mice and rats following a single oral dose of 100 mg 9-cis-retinaldehyde (9-c-RAL)/kg body weight. 9-Cis-retinoyl-beta-D-glucuronide (9-c-RAG), a metabolite not found in vivo before, was a major metabolite of 9-c-RA in mouse plasma and was also present in all mouse tissues examined as well as in rat plasma. In both species putative oxidation products of retinoic acids and high levels of retinyl esters were found. Concentrations of retinoic acid isomers and retinoyl-beta-D-glucuronides in the mouse plasma greatly exceeded those of the rat plasma. The finding of high levels of 9-c-RAG underlines the importance of glucuronidation in the metabolism of retinoids.
视黄酸X受体（RXRs）的内源性配体9-顺式视黄酸（9-c-RA）也可与视黄酸受体（RARs）结合，在怀孕小鼠和大鼠单次口服100 mg 9-顺式视黄醛（9-c-RAL）/kg体重后，对其体内代谢情况进行了研究。9-顺式视黄酰-β-D-葡萄糖醛酸苷（9-c-RAG）是一种之前在体内未发现的代谢产物，它是小鼠血浆中9-c-RA的主要代谢产物，在所检测的所有小鼠组织以及大鼠血浆中也有存在。在这两个物种中均发现了视黄酸的推定氧化产物和高水平的视黄酯。小鼠血浆中视黄酸异构体和视黄酰-β-D-葡萄糖醛酸苷的浓度大大超过大鼠血浆中的浓度。高水平9-c-RAG的发现突出了葡萄糖醛酸化在类视黄醇代谢中的重要性。
