Metabolism in vivo of all-trans-[11-3H]retinoic acid after an oral dose in rats. Characterization of retinoyl beta-glucuronide in the blood and other tissues.

Metabolism in vivo of all-trans-[11-3H]retinoic acid after an oral dose in rats. Characterization of retinoyl beta-glucuronide in the blood and other tissues.
复制标题

大鼠口服剂量后全反式[11-3H]视黄酸的体内代谢。

DOI:
10.1042/bj2770527
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发表时间:
1991
期刊:
The Biochemical journal
影响因子:
--
通讯作者:
Olson,JA
Olson,JA
中科院分区:
--
文献类型:
--
作者:
Barua,AB;Gunning,DB;Olson,JA

文献摘要

被引文献

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不久后[11-~3H]维甲酸(RA)(1.1×10(8)D.P.M.)大鼠口服维甲酸(115微克=0.38摩尔/鼠)或与未标记的维甲酸(22 mg=73.33摩尔/鼠)混合给药,在血清和小肠中被鉴定为一种重要的代谢物。在给药剂量中,70%的维甲酸在胃中保持不变,直到1h。在胃中还检测到大量的5,6-环氧维甲酸、4-羟基维甲酸、维甲酸酯和包括4-氧代维甲酸在内的几种极性维甲酸。大剂量组与大剂量组的类维A酸性质无明显差异,但大剂量组RAG/RA比值高于大剂量组。因此,在体内和体外具有生物活性的RAG在服用一剂RA后,在组织中迅速形成大量的RAG。
Soon after [11-3H]retinoic acid (RA) (1.1 x 10(8) d.p.m.) was administered orally to rats either as a large dose (115 micrograms = 0.38 mumol/rat) or mixed with unlabelled RA as a huge dose (22 mg = 73.33 mumol/rat), retinoyl beta-glucuronide (RAG) was identified and characterized as a significant metabolite in the serum and small intestine. Of the administered dose, 70% remained unchanged as retinoic acid in the stomach up to 1 h. Significant amounts of 5,6-epoxyretinoic acid, 4-hydroxyretinoic acid, esters of retinoic acid and several polar retinoids, including 4-oxoretinoic acid, were also detected in the stomach. No significant difference was observed in the nature of the retinoids found after a large or a huge dose; however, the ratio of RAG/RA was higher after a huge dose than after a large dose. Thus RAG, which is biologically active in vivo and in vitro, is formed quickly in significant amounts in tissues after a dose of RA.