Yasuda T, Mizunuma S, Kano Y, Saito K, Oshawa K
Tohoku College of Pharmacy, Miyagi, Japan.
Biol Pharm Bull. 1996 Mar;19(3):413-7. doi: 10.1248/bpb.19.413.
Examination was made of the urinary and biliary excretion of the metabolites of genistein and genistein, the major components of Glycine and Sophora genus in rats. The urine of rats administered genistein orally contained eight metabolites. Three of these metabolites, genistein 4'-O-sulfate (M-1), genistein 7-O-beta-D-glucuronide (M-3), genistein 4'-O-sulfate 7-O-beta-D-glucuronide (M-6), were identified from spectroscopic and chemical data. The bile of rats administered genistein orally contained M-2, M-3 and M-6. M-6, a major biliary metabolite, was isolated and identified from spectroscopic and chemical data. The urine or bile of rats treated with genistein, the glycoside of genistein, contained M-1-M-8 or M-2, M-3, M-6 in the above metabolites. These findings suggest that genistein is absorbed as genistein after hydrolysis in the gastrointestinal tract. The total cumulative amounts of the two metabolites and genistein excreted in the urine during 48h, or of M-6 excreted in the bile during 36h following the oral administration of genistein, were approximately 5.7% or 16.0% of the doses administered, respectively. The result show that M-1, M-3 and M-6, having a free hydroxyl, glucuronide- or sulfate-conjugated hydroxyls at the C-7 or C-4' position, are excreted in the urine and bile as parts of the metabolites of genistein.
对大鼠体内染料木黄酮和染料木苷（甘草属和槐属的主要成分）代谢物的尿液和胆汁排泄情况进行了研究。经口给予染料木黄酮的大鼠尿液中含有8种代谢物。通过光谱和化学数据鉴定出其中3种代谢物，即染料木黄酮4'-O-硫酸盐（M-1）、染料木黄酮7-O-β-D-葡萄糖醛酸苷（M-3）、染料木黄酮4'-O-硫酸盐7-O-β-D-葡萄糖醛酸苷（M-6）。经口给予染料木黄酮的大鼠胆汁中含有M-2、M-3和M-6。从光谱和化学数据中分离并鉴定出主要的胆汁代谢物M-6。用染料木苷（染料木黄酮的糖苷）处理的大鼠尿液或胆汁中含有上述代谢物中的M-1 - M-8或M-2、M-3、M-6。这些发现表明，染料木黄酮在胃肠道水解后以染料木黄酮的形式被吸收。口服染料木黄酮后48小时内尿液中排泄的两种代谢物和染料木黄酮的总累积量，或36小时内胆汁中排泄的M-6的总累积量，分别约为给药剂量的5.7%或16.0%。结果表明，在C-7或C-4'位具有游离羟基、葡萄糖醛酸或硫酸盐共轭羟基的M-1、M-3和M-6，作为染料木黄酮代谢物的一部分排泄到尿液和胆汁中。
