Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Urinary and Biliary Metabolites of Daidzin and Daidzein in Rats
Takaaki YASUDAYoshihiro KANOKen-ichi SAITOKeisuke OHSAWA
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JOURNAL FREE ACCESS

1994 Volume 17 Issue 10 Pages 1369-1374

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Abstract
Examination was made of the urinary and biliary excretion of metabolites of daidzin and daidzein, the major components of roots of Pueraria lobata OHWI (Leguminosae) in rats. The urine of rats administered daidzin orally contained four major metabolites, daidzein 7, 4'-di-O-sulfate (M-1), daidzein 7-O-β-D-glucuronide (M-2), daidzein 4'-O-sulfate (M-3), daidzein (M-4), as determined from spectroscopic and chemical data. The urine of rats treated with daidzein contained M-2-M-4 in the above metabolites. Total cumulative amounts of the four metabolites excreted in the urine at 48 h following the oral administration of daidzin and daidzein were approximately 4.8% and 4.6% of the doses administered, respectively. The bile of rats administered daidzin orally contained M-1-M-4. Daidzein 7-O-β-D-glucuronide 4'-O-sulfate (M-5), a major biliary metabolite, was identified by the high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometery (LC-MS) and nulcear magnetic resonance (NMR) spectra. At least daidzin appeared to be hydrolyzed to aglycone after absorption in the body, and as a part of metabolites, M-1-M-4 having free hydroxyl, glucuronided or sulfated hydroxyls at the C-7 position, may then be excreted in the urine and bile.
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© The Pharmaceutical Society of Japan
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