Pharmacokinetics and bioavailability of the isoflavone biochanin A in rats

Biochanin A (BCA) is a dietary isoflavone present in legumes, most notably red clover, and in many herbal dietary supplements. BCA has been reported to have chemopreventive properties and is metabolized to the isoflavone genistein (GEN), BCA conjugates, and GEN conjugates. The metabolites may contri...

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Bibliographic Details
Published in:The AAPS journal 2006-07, Vol.8 (3), p.E433-E442
Main Authors: Moon, Young Jin, Sagawa, Kazuko, Frederick, Kosea, Zhang, Shuzhong, Morris, Marilyn E
Format: Article
Language:English
Subjects:
Animals
Biological Availability
Biotransformation
Genistein - analysis
Genistein - blood
Genistein - metabolism
Genistein - pharmacokinetics
Glycine max - chemistry
Male
Rats
Rats, Sprague-Dawley
Trifolium - chemistry
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Summary:Biochanin A (BCA) is a dietary isoflavone present in legumes, most notably red clover, and in many herbal dietary supplements. BCA has been reported to have chemopreventive properties and is metabolized to the isoflavone genistein (GEN), BCA conjugates, and GEN conjugates. The metabolites may contribute to the chemopreventive effects of BCA. The absorption, metabolism, and disposition of BCA have not been determined in rats. Our objective was to evaluate the pharmacokinetics and metabolism of BCA in rats. Male Sprague-Dawley rats were administered BCA by intravenous injection (1 and 5 mg/kg), by intraperitoneal injection (5 and 50 mg/kg), and orally (5 and 50 mg/kg). Plasma and bile samples were enzymatically hydrolyzed in vitro to determine conjugate concentrations for BCA and GEN. Equilibrium dialysis was used to determine protein binding. The BCA and GEN concentrations in plasma, urine, and bile were determined by liquid chromatography-tandem mass spectrometry (LC/MS/MS). The pharmacokinetic parameters of BCA were analyzed by noncompartmental analysis. Significant levels of BCA conjugates and GEN conjugates were detected in plasma and bile. Both BCA and GEN were found to have a high clearance and a large apparent volume of distribution; the bioavailability of both was poor (
ISSN:1550-7416
1550-7416
DOI:10.1208/aapsj080351