Tissue Distribution and Elimination of Estrogenic and Anti-Inflammatory Catechol Metabolites from Sesaminol Triglucoside in Rats

Sesaminol triglucoside (STG) is the main sesame (Sesamum indicum L.) lignan. Like many other plant lignans, STG can be converted to the mammalian lignans by intestinal microbiota. The objectives of the present study were to investigate the distribution of STG metabolite in rats, and the effects of S...

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Bibliographic Details
Published in:Journal of agricultural and food chemistry 2010-07, Vol.58 (13), p.7693-7700
Main Authors: Jan, Kuo-Ching, Ku, Kuo-Lung, Chu, Yan-Hwa, Hwang, Lucy Sun, Ho, Chi-Tang
Format: Article
Language:English
Subjects:
animal models
Animals
anti-inflammatory activity
Anti-Inflammatory Agents - analysis
Anti-Inflammatory Agents - metabolism
Anti-Inflammatory Agents - pharmacokinetics
Biological and medical sciences
catechol
Catechols - analysis
Catechols - metabolism
Catechols - pharmacokinetics
Cell Line
Chemical Aspects of Biotechnology/Molecular Biology
estrogenic properties
Estrogens - analysis
Estrogens - metabolism
Estrogens - pharmacokinetics
experimental diets
Food industries
free radical scavengers
Fundamental and applied biological sciences. Psychology
Glucosides - analysis
Glucosides - metabolism
Glucosides - pharmacokinetics
glycosides
Humans
intestinal microorganisms
lignan glycosides
lignans
metabolites
Mice
Plant Extracts - analysis
Plant Extracts - metabolism
Plant Extracts - pharmacokinetics
Rats
Rats, Sprague-Dawley
sesaminol triglucoside
Sesamum - chemistry
Sesamum indicum
Tissue Distribution
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Summary:Sesaminol triglucoside (STG) is the main sesame (Sesamum indicum L.) lignan. Like many other plant lignans, STG can be converted to the mammalian lignans by intestinal microbiota. The objectives of the present study were to investigate the distribution of STG metabolite in rats, and the effects of STG and its metabolite on in vitro inflammation and estrogenic activities. STG was metabolized via intestinal microflora to a biologically active catechol moiety which would then be absorbed into the body in rats. After oral administration of STG to Sprague−Dawley rats, the concentrations of major STG metabolites in rectum, cecum, colon, and small intestines are higher than those in liver, lung, kidney, and heart. Its concentration in brain is low but detectable. The present study demonstrates that STG may be metabolized to form the catechol metabolites first by intestinal microflora and then incorporated via intestine absorption into the cardiovascular system and transported to other tissues. Results showed that the catechol metabolites were found to be able to penetrate the tail end of intestines (large intestine) and go through urinary excretion. STG metabolites significantly reduced the production of IL-6 and TNF-α in RAW264.7 murine macrophages stimulated with lipopolysaccharide. The estrogenic activities of STG metabolites were also established by ligand-dependent transcriptional activation through estrogen receptors. This study clearly shows that STG has anti-inflammatory and estrogenic activities via metabolism of intestinal microflora.
ISSN:0021-8561
1520-5118
DOI:10.1021/jf1009632