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Vol. 29, Issue 6, 789-793, June 2001
)-Epigallocatechin in Humans
Laboratory for Cancer Research The possible beneficial effects of tea consumption have attracted a
great deal of attention. Many of the biological effects have been
attributed to tea catechins, but the metabolic fate of these compounds
is not clear. In the present study, a major metabolite observed in
human blood and urine samples after green tea administration was
identified as a O-methylated derivative of
(
(X.M., M.-J.L., C.L.,
C.S.Y.),
Department of Chemistry (S.Sh.),
and Department of
Food Science
(N.Z., S.Sa., C.-T.H.), Rutgers,
The State
University of New Jersey,
Piscataway, New Jersey
)-epigallocatechin (EGC) by comparison with products from chemical
and enzymatic O-methylation of EGC. The structure of this metabolite was elucidated as
4'-O-methyl-(
)-epigallocatechin (4'-O-MeEGC) by 1H and 13C NMR
and heteronuclear multiple bond connectivity experiment. The
human plasma level of 4'-O-MeEGC reached its peak value
within the first 2 h following tea ingestion. Its maximum
concentration was 4 to 6 times higher than that of EGC. The half-lives
of EGC and 4'-O-MeEGC in the blood were 1.02 ± 0.07 and 4.39 ± 1.14 h, respectively. The amount of
4'-O-MeEGC excreted in urine was about 3 times higher
than that of EGC, and 88% of 4'-O-MeEGC was excreted in
urine within 8 h. The present structural information and
concentration-time profile of this metabolite provide the basis for
understanding the biotransformation of EGC and for future elucidation
of its biological activities.
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