Abstract：
:The health effects of green tea are associated with catechins: (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin, (-)-epicatechin-3-O-gallate, and (-)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biological activities. Herein, absorption, distribution, metabolism, excretion, and toxicity properties of in vivo detected metabolites of green tea catechins (GTCs) have been analyzed in silico. The influence of metabolic transformations on absorption, distribution, metabolism, and excretion profiles of GTCs corresponds to the effects of size, charge, and lipophilicity, as already observed for other small molecules. Mutagenic, carcinogenic, or liver toxic effects were predicted only for a few metabolites. Similar to galloylated GTCs EGCG and (--)-epicatechin-3-O-gallate, the sulfo-conjugates were predicted to bind at the warfarin binding site. The low free plasma concentration of these derivatives may be consequential to their serum albumin binding. The activity cliff detected for methylated conjugates of EGCG indicates that GTCs' pro-oxidative activity in bound state comes primarily from free hydroxyl groups of the pyrogallol ring B.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Matić S,Jadrijević-Mladar Takač M,Barbarić M,Lučić B,Gall Trošelj K,Stepanić Vdoi
10.1016/j.xphs.2018.07.026subject
Has Abstractpub_date
2018-11-01 00:00:00pages
2957-2964issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(18)30483-0journal_volume
107pub_type
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