Contribution of presystemic hepatic extraction to the low oral bioavailability of green tea catechins in rats

Yan Cai, Nathan D. Anavy, Hsiao-Hui Chow

Research output: Contribution to journalArticle

94 Citations (Scopus)

Abstract

Green tea and green tea catechins have been shown to possess potent cancer-preventive activities in rodent cancer models. At present, epidemiological evidence of the protective effect of green tea consumption against the development of human cancers is not conclusive. Oral bioavailability of green tea catechins has been shown to be low in animals and possibly in humans. This study is designed to determine the contribution of first-pass hepatic elimination to the low oral bioavailability of green tea catechins. Green tea catechin mixture was dosed to rats by intravenous or intraportal infusion. Blood samples were collected after dosing and analyzed using high-performance liquid chromatography with the coulometric electrode array detection system. The systemic clearance of epigallocatechin gallate (EGCG), epigallocatechin (EGC), and epicatechin (EC) was 8.9, 6.3, and 9.4 ml/min, respectively. The steady state volume of distribution (Vss) of EGCG, EGC, and EC was 432, 220, and 187 ml, respectively. We found that high percentage of green tea catechins escaped first-pass hepatic elimination, with 87.0, 108.3, and 94.9% of EGCG, EGC, and EC, respectively, available in the systemic blood following intraportal infusion. Our results suggest that factors within the gastrointestinal tract such as limited membrane permeability, transporter mediated intestinal secretion, or gut wall metabolism may contribute more significantly to the low oral bioavailability of green tea catechins.

Original languageEnglish (US)
Pages (from-to)1246-1249
Number of pages4
JournalDrug Metabolism and Disposition
Volume30
Issue number11
DOIs
StatePublished - Nov 1 2002

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Catechin
Tea
Biological Availability
Rats
Liver
Blood
Intestinal Secretions
Neoplasms
Membrane Transport Proteins
High performance liquid chromatography
Human Development
Metabolism
Gastrointestinal Tract
Rodentia
Permeability
Electrodes
Animals
High Pressure Liquid Chromatography
Membranes

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Cite this

Contribution of presystemic hepatic extraction to the low oral bioavailability of green tea catechins in rats. / Cai, Yan; Anavy, Nathan D.; Chow, Hsiao-Hui.

In: Drug Metabolism and Disposition, Vol. 30, No. 11, 01.11.2002, p. 1246-1249.

Research output: Contribution to journalArticle

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