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Nutrient Metabolism

Epigallocatechin-3-Gallate Is Absorbed but Extensively Glucuronidated Following Oral Administration to Mice^1,2

Departments of Chemical Biology and ^* Pharmacy Practice and Administration, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854

²To whom correspondence and reprint requests should be addressed. E-mail: csyang{at}rci.rutgers.edu.

Epigallocatechin-3-gallate (EGCG), the most abundant catechin in green tea (Camellia sinensis), has shown cancer preventive activity in animal models. The bioavailability of EGCG in the most commonly used animal species, mice, is poorly understood. Moreover, the pharmacokinetic parameters of EGCG have not been reported previously in mice. Here we report that after administration of EGCG intravenously at 21.8 µmol/kg or intragastrically at 163.8 µmol/kg, the peak plasma levels of EGCG in male CF-1 mice were 2.7 ± 0.7 and 0.28 ± 0.08 µmol/L, respectively. EGCG was present mainly (50–90%) as the glucuronide. The plasma bioavailability of EGCG after intragastric administration was higher than previously reported in rats (26.5 ± 7.5% vs. 1.6 ± 0.6%). The conjugated EGCG displayed a shorter t_1/2 (82.8–211.5 vs 804.9–1102.3 min) than unconjugated EGCG (P < 0.01, Student’s t test). EGCG was present in the unconjugated form in the lung, prostate and other tissues at levels of 0.31–3.56 nmol/g after intravenous administration. Although intragastric administration resulted in lower levels in most tissues compared with intravenous administration (e.g., 0.006 ± 0.004 vs. 2.66 ± 1.0 nmol/g in the lung), the levels in the small intestine and colon were high at 45.2 ± 13.5 and 7.86 ± 2.4 nmol/g, respectively. This is the first report of the pharmacokinetic parameters of EGCG in mice. Such information provides a basis for understanding the bioavailability of EGCG in mice and should aid in understanding the cancer preventive activity of EGCG.

KEY WORDS: • epigallocatechin-3-gallate • pharmacokinetics • green tea • mice

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