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6. Mechanism of Anti-obese Effects of 'Benifuuki' Green Tea

Author

Oritani, Yukihiro, primary, Matsui, Yuko, additional, Kurita, Ikuko, additional, Kinoshita, Yosuke, additional, Kawakami, Shinpei, additional, Yanae, Koji, additional, Nishimura, Eisaku, additional, Kato, Masatoshi, additional, Sai, Masahiko, additional, Matsumoto, Ichiro, additional, Abe, Keiko, additional, Maeda-Yamamoto, Mari, additional, and Kamei, Masanori, additional

Published
2009
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8. Comparison of (-)-epigallocatechin-3-O-gallate (EGCG) and O-methyl EGCG bioavailability in rats.

Author

Oritani Y, Setoguchi Y, Ito R, Maruki-Uchida H, Ichiyanagi T, and Ito T

Subjects
Animals, Area Under Curve, Biological Availability, Catechin pharmacokinetics, Gallic Acid pharmacokinetics, Male, Rats, Rats, Sprague-Dawley, Camellia sinensis chemistry, Catechin analogs & derivatives, Gallic Acid analogs & derivatives, Plant Extracts pharmacokinetics, Tea chemistry
Abstract

(-)-Epigallocatechin-3-O-(3-O-methyl)gallate (EGCG3″Me) and (-)-epigallocatechin-3-O-(4-O-methyl)gallate (EGCG4″Me) are O-methyl derivatives of (-)-epigallocatechin-3-O-gallate (EGCG) present in tea cultivars such as Benifuuki. Although O-methyl EGCGs have various bioactivities, their bioavailabilities have not been determined. In this study, we compared the bioavailability of EGCG and O-methyl EGCGs in rats, and clarified the pharmacokinetics of O-methyl EGCGs. Following oral administration (100 mg/kg), the areas under the concentration-time curves (AUCs) for EGCG, EGCG3″Me, and EGCG4″Me were 39.6 ± 14.2 µg·h/L, 317.2 ± 43.7 µg·h/L, and 51.9 ± 11.0 µg·h/L, respectively. The AUC after intravenous administration (10 mg/kg) was 2772 ± 480 µg·h/L for EGCG, 8209 ± 549 µg·h/L for EGCG3″Me, and 2465 ± 262 µg·h/L for EGCG4″Me. The bioavailability of EGCG3″Me (0.38%) was the highest (EGCG: 0.14% and EGCG4″Me: 0.21%). The distribution volume of EGCG3″Me (0.26 ± 0.02 L/kg) was the lowest (EGCG: 0.94 ± 0.16 L/kg and EGCG4″Me: 0.93 ± 0.14 L/kg). These results suggested that the higher AUC of EGCG3″Me after oral administration was related to its high bioavailability and low distribution volume. These findings supported the stronger bioactivity of EGCG3″Me in vivo.

Published
2013
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