Comparison of (-)-Epigallocatechin-3-O-gallate (EGCG) and O-Methyl EGCG Bioavailability in Rats
Comparison of (-)-Epigallocatechin-3-O-gallate (EGCG) and O-Methyl EGCG Bioavailability in Rats
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DOI：
10.1248/bpb.b13-00349
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发表时间：
2013-10-01
影响因子：
2
通讯作者：
Ito, Tatsuhiko
中科院分区：
文献类型：
--
作者：
Oritani, Yukihiro;Setoguchi, Yuko;Ito, Tatsuhiko
（-）-表没食子儿茶素-3-O-（3-O-甲基）没食子酸酯（EGCG 3 ″ Me）和（-）-表没食子儿茶素-3-O-（4-O-甲基）没食子酸酯（EGCG 4 ″ Me）是存在于茶树栽培品种如Benifuuki中的（-）-表没食子儿茶素-3-O-没食子酸酯（EGCG）的O-甲基衍生物。虽然O-甲基EGCG具有多种生物活性，但其生物利用度尚未确定。本研究比较了表没食子儿茶素没食子酸酯（EGCG）和O-甲基表没食子酸酯（O-methyl EGCGs）在大鼠体内的生物利用度，阐明了O-甲基表没食子酸酯的药代动力学。口服给药（100 mg/kg）后，EGCG、EGCG 3“”Me和EGCG 4“”Me的浓度-时间曲线下面积（AUC）分别为39.6 +/- 14.2 μ g.h/L、317.2 +/- 43.7 μ g.h/L和51.9 +/- 11.0 μ g.h/L。静脉给药后的AUC对于EGCG（10 mg/kg），生物利用度为2772 +/- 480 μ g.h/L，对于EGCG 3-Me为8209 +/- 549 μ g.h/L，对于EGCG 4-Me为2465 +/- 262 μ g.h/L。（0.38%）最高（EGCG：0.14%和EGCG_（4-Me）：0.21%）。表没食子儿茶素没食子酸酯（EGCG）的分布容积最小，为0.94 ± 0.16L/kg，表没食子酸酯（EGCG）的分布容积最小，为0.93 ± 0.14L/kg。这些结果表明，口服给药后EGCG 3-Me的AUC较高，与其生物利用度高和分布容积低有关。这些结果支持EGCG 3 "Me在体内具有更强的生物活性。
(-)-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 mu g.h/L, 317.2 +/- 43.7 mu g.h/L, and 51.9 +/- 11.0 mu g.h/L, respectively. The AUC after intravenous administration (10 mg/kg) was 2772 +/- 480 mu g.h/L for EGCG, 8209 +/- 549 mu g.h/L for EGCG3 '' Me, and 2465 +/- 262 mu g.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 +/- 0.02L/kg) was the lowest (EGCG: 0.94 +/- 0.16L/kg and EGCG4 '' Me: 0.93 +/- 0.14L/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.