Glucuronides of tea catechins: Enzymology of biosynthesis and biological activities
文献类型:期刊论文
作者 | Lu, H; Meng, XF; Li, C; Sang, SM; Patten, C; Sheng, SQ; Hong, JG; Bai, NS; Winnik, B; Ho, CT |
刊名 | DRUG METABOLISM AND DISPOSITION
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出版日期 | 2003-04 |
卷号 | 31期号:4页码:452-461 |
ISSN号 | 0090-9556 |
DOI | 10.1124/dmd.31.4.452 |
文献子类 | Article |
英文摘要 | (-)-Epigallocatechin gallate (EGCG) and (-)-epigallocatechin (EGC) are major green tea catechins with antioxidant and anticancer activities. In this study, we characterized the glucuronidation of EGCG and EGC in human, mouse, and rat microsomes and by nine different human UGT 1A and 2B isozymes expressed in insect cells. Six EGCG and EGC glucuronides were biosynthesized, and their structures were identified for the first time. (-)-EGCG-4"-O-glucuronide was the major EGCG glucuronide formed in all incubations. The catalytic efficiency (V-max/K-m) for (-)-EGCG-4"-O-glucuronide formation followed the order: mouse intestine > mouse liver > human liver > rat liver >> rat small intestine. The UGT-catalyzed glucuronidation of EGC was much lower than that of EGCG. The V-max/K-m for (-)-EGC-3'-O-glucuronide followed the following order: mouse liver > human liver > rat liver > rat and mouse small intestine. Human UGT1A1, 1A8, and 1A9 had high activities with EGCG. UGT1A8, an intestine-specific UGT, had the highest V-max/K-m for EGCG but low activity with EGC. Mice appeared to be more similar to humans than rats to humans in the glucuronidation of EGCG and EGC. Some of these catechin glucuronides retained the activities of their parent compounds in radical scavenging and in inhibiting the release of arachidonic acid from HT-29 human colon cancer cells. These results provide foundations for understanding the biotransformation and biological activities of tea catechins. |
WOS关键词 | UDP-GLUCURONOSYLTRANSFERASE ACTIVITY ; SMALL-INTESTINE ; GREEN TEA ; INTERINDIVIDUAL VARIATION ; MASS-SPECTROMETRY ; IDENTIFICATION ; POLYPHENOLS ; LIVER ; HUMANS ; RATS |
资助项目 | NCI NIH HHS[CA 88961] ; NCI NIH HHS[CA 56673] |
WOS研究方向 | Pharmacology & Pharmacy |
语种 | 英语 |
WOS记录号 | WOS:000181852500015 |
出版者 | AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS |
源URL | [http://119.78.100.183/handle/2S10ELR8/274249] ![]() |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Yang, CS |
作者单位 | 1.Environm & Occupat Hlth Sci Inst, Piscataway, NJ USA 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China 3.BD Biosci, Woburn, MA USA 4.Rutgers State Univ, Dept Biol Chem, Ernest Mario Sch Pharm, Piscataway, NJ 08854 USA 5.Rutgers State Univ, Dept Food Sci, Piscataway, NJ 08854 USA 6.Rutgers State Univ, Ctr Adv Food Technol, Piscataway, NJ 08854 USA 7.Rutgers State Univ, Dept Chem, Piscataway, NJ 08854 USA |
推荐引用方式 GB/T 7714 | Lu, H,Meng, XF,Li, C,et al. Glucuronides of tea catechins: Enzymology of biosynthesis and biological activities[J]. DRUG METABOLISM AND DISPOSITION,2003,31(4):452-461. |
APA | Lu, H.,Meng, XF.,Li, C.,Sang, SM.,Patten, C.,...&Yang, CS.(2003).Glucuronides of tea catechins: Enzymology of biosynthesis and biological activities.DRUG METABOLISM AND DISPOSITION,31(4),452-461. |
MLA | Lu, H,et al."Glucuronides of tea catechins: Enzymology of biosynthesis and biological activities".DRUG METABOLISM AND DISPOSITION 31.4(2003):452-461. |
入库方式: OAI收割
来源:上海药物研究所
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