中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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
出版日期2003-04
卷号31期号:4页码:452-461
ISSN号0090-9556
DOI10.1124/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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