Green tea flavonols inhibit glucosidase II

被引:46
作者
Gamberucci, Alessandra
Konta, Laura
Colucci, Angela
Giunti, Roberta
Magyar, Judit E.
Mandl, Jozsef
Banhegyi, Gabor
Benedetti, Angelo
Csala, Miklos [1 ]
机构
[1] Semmelweis Univ, Hungarian Acad Sci, Dept Med Chem Mol Biol & Pathobiochem, Endoplasm Reticulum Res Grp, H-1085 Budapest, Hungary
[2] Univ Siena, Dept Physiopathol Expt Med & Publ Hlth, I-53100 Siena, Italy
[3] Santa Maria Scotte Hsop, Unit Dev Biomed Res, I-53100 Siena, Italy
关键词
green tea; endoplasmic reticulum; glucosidase II; kinetics; inhibition; rat liver;
D O I
10.1016/j.bcp.2006.05.016
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Green tea is getting into the focus of scientific interest due to its beneficial health effects, most of which are attributed to its catechin content. Polyphenolic tea catechins have antioxidant, antiproliferative, antiarigiogenic and proapoptotic effects, which makes them promising anticancer compounds. Other poly-hydroxy molecules have similar antitumor potentials through the inhibition of glucosidase II, which affects the glycoprotein maturation and quality control in the endoplasmic reticulum. We investigated the effect of tea catechins on glucosidase II activity in rat liver microsomes using 4-methylumbelliferyl glucoside and 4-nitrophenyl glucoside as substrates. A concentration-dependent inhibition with non-competitive kinetics was found. The IC50 and K-i values for certain tea catechins were comparable with those of N-butyldeoxynojirimycin, the widely used glucosidase inhibitor. The possible interference of tea catechins with the glycoprotein processing in the endoplasmic reticulum should be considered as a potential mechanism of their dietary or pharmacological effects. (c) 2006 Elsevier Inc. All rights reserved.
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页码:640 / 646
页数:7
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