Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/196986
Type: Artigo de periódico
Title: Differential Effects Of Flavonoids On Bovine Kidney Low Molecular Mass Protein Tyrosine Phosphatase.
Author: Miranda, Márcio A
Okamoto, André K
Ferreira, Carmen V
Silva, Thelma L
Granjeiro, José M
Aoyama, Hiroshi
Abstract: Among the structurally related flavonoids tested on the bovine kidney low molecular weight protein tyrosine phosphatase (LMrPTP) activity, quercetin activated by about 2.6-fold the p-nitrophenyl-phosphate (p-NPP)-directed reaction, in contrast to morin that acted as a competitive inhibitor, with Ki values of 87, 73 and 50 microM for p-NPP, FMN, and tyrosine-phosphate, respectively. Other related flavonoids, such as rutin, kaempferol, catechin, narigin, phloretin and taxifolin did not significantly affect the LMrPTP activity. The positions of the hydroxyl groups in the structures of the flavonoids were important for their distinct effects on LMrPTP activity. The hydroxyl groups at C3' and C4' and the presence of a double bond at C2 and C3 were essential for the activating effect of quercetin. The absence of the 3'-OH (kaempferol), absence of the double bond (taxifolin) and the presence of the sugar rutinose at the 3-OH (rutin) suppressed the effect of quercetin. The C2'- and C4'-hydroxyl groups, the presence of the double bond, and a C4-ketone group were important requirements for the inhibitory effects of morin.
Subject: Animals
Cattle
Chemistry, Pharmaceutical
Dose-response Relationship, Drug
Drug Design
Enzyme Inhibitors
Flavonoids
Flavonols
Hydrogen-ion Concentration
Hydrolysis
Kidney
Kinetics
Models, Chemical
Molecular Weight
Protein Tyrosine Phosphatases
Quercetin
Citation: Journal Of Enzyme Inhibition And Medicinal Chemistry. v. 21, n. 4, p. 419-25, 2006-Aug.
Rights: fechado
Identifier DOI: 10.1080/14756360500179523
Address: http://www.ncbi.nlm.nih.gov/pubmed/17059175
Date Issue: 2006
Appears in Collections:Unicamp - Artigos e Outros Documentos

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