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Pak J Pharm Sci ; 28(2): 421-4, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25730798

RESUMO

Protein tyrosine phosphatases (PTPs) are enzymes that catalyze protein tyrosine dephosphorylation of which Src homology phosphatase-1 (SHP-1) is one of the best-validated, a widely distributed intracellular tyrosine phosphatase that contains two SH2 domains. Down regulation of SHP-1 tyrosine phosphatases was significantly increased sensitivity to insulin in insulin signaling pathway. Through in vitro enzymatic reaction kinetics experiment, we found that the extract of Perilla stem was a potential inhibitor to δSHP-1, the catalytic domain of SHP-1 protein tyrosine phosphatase, and its IC(50) was 4ug/ml, and was more sensitive towards SHP-1than other PTPs, which indicated that SHP-1 might be a target of the extract of Perilla stem. It can strengthened the level of tyrosine phosphorylation of insulin receptor (IR) and extracellular signal-regulated protein kinase (ERK) in HepG2 cells, and then activated the insulin signaling pathway through inhibiting the protein phosphorylation of SHP-1. These results demonstrated that the extract of Perilla stem could play an important role for diabetes treatment through inhibiting the level of SHP-1 in insulin signaling pathway.


Assuntos
Insulina/fisiologia , Perilla , Extratos Vegetais/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 6/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Células Hep G2 , Humanos , Fosforilação , Caules de Planta
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