An extract of Perilla stem inhibits Src homology phosphatase-1 (SHP)-1 and influences insulin signaling.

PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES(2015)

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摘要
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 intracelliilar 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 Delta SHP-1, the catalytic domain of SHIP-1 protein tyrosine phosphatase, and its IC50 was 4ug/ml, and was more sensitive towards SHP-lthan 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 pathviay.
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关键词
SHP-1,Perilla stem,inhibitor,insulin sensitivity
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