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首页> 外文期刊>Cellular Physiology and Biochemistry >Stearic Acid Serves as a Potent Inhibitor of Protein Tyrosine Phosphatase 1B
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Stearic Acid Serves as a Potent Inhibitor of Protein Tyrosine Phosphatase 1B

机译：硬脂酸作为蛋白质酪氨酸磷酸酶1B的有效抑制剂。

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biBackground/Aims /i/bFree fatty acids (FFAs) are implicated in diverse signal transduction pathways. The present study investigated the effects of the saturated FFA stearic acid on protein tyrosine phosphatase 1B (PTP1B) activity, Akt activity, and glucose uptake into cells relevant to insulin signal. biMethods /i/bPTP1B activity was assayed under the cell-free conditions. Phosphorylation of insulin receptor and Akt and glucose uptake into cells were monitored in differentiated 3T3-L1-GLUT4myc adipocytes. biResults /i/bIn the cell-free PTP1B assay, stearic acid suppressed PTP1B activity in a concentration (1-30 µM)-dependent manner. For 3T3-L1-GLUT4myc adipocytes insulin phosphorylated insulin receptor at Tyr1185 and Akt at Thr308 and Ser473 in a concentration (100 fM-100 nM)-dependent manner and stimulated glucose uptake into cells in a concentration (0.1-100 nM)-dependent manner. Stearic acid (30 µM) significantly increased insulin-induced phosphorylation of insulin receptor at Tyr1185, but insulin-induced phosphorylation of Akt was not significantly enhanced. Stearic acid (30 µM) by itself promoted glucose uptake into adipocytes. biConclusion /i/bThe results of the present study indicate that stearic acid serves as a potent PTP1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes.
机译：背景/目标 游离脂肪酸（FFA）与多种信号转导途径有关。本研究调查了饱和FFA硬脂酸对蛋白质酪氨酸磷酸酶1B（PTP1B）活性，Akt活性和葡萄糖摄入与胰岛素信号有关的细胞的影响。 方法 PTP1B活性是在无细胞条件下测定的。在分化的3T3-L1-GLUT4myc脂肪细胞中监测胰岛素受体的磷酸化和Akt以及葡萄糖摄取到细胞中。 结果 在无细胞PTP1B分析中，硬脂酸以浓度（1-30 µM）依赖性方式抑制PTP1B活性。对于3T3-L1-GLUT4myc脂肪细胞，Tyr1185处的胰岛素磷酸化胰岛素受体和Thr308和Ser473处的Akt胰岛素以浓度（100 fM-100 nM）依赖性方式被刺激，并且葡萄糖以浓度（0.1-100 nM）依赖性方式刺激细胞摄取葡萄糖。 。硬脂酸（30 µM）显着增加Tyr1185处胰岛素诱导的胰岛素受体的磷酸化，但胰岛素诱导的Akt磷酸化没有显着增强。硬脂酸（30 µM）本身可促进葡萄糖吸收进入脂肪细胞。 结论 本研究结果表明，硬脂酸是有效的PTP1B抑制剂，可能导致胰岛素受体信号转导增强，刺激葡萄糖吸收进入脂肪细胞。

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