Department of Endocrinology, The First Affiliated Hospital of Xinjiang Medical University, Urumqi, Xinjiang, China.
Department of Endocrinology, People's Hospital of Shenzhen Baoan District, Shenzhen, Guangdong, China.
J Physiol Pharmacol. 2023 Apr;74(2). doi: 10.26402/jpp.2023.2.04. Epub 2023 Jul 10.
Patients with type 2 diabetes respond differently to sitagliptin, an oral anti-hyperglycemic medication. Patients whose blood sugar levels were effectively managed while using sitagliptin had significantly lower levels of a protein called suppressor of cytokine signaling 3 (SOCS3), according to our earlier research. In this study, we established an in vitro insulin resistance cell model for human HepG2 cells to investigate the possible mechanism of the effect of sitagliptin on glucose metabolism via the SOCS3/phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) pathway. Since insulin resistance first develops in the liver, palmitic acid was used to generate an insulin resistance cell model in human HepG2 cells, after which small interfering ribonucleic acid (siRNA)-SOCS3 and sitagliptin were used to intervene. We then examined the changes in cell viability and biochemical indices in the insulin resistance cell model. SOCS3, Akt, and glycogen synthase kinase 3beta (GSK-3β) gene expression levels were quantified using reverse transcription-polymerase chain reaction, and the protein expression levels of SOCS3, Akt, phosphorylated Akt (p-Akt), GSK-3β, and phosphorylated GSK-3β (p-GSK-3β) were quantified using Western blot. In results: the expression of the SOCS3 gene was considerably raised in both the insulin resistance model group and the insulin resistance model + siRNA-negative control group, but decreased following treatment with sitagliptin. After sitagliptin intervention, the protein expression of Akt, p-Akt, and p-GSK-3β were dramatically decreased in the model group, while SOCS3 was significantly decreased. We conclude that sitagliptin can reduce insulin resistance by downregulating SOCS3 and regulating glucose metabolism in a hypoglycemic manner.
2 型糖尿病患者对西他列汀这种口服降血糖药物的反应各有不同。根据我们早前的研究,使用西他列汀后血糖水平得到有效控制的患者,一种名为细胞因子信号转导抑制因子 3(SOCS3)的蛋白质水平显著降低。在这项研究中,我们建立了体外人 HepG2 细胞胰岛素抵抗细胞模型,以研究西他列汀通过 SOCS3/磷酸肌醇 3-激酶(PI3K)/蛋白激酶 B(Akt)通路对葡萄糖代谢产生影响的可能机制。由于胰岛素抵抗首先发生在肝脏,我们使用棕榈酸来生成人 HepG2 细胞的胰岛素抵抗细胞模型,然后使用小干扰核糖核酸(siRNA)-SOCS3 和西他列汀进行干预。接着,我们检测了胰岛素抵抗细胞模型中细胞活力和生化指标的变化。使用逆转录聚合酶链反应定量检测 SOCS3、Akt 和糖原合酶激酶 3β(GSK-3β)基因的表达水平,使用 Western blot 定量检测 SOCS3、Akt、磷酸化 Akt(p-Akt)、GSK-3β 和磷酸化 GSK-3β(p-GSK-3β)的蛋白表达水平。结果显示:胰岛素抵抗模型组和胰岛素抵抗模型+siRNA 阴性对照组 SOCS3 基因的表达均显著升高,但经西他列汀处理后下降。西他列汀干预后,模型组中 Akt、p-Akt 和 p-GSK-3β 的蛋白表达显著下降,而 SOCS3 则明显下降。我们得出结论,西他列汀可以通过下调 SOCS3 并以降低血糖的方式调节葡萄糖代谢,从而减轻胰岛素抵抗。