INSERM, UMR-S 872, Centre de Recherches des Cordeliers and Université Pierre et Marie Curie-Paris, Paris, France.
Diabetes Obes Metab. 2010 Oct;12 Suppl 2:83-92. doi: 10.1111/j.1463-1326.2010.01275.x.
Steatosis is an accumulation of triglycerides in the liver. Although an excessive availability of plasma fatty acids is an important determinant of steatosis, lipid synthesis from glucose (lipogenesis) is now also considered as an important contributing factor. Lipogenesis is an insulin- and glucose-dependent process that is under the control of specific transcription factors, sterol regulatory element binding protein 1c (SREBP-1c), activated by insulin and carbohydrate response element binding protein (ChREBP) activated by glucose. Insulin induces the maturation of SREBP-1c by a proteolytic mechanism initiated in the endoplasmic reticulum (ER). SREBP-1c in turn activates glycolytic gene expression, allowing glucose metabolism, and lipogenic genes in conjunction with ChREBP. Lipogenesis activation in the liver of obese markedly insulin-resistant steatotic rodents is then paradoxical. Recent data suggest that the activation of SREBP-1c and thus of lipogenesis is secondary in the steatotic liver to an ER stress. The ER stress activates the cleavage of SREBP-1c independent of insulin, thus explaining the paradoxical stimulation of lipogenesis in an insulin-resistant liver. Inhibition of the ER stress in obese rodents decreases SREBP-1c activation and lipogenesis and improves markedly hepatic steatosis and insulin sensitivity. ER is thus a new partner in steatosis and metabolic syndrome which is worth considering as a potential therapeutic target.
脂肪变性是肝脏中甘油三酯的积累。尽管血浆脂肪酸的过度供应是脂肪变性的一个重要决定因素,但现在也认为从葡萄糖合成脂质(脂肪生成)是一个重要的促成因素。脂肪生成是一个胰岛素和葡萄糖依赖性的过程,受特定转录因子的控制,固醇调节元件结合蛋白 1c(SREBP-1c),由胰岛素激活,碳水化合物反应元件结合蛋白(ChREBP)由葡萄糖激活。胰岛素通过内质网(ER)中的蛋白水解机制诱导 SREBP-1c 的成熟。SREBP-1c 反过来激活糖酵解基因表达,允许葡萄糖代谢,并与 ChREBP 一起激活脂肪生成基因。因此,肥胖和明显胰岛素抵抗的脂肪肝动物肝脏中的脂肪生成激活是矛盾的。最近的数据表明,在脂肪肝中,SREBP-1c 的激活,因此脂肪生成的激活是 ER 应激的继发事件。ER 应激激活 SREBP-1c 的切割不依赖于胰岛素,从而解释了胰岛素抵抗肝脏中脂肪生成的悖论性刺激。在肥胖的啮齿动物中抑制 ER 应激可降低 SREBP-1c 的激活和脂肪生成,并显著改善肝脂肪变性和胰岛素敏感性。因此,ER 是脂肪变性和代谢综合征的一个新伙伴,值得考虑作为一个潜在的治疗靶点。