Kaliman P, Viñals F, Testar X, Palacín M, Zorzano A
Departament de Bioquímica i Fisiologia, Facultat de Biologia, Universitat de Barcelona, Spain.
Biochem J. 1995 Dec 1;312 ( Pt 2)(Pt 2):471-7. doi: 10.1042/bj3120471.
In this study we have used wortmannin, a highly specific inhibitor of phosphatidylinositol (PI) 3-kinase, to assess the role of this enzyme on GLUT1 glucose carrier distribution and glucose transport activity in myoblasts from two skeletal-muscle cell lines, L6E9 and Sol8. As detected in L6E9 cells, myoblasts exhibited basal and insulin-stimulated PI 3-kinase activities. Incubation of intact myoblasts with wortmannin resulted in a marked inhibition of both basal and insulin-stimulated PI 3-kinase activities. L6E9 and Sol8 myoblasts showed basal and insulin-stimulated glucose transport activities, both of them inhibited by wortmannin in a dose-dependent manner (IC50 approximately 10-20 nM). Concomitantly, immunofluorescence analysis revealed that 1 h treatment with wortmannin led to a dramatic intracellular accumulation of GLUT1 carriers (the main glucose transporter expressed in L6E9 and Sol8 myoblasts) in both cell systems. The effect of wortmannin on GLUT1 cellular redistribution was independent of the presence of insulin. The cellular distribution of two structural plasma-membrane components such as beta 1-integrin or the alpha 1 subunit of the Na(+)-K(+)-ATPase were unaffected by wortmannin in both the absence and the presence of insulin. As a whole, our results indicate that PI 3-kinase is necessary to basal and insulin-stimulated glucose transport in L6E9 and Sol8 myoblasts. Moreover, immunofluorescence assays suggest that in both cellular models there is a constitutive GLUT 1 trafficking pathway (independent of insulin) that involves PI 3-kinase and which, when blocked, locks GLUT1 in a perinuclear compartment.
在本研究中,我们使用了渥曼青霉素(一种磷脂酰肌醇(PI)3激酶的高度特异性抑制剂)来评估该酶在来自两种骨骼肌细胞系L6E9和Sol8的成肌细胞中对葡萄糖转运蛋白1(GLUT1)葡萄糖载体分布及葡萄糖转运活性的作用。如在L6E9细胞中检测到的那样,成肌细胞表现出基础的和胰岛素刺激的PI 3激酶活性。用渥曼青霉素孵育完整的成肌细胞导致基础的和胰岛素刺激的PI 3激酶活性均受到显著抑制。L6E9和Sol8成肌细胞表现出基础的和胰岛素刺激的葡萄糖转运活性,二者均被渥曼青霉素以剂量依赖方式抑制(半数抑制浓度约为10 - 20 nM)。同时,免疫荧光分析显示,用渥曼青霉素处理1小时导致在两个细胞系统中GLUT1载体(L6E9和Sol8成肌细胞中表达的主要葡萄糖转运体)在细胞内大量积累。渥曼青霉素对GLUT1细胞再分布的作用与胰岛素的存在无关。两种质膜结构成分(如β1整合素或钠钾ATP酶的α1亚基)的细胞分布在有无胰岛素的情况下均不受渥曼青霉素影响。总体而言,我们的结果表明,PI 3激酶对于L6E9和Sol8成肌细胞中的基础和胰岛素刺激的葡萄糖转运是必需的。此外,免疫荧光测定表明,在这两种细胞模型中都存在一条组成型的GLUT1转运途径(独立于胰岛素),该途径涉及PI 3激酶,并且当被阻断时,会将GLUT1锁定在核周区室中。