Valasek Mark A, Weng Jian, Shaul Philip W, Anderson Richard G W, Repa Joyce J
Department of Physiology, The University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390, USA.
J Biol Chem. 2005 Jul 29;280(30):28103-9. doi: 10.1074/jbc.M504609200. Epub 2005 May 26.
Caveolin-1 (CAV1) is the structural protein of the filamentous coat that decorates the cytoplasmic surface of each caveola. Cell culture studies have implicated CAV1 in playing an important role in intracellular cholesterol trafficking. In addition, it has been reported that CAV1 forms a detergent-resistant protein complex with Annexin-2 in enterocytes that can be disrupted by the cholesterol absorption inhibitor ezetimibe, suggesting a possible role for CAV1 in cholesterol absorption. In this report, we have evaluated cholesterol homeostasis in Cav1 knock-out mice. Deletion of CAV1 does not result in either a compensatory increase of CAV2 or CAV3 in intestine. In addition, Cav1 knock-out mice display normal mRNA and protein levels of Annexin-2 or the putative cholesterol transport protein Niemann-Pick C1-like 1 (NPC1L1) in proximal intestinal mucosa. Fractional cholesterol absorption and fecal neutral sterol excretion are statistically similar in Cav1 knock-out mice and their wild-type littermates. Moreover, oral administration of ezetimibe is equally effective in decreasing cholesterol absorption in Cav1 null mice and wild-type controls. The mRNA expression levels of genes sensitive to intracellular cholesterol concentration (ATP-binding cassette transporters ABCA1 and ABCG5, hydroxymethylglutaryl-CoA synthase and the LDL receptor) are similarly altered in the proximal intestinal mucosa of Cav1 null and wild-type mice following ezetimibe treatment. These results demonstrate that CAV1 is not required for cholesterol absorption or ezetimibe sensitivity in the mouse.
小窝蛋白-1(CAV1)是构成丝状衣被的结构蛋白,该衣被覆盖在每个小窝的细胞质表面。细胞培养研究表明,CAV1在细胞内胆固醇转运中发挥重要作用。此外,有报道称,CAV1在肠细胞中与膜联蛋白-2形成抗去污剂蛋白复合物,该复合物可被胆固醇吸收抑制剂依泽替米贝破坏,这表明CAV1在胆固醇吸收中可能发挥作用。在本报告中,我们评估了Cav1基因敲除小鼠的胆固醇稳态。CAV1的缺失并未导致肠道中CAV2或CAV3的代偿性增加。此外,Cav1基因敲除小鼠近端肠黏膜中膜联蛋白-2或假定的胆固醇转运蛋白尼曼-匹克C1样1蛋白(NPC1L1)的mRNA和蛋白水平正常。Cav1基因敲除小鼠及其野生型同窝小鼠的胆固醇吸收分数和粪便中性固醇排泄在统计学上相似。此外,口服依泽替米贝在降低Cav1基因敲除小鼠和野生型对照的胆固醇吸收方面同样有效。依泽替米贝治疗后,Cav1基因敲除小鼠和野生型小鼠近端肠黏膜中对细胞内胆固醇浓度敏感的基因(ATP结合盒转运蛋白ABCA1和ABCG5、羟甲基戊二酰辅酶A合酶和低密度脂蛋白受体)的mRNA表达水平发生了类似的变化。这些结果表明,小鼠的胆固醇吸收或对依泽替米贝的敏感性并不需要CAV1。