Hamilton D Lee, Beall Craig, Jeromson Stewart, Chevtzoff Cyrille, Cuthbertson Daniel J, Ashford Michael L J
Division of Cardiovascular and Diabetes Medicine, Medical Research Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK,
J Physiol Sci. 2014 Jan;64(1):13-20. doi: 10.1007/s12576-013-0285-4. Epub 2013 Sep 17.
Knockout of Kv1.3 improves glucose homeostasis and confers resistance to obesity. Additionally, Kv1.3 inhibition enhances glucose uptake. This is thought to occur through calcium release. Kv1.3 inhibition in T-lymphocytes alters mitochondrial membrane potential, and, as many agents that induce Ca(2+) release or inhibit mitochondrial function activate AMPK, we hypothesised that Kv1.3 inhibition would activate AMPK and increase glucose uptake. We screened cultured muscle with a range of Kv1.3 inhibitors for their ability to alter glucose uptake. Only Psora4 increased glucose uptake in C2C12 myotubes. None of the inhibitors had any impact on L6 myotubes. Magratoxin activated AMPK in C2C12 myotubes and only Pap1 activated AMPK in the SOL. Kv1.3 inhibitors did not alter cellular respiration, indicating a lack of effect on mitochondrial function. In conclusion, AMPK does not mediate the effects of Kv1.3 inhibitors and they display differential effects in different skeletal muscle cell lines without impairing mitochondrial function.
敲除Kv1.3可改善葡萄糖稳态并赋予抗肥胖能力。此外,抑制Kv1.3可增强葡萄糖摄取。这被认为是通过钙释放发生的。T淋巴细胞中Kv1.3的抑制会改变线粒体膜电位,并且由于许多诱导Ca(2+)释放或抑制线粒体功能的药物会激活AMPK,我们推测抑制Kv1.3会激活AMPK并增加葡萄糖摄取。我们用一系列Kv1.3抑制剂筛选培养的肌肉,以检测它们改变葡萄糖摄取的能力。只有Psora4增加了C2C12肌管中的葡萄糖摄取。这些抑制剂对L6肌管均无任何影响。马格拉毒素在C2C12肌管中激活了AMPK,只有Pap1在比目鱼肌中激活了AMPK。Kv1.3抑制剂未改变细胞呼吸,表明对线粒体功能没有影响。总之,AMPK不介导Kv1.3抑制剂的作用,它们在不同的骨骼肌细胞系中表现出不同的作用,且不损害线粒体功能。