Effect of cholesterol depletion on the pore dilation of TRPV1

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• 作者：Erik T Jansson (1)
  Carolina L Trkulja (1)
  Aikeremu Ahemaiti (1)
  Maria Millingen (1)
  Gavin DM Jeffries (1)
  Kent Jardemark (1) (2)
  Owe Orwar (1)
  
• 关键词：TRPV1 ; Cholesterol ; M尾CD ; Capsaicin ; Acidic pH ; YO ; PRO ; Ion ; permeability ; NMDG
• 刊名：Molecular Pain
• 出版年：2013
• 出版时间：December 2013
• 年：2013
• 卷：9
• 期：1
• 全文大小：406KB
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• 作者单位：Erik T Jansson (1)
  Carolina L Trkulja (1)
  Aikeremu Ahemaiti (1)
  Maria Millingen (1)
  Gavin DM Jeffries (1)
  Kent Jardemark (1) (2)
  Owe Orwar (1)
  
  1. Department of Chemical and Biological Engineering, Chalmers University of Technology, SE-412 96, G枚teborg, Sweden
  2. Department of Physiology and Pharmacology, Karolinska Institutet, SE-171 77, Stockholm, Sweden
  

文摘

The TRPV1 ion channel is expressed in nociceptors, where pharmacological modulation of its function may offer a means of alleviating pain and neurogenic inflammation processes in the human body. The aim of this study was to investigate the effects of cholesterol depletion of the cell on ion-permeability of the TRPV1 ion channel. The ion-permeability properties of TRPV1 were assessed using whole-cell patch-clamp and YO-PRO uptake rate studies on a Chinese hamster ovary (CHO) cell line expressing this ion channel. Prolonged capsaicin-induced activation of TRPV1 with N-methyl-D-glucamine (NMDG) as the sole extracellular cation, generated a biphasic current which included an initial outward current followed by an inward current. Similarly, prolonged proton-activation (pH 5.5) of TRPV1 under hypocalcemic conditions also generated a biphasic current including a fast initial current peak followed by a larger second one. Patch-clamp recordings of reversal potentials of TRPV1 revealed an increase of the ion-permeability for NMDG during prolonged activation of this ion channel under hypocalcemic conditions. Our findings show that cholesterol depletion inhibited both the second current, and the increase in ion-permeability of the TRPV1 channel, resulting from sustained agonist-activation with capsaicin and protons (pH 5.5). These results were confirmed with YO-PRO uptake rate studies using laser scanning confocal microscopy, where cholesterol depletion was found to decrease TRPV1 mediated uptake rates of YO-PRO. Hence, these results propose a novel mechanism by which cellular cholesterol depletion modulates the function of TRPV1, which may constitute a novel approach for treatment of neurogenic pain.