Capsaicin Fluidifies the Membrane and Localizes Itself near the Lipid鈥揥ater Interface

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• 作者：Alejandro Torrecillas ; Monika Schneider ; Ana M. Fern谩ndez-Mart铆nez ; Alessio Ausili ; Ana M. de Godos ; Senena Corbal谩n-Garc铆a ; Juan C. G贸mez-Fern谩ndez
• 刊名：ACS Chemical Neuroscience
• 出版年：2015
• 出版时间：October 21, 2015
• 年：2015
• 卷：6
• 期：10
• 页码：1741-1750
• 全文大小：564K
• ISSN：1948-7193

文摘

Capsaicin is the chemical responsible for making some peppers spicy hot, but additionally it is used as a pharmaceutical to alleviate different pain conditions. Capsaicin binds to the vanilloid receptor TRPV1, which plays a role in coordinating chemical and physical painful stimuli. A number of reports have also shown that capsaicin inserts in membranes and its capacity to modify them may be part of its molecular mode of action, affecting the activity of other membrane proteins. We have used differential scanning calorimetry, X-ray diffraction, ³¹P NMR, and ²H NMR spectroscopy to show that capsaicin increases the fluidity and disorder of 1,2-palmitoyl-sn-glycero-3-phosphocholine membrane models. By using ¹H NOESY MAS NMR based on proton鈥損roton cross-peaks between capsaicin and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine resonances, we determined the location profile of this molecule in a fluid membrane concluding that it occupies the upper part of the phospholipid monolayer, between the lipid鈥搘ater interface and the double bond of the acyl chain in position sn-2. This location explains the disorganization of the membrane of both the lipid鈥搘ater interface and the hydrophobic palisade.