McHenry Austin J, Sciacca Michele F M, Brender Jeffrey R, Ramamoorthy Ayyalusamy
Biophysics and Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109-1055, USA.
Biochim Biophys Acta. 2012 Dec;1818(12):3019-24. doi: 10.1016/j.bbamem.2012.07.021. Epub 2012 Aug 1.
The activity of antimicrobial peptides has been shown to depend on the composition of the target cell membrane. The bacterial selectivity of most antimicrobial peptides has been attributed to the presence of abundant acidic phospholipids and the absence of cholesterol in bacterial membranes. The high amount of cholesterol present in eukaryotic cell membranes is thought to prevent peptide-induced membrane disruption by increasing the cohesion and stiffness of the lipid bilayer membrane. While the role of cholesterol on an antimicrobial peptide-induced membrane disrupting activity has been reported for simple, homogeneous lipid bilayer systems, it is not well understood for complex, heterogeneous lipid bilayers exhibiting phase separation (or "lipid rafts"). In this study, we show that cholesterol does not inhibit the disruption of raft-containing 1,2-dioleoyl-sn-glycero-3-phosphocholine:1,2-dipalmitoyol-sn-glycero-3-phosphocholine model membranes by four different cationic antimicrobial peptides, MSI-78, MSI-594, MSI-367 and MSI-843 which permeabilize membranes. Conversely, the presence of cholesterol effectively inhibits the disruption of non-raft containing 1,2-dioleoyl-sn-glycero-3-phosphocholine or 1,2-dipalmitoyol-sn-glycero-3-phosphocholine lipid bilayers, even for antimicrobial peptides that do not show a clear preference between the ordered gel and disordered liquid-crystalline phases. Our results show that the peptide selectivity is not only dependent on the lipid phase but also on the presence of phase separation in heterogeneous lipid systems.
抗菌肽的活性已被证明取决于靶细胞膜的组成。大多数抗菌肽的细菌选择性归因于细菌膜中存在丰富的酸性磷脂且缺乏胆固醇。真核细胞膜中存在的大量胆固醇被认为通过增加脂质双层膜的内聚力和硬度来防止肽诱导的膜破坏。虽然对于简单、均匀的脂质双层系统,胆固醇对抗菌肽诱导的膜破坏活性的作用已有报道,但对于表现出相分离(或“脂筏”)的复杂、异质脂质双层,人们对此还了解甚少。在本研究中,我们发现胆固醇并不抑制含脂筏的1,2 - 二油酰 - sn - 甘油 - 3 - 磷酸胆碱:1,2 - 二棕榈酰 - sn - 甘油 - 3 - 磷酸胆碱模型膜被四种不同的阳离子抗菌肽(MSI - 78、MSI - 594、MSI - 367和MSI - 843)破坏,这些抗菌肽可使膜通透。相反,胆固醇的存在有效地抑制了不含脂筏的1,2 - 二油酰 - sn - 甘油 - 3 - 磷酸胆碱或1,2 - 二棕榈酰 - sn - 甘油 - 3 - 磷酸胆碱脂质双层的破坏,即使对于在有序凝胶相和无序液晶相之间没有明显偏好的抗菌肽也是如此。我们的结果表明,肽的选择性不仅取决于脂质相,还取决于异质脂质系统中相分离的存在。