Comparative study of the membrane-permeabilizing activities of mastoparans and related histamine-releasing agents in bacteria, erythrocytes, and mast cells
Comparative study of the membrane-permeabilizing activities of mastoparans and related histamine-releasing agents in bacteria, erythrocytes, and mast cells
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DOI：
10.1016/j.bbamem.2010.10.007
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发表时间：
2011-01-01
影响因子：
3.4
通讯作者：
Katsu, Takashi
中科院分区：
文献类型：
--
作者：
Nakao, Satoshi;Komagoe, Keiko;Katsu, Takashi
通过测量细菌、红细胞和肥大细胞的K+流出量，比较了乳癖菌和相关组胺释放剂的膜透化活性。还研究了细菌细胞活力、溶血和组胺释放以及红细胞形状的变化。所测试的化合物是mastoparans（HR 1，来自Polistes jadwagae的mastoparan和来自Vespula lewisii的mastoparan）、granuliberin R、肥大细胞脱粒肽和化合物48/80，以及抗微生物肽，如magainin I、magainin II、短杆菌肽S。和蜂毒肽。我们使用K+选择性电极来测定细胞质膜对K+的渗透性的变化。与肥大细胞表面在组胺释放过程中带负电荷一致，由于磷脂酰丝氨酸易位到细胞质膜的外小叶，组胺释放剂诱导K+从肥大细胞流出，这取决于它们增加富含带负电荷磷脂的细菌细胞质膜的渗透性的能力。本研究结果表明，两亲性肽，具有组胺释放和抗微生物的能力，诱导不仅细菌，但肥大细胞的细胞质膜的透化。在较高浓度下，Mastoparans增加了人红细胞膜的渗透性，并将正常的盘状形状改变为锯齿状。使用化合物48/80及其组分（单体、二聚体和三聚体），系统地改变分子的阳离子电荷数，确定了制备锯齿状形式的结构要求。(C)2010爱思唯尔有限公司版权所有。
The membrane-permeabilizing activities of mastoparans and related histamine-releasing agents were compared through measurements of K+ efflux from bacteria, erythrocytes, and mast cells. Changes in bacterial cell viability, hemolysis, and histamine release, as well as in the shape of erythrocytes were also investigated. The compounds tested were mastoparans (HR1, a mastoparan from Polistes jadwagae, and a mastoparan from Vespula lewisii), granuliberin R, mast cell-degranulating peptide, and compound 48/80, as well as antimicrobial peptides, such as magainin I, magainin II, gramicidin S. and melittin. We used a K+-selective electrode to determine changes in the permeability to K+ of the cytoplasmic membranes of cells. Consistent with the surface of mast cells becoming negatively charged during histamine release, due to the translocation of phosphatidylserine to the outer leaflet of the cytoplasmic membrane, histamine-releasing agents induced K+ efflux from mast cells, dependent on their ability to increase the permeability of bacterial cytoplasmic membranes rich in negatively charged phospholipids. The present results demonstrated that amphiphilic peptides, possessing both histamine-releasing and antimicrobial capabilities, induced the permeabilization of the cytoplasmic membranes of not only bacteria but mast cells. Mastoparans increased the permeability of membranes in human erythrocytes at higher concentrations, and changed the normal discoid shape to a crenated form. The structural requirement for making the crenated form was determined using compound 48/80 and its constituents (monomer, dimer, and trimer), changing systematically the number of cationic charges of the molecules. (C) 2010 Elsevier B.V. All rights reserved.