Department of Ophthalmology & Visual Sciences, University of Wisconsin, Madison, Wisconsin 53706, USA.
Antimicrob Agents Chemother. 2010 Oct;54(10):4275-89. doi: 10.1128/AAC.00495-10. Epub 2010 Jul 19.
The linear cationic amphiphilic EB peptide, derived from the FGF4 signal sequence, was previously shown to be virucidal and to block herpes simplex type I (HSV-1) entry (H. Bultmann, J. S. Busse, and C. R. Brandt, J. Virol. 75:2634-2645, 2001). Here we show that cells treated with EB (RRKKAAVALLPAVLLALLAP) for less than 5 min are also protected from infection with HSV-1. Though protection was lost over a period of 5 to 8 h, it was reinduced as rapidly as during the initial treatment. Below a 20 μM concentration of EB, cells gained protection in a serum-dependent manner, requiring bovine serum albumin (BSA) as a cofactor. Above 40 μM, EB coprecipitated with BSA under hypotonic conditions. Coprecipitates retained antiviral activity and released active peptide. NaCl (≥0.3 M) blocked coprecipitation without interfering with antiviral activity. As shown for β-galactosidase, EB below 20 μM acted as an enzyme inhibitor, whereas above 40 to 100 μM EB, β-galactosidase was precipitated as was BSA or other unrelated proteins. Pyrene fluorescence spectroscopy revealed that in the course of protein aggregation, EB acted like a cationic surfactant and self associated in a process resembling micelle formation. Both antiviral activity and protein aggregation did not depend on stereospecific EB interactions but depended strongly on the sequence of the peptide's hydrophobic tail. EB resembles natural antimicrobial peptides, such as melittin, but when acting in a nonspecific detergent-like manner, it primarily seems to target proteins.
线性阳离子两亲性 EB 肽来源于 FGF4 信号序列,先前已被证明具有抗病毒活性,并能阻止单纯疱疹 I 型(HSV-1)进入(H. Bultmann、J. S. Busse 和 C. R. Brandt,J. Virol. 75:2634-2645,2001)。在这里,我们表明,用 EB(RRKKAAVALLPAVLLALLAP)处理少于 5 分钟的细胞也能免受 HSV-1 感染。尽管保护作用在 5 至 8 小时内丧失,但它的重新诱导速度与初始处理一样快。在低于 20 μM 的 EB 浓度下,细胞以依赖血清的方式获得保护,需要牛血清白蛋白(BSA)作为辅助因子。在 40 μM 以上,EB 在低渗条件下与 BSA 共沉淀。共沉淀物保留抗病毒活性并释放活性肽。NaCl(≥0.3 M)阻断共沉淀而不干扰抗病毒活性。如β-半乳糖苷酶所示,低于 20 μM 的 EB 作为酶抑制剂起作用,而高于 40 至 100 μM 的 EB,β-半乳糖苷酶与 BSA 或其他不相关的蛋白质一起沉淀。芘荧光光谱显示,在蛋白质聚集过程中,EB 像阳离子表面活性剂一样起作用,并以类似于胶束形成的过程进行自缔合。抗病毒活性和蛋白质聚集都不依赖于 EB 相互作用的立体特异性,而是强烈依赖于肽疏水性尾部的序列。EB 类似于天然抗菌肽,如蜂毒素,但当以非特异性去污剂样方式起作用时,它主要似乎针对蛋白质。