Center for Cancer Research Nanobiology Program, National Cancer Institute-Frederick, SAIC-Frederick, Frederick, Maryland, USA.
Biophys J. 2011 Apr 6;100(7):1775-83. doi: 10.1016/j.bpj.2011.01.072.
Protegrin-1 (PG-1) is an 18 residues long, cysteine-rich β-sheet antimicrobial peptide (AMP). PG-1 induces strong cytotoxic activities on cell membrane and acts as a potent antibiotic agent. Earlier we reported that its cytotoxicity is mediated by its channel-forming ability. In this study, we have examined the amyloidogenic fibril formation properties of PG-1 in comparison with a well-defined amyloid, the amyloid-β (Aβ(1-42)) peptide. We have used atomic force microscopy (AFM) and thioflavin-T staining to investigate the kinetics of PG-1 fibrils growth and molecular dynamics simulations to elucidate the underlying mechanism. AFM images of PG-1 on a highly hydrophilic surface (mica) show fibrils with morphological similarities to Aβ(1-42) fibrils. Real-time AFM imaging of fibril growth suggests that PG-1 fibril growth follows a relatively fast kinetics compared to the Aβ(1-42) fibrils. The AFM results are in close agreement with results from thioflavin-T staining data. Furthermore, the results indicate that PG-1 forms fibrils in solution. Significantly, in contrast, we do not detect fibrillar structures of PG-1 on an anionic lipid bilayer 2-dioleoyl-sn-glycero-3-phospho-L-serine/1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine; only small PG-1 oligomers can be observed. Molecular dynamics simulations are able to identify the presence of these small oligomers on the membrane bilayer. Thus, our current results show that cytotoxic AMP PG-1 is amyloidogenic and capable of forming fibrils. Overall, comparing β-rich AMPs and amyloids such as Aβ, in addition to cytotoxicity and amyloidogenicity, they share a common structural motif, and are channel forming. These combined properties support a functional relationship between amyloidogenic peptides and β-sheet-rich cytolytic AMPs, suggesting that amyloids channels may have an antimicrobial function.
防御素-1(PG-1)是一种 18 个氨基酸长的富含半胱氨酸的β-折叠抗菌肽(AMP)。PG-1 对细胞膜具有强烈的细胞毒性作用,并具有很强的抗生素作用。我们之前报道过,其细胞毒性是通过其形成通道的能力介导的。在这项研究中,我们比较了 PG-1 的淀粉样纤维形成特性与一种明确的淀粉样蛋白,即淀粉样β(Aβ(1-42))肽。我们使用原子力显微镜(AFM)和噻唑蓝 T 染色来研究 PG-1 纤维生长的动力学,并进行分子动力学模拟以阐明潜在的机制。PG-1 在高亲水性表面(云母)上的 AFM 图像显示出与 Aβ(1-42)纤维相似的形态纤维。实时 AFM 成像表明,PG-1 纤维的生长动力学相对较快,与 Aβ(1-42)纤维相比。AFM 结果与噻唑蓝 T 染色数据非常吻合。此外,结果表明 PG-1 在溶液中形成纤维。值得注意的是,相比之下,我们在阴离子脂质双层 2-二油酰基-sn-甘油-3-磷酸-L-丝氨酸/1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸乙醇胺上没有检测到 PG-1 的纤维状结构;只能观察到 PG-1 的小寡聚物。分子动力学模拟能够识别这些小寡聚物在膜双层上的存在。因此,我们目前的结果表明,细胞毒性 AMP PG-1 具有淀粉样特性,能够形成纤维。总的来说,除了细胞毒性和淀粉样特性外,与富含β的 AMP 和淀粉样蛋白如 Aβ 相比,它们还具有共同的结构基序,并且是形成通道的。这些综合特性支持了淀粉样肽和富含β-折叠的细胞毒性 AMP 之间的功能关系,表明淀粉样通道可能具有抗菌功能。