Unité de Génie Enzymatique et Cellulaire UMR 7025 CNRS, Université de Picardie Jules Verne, Amiens, 80039, France.
Unité de Génie Enzymatique et Cellulaire UMR 7025 CNRS, Université de Picardie Jules Verne, Amiens, 80039, France.
Arch Biochem Biophys. 2022 Jan 15;715:109095. doi: 10.1016/j.abb.2021.109095. Epub 2021 Nov 24.
As Cecropin XJ, Cecropin A from Bombyx mori is one of the very few antimicrobial peptides having shown activity against esophageal cancer cells. It displays remarkable sequence-similarity to Cecropin XJ but slightly enhanced activity. In this work we show by NMR that both peptides are unstructured in solution but get structured in the presence of DPC micelles, mimicking the surface of biological membranes. In order to get insight into the molecular basis of its anticancer, antimicrobial and antifungal activity, we have investigated by MD simulations their interaction with a large variety of lipid bilayers mimicking cancer, mitochondrial, bacterial and fungal membranes. At variance with CecXJ, organized in two main helices, CecA tends to form a three helix bundle resulting in enhanced adaptability to its membrane targets. A specificity for the headgroup of phosphatidylserine and affinity for phosphatidylglycerol and cardiolipin may account for its selective targeting of cancer, bacterial and mitochondrial membranes, respectively.
作为 Cecropin XJ,家蚕的 Cecropin A 是少数几种对食管癌细胞具有活性的抗菌肽之一。它与 Cecropin XJ 显示出显著的序列相似性,但活性略有增强。在这项工作中,我们通过 NMR 表明,这两种肽在溶液中均无结构,但在 DPC 胶束存在下形成结构,模拟生物膜的表面。为了深入了解其抗癌、抗菌和抗真菌活性的分子基础,我们通过 MD 模拟研究了它们与各种模拟癌症、线粒体、细菌和真菌膜的脂质双层的相互作用。与组织成两个主要螺旋的 CecXJ 不同,CecA 倾向于形成三螺旋束,从而增强了对其膜靶标的适应性。对磷脂酰丝氨酸头部基团的特异性以及对磷脂酰甘油和心磷脂的亲和力可能分别解释了其对癌症、细菌和线粒体膜的选择性靶向。