Limwongyut Jakkarin, Liu Yang, Chilambi Gayatri Shankar, Seviour Thomas, Hinks Jamie, Mu Yuguang, Bazan Guillermo C
Center for Polymers and Organic Solids, Department of Chemistry and Biochemistry, University of California Santa Barbara CA 93106 USA
School of Biological Sciences, Nanyang Technological University 637551 Singapore.
RSC Adv. 2018 Nov 29;8(70):39849-39853. doi: 10.1039/c8ra08069k. eCollection 2018 Nov 28.
A three-dimensional conjugated oligoelectrolyte (COE) bearing a [2.2]paracyclophane unit (COE2-3-pCp) was synthesized. Its biological activity was determined both and within the context of membrane perturbation and biocompatibility. Molecular dynamics simulations indicate that, compared to its linear analog (COE2-3C), COE2-3-pCp introduces more lipid disorder with higher extent of membrane thinning. COE2-3-pCp also exhibits a higher MIC towards K12 and yeast, while maintaining similar levels of membrane permeabilization. These findings suggest a new design of COEs as biocompatible cell permeabilizers.
合成了一种带有[2.2]对环芳烷单元的三维共轭寡电解质(COE)(COE2-3-pCp)。在膜扰动和生物相容性的背景下测定了其生物活性。分子动力学模拟表明,与其线性类似物(COE2-3C)相比,COE2-3-pCp引入了更多的脂质无序,膜变薄程度更高。COE2-3-pCp对K12和酵母也表现出更高的最低抑菌浓度,同时保持相似水平的膜通透性。这些发现表明了一种作为生物相容性细胞通透剂的COE新设计。