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一种天然存在的八肽的pH值和浓度依赖性超分子自组装

pH- and concentration-dependent supramolecular self-assembly of a naturally occurring octapeptide.

作者信息

Ghosh Goutam, Fernández Gustavo

机构信息

Organisch-Chemisches Institut, Westfälische Wilhelms-Universität Münster, Correnstraße 40, 48149 Münster, Germany.

出版信息

Beilstein J Org Chem. 2020 Aug 17;16:2017-2025. doi: 10.3762/bjoc.16.168. eCollection 2020.

Abstract

Peptide-based biopolymers represent highly promising biocompatible materials with multiple applications, such as tailored drug delivery, tissue engineering and regeneration, and as stimuli-responsive materials. Herein, we report the pH- and concentration-dependent self-assembly and conformational transformation of the newly synthesized octapeptide PEP-1. At pH 7.4, PEP-1 forms β-sheet-rich secondary structures into fractal-like morphologies, as verified by circular dichroism (CD), Fourier-transform infrared (FTIR) spectroscopy, thioflavin T (ThT) fluorescence spectroscopy assay, and atomic force microscopy (AFM). Upon changing the pH value (using pH 5.5 and 13.0), PEP-1 forms different types of secondary structures and resulting morphologies due to electrostatic repulsion between charged amino acids. PEP-1 can also form helical or random-coil secondary structures at a relatively low concentration. The obtained pH-sensitive self-assembly behavior of the target octapeptide is expected to contribute to the development of novel drug nanocarrier assemblies.

摘要

基于肽的生物聚合物是极具前景的生物相容性材料,具有多种应用,如定制药物递送、组织工程与再生以及作为刺激响应材料。在此,我们报告了新合成的八肽PEP-1的pH和浓度依赖性自组装及构象转变。在pH 7.4时,PEP-1形成富含β-折叠的二级结构,呈分形样形态,这通过圆二色性(CD)、傅里叶变换红外(FTIR)光谱、硫黄素T(ThT)荧光光谱分析和原子力显微镜(AFM)得到验证。改变pH值(使用pH 5.5和13.0)时,由于带电氨基酸之间的静电排斥作用,PEP-1形成不同类型的二级结构及相应形态。在相对较低浓度下,PEP-1也能形成螺旋或无规卷曲二级结构。目标八肽所呈现的pH敏感自组装行为有望推动新型药物纳米载体组装体的发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3a/7445398/c8c66d3f0f6f/Beilstein_J_Org_Chem-16-2017-g006.jpg

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