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Correlation between the secondary structure and surface activity of β-sheet forming cationic amphiphilic peptides and their anticancer activity

化学 两亲性 圆二色性 细胞毒性 癌细胞 赫拉 蛋白质二级结构 生物化学 立体化学 癌症 体外 生物 有机化学 遗传学 聚合物 共聚物
作者
Roja Hadianamrei,Mhd Anas Tomeh,Stephen Brown,Jiqian Wang,Xiubo Zhao
出处
期刊:Colloids and Surfaces B: Biointerfaces [Elsevier]
卷期号:209: 112165-112165 被引量:17
标识
DOI:10.1016/j.colsurfb.2021.112165
摘要

Cancer is one of the main causes of death worldwide. The current cancer treatment strategies often lack selectivity for cancer cells resulting in dose-limiting adverse effects and reduced quality of life. Recently, anticancer peptides (ACPs) have emerged as an alternative treatment with higher selectivity, less adverse effects, and lower propensity for drug resistance. However, most of the current studies on the ACPs are focused on α-helical ACPs and there is lack of systematic studies on β-sheet forming ACPs. Herein we report the development of a new series of rationally designed short cationic amphiphilic β-sheet forming ACPs and their structure activity relationship. The peptides had the general formula (XY1XY2)3, with X representing hydrophobic amino acids (isoleucine (I) or leucine (L)), Y1 and Y2 representing cationic amino acids (arginine (R) or lysine (K)). The cytotoxicity of the designed ACPs in HCT 116 colorectal cancer, HeLa cervical cancer and human dermal fibroblast (HDF) cells was assessed by MTT test. The physicochemical properties of the peptides were characterized by various techniques including RP-HPLC, LC-MS, and Circular Dichroism (CD) spectroscopy. The surface activity of the peptides at the air-water interface and their interaction with the lipid monolayers as models for cell membranes were studied by Langmuir trough. The peptides consisting of I with R and K had selective anticancer activity while the combination of L and R diminished the anticancer activity of the peptides but rendered them more toxic to HDFs. The anticancer activity of the peptides was directed by their surface activity (amphiphilicity) and their secondary structure in hydrophobic surfaces including cancer cell membranes. The selectivity of the peptides for cancer cells was a result of their higher penetration into cancer cell membranes compared to normal cell membranes. The peptides exerted their anticancer activity by disrupting the mitochondrial membranes and eventually apoptosis. The results presented in this study provide an insight into the structure-activity relationship of this class of ACPs which can be employed as guidance to design new ACPs with improved anticancer activity and lower toxicity against normal cells.
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