Pro的引入对抗菌肽活性的影响研究

Effect of Pro introduction on antimicrobial peptide activity

Pro由于不具有酰胺氢,不能形成链内氢键,因而会使多肽链中的α-螺旋中断,产生1个"结节",它是α-螺旋的破坏者。为了研究Pro对抗菌肽活性的影响,设计合成了1条具有25个氨基酸残基的抗菌肽AM-3,与之前设计合成的具有较好抗肿瘤活性和药物选择性的AM-4唯一不同是,N端第11位,AM-3是Pro,AM-4是Ahx。实验研究表明,AM-3的α-螺旋成分含量,体外抗肿瘤活性和溶血活性与AM-4没有明显的差异;通过荧光显微镜观察,AM-3同样具有快速高效的抗肿瘤活性,对正常细胞(NIH-3T3)的杀伤力低于肿瘤细胞(HEPG-2),说明AM-3也具有一定的选择性毒性。

Pro does not have amide hydrogen,can not form hydrogen bonds in the chain,so it will break the alpha-helix in the polypeptide chain,resulting in a "nodule",which is the destroyer of alpha-helix.In order to study the effect of Pro on antimicrobial peptide activity,an antimicrobial peptide AM-3 with 25 amino acid residues was designed and synthesized.The only difference between AM-3 and AM-4,which had better antitumor activity and drug selectivity,was that AM-3 was Pro,AM-4 was Ahx.The results showed that there was no significant difference between AM-3 and AM-4 in the content of alpha-helix components,anti-tumor activity and hemolytic activity in vitro;fluorescence microscopy showed that AM-3 also had rapid and effective anti-tumor activity,and its killing ability to normal cells(NIH-3T3)was lower than that of tumor cells(HEPG-2),indicating that AM-3 also had certain anti-tumor activity.Selective toxicity.