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目的:研究人格拉利素功能肽段一级结构与活性的关系。方法:依据确定的生物学活性,在人格拉利素功能肽段CM19的基础上,利用抗菌肽的特点及已知的抗菌肽构效关系研究结果对CM19进行氨基酸取代、缺失及随机排列设计合成5条肽段,通过试管法和平板法检测相应肽段的抗菌活性。结果:CM19氨基端第一个半胱氨酸在发挥抗菌作用中是必需的;阳性电荷数的增加或者分布不合适不改善抗菌活性;氨基酸的排列顺序明显降低抗菌活性;CM19羧基端7肽无明显的抗菌作用。CM12具有广谱抗菌作用,不但对非耐药菌而且对耐药菌具有同样的作用。结论:氨基酸的取代、缺失及排列对人格拉利素肽段的抗菌功能具有明显的影响。
Objective: To study the relationship between primary structure and activity of human prednisolone functional peptide. Methods: According to the determined biological activity, the amino acid substitutions, deletions and random arrangements of CM19 were designed and synthesized based on the characteristics of human placenta functional peptide CM19 and the known antibacterial peptide structure-activity relationship Five peptides were tested for the antimicrobial activity of the corresponding peptides by in vitro and in vitro methods. Results: The first cysteine at the amino terminal of CM19 was necessary to exert antibacterial effect. The increase or distribution of positive charge was not suitable to improve antibacterial activity. The order of amino acids significantly reduced the antibacterial activity. Obvious antibacterial effect. CM12 has a broad spectrum antibacterial effect, not only for non-resistant bacteria but also for resistant bacteria. CONCLUSION: The amino acid substitutions, deletions and alignments have a significant effect on the antibacterial function of human plasmicin.