新型阳离子抗菌肽的脂肪链修饰及抗菌活性

发布时间：2018-05-06 08:40

本文选题：阳离子抗菌肽 + 固相合成　；参考：《中国医药工业杂志》2017年02期

【摘要】：本研究以抗菌肽XAMP2(1)为模板,在其序列的N端(第2位氨基酸)、中间部位(第6位氨基酸)和C端(第10位氨基酸)分别连接棕榈酸、月桂酸和正辛酸脂肪链,设计了9条具有新型结构的抗菌肽(2~10),用固相合成法合成,以反相高效液相色谱法分离纯化,并用微量肉汤稀释法测定抗菌活性。改造后得到的抗菌肽5的抗菌活性较1有所提高,其抗大肠杆菌和铜绿假单胞菌的活性均为2μg/ml,比1增强2倍;其抗耐药鲍曼不动杆菌的活性为2μg/ml,比1增强4倍。同时还探讨了脂肪链长度和修饰位点对抗菌活性的影响。
[Abstract]:In this study, the antibacterial peptide XAMP2 (1) was used as a template. At the N end of its sequence (second bit amino acid), the intermediate (sixth - bit amino acid) and the C end (Tenth - bit amino acid), respectively, palmitic acid, lauric acid and octanoic acid fat chain were used to design 9 new structure antibacterial peptides (2~10), which were synthesized by solid phase synthesis and separated by Reversed Phase High Performance Liquid Chromatography The antibacterial activity of the antibacterial peptide 5 was improved, the activity of anti Escherichia coli and Pseudomonas aeruginosa was 2 u g/ml and 2 times more than 1, and the activity of anti resistant Acinetobacter Bauman was 2 g/ml and 4 times higher than 1. Meanwhile, the length and modification of fat chain were also discussed. The effect of loci on antibacterial activity.

【作者单位】：中国医药工业研究总院上海医药工业研究院创新药物与制药工艺国家重点实验室;正大天晴药业集团股份有限公司;
【分类号】：R96

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