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新型陽(yáng)離子抗菌肽的脂肪鏈修飾及抗菌活性

發(fā)布時(shí)間:2018-05-06 08:40

  本文選題:陽(yáng)離子抗菌肽 + 固相合成。 參考:《中國(guó)醫(yī)藥工業(yè)雜志》2017年02期


【摘要】:本研究以抗菌肽XAMP2(1)為模板,在其序列的N端(第2位氨基酸)、中間部位(第6位氨基酸)和C端(第10位氨基酸)分別連接棕櫚酸、月桂酸和正辛酸脂肪鏈,設(shè)計(jì)了9條具有新型結(jié)構(gòu)的抗菌肽(2~10),用固相合成法合成,以反相高效液相色譜法分離純化,并用微量肉湯稀釋法測(cè)定抗菌活性。改造后得到的抗菌肽5的抗菌活性較1有所提高,其抗大腸桿菌和銅綠假單胞菌的活性均為2μg/ml,比1增強(qiáng)2倍;其抗耐藥鮑曼不動(dòng)桿菌的活性為2μg/ml,比1增強(qiáng)4倍。同時(shí)還探討了脂肪鏈長(zhǎng)度和修飾位點(diǎn)對(duì)抗菌活性的影響。
[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.

【作者單位】: 中國(guó)醫(yī)藥工業(yè)研究總院上海醫(yī)藥工業(yè)研究院創(chuàng)新藥物與制藥工藝國(guó)家重點(diǎn)實(shí)驗(yàn)室;正大天晴藥業(yè)集團(tuán)股份有限公司;
【分類(lèi)號(hào)】:R96

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