Synthetic mimic of antimicrobial peptide with nonmembrane-disrupting antibacterial properties.

Synthetic mimic of antimicrobial peptide with nonmembrane-disrupting antibacterial properties.
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DOI:
10.1021/bm800855t
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发表时间:
2008-11
期刊:
影响因子:
6.2
通讯作者:
Tew GN
Tew GN
中科院分区:
化学2区
文献类型:
--
作者:
Gabriel GJ;Madkour AE;Dabkowski JM;Nelson CF;Nüsslein K;Tew GN

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采用开环易位聚合法,以降冰片烯单体为原料合成了聚胍氧降冰片烯(PGON)。观察到该聚合物对革兰氏阴性和革兰氏阳性细菌具有强抗菌性,并且对人红细胞具有非溶血性。时间杀菌研究表明,这种聚合物是致命的,而不仅仅是抑菌的。与先前报道的SMAMP(抗菌肽的合成模拟物)形成鲜明对比,PGON在囊泡染料渗漏测定和显微镜实验中没有破坏膜。PGON的独特生物学性质,以类似于细胞穿透肽的相同方式,强烈鼓励检查其他新的含胍基的大分子作为强大的和选择性的抗微生物剂。
Polyguanidinium oxanorbornene (PGON) was synthesized from norbornene monomers via ring-opening metathesis polymerization. This polymer was observed to be strongly antibacterial against Gram-negative and Gram-positive bacteria as well as nonhemolytic against human red blood cells. Time-kill studies indicated that this polymer is lethal and not just bacteriostatic. In sharp contrast to previously reported SMAMPs (synthetic mimics of antimicrobial peptides), PGON did not disrupt membranes in vesicle-dye leakage assays and microscopy experiments. The unique biological properties of PGON, in same ways similar to cell-penetrating peptides, strongly encourage the examination of other novel guanidino containing macromolecules as powerful and selective antimicrobial agents.
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