MECHANISM OF POLYMYXIN-B-ACTION AND SELECTIVITY TOWARD BIOLOGIC MEMBRANES

MECHANISM OF POLYMYXIN-B-ACTION AND SELECTIVITY TOWARD BIOLOGIC MEMBRANES
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DOI:
10.1021/bi00735a014
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发表时间:
1973-01-01
期刊:
影响因子:
2.9
通讯作者:
FEINGOLD, DS
FEINGOLD, DS
中科院分区:
生物学3区
文献类型:
--
作者:
HSUCHEN, CC;FEINGOLD, DS

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Chuen-Chin HsuChen 和 David S. Feingold* 摘要:使用水悬浮液(脂质体)中的脂质小球作为模型系统,研究了多粘菌素抗生素的作用选择性;捕获的葡萄糖标记物的释放是膜损伤的指标。据观察,多粘菌素 B 诱导的葡萄糖释放是一个区分具有各种“极头”结构的磷脂的特定过程。由磷脂酰乙醇胺制备的脂质体对多粘菌素B极其敏感,而由N-甲基取代的类似物(N-甲基磷脂酰乙醇胺、MY-二甲基磷脂酰乙醇胺、磷脂酰胆碱)制备的脂质体对抗生素不敏感。磷脂酰乙醇胺的 N-甲基化类似物保护含有磷脂酰乙醇胺的脂质体免受多粘菌素 B 的影响。这种保护的效率是类似物摩尔百分比的函数
Chuen-Chin HsuChen and David S. Feingold* abstract: The selectivity of action of the polymyxin antibiotics was studied using lipid spherules in aqueous suspension (liposomes) as a model system; the release of trapped glucose marker was the index of membrane damage. The polymyxin B induced glucose release was observed to be a specific process which differentiates among phospholipids with various “polar head” structures. Liposomes prepared from phos-phatidylethanolamine were extremely sensitive to polymyxin B while none of those prepared from the VV-methyl-substituted analogs (jV-methylphosphatidylethanolamine, MY-dimethylphosphatidylethanolamine, phosphatidylcholine) were sensi-tive to the antibiotic. The N-methylated analogs of phosphatidylethanolamine protected phosphatidylethanolamine-containing liposomes from polymyxin B. The efficiency of this protection was a function of the molar percent of the analog