Mechanism of action of habekacin, a novel amino acid-containing aminoglycoside antibiotic
Mechanism of action of habekacin, a novel amino acid-containing aminoglycoside antibiotic
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DOI：
10.1128/aac.24.5.797
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发表时间：
1983-11
影响因子：
4.9
通讯作者：
Nobuo Tanaka;Keita Matsunaga;Aiko Hirata;Yoko Matsuhisa;Toshio;Nishimura
中科院分区：
文献类型：
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作者：
Nobuo Tanaka;Keita Matsunaga;Aiko Hirata;Yoko Matsuhisa;Toshio;Nishimura
利用大肠杆菌Q-13对哈贝卡星活性的分子基础进行了研究。电子显微镜研究表明，经哈贝卡星处理的细胞上形成了大量来自外膜的气泡。胞浆内容物渗入滤过泡的腔内，部分增大的滤过泡的细胞膜被破坏。在无细胞系统中，哈贝卡星干扰多肽合成，导致密码子误读，并抑制核糖体上N-乙酰苯丙氨酰-tRNA从受体位置到供体位置的移位。[~3H]哈贝卡星与50S和30S核糖体亚基结合。目前的实验表明，哈贝卡星的作用机制与地贝卡星、卡那霉素、庆大霉素等含2-脱氧链胺的氨基糖苷类抗生素及有关物质相似。膜损伤与核糖体功能抑制的关系仍有待确定。
The molecular basis for activity of habekacin was studied by using Escherichia coli Q-13. Electron microscopic studies revealed that numerous blebs, derived from the outer membrane, were formed on cells treated with habekacin. Cytoplasmic contents leaked into the lumina of blebs, and the membrane of some enlarged blebs was disrupted. In a cell-free system, habekacin interfered with polypeptide synthesis, caused codon misreading, and inhibited translocation of N-acetylphenylalanyl-tRNA from the acceptor site to the donor site on ribosomes. [3H]habekacin bound to both 50S and 30S ribosomal subunits. The current experiments indicated that the mechanism of action of habekacin is similar to that of 2-deoxystreptamine-containing aminoglycoside antibiotics such as dibekacin, kanamycin, gentamicin, and related substances. The relationship of membrane damage to inhibition of ribosomal functions remains to be determined.