Kimura K, Ikeda Y, Kagami S, Yoshihama M, Suzuki K, Osada H, Isono K
Research Institute of Life Science, Snow Brand Milk Products Co., Ltd., Tochigi, Japan.
J Antibiot (Tokyo). 1998 Dec;51(12):1099-104. doi: 10.7164/antibiotics.51.1099.
We examined the inhibitory activity against bacterial peptidoglycan biosynthesis, mammalian glycoprotein biosynthesis and growth of BALB/3T3 cells of four different types of liposidomycins which have the structure with or without sulfate and/or 3-methylglutaric acid moieties. Liposidomycins inhibited peptidoglycan biosynthesis about 30 to 500 times more effectively than tunicamycin, whereas liposidomycins inhibited mammalian glycoprotein biosynthesis about 30 to 300 times less effectively than tunicamycin. When the cytotoxic effect of liposidomycins and tunicamycin on the growth of mammalian cells were compared, liposidomycins did not show toxicity against BALB/3T3 cell at 25 microg/ml, though tunicamycin inhibited cell growth by 50% at 0.05 microg/ml. On the basis of these results, it is concluded that liposidomycins are selective antibiotics showing highly specific inhibition toward bacterial peptidoglycan biosynthesis.
我们研究了四种不同类型的脂霉素对细菌肽聚糖生物合成、哺乳动物糖蛋白生物合成以及BALB/3T3细胞生长的抑制活性，这些脂霉素具有含或不含硫酸根和/或3-甲基戊二酸部分的结构。脂霉素抑制肽聚糖生物合成的效率比衣霉素高约30至500倍，而脂霉素抑制哺乳动物糖蛋白生物合成的效率比衣霉素低约30至300倍。当比较脂霉素和衣霉素对哺乳动物细胞生长的细胞毒性作用时，脂霉素在25微克/毫升时对BALB/3T3细胞没有毒性，而衣霉素在0.05微克/毫升时可抑制细胞生长50%。基于这些结果，可以得出结论，脂霉素是对细菌肽聚糖生物合成具有高度特异性抑制作用的选择性抗生素。
