Champney W S, Tober C L, Burdine R
Department of Biochemistry and Molecular Biology, J.H. Quillen College of Medicine, East Tennessee State University, Johnson City, TN 37614, USA.
Curr Microbiol. 1998 Dec;37(6):412-7. doi: 10.1007/s002849900402.
Nine structurally similar macrolide antibiotics were tested at a concentration of 0.5 microg/ml for their relative inhibitory effects on ribosome functions in Staphylococcus aureus cells. Eight of the compounds examined inhibited protein synthesis at this concentration. Seven of the nine compounds were also effective in blocking formation of the 50S ribosomal subunit. Roxithromycin and 14-hydroxy clarithromycin inhibited protein synthesis to a greater extent than they affected 50S subunit formation. Conversely, the compound 11, 12-carbonate-3 deoxy-clarithromycin affected 50S assembly more than translation. Only clarithromycin had any effect on 30S ribosomal subunit assembly. The decline in growth rate and cell number was proportional to the effect on ribosome formation or function by each compound. These inhibitory activities can be related to structural differences between these macrolide antibiotics.
对九种结构相似的大环内酯类抗生素进行了测试，其浓度为0.5微克/毫升，以研究它们对金黄色葡萄球菌细胞核糖体功能的相对抑制作用。在所检测的化合物中，有八种在该浓度下抑制蛋白质合成。九种化合物中的七种在阻断50S核糖体亚基形成方面也有效。罗红霉素和14-羟基克拉霉素对蛋白质合成的抑制作用比对50S亚基形成的影响更大。相反，化合物11,12-碳酸酯-3-脱氧-克拉霉素对50S组装的影响大于对翻译的影响。只有克拉霉素对30S核糖体亚基组装有任何影响。生长速率和细胞数量的下降与每种化合物对核糖体形成或功能的影响成正比。这些抑制活性可能与这些大环内酯类抗生素之间的结构差异有关。
