Fournet M P, Barre J, Zini R, Deforges L, Duval J, Tillement J P
J Pharm Pharmacol. 1987 Apr;39(4):319-22. doi: 10.1111/j.2042-7158.1987.tb06278.x.
Parameters of erythromycin binding to Staphylococcus aureus were measured in-vitro using an equilibrium method with [3H]erythromycin. The dissociation constant of the complex, erythromycin-S. aureus sensitive strain, was KD = 0.11 microM. The maximal binding, representing the density of binding sites was 14,847 molecules/cell. No binding was detectable on the constitutive resistant strain. Macrolides, streptogramins and lincosamides displaced bound [3H]erythromycin by a competitive process indicating that these compounds share common binding sites on the bacteria, i.e. 50 S ribosomal subunits. A good correlation (r = 0.99) was demonstrated between the corresponding inhibition constants (Ki) and the minimal inhibitory concentration. It is proposed that knowledge of the binding parameters provides a good indication of bacterial susceptibility and may serve as a useful adjunct in developing new compounds.
采用[3H]红霉素平衡法在体外测定红霉素与金黄色葡萄球菌结合的参数。复合物（红霉素-金黄色葡萄球菌敏感菌株）的解离常数KD = 0.11微摩尔。代表结合位点密度的最大结合量为14,847个分子/细胞。在组成型耐药菌株上未检测到结合。大环内酯类、链阳菌素类和林可酰胺类通过竞争过程取代结合的[3H]红霉素，表明这些化合物在细菌上共享共同的结合位点，即50 S核糖体亚基。相应的抑制常数（Ki）与最低抑菌浓度之间显示出良好的相关性（r = 0.99）。有人提出，结合参数的知识可为细菌敏感性提供良好指示，并可能在开发新化合物时作为有用的辅助手段。
