Di Giambattista M, Vannuffel P, Sunazuka T, Jacob T, Omura S, Cocito C
J Antimicrob Chemother. 1986 Sep;18(3):307-15. doi: 10.1093/jac/18.3.307.
The affinity of ribosomes for VS (virginiamycin S, a type B synergimycin) is known to be increased by VM (virginiamycin M, a type A synergimycin). Erythromycin, a macrolide, displaces ribosome-bound VS in the absence of VM, but is ineffective in its presence. In the present work, the ability of spiramycin and tylosin (macrolide subgroups) derivatives to displace ribosome-bound VS, in the presence and in the absence of VM, has been explored. All macrolides with in-vitro activity displaced ribosome-bound VS: the displacement curves produced by tylosin and spiramycin derivatives virtually overlapped. When VM was added to these systems, displaced VS became readily attached to ribosomes in the case of erythromycin, did not bind appreciably within 20 min incubation in the presence of tylosin, and underwent a slow binding in the case of an N-substituted tylosin. The 16-membered macrolides (leucomycin, spiramycin and tylosin subgroups) can therefore be distinguished from the 14-membered macrolides (erythromycin subgroup) by the antagonistic effect displayed toward VM.
已知核糖体对维吉尼亚霉素S（一种B型协同霉素）的亲和力会因维吉尼亚霉素M（一种A型协同霉素）而增强。大环内酯类抗生素红霉素在不存在维吉尼亚霉素M的情况下可取代与核糖体结合的维吉尼亚霉素S，但在其存在时则无效。在本研究中，已探究了螺旋霉素和泰乐菌素（大环内酯类亚组）衍生物在存在和不存在维吉尼亚霉素M的情况下取代与核糖体结合的维吉尼亚霉素S的能力。所有具有体外活性的大环内酯类抗生素都能取代与核糖体结合的维吉尼亚霉素S：泰乐菌素和螺旋霉素衍生物产生的取代曲线几乎重叠。当将维吉尼亚霉素M添加到这些体系中时，在红霉素的情况下，被取代的维吉尼亚霉素S很容易重新附着到核糖体上；在泰乐菌素存在的情况下，在20分钟的孵育时间内不会明显结合；而在N-取代泰乐菌素的情况下会发生缓慢结合。因此，16元大环内酯类抗生素（柱晶白霉素、螺旋霉素和泰乐菌素亚组）可通过对维吉尼亚霉素M表现出的拮抗作用与14元大环内酯类抗生素（红霉素亚组）区分开来。
