Roche Y, Gougerot-Pocidalo M A, Fay M, Forest N, Pocidalo J J
J Antimicrob Chemother. 1986 Feb;17(2):195-203. doi: 10.1093/jac/17.2.195.
Macrolides are actively concentrated by leucocytes. The dose-effect responses of spiramycin (Sp) and erythromycin (Er) on phytohaemagglutinin (PHA) and pokeweed mitogen (PWM) stimulated human mononuclear leucocytes (MNL) were studied. Cell viability was not altered at any antibiotic concentration (1-100 mg/l). Both Sp and Er showed dose-related inhibition of the proliferative response of PHA and PWM stimulated MNL. Very marked effects were observed at high antibiotic concentrations and the effects observed at low concentrations (1-10), although small, were also significant. Similar results were observed for the mitogen PWM. A decrease in tritiated thymidine (3H-TdR) incorporation occurred only if Sp and Er were added during the first 8 h of culture. Sp and Er also induced a decrease in tritiated uridine (3H-UdR) uptake. These data suggest that Sp and Er interfered with an early event in the cell cycle. However Sp did not affect PHA binding to MNL. The clinical significance of these findings is discussed.
大环内酯类药物可被白细胞主动摄取。研究了螺旋霉素(Sp)和红霉素(Er)对植物血凝素(PHA)和商陆有丝分裂原(PWM)刺激的人单核白细胞(MNL)的剂量效应反应。在任何抗生素浓度(1-100mg/l)下,细胞活力均未改变。Sp和Er均显示出对PHA和PWM刺激的MNL增殖反应的剂量依赖性抑制。在高抗生素浓度下观察到非常显著的效应,而在低浓度(1-10)下观察到的效应虽然较小,但也具有显著性。对于有丝分裂原PWM也观察到了类似结果。仅当在培养的前8小时内加入Sp和Er时,才会出现氚标记胸腺嘧啶核苷(3H-TdR)掺入减少的情况。Sp和Er还导致氚标记尿苷(3H-UdR)摄取减少。这些数据表明Sp和Er干扰了细胞周期中的早期事件。然而,Sp并不影响PHA与MNL的结合。讨论了这些发现的临床意义。