Department of Early Diagnosis of Arthritis, Institute of Rheumatology, Spartanska 1, 02-627 Warsaw, Poland.
Mediators Inflamm. 2012;2012:636157. doi: 10.1155/2012/636157. Epub 2012 Aug 21.
Macrolides are a group of antibiotics with a distinctive macrocyclic lactone ring combined with sugars (cladinose, desosamine). The action of macrolides is to block protein synthesis by binding to the subunit of 50S ribosome of bacteria. Prototype macrolide was erythromycin, which came into clinical practice in the 50s of the 20th century. Its antimicrobial spectrum covers the scope of the penicillins but is extended to the impact of atypical bacteria. In the 90 s more drugs of this group were synthesized-they have less severe side effects than erythromycin, extended spectrum of Gram-negative bacteria. Macrolides are effective in treating mycobacterial infections especially in patients infected with HIV. It is now known that in addition to antibacterial abilities, macrolides have immunomodulatory effects-they inhibit the production of proinflammatory cytokines (TNF, IL1, 6, and 8) affect transcription factors (NF-κB) as well as costimulaton (CD 80) and adhesion molecules (ICAM). This review article focused not only on the their antimicrobial abilities but also on efficacy in the treatment of several inflammatory disorders independent of the infectious agent. Their wider use as immunomodulators requires further study, which can lead to an extension of indications for their administration.
大环内酯类是一组具有独特大环内酯环与糖(克拉定糖、去氧氨基糖)结合的抗生素。大环内酯类的作用是通过与细菌 50S 核糖体亚基结合来阻断蛋白质合成。第一代大环内酯类药物是红霉素,于 20 世纪 50 年代进入临床实践。其抗菌谱涵盖了青霉素的范围,但扩展到了非典型细菌的影响。90 年代合成了更多此类药物——它们比红霉素的副作用更小,对革兰氏阴性菌的谱更广。大环内酯类药物在治疗分枝杆菌感染方面非常有效,特别是在感染 HIV 的患者中。现在已知,除了抗菌能力外,大环内酯类还具有免疫调节作用——它们抑制促炎细胞因子(TNF、IL1、6 和 8)的产生,影响转录因子(NF-κB)以及共刺激(CD80)和粘附分子(ICAM)。这篇综述文章不仅关注它们的抗菌能力,还关注它们在治疗几种独立于感染因子的炎症性疾病方面的疗效。它们作为免疫调节剂的更广泛应用需要进一步研究,这可能会扩大其给药适应症。