Diabetes Center, First Department of Propaedeutic Internal Medicine, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, 11527 Athens, Greece.
Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, 11527 Athens, Greece.
Biomolecules. 2024 Jun 30;14(7):783. doi: 10.3390/biom14070783.
Tetracyclines constitute a unique class of antibiotic agents, widely prescribed for both community and hospital infections due to their broad spectrum of activity. Acting by disrupting protein synthesis through tight binding to the 30S ribosomal subunit, their interference is typically reversible, rendering them bacteriostatic in action. Resistance to tetracyclines has primarily been associated with changes in pump efflux or ribosomal protection mechanisms. To address this challenge, tetracycline molecules have been chemically modified, resulting in the development of third-generation tetracyclines. These novel tetracyclines offer significant advantages in treating infections, whether used alone or in combination therapies, especially in hospital settings. Beyond their conventional antimicrobial properties, research has highlighted their potential non-antibiotic properties, including their impact on immunomodulation and malignancy. This review will focus on third-generation tetracyclines, namely tigecycline, eravacycline, and omadacycline. We will delve into their mechanisms of action and resistance, while also evaluating their pros and cons over time. Additionally, we will explore their therapeutic potential, analyzing their primary indications of prescription, potential future uses, and non-antibiotic features. This review aims to provide valuable insights into the clinical applications of third-generation tetracyclines, thereby enhancing understanding and guiding optimal clinical use.
四环素类属于一类独特的抗生素药物，由于其广泛的活性谱，被广泛用于社区和医院感染的治疗。通过与 30S 核糖体亚基紧密结合来干扰蛋白质合成，它们的干扰通常是可逆的，因此具有抑菌作用。对四环素类药物的耐药性主要与泵外排或核糖体保护机制的改变有关。为了解决这一挑战，已经对四环素类药物进行了化学修饰，从而开发出了第三代四环素类药物。这些新型的四环素类药物在治疗感染方面具有显著的优势，无论是单独使用还是联合治疗，尤其是在医院环境中。除了传统的抗菌特性外，研究还强调了它们的潜在非抗生素特性，包括它们对免疫调节和恶性肿瘤的影响。本综述将重点介绍第三代四环素类药物，即替加环素、依拉环素和奥马环素。我们将深入探讨它们的作用机制和耐药机制，同时随着时间的推移评估它们的优缺点。此外，我们还将探讨它们的治疗潜力，分析它们的主要处方适应证、潜在的未来用途和非抗生素特性。本综述旨在为第三代四环素类药物的临床应用提供有价值的见解，从而增强对其的理解并指导最佳临床应用。
