University of New South Wales Department of Surgery, St George Hospital, Sydney, Australia.
Mini Rev Med Chem. 2012 Jan;12(1):44-52. doi: 10.2174/138955712798868977.
Tetracyclines are an amazing class of chemical agents with multiple therapeutic potential. Structural modification of the original natural tetracyclines led to the synthesis and development of doxycycline and minocycline, compounds with higher lipophilicity, better oral pharmacokinetics and higher potency. Due to diverse pharmacological properties, these drugs are now under extensive investigation for use in the treatment of various disparate diseases. In recent years, several studies have conclusively reported anti-inflammatory, immune-modulating and neuroprotective effects of these compounds. There are currently over 200 ongoing clinical trials on tetracyclines. These studies extend over a wide range of diseases including dermatological diseases, behavior and mental disorders, immune system disorders, cardiovascular diseases, and cancer. In this review we will discuss the chemistry and pharmacology of these agents, and describe how their inhibitory effect on matrix metalloproteinase and on pro-inflammatory cytokines has kindled renewed interest in them. Based on the reports from pre-clinical and clinical trials, the therapeutic potential and application of tetracyclines may well be redefined and extensively extended.
四环素类是一类具有多种治疗潜力的神奇化学药物。对原始天然四环素进行结构修饰，导致了强力霉素和二甲胺四环素的合成和发展，这些化合物具有更高的亲脂性、更好的口服药代动力学和更高的效力。由于具有多种药理学特性，这些药物目前正在广泛研究用于治疗各种不同的疾病。近年来，有几项研究明确报告了这些化合物的抗炎、免疫调节和神经保护作用。目前有超过 200 项关于四环素的临床试验正在进行。这些研究涵盖了广泛的疾病，包括皮肤病、行为和精神障碍、免疫系统疾病、心血管疾病和癌症。在这篇综述中，我们将讨论这些药物的化学和药理学，并描述它们对基质金属蛋白酶和促炎细胞因子的抑制作用如何重新引起人们的兴趣。基于临床前和临床试验的报告，四环素的治疗潜力和应用可能会被重新定义和广泛扩展。
