Fürst Robert, Zündorf Ilse, Dingermann Theo
Institute of Pharmaceutical Biology, Biocenter, Goethe University, Frankfurt/Main.
Planta Med. 2017 Aug;83(12-13):977-984. doi: 10.1055/s-0043-105390. Epub 2017 Mar 15.
In the 19th century, cardio-active steroid glycosides, shortly cardiac glycosides, were scientifically established as drugs against heart failure. Their , cellular, and molecular actions as well as their predominant target, Na-K-ATPase, have been comprehensively investigated in the 20th century and the discovery of endogenous cardiac glycosides has fostered this research field. In the last years, however, results from clinical trials and meta-analyses have questioned their therapeutic value due to efficacy and safety issues. This has led to a considerable decline of their usage. Beyond the cardiovascular system, cardiac glycosides have been increasingly recognized as antitumor compounds and Na-K-ATPase has evolved into a promising drug target in oncology. A wealth of review articles exists that intensively discuss these topics. Surprisingly, the anti-inflammatory actions of cardiac glycosides, which were discovered in the 1960s, have so far hardly been perceived and have not yet been summarized. This review provides an overview of the and actions of cardiac glycosides on inflammatory processes and of the signaling mechanisms responsible for these effects: cardiac glycosides have been found to decrease inflammatory symptoms in different animal models of acute and chronic inflammation. Regarding the underlying mechanisms most research has focused on leukocytes. In these cells, cardiac glycosides primarily inhibit cell proliferation and the secretion of proinflammatory cytokines.
在19世纪，心脏活性甾体糖苷，简称强心苷，被科学地确立为治疗心力衰竭的药物。在20世纪，人们对其细胞和分子作用以及主要靶点钠钾ATP酶进行了全面研究，内源性强心苷的发现推动了这一研究领域的发展。然而，近年来，由于疗效和安全性问题，临床试验和荟萃分析的结果对其治疗价值提出了质疑。这导致其使用量大幅下降。除了心血管系统，强心苷越来越被认为是抗肿瘤化合物，钠钾ATP酶已成为肿瘤学中一个有前景的药物靶点。有大量综述文章深入讨论了这些话题。令人惊讶的是，20世纪60年代发现的强心苷的抗炎作用至今几乎未被关注，也尚未得到总结。本综述概述了强心苷对炎症过程的作用及其作用机制：已发现强心苷可减轻不同急性和慢性炎症动物模型中的炎症症状。关于潜在机制，大多数研究集中在白细胞上。在这些细胞中，强心苷主要抑制细胞增殖和促炎细胞因子的分泌。
