Department of Basic Pharmaceutical Sciences, West Virginia University, Morgantown, WV, USA.
Exp Hematol Oncol. 2012 Apr 5;1(1):4. doi: 10.1186/2162-3619-1-4.
A growing body of evidence indicates that digitoxin cardiac glycoside is a promising anticancer agent when used at therapeutic concentrations. Digitoxin has a prolonged half-life and a well-established clinical profile. New scientific avenues have shown that manipulating the chemical structure of the saccharide moiety of digitoxin leads to synthetic analogs with increased cytotoxic activity. However, the anticancer mechanism of digitoxin or synthetic analogs is still subject to study while concerns about digitoxin's cardiotoxicity preclude its clinical application in cancer therapeutics. This review focuses on digitoxin and its analogs, and their cytotoxicity against cancer cells. Moreover, a new perspective on the pharmacological aspects of digitoxin and its analogs is provided to emphasize new research directions for developing potent chemotherapeutic drugs.
越来越多的证据表明，洋地黄毒苷类糖苷在治疗浓度下是一种很有前途的抗癌药物。洋地黄毒苷半衰期长，临床特征明确。新的科学途径表明，操纵洋地黄毒苷糖部分的化学结构会导致具有增强细胞毒性活性的合成类似物。然而，洋地黄毒苷或合成类似物的抗癌机制仍在研究中，而对洋地黄毒苷心脏毒性的担忧排除了其在癌症治疗中的临床应用。本综述重点介绍了洋地黄毒苷及其类似物，以及它们对癌细胞的细胞毒性。此外，还提供了洋地黄毒苷及其类似物药理学方面的新视角，强调了开发有效化疗药物的新研究方向。
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