Digitoxin and its analogs as novel cancer therapeutics.
Digitoxin and its analogs as novel cancer therapeutics.
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DOI：
10.1186/2162-3619-1-4
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发表时间：
2012-04-05
影响因子：
10.9
通讯作者：
Dinu CZ
中科院分区：
文献类型：
--
作者：
Elbaz HA;Stueckle TA;Tse W;Rojanasakul Y;Dinu CZ
越来越多的证据表明，洋地黄素心糖苷在治疗浓度下是一种很有前途的抗癌药物。地地黄毒素具有较长的半衰期和良好的临床表现。新的科学途径表明，操纵洋地黄毒素的糖部分的化学结构导致合成类似物具有增加的细胞毒性活性。然而，洋地黄素或其合成类似物的抗癌机制仍有待研究，而对洋地黄素心脏毒性的担忧阻碍了其在癌症治疗中的临床应用。本文就洋地黄毒素及其类似物及其对癌细胞的细胞毒性进行综述。此外，为地黄霉素及其类似物的药理研究提供了新的视角，为开发强效化疗药物提供了新的研究方向。
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.