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Open Access Highly Accessed Review

Digitoxin and its analogs as novel cancer therapeutics

Hosam A Elbaz1, Todd A Stueckle14, William Tse2, Yon Rojanasakul15* and Cerasela Zoica Dinu36*

Author Affiliations

1 Department of Basic Pharmaceutical Sciences, West Virginia University, Morgantown, WV, USA

2 Mary Babb Randolph Cancer Center, West Virginia University, Morgantown, WV, USA

3 Department of Chemical Engineering, West Virginia University, Morgantown, WV, USA

4 National Institute for Occupational Safety and Health, Morgantown, WV, USA

5 Department of Basic Pharmaceutical Sciences, West Virginia University, PO Box 9530, 1 Medical Center Drive, Morgantown, WV 26506, USA

6 Department of Chemical Engineering, West Virginia University, College of Engineering and Mineral Resources, PO Box 6102, ESB 445, Morgantown, WV 26506, USA

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Experimental Hematology & Oncology 2012, 1:4  doi:10.1186/2162-3619-1-4

Published: 5 April 2012

Abstract

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.