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Drug Discov Today. 2009 Sep;14(17-18):885-90. doi: 10.1016/j.drudis.2009.05.015. Epub 2009 Jun 9.

Targeting mitochondrial apoptosis by betulinic acid in human cancers.

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University Children's Hospital, Eythstr. 24, D-89075 Ulm, Germany.


Betulinic acid (BA) is a naturally occurring pentacyclic triterpene that exhibits a variety of biological activities including potent antitumor properties. This anticancer activity has been linked to its ability to directly trigger mitochondrial membrane permeabilization, a central event in the apoptotic process that seals the cell's fate. In contrast to the potent cytotoxicity of BA against a variety of cancer types, non-neoplastic cells as well as normal tissue remain relatively resistant to BA, thus pointing to a therapeutic window. Because agents that exert a direct action on mitochondria may bypass resistance to conventional chemotherapeutics, there is increasing interest to develop such compounds as experimental cancer therapeutics. Thus, mitochondrion-targeted agents such as BA hold great promise as a novel approach to overcome certain forms of drug resistance in human cancers.

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