Targeting mitochondrial apoptosis by betulinic acid in human cancers.

Autor: Fulda S; University Children's Hospital, Eythstr. 24, D-89075 Ulm, Germany. simone.fulda@uniklinik-ulm.de, Kroemer G
Jazyk: angličtina
Zdroj: Drug discovery today [Drug Discov Today] 2009 Sep; Vol. 14 (17-18), pp. 885-90. Date of Electronic Publication: 2009 Jun 09.
DOI: 10.1016/j.drudis.2009.05.015
Abstrakt: 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.
Databáze: MEDLINE