Fulda Simone, Kroemer Guido
University Children's Hospital, Eythstr. 24, D-89075 Ulm, Germany.
Drug Discov Today. 2009 Sep;14(17-18):885-90. doi: 10.1016/j.drudis.2009.05.015. Epub 2009 Jun 9.
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.
桦木酸（BA）是一种天然存在的五环三萜，具有多种生物活性，包括强大的抗肿瘤特性。这种抗癌活性与其直接引发线粒体膜通透性改变的能力有关，线粒体膜通透性改变是凋亡过程中的核心事件，决定了细胞的命运。与BA对多种癌症类型的强大细胞毒性相反，非肿瘤细胞以及正常组织对BA仍具有相对抗性，因此存在一个治疗窗口。由于直接作用于线粒体的药物可能绕过对传统化疗药物的抗性，人们越来越有兴趣开发此类化合物作为实验性癌症治疗药物。因此，像BA这样的线粒体靶向药物作为克服人类癌症某些形式耐药性的新方法具有巨大潜力。
