Fulda Simone
University Children's Hospital, Ulm, Germany.
Mol Nutr Food Res. 2009 Jan;53(1):140-6. doi: 10.1002/mnfr.200700491.
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, nonmalignant cells and normal tissue remained relatively resistant to BA, indicating a therapeutic window. Since agents that exert a direct action on mitochondria may trigger cell death under circumstances in which standard chemotherapeutics fail, 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 bypass 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，而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形成对比的是，非恶性细胞和正常组织对BA相对耐药，这表明存在治疗窗口。由于直接作用于线粒体的药物在标准化疗药物失效的情况下可能引发细胞死亡，因此开发此类化合物作为实验性癌症治疗药物的兴趣日益浓厚。因此，像BA这样的线粒体靶向药物作为一种绕过人类癌症某些形式耐药性的新方法，具有巨大的潜力。
