新型线粒体靶向抗肿瘤药物初探

Novel Mitochondrion Targeting Antit-umor Drug Study

本文简要介绍了以线粒体为靶点的一类抗肿瘤药物——电子移位亲脂性阳离子(DLC)及其作用机制。线粒体是半自主性的细胞器。它提供了细胞所需能量,调节细胞Ca2+的动态平衡,维持细胞的电势平衡作用,参与细胞凋亡过程及衰老等多种病理生理的代谢过程。线粒体是有效地治疗癌症和其它疾病的作用靶点。电子移位亲脂性阳离子(DLC)是一类具有亲油和亲水双亲性阳离子化合物。它能够在线粒体跨膜电位的推动下,聚集于细胞线粒体部位。由于肿瘤细胞的线粒体膜电位高于正常细胞,可提供推动力使DLC在肿瘤细胞线粒体内选择性地积聚,而DLC在高浓度下将表现出线粒体毒性,导致肿瘤细胞死亡。

This paper briefly introduces the mitochodrial targeted a antineoplastic agents -- Delocalized lipophilic cation （DLC） and its mechanism of action. Mitochondria are semi-autonomous organelle. It provides the cell energy required for the regulation of cellular Ca2＋, dynamic balance, maintaining the cell potential balance, involved in the apoptotic process and aging, a variety of pathological and physiological metabolism, mitochondrial is effective in the treatment of cancer and other diseases of the target. Delocalized lipophilic cation （DLC） is a class of lipophilic and hydrophilic amphiphilic cationic compounds. It is capable of mitochondrial transmembrane potential drive below, gathered in the mitochondria of parts. Since the tumor cells of the mitochondrial membrane potential was higher than normal cells, may provide the impetus to DLC in tumor cell mitochondria within selective accumulation, and the DLC in high concentration would be shown by mitochondrial toxicity, lead to tumor cell death.