Wang Shaoru, Wang Qilong, Wang Yan, Liu Lin, Weng Xiaocheng, Li Guorui, Zhang Xiaolian, Zhou Xiang
College of Chemistry and Molecular Sciences, Wuhan University, Hubei, Wuhan 430072, PR China.
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6505-8. doi: 10.1016/j.bmcl.2008.10.047. Epub 2008 Oct 14.
Three water soluble anthraquinone derivatives were designed and synthesized employing click chemistry to prepare novel and potent antitumor drugs. An MTT assay indicated that all compounds had significant inhibitory activity against BGC gastric cancer cells in vitro. Apoptosis induced by these compounds was observed by flow cytometry and laser confocal microscopy. Mechanistic analysis showed that these compounds induced the generation of several reactive oxygen species, the loss of mitochondrial membrane potential (Delta psi m), the transition of mitochondrial permeability, and the release of cytochrome C from the mitochondrion to cytoplasm. These results suggest that the anthraquinones might be potential lead compounds for the cancer chemotherapy.
设计并合成了三种水溶性蒽醌衍生物，采用点击化学法制备新型高效抗肿瘤药物。MTT 法检测表明，所有化合物在体外对 BGC 胃癌细胞均具有显著的抑制活性。通过流式细胞术和激光共聚焦显微镜观察了这些化合物诱导的细胞凋亡。机制分析表明，这些化合物诱导了多种活性氧的产生、线粒体膜电位（Δψm）的丧失、线粒体通透性的转变以及细胞色素 C 从线粒体释放到细胞质中。这些结果表明，蒽醌类化合物可能是癌症化疗的潜在先导化合物。
