Department of Chemistry, Jinan University, Guangzhou 510632, People's Republic of China.
Inorg Chem. 2010 Jul 19;49(14):6366-8. doi: 10.1021/ic100277w.
The limitations of cisplatin-based chemotherapy, including high toxicity, undesirable side effects, and drug resistance, have motivated extensive investigations into alternative metal-based cancer therapies. Ruthenium (Ru) possesses several favorable properties suited to rational anticancer drug design and biological applications. In the present study, we synthesized a series of ruthenium polypyridyl complexes containing N,N-chelating ligands, examined their anticancer activities, and elucidated the molecular mechanisms through which they caused the cancer cell death. The results demonstrated that Ru(phen)(2)-p-MOPIP(2).2H(2)O (RuPOP), a complex with potent antiproliferative activity, is able to induce mitochondria-mediated and caspase-dependent apoptosis in human cancer cells. On the basis of these results, we suggest that RuPOP may be a candidate for further evaluation as a chemopreventive and chemotherapeutic agent for human cancers, especially for melanoma.
顺铂为基础的化疗的局限性，包括高毒性、不良副作用和耐药性，促使人们广泛研究替代金属为基础的癌症治疗方法。钌（Ru）具有一些适合合理抗癌药物设计和生物应用的有利特性。在本研究中，我们合成了一系列含有 N，N-螯合配体的钌多吡啶配合物，研究了它们的抗癌活性，并阐明了它们导致癌细胞死亡的分子机制。结果表明，Ru(phen)(2)-p-MOPIP(2).2H(2)O（RuPOP），一种具有强大增殖抑制活性的配合物，能够诱导人癌细胞中线粒体介导和 caspase 依赖性凋亡。基于这些结果，我们认为 RuPOP 可能是作为人类癌症的化学预防和化学治疗剂的候选物，特别是对黑色素瘤。
