J Med Chem：科学家发现治疗绦虫感染的新药物

研究者发现了一些可以阻止绦虫感染的药物

(Credit: Image courtesy of American Chemical Society)

近日，来自国外的科学家发现了一系列可以阻止绦虫感染的药物，这些绦虫可以在人类中引起非常罕见而且威胁生命健康的疾病，相关研究成果刊登在了国际杂志Journal of Medicinal Chemical上，文章中，作者指出，特殊抗癌的有机金属物质可以帮助我们有效抵御绦虫的感染。

研究者Carsten Vock表示，泡型包虫病（AE）是由多房棘球绦虫引起的一种寄生虫病，虽然很罕见，如果没有得到及时治疗，AE这种疾病可以在10-20年里引起至少94%的寄主死亡，大部分的感染发生在北半球，比如中亚、中国的西北部、日本和欧洲的部分地区。人们一般通过食用被绦虫污染的鸡蛋而被感染。外科手术是AE的最好治疗选择，但是外科手术并不能将所有绦虫清除，目前AE的药物并不能治愈疾病，只能使得绦虫不扩大感染，而且这些药物必须长期服用。AE病人中，绦虫可以引起瘤样生长，这将会扩展并且转移到机体的不同组织。于此同时，这也给了科学家灵感，科学家观察是否抗癌制剂---钌错合物（ruthenium complexes）可以用于进行绦虫感染的治疗。

研究小组准备并且评估了好几种钌错合物在抵御绦虫感染的潜在治疗效果，实验室研究表明，有一些钌错合物对于杀死绦虫非常有效，而且对于机体细胞也是低毒的，后期研究者将会在AE病人中进行深入的检验和研究。这项研究由瑞士国家科学自然基金等机构支持。（生物谷：T.Shen编译）

doi:10.1021/jm300291a
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A New Promising Application for Highly Cytotoxic Metal Compounds: η6-Areneruthenium(II) Phosphite Complexes for the Treatment of Alveolar Echinococcosis

Tatiana Küster‡, Nadine Lense†, Fabienne Barna‡, Andrew Hemphill*‡, Markus K. Kindermann†, Joachim W. Heinicke†, and Carsten A. Vock*†

Two series of η6-areneruthenium(II) phosphite complexes were prepared, characterized, and evaluated in vitro for their toxic potential against Echinococcus multilocularis metacestodes. Neutral complexes of general formula [(η6-p-cymene)RuCl2{P(OR)3}] (R = Et, iPr, Ph) with two easily exchangable chloride ligands showed only minor toxicity, whereas the substitution of these moieties against a β-diketonate (2,2,6,6-tetramethylheptanedionate) ligand led to hydrolytically stable complex salts of type [(η6-p-cymene)Ru(β-diketonate){P(OR)3}][BF4] (R = Et, iPr, Ph) with comparable in vitro toxicity (50% PGI release at c = 1.4 – 4.7 μM) to the reference drug nitazoxanide (50% PGI release at c = 1.2 μM). In addition, the latter complexes were highly toxic against rat hepatoma cells (IC50 = 0.40–2.0 μM) and less toxic against human foreskin fibroblasts (IC50 = 1.1–2.9 μM) and Vero cells (IC50 = 1.2–8.9 μM). The measured cytotoxicities against mammalian cells are, to the best of our knowledge, among the highest ever observed for ruthenium-based complexes. In conclusion, complex salts of type [(η6-p-cymene)Ru(β-diketonate){P(OR)3}][BF4] might be interesting candidates for further development toward anthelmintic drugs and/or highly cytotoxic metal compounds.