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Polyoxometalate-biomolecule conjugates: A new approach to create hybrid drugs for cancer therapeutics

机译:多金属氧酸盐-生物分子共轭物:一种新的制备用于癌症治疗的混合药物的方法

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Some polyoxometalate (POM) clusters have demonstrated attractive anticancer properties. Unfortunately, their cytotoxicity upon normal cell is one of fateful side effects obstructing their further clinic application as inorganic drugs. In this communication, we report a new approach to create hybrid drugs potentially for cancer therapeutics. At first, the POM cluster bioconjugates were created by attaching the bioactive ligands on an amine grafted POM via simple amidation reaction. The cytotoxicity study with breast cancer cells (MCF-7 and MDA-MB-231) and non-cancerous breast epithelial cell (MCF-10A) showed that rationally selected ligands with cancer-cell targeting ability on POM-biomolecule conjugates can impart enhanced anti-tumor activity and selectivity, thus representing a new concept to develop novel POM-biomolecule hybrid drugs with the potential synergistic effect: increased bioactivity and lower side effect. ? 2012 Elsevier Ltd. All rights reserved.
机译:一些多金属氧酸盐(POM)簇已显示出有吸引力的抗癌特性。不幸的是,它们对正常细胞的细胞毒性是致命的副作用之一,阻碍了它们作为无机药物的进一步临床应用。在本交流中,我们报告了一种新的方法来创建可能用于癌症治疗的混合药物。首先,通过简单的酰胺化反应将生物活性配体附着在胺接枝的POM上,从而创建POM簇生物共轭物。对乳腺癌细胞(MCF-7和MDA-MB-231)和非癌性乳腺癌上皮细胞(MCF-10A)的细胞毒性研究表明,合理选择对POM生物分子结合物具有癌细胞靶向能力的配体可以赋予增强的抗肿瘤活性和选择性,从而代表了开发具有潜在协同作用的新型POM生物分子杂交药物的新概念:增加的生物活性和较低的副作用。 ? 2012 Elsevier Ltd.保留所有权利。

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