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前药铂-A:顺铂和阿司匹林的同时释放。

The prodrug platin-A: simultaneous release of cisplatin and aspirin.

机构信息

NanoTherapeutics Research Laboratory, Department of Chemistry, University of Georgia, Athens, GA 30602 (USA) http://shanta.chem.uga.edu.

出版信息

Angew Chem Int Ed Engl. 2014 Feb 10;53(7):1963-7. doi: 10.1002/anie.201308899. Epub 2014 Jan 22.

Abstract

Cancer-associated inflammation induces tumor progression to the metastatic stage, thus indicating that a chemo-anti-inflammatory strategy is of interest for the management of aggressive cancers. The platinum(IV) prodrug Platin-A was designed to release cisplatin and aspirin to ameliorate the nephrotoxicity and ototoxicity caused by cisplatin. Platin-A exhibited anticancer and anti-inflammatory properties which are better than a combination of cisplatin and aspirin. These findings highlight the advantages of combining anti-inflammatory treatment with chemotherapy when both the drugs are delivered in the form of a single prodrug.

摘要

癌症相关炎症会促使肿瘤进展至转移阶段,因此表明化疗-抗炎策略对于侵袭性癌症的治疗具有重要意义。顺铂(IV)前药 Platin-A 的设计目的是释放顺铂和阿司匹林,以改善顺铂引起的肾毒性和耳毒性。Platin-A 表现出优于顺铂和阿司匹林联合使用的抗癌和抗炎特性。这些发现强调了在以单一前药形式给予两种药物时,将抗炎治疗与化疗相结合的优势。

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