Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, IS-107, Iceland.
J Pharm Sci. 2013 Oct;102(10):3485-512. doi: 10.1002/jps.23681. Epub 2013 Aug 7.
Calix[n]arenes (CAs) are supramolecular compounds able to form guest-host inclusion complexes with metal ions, small organic molecules, and small moieties of larger molecules. Although the CA literature is extensive, relatively few publications deal with water-soluble CAs, especially those containing nitrogen-based functionality. These CAs possess antibacterial and antifungal activity. Because of their molecular structure, they are surface active and also able to form water-soluble drug complexes, giving additional potential as enabling pharmaceutical excipients. This article provides an overview of the published data regarding synthesis, physicochemical properties, and pharmaceutical application of water-soluble CAs with emphasis on those that contain nitrogen-based substituents in their structure, particularly aminoCAs. In particular, it describes state-of-the-art in complexation of water-soluble CAs with pharmaceutically relevant ions and organic molecules up to amino acids, DNA, and proteins.
冠醚(CA)是超分子化合物,能够与金属离子、小分子有机分子和大分子的小分子部分形成主客体包合络合物。尽管 CA 的文献很多,但涉及水溶性 CA 的出版物相对较少,尤其是那些含有含氮功能基的 CA。这些 CA 具有抗菌和抗真菌活性。由于其分子结构,它们具有表面活性,并且还能够形成水溶性药物络合物,因此作为赋形剂具有额外的潜力。本文综述了有关水溶性 CA 的合成、物理化学性质和药物应用的已发表数据,重点介绍了那些在其结构中含有含氮取代基的 CA,特别是氨基 CA。特别是,它描述了水溶性 CA 与药学相关离子和有机分子(直至氨基酸、DNA 和蛋白质)形成络合物的最新进展。