d-Amino Acids Boost the Selectivity and Confer Supramolecular Hydrogels of a Nonsteroidal Anti-Inflammatory Drug (NSAID)

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• 作者：Jiayang Li ; Yi Kuang ; Yuan Gao ; Xuewen Du ; Junfeng Shi ; Bing Xu
• 刊名：The Journal of the American Chemical Society
• 出版年：2013
• 出版时间：January 16, 2013
• 年：2013
• 卷：135
• 期：2
• 页码：542-545
• 全文大小：296K
• 年卷期：v.135,no.2(January 16, 2013)
• ISSN：1520-5126

文摘

As systemically used therapeutics for treating acute or chronic pains or inflammations, nonsteroidal anti-inflammatory drugs (NSAIDs) also associate with the adverse gastrointestinal and renal effects and cardiovascular risks. Thus, it is beneficial to develop topical gels that selectively inhibit cyclooxygenase-2 (COX-2) for the management of local inflammation. In this work, we demonstrate that the covalent conjugation of d-amino acids to naproxen (i.e., a NSAID) not only affords supramolecular hydrogelators for the topical gels but also unexpectedly and significantly elevates the selectivity toward COX-2 about 20脳 at little expense of the activity of naproxen. This work illustrates a previously unexplored approach that employs d-amino acids for the development of functional molecules that have dual or multiple roles and exceptional biostability, which offers a new class of molecular hydrogels of therapeutic agents.