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将药物转化为凝胶剂:N-乙酰-L-半胱氨酸和金属货币盐的超分子水凝胶。

Converting drugs into gelators: supramolecular hydrogels from N-acetyl-L-cysteine and coinage-metal salts.

机构信息

CIDETEC, Centre for Electrochemical Technologies, New Materials Department, Paseo Miramón 196, 20009 Donostia-San Sebastián, Spain.

出版信息

Org Biomol Chem. 2010 Dec 7;8(23):5455-8. doi: 10.1039/c0ob00311e. Epub 2010 Sep 30.

DOI:10.1039/c0ob00311e
PMID:20882249
Abstract

Here we present the concept of metallophilic hydrogels, supramolecular systems in which the gelator species are metal-thiolates that self-assemble through metallophilic attractions. The principle is applied for a small drug, the mucolytic agent N-acetyl-l-cysteine (NAC), which readily forms hydrogels in the presence of Au(iii), Ag(i) and Cu(ii) salts. The resulting transparent hydrogels present pH induced sol/gel transition. Scanning electron microscopy (SEM) measurements reveal a microporous structure in form of flakes for the three of them. The low pH at which these hydrogels are formed (pH < 4) limits their direct use as drug-delivery systems, but still this system constitutes a novel method for easy and fast conversion of small drugs into potent hydrogelators. Future developments will help to fully develop the idea in order to create a new class of supramolecular drug-delivery systems.

摘要

在这里,我们提出了亲金属水凝胶的概念,这是一种超分子体系,其中凝胶剂物种是通过亲金属吸引力自组装的金属-硫醇盐。该原理适用于一种小分子药物,粘液溶解剂 N-乙酰-L-半胱氨酸 (NAC),它在 Au(iii)、Ag(i) 和 Cu(ii)盐的存在下很容易形成水凝胶。所得的透明水凝胶呈现出 pH 诱导的溶胶/凝胶转变。扫描电子显微镜 (SEM) 测量显示,这三种物质均呈现出薄片形式的微孔结构。这些水凝胶形成的低 pH(pH < 4)限制了它们作为药物输送系统的直接应用,但该系统仍然为将小分子药物转化为有效水凝胶剂提供了一种新颖的方法。未来的发展将有助于充分开发这一理念,以创建一类新的基于超分子的药物输送系统。

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N-Acetyl cysteine abrogates silver-induced reactive oxygen species in human cells without altering silver-based antimicrobial activity.
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