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三嗪树状大分子作为药物传递系统:从合成到治疗。

Triazine dendrimers as drug delivery systems: from synthesis to therapy.

机构信息

Department of Chemistry, Texas Christian University, Fort Worth, TX 76129, USA.

出版信息

Adv Drug Deliv Rev. 2012 Jun 15;64(9):826-35. doi: 10.1016/j.addr.2012.03.008. Epub 2012 Mar 20.

DOI:10.1016/j.addr.2012.03.008
PMID:22465784
Abstract

The use of triazine dendrimers as drug delivery systems benefits from their synthetic versatility and well-defined structure. Triazine dendrimers can be designed and readily synthesized to display orthogonally functional surfaces that facilitate post-synthetic manipulation such as attachment of drug, PEGylation, and/or the installation of ligands or reporting groups. The synthesis is scalable, and large generations can be accessed. To date, triazine dendrimers have been probed for a variety of medicinal applications including drug delivery with an emphasis on cancer, nonviral DNA and RNA delivery systems, in sensing applications, and as bioactive materials. Specifically, triazine adducts with paclitaxel, camptothecin, brefeldin A, and desferrioxamine have been prepared and assessed. Paclitaxel constructs show promising activity in vivo. The use of these materials in fluorescence-based glucose sensors is being pursued. Glycosylated triazine dendrimers interfere with signal transduction in the Toll-4 receptor pathway.

摘要

三嗪树状大分子作为药物传递系统的应用得益于其合成的多功能性和明确的结构。三嗪树状大分子可以被设计并易于合成,以展示正交功能表面,从而便于进行后期的合成操作,如药物的连接、聚乙二醇化和/或配体或报告基团的安装。这种合成方法具有可扩展性,可以获得较大的代数。迄今为止,三嗪树状大分子已被用于多种药物应用的研究,包括药物传递(重点是癌症)、非病毒 DNA 和 RNA 传递系统、传感应用以及生物活性材料。具体来说,已经制备和评估了紫杉醇、喜树碱、布雷菲德菌素 A 和去铁胺的三嗪加合物。紫杉醇构建体在体内表现出有希望的活性。正在研究将这些材料用于基于荧光的葡萄糖传感器中。糖基化三嗪树状大分子干扰 Toll-4 受体途径中的信号转导。

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