水溶性非环状分子容器的靶向药物传递

项目名称： 水溶性非环状分子容器的靶向药物传递

项目编号： No.21472149

项目类型： 面上项目

立项/批准年度： 2015

项目学科： 数理科学和化学

项目作者： 曹利平

作者单位： 西北大学

项目金额： 85万元

中文摘要： 自然界的生物系统中，生物蛋白质主体参与生命体众多生理活动，扮演着极为关键的角色。受此启发，新型分子容器的设计与合成一直以来都是超分子化学的研究热点领域之一，例如冠醚、环糊精、杯芳烃、葫芦脲以及柱芳烃等经典大环分子的合成扩展了超分子化学的研究内容，并被广泛应用于分子机器、仿生系统、超分子催化、刺激响应聚合物等领域。与此同时，抗癌药物的溶解性和靶向传递等难题一直困扰着生化、药物等领域的研究。分子容器的药物传递体系是一类新颖的研究策略；我们在葫芦脲大环结构的基础上，设计和合成一系列具有C型结构的非环状分子容器，并着眼于药物传递领域，将这些功能性的非环状分子容器应用于解决药物传递过程中的众多难题，例如提高药物溶解性和赋予药物靶向传递能力等。本研究将以此为起点，期待该类新型的非环状分子容器能广泛应用于药物增溶和靶向传递等方面的研究，探寻出水溶性功能化主客体复合物对改善药物高效利用的新方法与新途径。

中文关键词： 超分子化学；主客体化学；分子识别；分子容器；药物传递

英文摘要： In biological system, protein hosts involving various physiological activities play a very important role. Inspired by Nature, the rational design of new molecular containers that can complex analytes with high affinity and selectivity represents a hot area of supramolecular chemistry, in particular for systems operating in aqueous solutions. For examples, crown ether, cyclodextrin, calixarene, cucurbituril and pillararene have been used to create a number of applications including molecular machines, biomimetic systems, supramolecular catalysts, and stimuli responsive polymers. At the same time, it is huge challenging for both biologists and chemists to solve the poor solubility and non-targeted delivery of anticancer drugs. Molecular containers, which have the ability to encapsulate a therapeutic agent non-covalently within their cavity, have gained enormous attention in recent years. Herein, we design and synthesize a series of acyclic molecular container with a C-shaped, which are potential applications as drug delivery system for enhancing the solubility of drug and targeting drug to cancer cell. From this start, we hope this series of acyclic molecular containers that have excellent aqueous solubility and targeted ability will be widely used on solventing drug and targeted delivery. Accordingly, it is straightforward to imagine that explore a new route to achieve highly effective use of anti-cancer drugs by host-guest complex.

英文关键词： supramolecular chemistry;host-guest chemistry;molecular recognition;molecular container;drug delivery