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首页> 外文期刊>Chemistry: A European journal >A Trimodal Closomer Drug-Delivery System Tailored with Tracing and Targeting Capabilities
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A Trimodal Closomer Drug-Delivery System Tailored with Tracing and Targeting Capabilities

机译：具有追踪和靶向能力的三峰式Closomer药物递送系统

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摘要

The construction and application of a unique monodisperse closomer drug-delivery system (CDDS) integrating three different functionalities onto an icosahedral closo-dodecaborane [B-12](2-) scaffold is described. Eleven B-OH vertices of [closo-B-12(OH)(12)](2-) were used to attach eleven copies of the anticancer drug chlorambucil and the targeting vector glucosamine through a bifurcating lysine linker. The remaining twelfth vertex was used to attach a fluorescent imaging probe. The presence of multiple glucosamine units offered a monodisperse and highly water-soluble CDDS with a high payload of therapeutic cargo. This array enhanced the penetration of the drug into cancer cells by exploiting the overexpression of GLUT-1 receptors present on cancer cells. About 15-fold enhancement in cytotoxicity was observed for CDDS-1 against Jurkat cells, compared to CDDS-2, which lacks the GLUT-1 targeting glucosamine. A cytotoxicity comparison of CDDS-1 against colorectal RKO cells and its GLUT-1 knock-out version confirmed that GLUT-1 mediates endocytosis. Using fluorescent markers both CDDS-1 and -2 were traced to the mitochondria, a novel target for alkylating agents.
机译：描述了将三种不同功能整合到二十面体closo-dodecaborane [B-12]（2-）支架上的独特的单分散性closomer药物递送系统（CDDS）的构建和应用。 [closo-B-12（OH）（12）]（2-）的11个B-OH顶点用于通过分叉的赖氨酸接头连接11个拷贝的抗癌药物苯丁酸氮芥和靶向载体氨基葡萄糖。其余的第十二个顶点用于连接荧光成像探针。多个氨基葡萄糖单元的存在提供了单分散的，高度水溶性的CDDS，以及高负载的治疗性货物。该阵列通过利用癌细胞上存在的GLUT-1受体的过表达来增强药物对癌细胞的渗透。与缺少GLUT-1靶向葡萄糖胺的CDDS-2相比，针对Jurkat细胞的CDDS-1的细胞毒性提高了约15倍。 CDDS-1对结直肠RKO细胞及其GLUT-1敲除版本的细胞毒性比较证实，GLUT-1介导了内吞作用。使用荧光标记，将CDDS-1和-2都追踪到线粒体，这是烷化剂的新靶标。

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