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用于肾功能无创实时经皮评估的两性离子近红外荧光剂。

Zwitterionic near infrared fluorescent agents for noninvasive real-time transcutaneous assessment of kidney function.

作者信息

Huang Jiaguo, Weinfurter Stefanie, Daniele Cristina, Perciaccante Rossana, Federica Rodeghiero, Della Ciana Leopoldo, Pill Johannes, Gretz Norbert

机构信息

Medical Research Center , Medical Faculty Mannheim , University of Heidelberg , Theodor-Kutzer-Ufer 1-3 , 68167 , Mannheim , Germany . Email:

Cyanagen S.r.l. , Via degli Stradelli Guelfi 40/C , 40138 Bologna , BO , Italy.

出版信息

Chem Sci. 2017 Apr 1;8(4):2652-2660. doi: 10.1039/c6sc05059j. Epub 2017 Jan 11.

Abstract

We developed novel zwitterionic near infrared (NIR) fluorescent agents (ABZWCY-HPβCD and AAZWCY-HPβCD), which exhibit favorable hydrophilicity, low plasma protein binding, high stability and non-toxicity. These attractive characteristics ensure that they are excreted rapidly, without any skin accumulation or metabolism . More importantly, zwitterionic HPβCD based agents can be efficiently filtrated by the glomerulus and completely excreted through the kidneys into urine without reabsorption or secretion in the kidney proximal tubule. Relying on these novel zwitterionic NIR agents and a transcutaneous device, we demonstrate a rapid, robust and biocompatible approach for assessing kidney function in rat models of both healthy rats and those with kidney disease, without the need for time-consuming blood/urine sample preparation. Our work provides a promising tool for real-time non-invasive kidney function assessment in preclinical applications.

摘要

我们开发了新型两性离子近红外(NIR)荧光剂(ABZWCY-HPβCD和AAZWCY-HPβCD),它们具有良好的亲水性、低血浆蛋白结合率、高稳定性和无毒性。这些吸引人的特性确保它们能迅速排出,不会在皮肤中积累或发生代谢。更重要的是,基于两性离子HPβCD的试剂可被肾小球有效滤过,并通过肾脏完全排泄到尿液中,而不会在近端肾小管中重吸收或分泌。依靠这些新型两性离子近红外试剂和一种经皮装置,我们展示了一种快速、可靠且生物相容的方法,可用于评估健康大鼠和肾病大鼠模型的肾功能,而无需耗时的血液/尿液样本制备。我们的工作为临床前应用中的实时无创肾功能评估提供了一个有前景的工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a0b/5431684/e30d9b5cfa92/c6sc05059j-s1.jpg

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