一种用于急性肾损伤的逐步靶向姜黄素衍生物，Ser@TPP@CUR。
A Stepwise Targeting Curcumin Derivative, Ser@TPP@CUR, for Acute Kidney Injury.
作者信息
Yan Xia, Tan Xue-Ying, Li Yi-Xuan, Wang Hong-Bo, Jin Jian-Bo, Mao Ying-Rui, Hu Jing-Bo, Wu Ling-Hui
机构信息
Li Dak Sum Yip Yio Chin Kenneth Li Marine Biopharmaceutical Research Center, Department of Marine Pharmacy, College of Food and Pharmaceutical Sciences, Ningbo University, Ningbo 315800, China.
College of Pharmacy, Zhejiang Pharmaceutical College, Ningbo 315100, China.
出版信息
ACS Med Chem Lett. 2022 Mar 8;13(4):554-559. doi: 10.1021/acsmedchemlett.1c00585. eCollection 2022 Apr 14.
Abstract
Based on the pathological mechanisms of acute kidney injury (AKI), a stepwise targeting curcumin derivative, Ser@TPP@CUR, was developed in this study. Ser@TPP@CUR can be specifically internalized by renal tubular epithelial cells via KIM-1 receptor-mediated endocytosis and then actively distributed in mitochondria under the effect of TPP, a mitochondrial targeting molecule. Both in vitro and in vivo results showed that Ser@TPP@CUR effectively ameliorated injured renal tubular epithelial cells and improved renal functions of AKI mice.
摘要
基于急性肾损伤（AKI）的病理机制，本研究开发了一种逐步靶向的姜黄素衍生物Ser@TPP@CUR。Ser@TPP@CUR可通过KIM-1受体介导的内吞作用被肾小管上皮细胞特异性内化，然后在线粒体靶向分子TPP的作用下主动分布于线粒体中。体外和体内实验结果均表明，Ser@TPP@CUR能有效改善受损的肾小管上皮细胞，并改善AKI小鼠的肾功能。
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