A Stepwise Targeting Curcumin Derivative, Ser@TPP@CUR, for Acute Kidney Injury

  • ACS Med Chem Lett. 2022 Mar 8;13(4):554-559. doi: 10.1021/acsmedchemlett.1c00585.
Xia Yan  1 ,  Xue-Ying Tan  2 ,  Yi-Xuan Li  3 ,  Hong-Bo Wang  4 ,  Jian-Bo Jin  4 ,  Ying-Rui Mao  5 ,  Jing-Bo Hu  3 ,  Ling-Hui Wu  6
Affiliations
  • 1. 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.
  • 2. College of Pharmacy, Zhejiang Pharmaceutical College, Ningbo 315100, China.
  • 3. Faculty of Materials Science and Chemical Engineering, Ningbo University, Ningbo 315211, China.
  • 4. Department of Pharmacy, Ningbo University Affiliated Yangming Hospital, Yuyao 315400, China.
  • 5. Medical College, Ningbo University, Ningbo 315211, China.
  • 6. Department of Nephrology, The People's Hospital of Lishui, The Sixth Affiliated Hospital of Wenzhou Medical University, Lishui 323000, China.
PMID: 35450367 DOI: 10.1021/acsmedchemlett.1c00585
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.

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