2. Academic Validation
  3. A Druglike Ferrostatin-1 Analogue as a Ferroptosis Inhibitor and Photoluminescent Indicator

A Druglike Ferrostatin-1 Analogue as a Ferroptosis Inhibitor and Photoluminescent Indicator

  • Angew Chem Int Ed Engl. 2025 May 12;64(20):e202502195. doi: 10.1002/anie.202502195.
Jiangkun Yan 1 2,  Luo Bao 1 2,  Huicong Liang 3,  Li Zhao 4,  Ming Liu 1 2,  Lingxiu Kong 1 2,  Xuejing Fan 1 2,  Chunhui Liang 5,  Tongtong Liu 6,  Xinyu Han 1 2,  Kangnan Wang 7,  Chuanbin Shen 1 2,  Wanyang Sun 6,  Xin Zhou 8,  Bo Chu 5,  Michael J McGlinchey 9,  Ximing Xu 3,  Xue Qiu 1 2,  Yong Wang 1 2
Affiliations

Affiliations

  • 1 Key Laboratory of Marine Drug, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, China.
  • 2 Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, 266237, P. R. China.
  • 3 Marine Biomedical Research Institute of Qingdao, School of Medicine and Pharmacy, Key Laboratory of Marine Drugs, Chinese Ministry of Education, Ocean University of China, Qingdao, 266003, Shandong, P. R. China.
  • 4 College of Science, China University of Petroleum (East China), Qingdao, 266580, Shandong, P. R. China.
  • 5 School of Basic Medical Science, Shandong University, Jinan, Shandong, 250012, P. R. China.
  • 6 Guangdong-Hong Kong-Macao Universities Joint Laboratory for the Internationalization of Traditional Chinese Medicine, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, 510632, P. R. China.
  • 7 State Key Laboratory of Crystal Materials, Shandong University, Jinan, 250100, Shandong, P. R. China.
  • 8 College of Chemistry and Chemical Engineering, Qingdao University, Qingdao, 266003, P. R. China.
  • 9 UCD School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland.
PMID: 39984310 DOI: 10.1002/anie.202502195
Abstract

Redox-based diagnostic and therapeutic applications have long suffered from a shortage of suitable drugs and probes of high specificity. In the context of anti-ferroptosis research for neurological diseases, the inaccessibility of a blood-brain barrier (BBB) permeable small molecular Ferroptosis inhibitor, and the lack of specific Ferroptosis probes, seriously impeded a deeper understanding of the mechanism of Ferroptosis and the development of clinically applicable drugs. We report herein a novel 1,3,4-thiadiazole-functionalized druglike ferrostatin analogue entitled Ferfluor-1 with superior anti-ferroptosis potency, favorable BBB permeability and in vivo activity against stroke and Parkinson's disease. Moreover, the exclusive pseudo-excited-state intramolecular proton-transfer (ESIPT) property of Ferfluor-1 via a long-distance hydrogen-bonding network makes it the first sensitive ratiometric photoluminescent probe to detect phospholipid hydroperoxides and a specific indicator for the fluctuation of Ferroptosis. These unprecedented advantages not only make Ferfluor-1 a potential tool for ferroptosis-related diagnostic and therapeutic applications in the central nervous system, but also pave the way to developing new theragnostic agents for precision redox detection and regulation.

Keywords

antioxidants; excited-state intramolecular proton-transfer; fluorescent probes; lipid peroxidation; oxidative stress.

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