2. Academic Validation
  3. A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy

A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy

  • J Med Chem. 2022 Feb 10;65(3):2225-2237. doi: 10.1021/acs.jmedchem.1c01736.
Yishen Liu 1 2 3 4,  Qianqian Li 5 3,  Meijia Gu 1,  Disheng Lu 1 2 3 4,  Xiaoxing Xiong 1,  Zhiyun Zhang 1 4,  Yanna Pan 1 4,  Yuqin Liao 1 4,  Qihang Ding 1 4,  Wanxia Gong 1 4,  Dean Shuailin Chen 6,  Mengting Guan 4,  Junzhu Wu 4,  Zhiquan Tian 2,  Hai Deng 7,  Lijuan Gu 1,  Xuechuan Hong 1 2 4,  Yuling Xiao 1 3
Affiliations

Affiliations

  • 1 Department of Neurosurgery, Central Laboratory, Renmin Hospital of Wuhan University, State Key Laboratory of Virology, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China.
  • 2 College of Science, Laboratory of Extreme Environmental Biological Resources and Adaptive Evolution, Research Center for Ecology, Tibet University, Lhasa 850000, China.
  • 3 Shenzhen Institute of Wuhan University, Shenzhen 518057, China.
  • 4 Center for Experimental Basic Medical Education, Hubei Provincial Key Laboratory of Developmentally Originated Disease and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE), Wuhan 430071, China.
  • 5 Hubei Key Laboratory for Processing and Application of Catalytic Materials, Huanggang Normal University, Huanggang 438000, China.
  • 6 Department of Chemistry, Pennsylvania State University, Philadelphia, Pennsylvania 19104, United States.
  • 7 Department of Chemistry, University of Aberdeen, Aberdeen AB24 3FX, U.K.
PMID: 34994554 DOI: 10.1021/acs.jmedchem.1c01736
Abstract

The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to Cancer cell Apoptosis. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.

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