Multifunctional AuI -based AIEgens: Manipulating Molecular Structures and Boosting Specific Cancer Cell Imaging and Theranostics

Jing Zhang; Hang Zou; Jinping Lei; Benzhao He; Xuewen He; Herman H Y Sung; Ryan T K Kwok; Jacky W Y Lam; Lei Zheng; Ben Zhong Tang

doi:10.1002/anie.202000048

Multifunctional Au^I -based AIEgens: Manipulating Molecular Structures and Boosting Specific Cancer Cell Imaging and Theranostics

Angew Chem Int Ed Engl. 2020 Apr 27;59(18):7097-7105. doi: 10.1002/anie.202000048. Epub 2020 Mar 5.

Authors

Jing Zhang¹, Hang Zou², Jinping Lei³, Benzhao He¹, Xuewen He¹, Herman H Y Sung¹, Ryan T K Kwok^{1

4}, Jacky W Y Lam^{1

4}, Lei Zheng², Ben Zhong Tang^{1

4

5}

Affiliations

¹ Department of Chemistry, Hong Kong Branch of Chinese National Engineering, Research Center for Tissue Restoration and Reconstruction, Institute for Advanced Study, Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.
² Department of Laboratory Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515, China.
³ School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
⁴ HKUST-Shenzhen Research Institute, No. 9 Yuexing 1st RD, South Area, Hi-tech Park, Nanshan, Shenzhen, 518057, China.
⁵ Center for Aggregation-Induced Emission, SCUT-HKUST Joint Research Institute, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou, 510640, China.

PMID: 32049411
DOI: 10.1002/anie.202000048

Abstract

Gold(I) N-heterocyclic carbene (Au^I -NHC) complexes have emerged as potential anticancer agents owing to their high cytotoxicity and stability. Integration of their above unique functions with customized aggregation-induced emission (AIE) luminogens to achieve specific bioimaging and efficient theranostics to cancer is highly desirable but is rarely studied. Now, a series of novel Au^I -NHC compounds were developed with AIE characteristics. A complex with a PPh₃ ligand was selected out as it could achieve both prominent specific imaging of various cancer cells and efficient inhibition of their growth with negligible toxic effects on normal cells due to the targeting binding and strong inhibition towards thioredoxin reductase. This complex could also act as a powerful radiosensitizer to boost the anticancer efficacy with performance superior to that of popularly used auranofin. It holds great potential as a specific and effective theranostic drug in cancer diagnosis and precise therapy.

Keywords: aggregation-induced emission; gold(I) complexes; radiosensitizers; specific bioimaging; thioredoxin reductase.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line
Cell Proliferation / drug effects
Cell Survival / drug effects
Coordination Complexes / chemical synthesis
Coordination Complexes / chemistry
Coordination Complexes / pharmacology*
Drug Design
Drug Screening Assays, Antitumor
Gold / chemistry
Gold / pharmacology*
Heterocyclic Compounds / chemistry
Heterocyclic Compounds / pharmacology*
Humans
Methane / analogs & derivatives*
Methane / chemistry
Methane / pharmacology
Molecular Structure
Optical Imaging*
Photochemotherapy
Precision Medicine
Theranostic Nanomedicine*

Substances

Antineoplastic Agents
Coordination Complexes
Heterocyclic Compounds
carbene
Gold
Methane