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.
Department of Laboratory Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515, China.
Angew Chem Int Ed Engl. 2020 Apr 27;59(18):7097-7105. doi: 10.1002/anie.202000048. Epub 2020 Mar 5.
Gold(I) N-heterocyclic carbene (Au -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 -NHC compounds were developed with AIE characteristics. A complex with a PPh 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.
金（I）氮杂环卡宾（Au-NHC）配合物因其高细胞毒性和稳定性而成为有潜力的抗癌药物。将其上述独特功能与定制的聚集诱导发射（AIE）发光体集成，以实现对癌症的特定生物成像和高效治疗，这是非常理想的，但很少有研究。现在，开发了一系列具有 AIE 特性的新型 Au-NHC 化合物。由于靶向结合和对硫氧还蛋白还原酶的强烈抑制作用，选择出带有 PPh 配体的复合物，因为它可以实现各种癌细胞的显著特异性成像，并有效抑制其生长，而对正常细胞几乎没有毒性作用。该复合物还可以作为一种强大的放射增敏剂，提高抗癌疗效，性能优于常用的金诺芬。它在癌症诊断和精确治疗方面作为一种特异性和有效的治疗药物具有巨大的潜力。
