National Engineering Research Center for Tissue Restoration and Reconstruction, Key Laboratory of Biomedical Engineering of Guangdong Province, Key Laboratory of Biomedical Materials and Engineering of the Ministry of Education, Innovation Center for Tissue Restoration and Reconstruction, School of Biomedical Science and Engineering, School of Medicine, School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510006, China.
Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning, 530200, China.
Angew Chem Int Ed Engl. 2022 Nov 14;61(46):e202212671. doi: 10.1002/anie.202212671. Epub 2022 Oct 17.
Compared with conventional closed-shell fluorophores, radical cations provide an opportunity for development of red-to-NIR fluorophores with small sizes and easy preparation. However, most radical cations reported in the literature suffer from poor stability in water solution and are almost non-emissive. To tackle this challenge, we herein develop a deep-red-emissive and water-stable pyrrole radical cation P⋅ -DPA-Zn, which can be easily generated from P-DPA-Zn by air oxidation. The deep-red-emissive P⋅ -DPA-Zn can be used for imaging-guided mitochondria-targeted delivery of Zn into cancer cells to promote mutant p53 proteins degradation and abrogate mutp53-manifested gain of function, including reduced chemotherapy resistance, inhibited cancer cell migration, decreased tumor cell colony and sphere formation. The water-stable and deep-red emissive pyrrole radical cation is thus promising for cancer theranostic applications.
与传统的闭壳层荧光团相比，自由基阳离子为开发小尺寸、易于制备的近红外荧光团提供了机会。然而，文献中报道的大多数自由基阳离子在水溶液中稳定性差，几乎没有发光。为了解决这一挑战，我们开发了一种深红光发射、水溶性的吡咯自由基阳离子 P⋅-DPA-Zn，它可以很容易地通过空气氧化从 P-DPA-Zn 中产生。深红光发射的 P⋅-DPA-Zn 可用于成像引导的线粒体靶向递锌进入癌细胞，以促进突变型 p53 蛋白的降解并消除 mutp53 表现出的功能获得，包括降低化疗耐药性、抑制癌细胞迁移、减少肿瘤细胞集落和球体形成。因此，这种水溶性、深红光发射的吡咯自由基阳离子有望用于癌症的治疗诊断应用。
