Li Yibin, Ma Teng, Jiang Hao, Li Wei, Tian Di, Zhu Jintao, Li Zhong'an
Hubei Engineering Research Center for Biomaterials and Medical Protective Materials, Key Laboratory for Material Chemistry of Energy Conversion and Storage, Ministry of Education, School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan, 430074, China.
Hubei Key Laboratory of Biomass Fibers and Eco - dyeing & Finishing, Department of Chemistry and Chemical Engineering, Wuhan Textile University, Wuhan, 430073, China.
Angew Chem Int Ed Engl. 2022 Jun 13;61(24):e202203093. doi: 10.1002/anie.202203093. Epub 2022 Apr 19.
Cyanines have been widely used as the photosensitizers (PSs) in the biomedical field, but controlling their molecular aggregates in nanoparticles (NPs) remains a major challenge. Moreover, the impact of aggregate behaviors of cyanines on the photosensitization is still unclear. Herein, the first anionic cyanine PSs based on a tricyanofuran end group have been designed by achieving supramolecular J-type aggregates in NPs via counterion engineering. Our results indicate that J-type aggregates in NPs can not only bring significantly red-shifted emission, negatively charged surface, and high photostability, but also enable a significant 5-fold increase in singlet oxygen generation efficiency compared to that in the nonaggregate state, providing strong experimental evidence for the superiority of J-aggregates in enhancing photosensitization. Thus, combined with the mitochondria-targeting ability, the J-type aggregate NPs show remarkable in vivo antitumor phototheranostic efficacy, making them have a potential for clinical use.
花菁已被广泛用作生物医学领域的光敏剂（PSs），但在纳米颗粒（NPs）中控制其分子聚集体仍然是一个重大挑战。此外，花菁聚集体行为对光致敏作用的影响仍不清楚。在此，通过抗衡离子工程在纳米颗粒中实现超分子J型聚集体，设计了首个基于三氰基呋喃端基的阴离子花菁光敏剂。我们的结果表明，纳米颗粒中的J型聚集体不仅能带来显著的红移发射、带负电荷的表面和高光稳定性，而且与非聚集状态相比，单线态氧生成效率能显著提高5倍，为J聚集体在增强光致敏作用方面的优越性提供了有力的实验证据。因此，结合线粒体靶向能力，J型聚集纳米颗粒在体内显示出显著的抗肿瘤光诊疗效果，使其具有临床应用潜力。
