Fungal infection poses and increased risk to human health. Photodynamic therapy (PDT) as an alternative antifungal approach garners much interest due to its minimal side effects and negligible antifungal drug resistance. Herein, we develop stereoisomeric photosensitizers ((Z)- and (E)-TPE-EPy) by harnessing different spatial configurations of one molecule. They possess aggregation-induced emission characteristics and ROS, viz. ¹O₂ and O₂^−• generation capabilities that enable image-guided PDT. Also, the cationization of the photosensitizers realizes the targeting of fungal mitochondria for antifungal PDT killing. Particularly, stereoisomeric engineering assisted by supramolecular assembly leads to enhanced fluorescence intensity and ROS generation efficiency of the stereoisomers due to the excited state energy flow from nonradiative decay to the fluorescence pathway and intersystem (ISC) process. As a result, the supramolecular assemblies based on (Z)- and (E)-TPE-EPy show dramatically lowered dark toxicity without sacrificing their significant phototoxicity in the photodynamic antifungal experiments. This study is a demonstration of stereoisomeric engineering of aggregation-induced emission photosensitizers based on (Z)- and (E)-configurations.

真菌感染对人类健康构成威胁并增加风险。光动力疗法 (PDT) 作为一种替代的抗真菌方法，由于其最小的副作用和可忽略不计的抗真菌耐药性而备受关注。在此，我们通过利用一个分子的不同空间构型开发立体异构光敏剂 (( Z )- 和 ( E )-TPE-EPy)。它们具有聚集诱导的发射特性和 ROS，即。¹ O ₂和 O ₂ ^-•启用图像引导 PDT 的生成功能。此外，光敏剂的阳离子化实现了真菌线粒体的靶向，用于抗真菌 PDT 杀伤。特别是，由于从非辐射衰变到荧光途径和系统间 (ISC) 过程的激发态能量流，超分子组装辅助的立体异构工程导致立体异构体的荧光强度和 ROS 生成效率增强。因此，基于 ( Z )- 和 ( E )-TPE-EPy 的超分子组装体在光动力抗真菌实验中显示出显着降低的暗毒性，而不会牺牲其显着的光毒性。本研究展示了基于（Z )- 和 ( E )- 配置。