Novel Water-Soluble Chlorin-Based Photosensitizer for Low-Fluence Photodynamic Therapy

Liu Wang; Guangzhe Li; Lei Cao; Kun Shao; Yueqing Li; Xi Zhang; Jianzhang Zhao; Weijie Zhao

doi:10.1021/acsptsci.1c00249

Novel Water-Soluble Chlorin-Based Photosensitizer for Low-Fluence Photodynamic Therapy

ACS Pharmacol Transl Sci. 2022 Jan 21;5(2):110-117. doi: 10.1021/acsptsci.1c00249. eCollection 2022 Feb 11.

Authors

Liu Wang¹, Guangzhe Li¹, Lei Cao¹, Kun Shao², Yueqing Li¹, Xi Zhang¹, Jianzhang Zhao², Weijie Zhao¹

Affiliations

¹ State Key Laboratory of Fine Chemicals, Department of Pharmaceutical Sciences, School of Chemical Engineering, Dalian University of Technology, Dalian 116024, China.
² State Key Laboratory of Fine Chemicals, School of Chemical Engineering, Dalian University of Technology, Dalian 116024, China.

Abstract

Photodynamic therapy (PDT), performed with low-fluence rates, can improve antitumor responses and prevent adverse effects. However, photosensitizers (PSs) for low-fluence PDT treatment are rarely reported. Herein, we exploited an amphiphilic chlorin-based PS, named DYSP-C34, which has a variety of beneficial biological properties, such as improved water solubility, better cellular permeability, specific localization and enhanced phototoxicity under low light dose irradiation. In addition, DYSP-C34 could effectively accumulate in a mouse subcutaneous xenograft tumor and exhibit substantial tumor regression after irradiation with an extremely low light fluence (6 J/cm²). Meanwhile, the excellent phototoxicity could stimulate the host immune system and lead to a strong inhibition of tumor growth synergistically. These results indicated the potential value of DYSP-C34 as a chlorin-type PS for low-fluence PDT application.