Thiophene π-Bridge Manipulation of NIR-II AIEgens for Multimodal Tumor Phototheranostics

Rui

Sen

NIR-Ⅱ FLI

Thiophene π-Bridge Manipulation of NIR-II AIEgens for Multimodal Tumor Phototheranostics

Journal:Angewandte Chemie-International Edition, IF=16.1

Pub Date:2024-02-12

First Author:Yixiong Gui, Yuanwei Wang, Deliang Wang

Corresponding Authors:Dingyuan Yan*, Ben Zhong Tang*, and Dong Wang*

Corresponding Author Institution:

School of Science and Engineering, Shenzhen Institute of Aggregate Science and Technology, The Chinese University of Hong Kong, Shenzhen (CUHK-Shenzhen), Shenzhen, 2001 Longxiang Boulevard, Longgang District, Shenzhen City, Guangdong 518172, China.

Introduction

Cancer

Based on the development of multimodal phototherapy diagnostic agents for tumor treatment, this study highlights the significance of AIEgens, particularly those with NIR-II fluorescence, as powerful tools for cancer therapy. Various thiophene π-bridges such as ortho-alkylated thiophene, 3,4-ethylenedioxythiophene, and benzo-thiophene have been commonly used to construct NIR-II AIEgens, but their subtle differences in therapeutic applications have not been thoroughly investigated. This paper systematically studies the AIEgen BTNS containing benzo-thiophene, which exhibits strong NIR-II fluorescence emission intensity, efficient reactive oxygen species (ROS) generation capability, and excellent photothermal conversion efficiency. Consequently, BTNS nanoparticles demonstrate unprecedented performance in tumor synergistic photodynamic/photothermal therapy guided by NIR-II fluorescence/photoacoustic/photothermal imaging.

Research

Contents

NIR-Ⅱ FLI

This research focuses on the precise modulation of thiophene π-bridges to develop NIR-II AIEgens for multimodal phototherapy of tumors. Benzo-thiophene, with its longer conjugation length and dense spatial barrier, stands out as the optimal candidate among the five commonly used π-bridges for constructing NIR-II AIEgens. Both experimental and theoretical studies demonstrate that BT-NS containing benzo-thiophene exhibits a twisted molecular skeleton, substantial NIR-II FLI quantum yield, excellent photothermal conversion efficiency for implementing PTT, and outstanding ROS generation capability for executing PDT. Leveraging these properties, BT-NS NPs successfully facilitated NIR-II FLI/PAI/PTI guided PDT/PTT tumor treatment in 4T1 tumor-bearing mice, showcasing remarkable therapeutic efficacy and good biocompatibility. This study undoubtedly provides valuable guidance for the on-demand design of multifunctional NIR-II AIEgens through π-bridge modulation.