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2025, 06, v.47 42-48
用于光热/光动力治疗的BODIPY衍生物合成及性能研究
基金项目(Foundation): 安徽省高校自然科学研究重点项目(2023AH050731); 安徽中医药大学科学研究基金项目(2021zryb01)
邮箱(Email): lili09@ahctm.edu.cn;
DOI: 10.13822/j.cnki.hxsj.2025.0066
投稿时间: 2025-03-31
投稿日期(年): 2025
终审时间: 2025-04-30
终审日期(年): 2025
审稿周期(年): 1
发布时间: 2025-06-15
出版时间: 2025-06-15
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摘要:

开发一种兼具光热治疗(PTT)与光动力治疗(PDT)协同效应的新型光敏分子。通过分子工程策略设计并合成了双三苯胺(TPA)取代的BODIPY二聚体,采用核磁共振(NMR)和高分辨质谱(HRMS)对目标化合物的分子结构进行确证。通过系统光物理性质发现,该分子在近红外区域(780~800 nm)展现出显著红移的特征吸收,较传统BODIPY单体(500 nm)红移了近400 nm,为深层组织光疗提供了有利条件。该化合物在808 nm激光激发下展现出双重治疗特性:一方面通过能量转移途径产生单线态氧(~1O2);另一方面表现出优异的光热转换效率(η=60.6%),其光热转换效率是临床常用光敏剂吲哚菁绿(ICG)的两倍。值得关注的是,其光热稳定性经连续6次激光循环后仍保持90%以上性能,显著优于ICG的快速光漂白特性。体外实验证实,该化合物对4T1乳腺癌细胞具有显著杀伤效果,优于市售光敏剂ICG,展现出更高的生物相容度与稳定性,在深层组织治疗应用中显示出重要潜力,为开发高效近红外光疗试剂提供了新的参考策略。

Abstract:

This study aims to develop a novel photosensitizer integrating synergistic photothermal therapy(PTT) and photodynamic therapy(PDT).A molecular engineering strategy was employed to design and synthesize a bis-triphenylamine(TPA)-substituted BODIPY dimer, with its molecular structure unambiguously confirmed by nuclear magnetic resonance and high-resolution mass spectrometry.Systematic photophysical characterization of the target compound revealed a remarkably red-shifted absorption band in the near-infrared region(780~800 nm),achieving a bathochromic shift of ~400 nm compared to conventional BODIPY monomers(λmax≈500 nm),which favors deep-tissue phototherapeutic applications.Under 808 nm laser irradiation, the target compound exhibited dual therapeutic functionalities: generation of singlet oxygen(~1O2) via energy transfer pathways, and exceptional photothermal conversion efficiency(η=60.6%),doubling that of the clinically used photosensitizer indocyanine green(ICG).Notably, the material retained over 90% of its photothermal performance after six consecutive laser cycles, demonstrating superior photostability compared to ICG rapid photobleaching behavior.In vitro experiments confirm significant tumor-killing effects against 4T1 cells, outperforming commercial photosensitizer ICG.The compound also displays enhanced biocompatibility and stability, showing important potential for deep-tissue therapeutic applications.This work provides a novel reference strategy for developing high-efficiency near-infrared phototherapeutic agents.

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基本信息:

DOI:10.13822/j.cnki.hxsj.2025.0066

中图分类号:TQ422;R730.5

引用信息:

[1]谢煜琦,姜渊,张蒙,等.用于光热/光动力治疗的BODIPY衍生物合成及性能研究[J].化学试剂,2025,47(06):42-48.DOI:10.13822/j.cnki.hxsj.2025.0066.

基金信息:

安徽省高校自然科学研究重点项目(2023AH050731); 安徽中医药大学科学研究基金项目(2021zryb01)

投稿时间:

2025-03-31

投稿日期(年):

2025

终审时间:

2025-04-30

终审日期(年):

2025

审稿周期(年):

1

发布时间:

2025-06-15

出版时间:

2025-06-15

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