BODIPY-Based Photothermal Agent Incorporating Azulene for Enhanced NIR Absorption and Tumor Ablation.

IF 4.5 2区医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL

Molecular Pharmaceutics Pub Date : 2025-05-05 Epub Date: 2025-04-01 DOI:10.1021/acs.molpharmaceut.5c00071

Kai Nishimura, Mikiya Kato, Tomoya Fukui, Kazuki Miura, Masato Tsuda, Satoshi Okada, Takanori Fukushima, Hiroyuki Nakamura

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引用次数: 0

Abstract

Photothermal therapy (PTT) is a promising minimally invasive treatment that converts light energy into localized heat for tumor ablation. Indocyanine green (ICG), the only clinically approved photothermal agent (PTA), suffers from rapid photobleaching and poor tumor retention, underscoring the urgent need for next-generation PTAs with improved properties. In this study, we report AzuGlu-BODIPY, a novel azulene-containing BODIPY-based PTA incorporating 1,2,3,4-tetrahydroquinoline and glucose, designed to overcome these limitations. AzuGlu-BODIPY demonstrates a high photothermal conversion efficiency (PCE) of 51%, effective near-infrared (NIR) absorption, and thermal stability in both dimethyl sulfoxide (DMSO) and aqueous solutions. In vitro studies revealed potent photothermal efficacy against cancer cell lines, with IC₅₀ values of 3.1-4.6 μM under 808 nm laser irradiation, while in vivo experiments showed complete tumor regression in 4T1 tumor-bearing mice following localized administration and laser treatment. These results suggest AzuGlu-BODIPY as a promising PTA and provide a versatile platform for advancing azulene-based PTAs with enhanced functionality for PTT.

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含Azulene的bodipy光热剂增强近红外吸收和肿瘤消融。

光热疗法（PTT）是一种将光能转化为局部热用于肿瘤消融的微创治疗方法。吲哚菁绿（ICG）是临床唯一批准的光热剂（PTA），存在光漂快、肿瘤滞留性差的问题，迫切需要性能更好的下一代光热剂。在这项研究中，我们报道了AzuGlu-BODIPY，一种新型的含azulu - bodipy的PTA，含有1,2,3,4-四氢喹啉和葡萄糖，旨在克服这些局限性。AzuGlu-BODIPY在二甲亚砜（DMSO）和水溶液中均表现出高达51%的光热转换效率（PCE）、有效的近红外（NIR）吸收和热稳定性。体外实验显示，在808 nm激光照射下，其对肿瘤细胞具有较强的光热作用，IC50值为3.1 ~ 4.6 μM；体内实验显示，局部给药和激光治疗后，4T1荷瘤小鼠的肿瘤完全消退。这些结果表明AzuGlu-BODIPY是一种很有前途的PTA，并为开发具有增强PTT功能的基于azulu - bodipy的PTA提供了一个多功能平台。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Molecular Pharmaceutics 医学-药学

CiteScore

8.00

自引率

6.10%

发文量

391

审稿时长

2 months

期刊介绍： Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.