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Mito-BWQ
BIOORGANIC CHEMISTRY · 2021 · IF 5.275

A mitochondria-targeted thiazoleorange-based photothermal agent for enhanced photothermal therapy for tumors

Wangqing Bian,Zhenxing Pan,Yakun Wang,Wei Long,Zefeng Chen,Niping Chen,Yaoxun Zeng,Jiongpeng Yuan,Xujie Liu,Yu-Jing Lu,Yan He,Kun Zhang

Organic small molecules with near-infrared (NIR) absorption hold great promise as the phototheranostic agents for clinical translation by virtue of their inherent merits such as well-defined chemical structure, high purity and good reproducibility. Probes that happen to be based on cyanine dyes exhibit strong NIR-absorbing and efficient photothermal conversion, representing a new class of photothermal agents (PAs) for photothermal therapy (PTT), and taking into account the heat susceptibility of Mitochondria (Mito), we designed and prepared a mitochondria-targeted organic small molecule (Mito-BWQ) based on thiazole orange maternal unit that can effectively kill tumor cells through the hyperpyrexia generated in the lesions under exogenous laser irradiation. The Confocal laser scanning microscope was employed to determine the preferential targeting of Mito-BWQ to the mitochondria of MCF-7 cells and U87 cells. When subjected to 600 nm laser radiation, Mito-BWQ produced an increase in temperature in test systems and this increase was dependent on both the laser power and probe concentration. In vitro tests, cytotoxicity was observed when cells were incubated with Mito-BWQ and exposed to laser irradiation. The PTT in vivo also showed that Mito-BWQ performed remarkably in tumor inhibition. This study thus provides a vital starting point for the creation of thiazole orange-based PTT formulations and promotes further advances in the field of PAs-based anticancer research and therapy.

CAS / MDL: 100587-95-9
研究领域: 肿瘤学 · 药学 · 生物医学工程 · 化学
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