A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy,Journal of Medicinal Chemistry

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A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-01-07 , DOI: 10.1021/acs.jmedchem.1c01736
Yishen Liu _{1,

2,

3,

4} , Qianqian Li _{3,

5} , Meijia Gu ₁ , Disheng Lu _{1,

2,

3,

4} , Xiaoxing Xiong ₁ , Zhiyun Zhang _{1,

4} , Yanna Pan _{1,

4} , Yuqin Liao _{1,

4} , Qihang Ding _{1,

4} , Wanxia Gong _{1,

4} , Dean Shuailin Chen ₆ , Mengting Guan ₄ , Junzhu Wu ₄ , Zhiquan Tian ₂ , Hai Deng ₇ , Lijuan Gu ₁ , Xuechuan Hong _{1,

2,

4} , Yuling Xiao _{1,

3}

Affiliation

The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG_2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to cancer cell apoptosis. HL-PEG_2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.

中文翻译：

用于协同化学光热疗法的第二近红外钌 (II) 多吡啶基配合物

顺铂的临床成功开启了金属药物应用的新纪元。然而，在实践中，耐药性、肿瘤复发和药物全身毒性使患者无法完全治愈。在此，我们成功地将电子受体 [1, 2, 5]噻二唑并[3,4- g ]喹喔啉转化为新型的第二近红外 (NIR-II) 荧光团H7。PEG化和螯合后，HL-PEG _2k表现出波长红移、增强的光热转换效率（41.77%）和对胶质瘤的抗肿瘤作用。探索了其在体内肿瘤追踪和图像引导的化学光热治疗方面的潜力。此后获得高水平的吸收和高分辨率的 NIR-II 成像结果。热疗效应可破坏溶酶体膜，进而加重线粒体功能障碍，使细胞周期停滞在G2期，最终导致癌细胞凋亡。HL-PEG _2k显示出优异的生物相容性，因此可以成为对抗肿瘤生长和复发的潜在治疗诊断平台。

更新日期：2022-02-10

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