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Lysosome-Specific Coumarin-Based Fluorescent Bioprobes for in Vivo Polarity Sensing and Cancer Treatment
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2023-09-14 , DOI: 10.1021/acs.bioconjchem.3c00361
Xian Chen 1 , Wenjing Wang 1 , Tangying Ye 1 , Jialu Kang 1 , Qianqiu Wang 2 , Wei Yang 1 , Heshuang Dai 2 , Kai Wang 1 , Jie Pan 1
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2023-09-14 , DOI: 10.1021/acs.bioconjchem.3c00361
Xian Chen 1 , Wenjing Wang 1 , Tangying Ye 1 , Jialu Kang 1 , Qianqiu Wang 2 , Wei Yang 1 , Heshuang Dai 2 , Kai Wang 1 , Jie Pan 1
Affiliation
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About 90% of cancer deaths worldwide are caused by the spread of cancer cells from the primary tumor to distant organs (metastasis). Therefore, there is an urgent need for an early diagnosis and treatment before cancer metastasis occurs. Lysosomes have emerged as attractive targets for cancer diagnosis and treatment because polar defects in lysosomes can induce apoptosis and cell death. Coumarin is a known polar-sensitive dye with good biocompatibility; because of this, we constructed two fluorescent probes of coumarin derivatives with the “D−π–A” structure, CouN-1 and CouN-2, through three simple reactions. In molecular design, due to morpholine’s prominent lysosomal targeting characteristics, it was used as both lysosomal targeting motifs and an electron donor (D), while coumarin was used as an electron acceptor (A). The experimental results strongly proved that CouN-1 and CouN-2 have a good linear relationship with the polarity change of Δf = 0.209–0.308. In addition, both in vitro and in vivo imaging results have shown that CouN-1 and CouN-2 can specifically identify and monitor tumor sites. In the cell uptake and apoptosis experiments, the two probes also showed a strong antiproliferation effect on cancer cells. All of these characteristics demonstrated the potential of these two polarity-sensitive biological probes, CouN-1 and CouN-2, in the diagnosis and treatment of cancer.
中文翻译：
用于体内极性传感和癌症治疗的溶酶体特异性香豆素荧光生物探针
全球约 90% 的癌症死亡是由癌细胞从原发肿瘤扩散到远处器官（转移）引起的。因此，迫切需要在癌症转移发生之前进行早期诊断和治疗。溶酶体已成为癌症诊断和治疗的有吸引力的靶标，因为溶酶体的极性缺陷可以诱导细胞凋亡和细胞死亡。香豆素是一种已知的极性敏感染料，具有良好的生物相容性；为此，我们通过三个简单的反应构建了两种具有“D−π–A”结构的香豆素衍生物荧光探针CouN-1和CouN-2。在分子设计中，由于吗啉具有突出的溶酶体靶向特性，它既被用作溶酶体靶向基序又被用作电子供体（D），而香豆素被用作电子受体（A）。实验结果有力地证明了CouN-1和CouN-2与Δf = 0.209-0.308的极性变化具有良好的线性关系。此外，体外和体内成像结果均表明CouN-1和CouN-2可以特异性识别和监测肿瘤部位。在细胞摄取和凋亡实验中，两种探针也表现出对癌细胞较强的抗增殖作用。所有这些特性都证明了这两种极性敏感的生物探针CouN-1和CouN-2在癌症诊断和治疗中的潜力。
更新日期：2023-09-14
中文翻译：
用于体内极性传感和癌症治疗的溶酶体特异性香豆素荧光生物探针
全球约 90% 的癌症死亡是由癌细胞从原发肿瘤扩散到远处器官（转移）引起的。因此，迫切需要在癌症转移发生之前进行早期诊断和治疗。溶酶体已成为癌症诊断和治疗的有吸引力的靶标，因为溶酶体的极性缺陷可以诱导细胞凋亡和细胞死亡。香豆素是一种已知的极性敏感染料，具有良好的生物相容性；为此，我们通过三个简单的反应构建了两种具有“D−π–A”结构的香豆素衍生物荧光探针CouN-1和CouN-2。在分子设计中，由于吗啉具有突出的溶酶体靶向特性，它既被用作溶酶体靶向基序又被用作电子供体（D），而香豆素被用作电子受体（A）。实验结果有力地证明了CouN-1和CouN-2与Δf = 0.209-0.308的极性变化具有良好的线性关系。此外，体外和体内成像结果均表明CouN-1和CouN-2可以特异性识别和监测肿瘤部位。在细胞摄取和凋亡实验中，两种探针也表现出对癌细胞较强的抗增殖作用。所有这些特性都证明了这两种极性敏感的生物探针CouN-1和CouN-2在癌症诊断和治疗中的潜力。
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