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一种新的特异性针对硫酸乙酰肝素的近红外荧光增强探针,它能够使小鼠结直肠癌细胞中的硫酸乙酰肝素水平可视化。

A new HS-specific near-infrared fluorescence-enhanced probe that can visualize the HS level in colorectal cancer cells in mice.

作者信息

Zhang Kun, Zhang Jie, Xi Zhen, Li Lu-Yuan, Gu Xiangxiang, Zhang Qiang-Zhe, Yi Long

机构信息

State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy , Tianjin Key Laboratory of Molecular Drug Research , Nankai University , Tianjin 300071 , China . Email:

State Key Laboratory of Organic-Inorganic Composites and Beijing Key Laboratory of Energy Environmental Catalysis , Beijing University of Chemical Technology (BUCT) , 15 Beisanhuan East Road, Chaoyang District , Beijing 100029 , China . Email:

出版信息

Chem Sci. 2017 Apr 1;8(4):2776-2781. doi: 10.1039/c6sc05646f. Epub 2017 Jan 17.

Abstract

Near-infrared (NIR) fluorescence-based sensors capable of selective detection of HS would be useful tools to understand the mechanisms of diseases. A new NIR fluorescence probe was developed for the detection of endogenous HS in colorectal cancer cells in mice. displayed an 87-fold fluorescence enhancement at 796 nm (with excitation at 730 nm) when reacted with HS in a buffer (pH 7.4). was water-soluble, cell-membrane-permeable, had low cytotoxicity and high selectivity and sensitivity for HS. The properties of enable its use in monitoring endogenous HS in living cells, tissues, and mice. The bioimaging results indicated that (1) d-Cys could induce endogenous HS production in living cells and stimulate angiogenesis; (2) tail intravenous injection of into mice generated strong fluorescence in the liver while intraperitoneal injection of d-Cys could further enhance fluorescence in the liver ; (3) importantly, endogenous HS in colorectal cancer cells (HCT116, HT29) and in murine tumor models could be quickly and selectively detected by intratumoral injection of . These results indicated that our new probe could serve as an efficient tool for the detection of cellular HS in living animals and even for cancer diagnosis.

摘要

能够选择性检测硫化氢(HS)的基于近红外(NIR)荧光的传感器将成为理解疾病机制的有用工具。一种新型近红外荧光探针被开发用于检测小鼠结肠癌细胞中的内源性HS。当在缓冲液(pH 7.4)中与HS反应时,它在796 nm处(激发波长为730 nm)显示出87倍的荧光增强。该探针具有水溶性、细胞膜通透性、低细胞毒性以及对HS的高选择性和高灵敏度。这些特性使其能够用于监测活细胞、组织和小鼠中的内源性HS。生物成像结果表明:(1)d-半胱氨酸可诱导活细胞内源性HS产生并刺激血管生成;(2)将该探针尾静脉注射到小鼠体内时肝脏产生强烈荧光,而腹腔注射d-半胱氨酸可进一步增强肝脏中的荧光;(3)重要的是,通过瘤内注射该探针可快速、选择性地检测结肠癌细胞(HCT116、HT29)和小鼠肿瘤模型中的内源性HS。这些结果表明,我们的新型探针可作为在活体动物中检测细胞内HS甚至用于癌症诊断的有效工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6f3/5426460/972de1898e01/c6sc05646f-s1.jpg

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