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卤素和吡啶协同跨血脑屏障调制,可视化癫痫脑中硫醇通量。

Synergistic Modulation by Halogens and Pyridine Crossing the Blood-Brain Barrier for Visualization of Thiol Flux in the Epileptic Brain.

机构信息

Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of the Ministry of Education, Chemical Biology Key Laboratory of Hebei Province, College of Chemistry & Environmental Science, Hebei University, Baoding 071002, China.

Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Institute of Molecular Science, Shanxi University, Taiyuan 030006, China.

出版信息

Anal Chem. 2022 Oct 18;94(41):14443-14452. doi: 10.1021/acs.analchem.2c03390. Epub 2022 Oct 5.

Abstract

Epilepsy is a nervous system disease, and seizures are closely related to oxidative stress. Thiols, as the main antioxidant in an organism, play a key role in regulating the redox balance and defending from oxidative stress. As a result of the complexity of the brain structure, there is still a lack of suitable detection methods of thiols to reveal the relationship between epilepsy and thiol level fluctuations. Therefore, by combining picolinate as the new recognition site for thiols, parallel synthesis, and the fluorescence rapid screening method, was developed as a rapid, highly sensitive, and selective probe to monitor thiols and . It is worth noting that effectively crossed the blood-brain barrier (BBB) to reveal the negative relationship between the level of thiols and the occurrence of epilepsy and may further provide important information for the prevention and treatment of thiol-related neurological diseases.

摘要

癫痫是一种神经系统疾病,癫痫发作与氧化应激密切相关。巯基作为生物体内的主要抗氧化剂,在调节氧化还原平衡和抵御氧化应激方面发挥着关键作用。由于大脑结构的复杂性,目前仍然缺乏合适的巯基检测方法来揭示癫痫与巯基水平波动之间的关系。因此,通过将吡啶甲酸酯作为新的巯基识别位点,结合平行合成和荧光快速筛选方法,开发了作为一种快速、高灵敏度和选择性的探针来监测巯基和 。值得注意的是, 有效地穿过血脑屏障 (BBB),揭示了巯基水平与癫痫发生之间的负相关关系,这可能为预防和治疗与巯基相关的神经疾病提供重要信息。

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