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首页> 外文期刊>Chemistry: A European journal >Benzothiazole-Based Neutral Ratiometric Fluorescence Sensor for Amyloid Fibrils
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Benzothiazole-Based Neutral Ratiometric Fluorescence Sensor for Amyloid Fibrils

机译：基于苯并噻唑的淀粉样原纤维中性比例荧光传感器

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Early detection of amyloid fibrils is very important for the timely diagnosis of several neurological diseases. Thioflavin-T (ThT) is a gold standard fluorescent probe for amyloid fibrils and has been used for the last few decades. However, due to its positive charge, ThT is incapable of crossing the blood-brain barrier and cannot be used for in vivo imaging of fibrils. In the present work, we synthesized a neutral ThT derivative, 2-[2'-Me,4'-(dimethylamino)phenyl]benzothiazole (2Me-DABT), which showed a strong affinity towards the amyloid fibrils. On association with the amyloid fibrils, 2Me-DABT not only showed a large increase in its emission intensity, but also, unlike ThT, a large blueshift in its emission spectrum was observed. Thus, unlike ThT, 2Me-DABT is a potential candidate for the ratiometric sensor of the amyloid fibrils. Detailed photophysical properties of 2Me-DABT in amyloid fibrils and different solvent media were studied to understand its sensory activity. Fluorescence resonance energy transfer (FRET) studies suggested that the sites of localization for ThT and 2Me-DABT in amyloid fibrils are not same and their average distance of separation in amyloid fibrils was determined. The experimental data was nicely supported by molecular docking studies, which confirmed the binding of 2Me-DABT in the inner core of the amyloid fibrils.
机译：早期检测淀粉样蛋白原纤维对于及时诊断几种神经系统疾病非常重要。硫黄素-T（ThT）是用于淀粉样蛋白原纤维的金标准荧光探针，已经使用了近几十年。然而，由于其正电荷，ThT无法穿过血脑屏障，因此不能用于原纤维的体内成像。在目前的工作中，我们合成了一种中性的ThT衍生物2- [2'-Me，4'-（二甲基氨基）苯基]苯并噻唑（2Me-DABT），它对淀粉样蛋白原纤维具有很强的亲和力。与淀粉样蛋白原纤维缔合后，2Me-DABT不仅显示出其发射强度大大增加，而且与ThT不同，还观察到了其发射光谱中的大蓝移。因此，与ThT不同，2Me-DABT是淀粉样原纤维比例传感器的潜在候选者。研究了2Me-DABT在淀粉样原纤维和不同溶剂介质中的详细光物理性质，以了解其感觉活性。荧光共振能量转移（FRET）研究表明，淀粉样蛋白原纤维中ThT和2Me-DABT的定位位点不同，并且确定了它们在淀粉样蛋白原纤维中的平均分离距离。分子对接研究很好地支持了实验数据，该研究证实了2Me-DABT在淀粉样原纤维内芯中的结合。

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