Barut Burak, Baş Hüseyin, Biyiklioğlu Zekeriya
Department of Biochemistry, Karadeniz Technical University, Trabzon Turkey.
Department of Chemistry, Karadeniz Technical University, Trabzon Turkey.
Turk J Chem. 2021 Oct 19;45(5):1567-1575. doi: 10.3906/kim-2105-69. eCollection 2021.
In this study, the synthesis of new monostyryl () and distyryl BODIPY dyes () containing pyridine groups has been reported for the first time. The acetylcholinesterase from (AChE), butyrylcholinesterase from equine serum (BuChE), α-glucosidase from and DNA hydrolytic cleavage actions of , , were investigated using various techniques. The results indicated that the compounds had varying inhibition properties against AChE, BuChE, and α-glucosidase. was the most potent compound on AChE with IC of 54.78 ± 4.51 µM, and Lineweaver-Burk plots indicated that the compound is bound to a site other than the active site as a noncompetitive inhibitor. The compound-protein binding experiment showed that changed the microenvironment around AChE. On the other hand, the compounds showed lower α-glucosidase inhibition than the positive control. The DNA hydrolytic cleavage effects were not observed on supercoiled plasmid DNA in the presence of the compounds as compared to negative controls. These findings suggested that might be a promising compound to treat Alzheimer's diseases.
在本研究中,首次报道了含吡啶基团的新型单苯乙烯基()和二苯乙烯基BODIPY染料()的合成。使用各种技术研究了来自(AChE)的乙酰胆碱酯酶、马血清中的丁酰胆碱酯酶(BuChE)、来自的α-葡萄糖苷酶以及、、的DNA水解切割作用。结果表明,这些化合物对AChE、BuChE和α-葡萄糖苷酶具有不同的抑制特性。是对AChE最有效的化合物,IC为54.78±4.51μM,Lineweaver-Burk图表明该化合物作为非竞争性抑制剂与活性位点以外的位点结合。化合物-蛋白质结合实验表明改变了AChE周围的微环境。另一方面,这些化合物对α-葡萄糖苷酶的抑制作用低于阳性对照。与阴性对照相比,在化合物存在下未观察到超螺旋质粒DNA的DNA水解切割作用。这些发现表明可能是治疗阿尔茨海默病的一种有前景的化合物。