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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Structural aspects of flavonoids as inhibitors of human butyrylcholinesterase.
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Structural aspects of flavonoids as inhibitors of human butyrylcholinesterase.

机译：黄酮类化合物作为人丁酰胆碱酯酶的抑制剂的结构方面。

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摘要

Selected flavonoids: galangin, kaempferol, quercetin, myricetin, fisetin, apigenin, luteolin and rutin, reversibly inhibited human butyrylcholinesterase (BChE, EC 3.1.1.8). Inhibition potency of the flavonoids we attributed to their chemical structure, i.e., the number of OH groups and their side on the phenyl ring. The most potent BChE inhibitor among the tested flavonoids was galangin, which showed 12 times higher preference for binding to BChE (7 micromol/L) than to the related enzyme human acetylcholinesterase (AChE, EC 3.1.1.7). Docking study showed that flavonoids bind to the BChE active site by forming multiple hydrogen bonds and pi-pi interactions. The UV-VIS (200-500 nm) absorption spectra of the flavonoid phosphate buffer solution (pH 7.4), with the exception of rutin, revealed time dependant changes indicating precipitation of flavonoids or in the case of myricetin, a change in the chemical structure resulting in a BChE non-inhibiting specie. Selected flavonoids showed no cytotoxic effect on HepG2 and A549 cell lines at concentrations up to 200 micromol/L. Cytotoxicity was observed only for fisetin, apigenin and luteolin in the THP-1 cell line with IC50 of 30, 60 and 70 micromol/L, respectively.
机译：选定的黄酮类化合物：Galangin，Kaempferol，槲皮素，霉味素，Fisetin，Apigenin，叶黄素和芦丁，可逆地抑制人丁酰胆碱酯酶（BCHE，EC 3.1.1.8）。黄酮类化合物的抑制效力归因于其化学结构，即苯环的OH基团及其侧面。测试的黄酮类化合物中最有效的BCHE抑制剂是Galangin，其偏好于与BCHE（7微摩洛/升）结合而不是与相关酶的乙酰胆碱酯酶（ACHE，EC 3.1.1.7）较高的偏好。对接研究表明，黄酮通过形成多种氢键和PI-PI相互作用来与BCHE活性部位结合。黄酮类磷酸盐缓冲溶液（pH7.4）的UV-Vis（200-500nm）吸收光谱除芦丁外，揭示了表明黄酮类化合物沉淀的时间依赖性变化，或在Myricetin的情况下，化学结构的变化导致BCHE无抑制物种。所选的黄酮类化合物对HepG2和A549细胞系的细胞毒性作用浓度高达200微摩尔/升。仅针对THP-1细胞系中的Fisetin，Apigenin和Lutteolin观察到细胞毒性分别与IC50的30,60和70微摩洛/升。

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