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Inhibitory activities of flavonoids from Eupatorium adenophorum against acetylcholinesterase
Pesticide Biochemistry and Physiology ( IF 4.7 ) Pub Date : 2020-11-01 , DOI: 10.1016/j.pestbp.2020.104701 Mengyue Li , Xi Gao , Mingxian Lan , Xianbin Liao , Fawu Su , Liming Fan , Yuhan Zhao , Xiaojiang Hao , Guoxing Wu , Xiao Ding
Pesticide Biochemistry and Physiology ( IF 4.7 ) Pub Date : 2020-11-01 , DOI: 10.1016/j.pestbp.2020.104701 Mengyue Li , Xi Gao , Mingxian Lan , Xianbin Liao , Fawu Su , Liming Fan , Yuhan Zhao , Xiaojiang Hao , Guoxing Wu , Xiao Ding
Fifteen flavonoids isolated from the Eupatorium adenophorum showed inhibitory activities against acetylcholinesterase (AChE) isolated from Caenorhabditis elegans and Spodoptera litura. Their IC50 values ranged from 12.54 to 89.06μg/mL and 12.08 to 86.01μg/mL, respectively against the AChE isolated from the nematode and insect species. AChE was inhibited in a dose-dependent manner by all tested flavonoids, The isolated compound quercetagetin-7-O-(6-O-caffeoyl-β-D-glucopyranoside) displayed the highest inhibitory effect against AChE from C. elegans and S. litura, with IC50 values of 12.54 μg/mL and 12.58 μg/mL, respectively. The structure-activity relationship of flavonoids on the inhibitory activities indicated that additional phenolic hydroxyl groups in the glucose were favorable for their inhibitory effects and the degree of increase in inhibitory activity also depended on the number of phenolic hydroxyl groups. The Lineweaver-Burk and Dixon plots indicated that quercetagetin-7-O-(6-O-caffeoyl-β-d-glucopyranoside) is a reversible inhibitor against AChE. Quercetagetin-7-O-(6-O-caffeoyl-β-d-glucopyranoside), 5,4'-Dihydroxytlavone and quercetin-3-O-β-d-glucopyranoside inhibited AChE in a mixed-type competitive manner and these compounds might be the dual binding site AChE inhibitors. Further, nine compounds showed poisonous effects against C. elegans and inhibitory effects on the growth and development of S. litura.
中文翻译:
紫茎泽兰黄酮类化合物对乙酰胆碱酯酶的抑制作用
从紫茎泽兰分离的 15 种黄酮类化合物对从秀丽隐杆线虫和斜纹夜蛾中分离的乙酰胆碱酯酶 (AChE) 显示出抑制活性。它们对从线虫和昆虫物种中分离的 AChE 的 IC50 值范围分别为 12.54 至 89.06μg/mL 和 12.08 至 86.01μg/mL。所有测试的黄酮类化合物都以剂量依赖性方式抑制 AChE,分离的化合物槲皮素-7-O-(6-O-咖啡酰-β-D-吡喃葡萄糖苷)对来自秀丽隐杆线虫和 S. elegans 的 AChE 显示出最高的抑制作用。斜纹夜蛾的 IC50 值分别为 12.54 μg/mL 和 12.58 μg/mL。黄酮类化合物对抑制活性的构效关系表明,葡萄糖中额外的酚羟基有利于其抑制作用,抑制活性的增加程度也取决于酚羟基的数量。Lineweaver-Burk 和 Dixon 图表明槲皮素-7-O-(6-O-咖啡酰-β-d-吡喃葡萄糖苷)是一种可逆的 AChE 抑制剂。Quercetagetin-7-O-(6-O-caffeoyl-β-d-glucopyranoside)、5,4'-Dihydroxytlavone 和 quercetin-3-O-β-d-glucopyranoside 以混合型竞争方式抑制 AChE,这些化合物可能是双结合位点 AChE 抑制剂。此外,九种化合物显示出对秀丽隐杆线虫的毒性作用和对斜纹夜蛾生长和发育的抑制作用。
更新日期:2020-11-01
中文翻译:
紫茎泽兰黄酮类化合物对乙酰胆碱酯酶的抑制作用
从紫茎泽兰分离的 15 种黄酮类化合物对从秀丽隐杆线虫和斜纹夜蛾中分离的乙酰胆碱酯酶 (AChE) 显示出抑制活性。它们对从线虫和昆虫物种中分离的 AChE 的 IC50 值范围分别为 12.54 至 89.06μg/mL 和 12.08 至 86.01μg/mL。所有测试的黄酮类化合物都以剂量依赖性方式抑制 AChE,分离的化合物槲皮素-7-O-(6-O-咖啡酰-β-D-吡喃葡萄糖苷)对来自秀丽隐杆线虫和 S. elegans 的 AChE 显示出最高的抑制作用。斜纹夜蛾的 IC50 值分别为 12.54 μg/mL 和 12.58 μg/mL。黄酮类化合物对抑制活性的构效关系表明,葡萄糖中额外的酚羟基有利于其抑制作用,抑制活性的增加程度也取决于酚羟基的数量。Lineweaver-Burk 和 Dixon 图表明槲皮素-7-O-(6-O-咖啡酰-β-d-吡喃葡萄糖苷)是一种可逆的 AChE 抑制剂。Quercetagetin-7-O-(6-O-caffeoyl-β-d-glucopyranoside)、5,4'-Dihydroxytlavone 和 quercetin-3-O-β-d-glucopyranoside 以混合型竞争方式抑制 AChE,这些化合物可能是双结合位点 AChE 抑制剂。此外,九种化合物显示出对秀丽隐杆线虫的毒性作用和对斜纹夜蛾生长和发育的抑制作用。