Acetylcholinesterase inhibitory activity of sesquiterpenoids isolated from Laggera pterodonta

doi:10.3389/fpls.2023.1074184

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	Acetylcholinesterase inhibitory activity of sesquiterpenoids isolated from Laggera pterodonta
	Li,Jinliang; Li,Fengchao; Wu,Guoxing; Gui,Furong; Li,Hongmei; Xu,Lili; Hao,Xiaojiang; Zhao,Yuhan; Ding,Xiao; Qin,Xiaoping
	2023
发表期刊	FRONTIERS IN PLANT SCIENCE
卷号	14 页码:1074184
摘要	Plant-derived natural products are important resources for pesticide discovery. Acetylcholinesterase (AChE) is a well-validated pesticide target, and inhibiting AChE proves fatal for insects. Recent studies have shown that the potential of various sesquiterpenoids as AChE inhibitors. However, few studies have been conducted with eudesmane-type sesquiterpenes with AChE inhibitory effects. Therefore, in this research, we isolated two new sesquiterpenes, laggeranines A (1) and B (2), along with six known eudesmane-type sesquiterpenes (3-8) from Laggera pterodonta, and characterized their structures and the inhibitory effect they exerted on AChE. The results showed that these compounds had certain inhibitory effects on AChE in a dose-dependent manner, of which compound 5 had the best inhibitory effect with IC50 of 437.33 +/- 8.33 mM. As revealed by the Lineweaver-Burk and Dixon plots, compound 5 was observed to suppress AChE activity reversibly and competitively. Furthermore, all compounds exhibited certain toxicity levels on C. elegans. Meanwhile, these compounds had good ADMET properties. These results are significant for the discovery of new AChE targeting compounds, and also enrich the bioactivity activity repertoire of L. pterodonta.
关键词	Laggera pterodonta sesquiterpenes acetylcholinesterase enzyme kinetics toxic effects DERIVATIVES FLAVONOIDS TERPENOIDS MECHANISM
学科领域	Plant Sciences
DOI	10.3389/fpls.2023.1074184
WOS记录号	WOS:000937438200001
引用统计	被引频次：1[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/74971
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Li,Jinliang,Li,Fengchao,Wu,Guoxing,et al. Acetylcholinesterase inhibitory activity of sesquiterpenoids isolated from Laggera pterodonta[J]. FRONTIERS IN PLANT SCIENCE,2023,14:1074184.
APA	Li,Jinliang.,Li,Fengchao.,Wu,Guoxing.,Gui,Furong.,Li,Hongmei.,...&Qin,Xiaoping.(2023).Acetylcholinesterase inhibitory activity of sesquiterpenoids isolated from Laggera pterodonta.FRONTIERS IN PLANT SCIENCE,14,1074184.
MLA	Li,Jinliang,et al."Acetylcholinesterase inhibitory activity of sesquiterpenoids isolated from Laggera pterodonta".FRONTIERS IN PLANT SCIENCE 14(2023):1074184.

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