Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities

doi:10.1039/d2md00156j

KIB OpenIR

	Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities
	Li, Tian-Ze; Hu, Jing; Sun, Jin-Jin; Huang, Xiao-Yan; Geng, Chang-An; Liu, Shu-Bai; Zhang, Xue-Mei; Chen, Ji-Jun
	2022
发表期刊	RSC MEDICINAL CHEMISTRY
卷号	13 期号:10 页码:1212-1224
摘要	Our previous study demonstrated that paeoveitol D, a benzofuran compound isolated from Paeonia veitchii, displayed activity on MT1 and MT2 receptors with agonistic ratios of 57.5% and 51.6% at a concentration of 1 mM. To explore the structure-activity relationships, 34 paeoveitol D derivatives were synthesized and evaluated for their MT1 and MT2 agonistic activities using the Fluo-8 calcium assay. Among them, 16 and 18 derivatives increased agonistic activities on the MT1 and MT2 receptors, respectively. Compound 18 indicated EC50 values of 21.0 and 298.9 mu M on MT1 and MT2 receptors in agonistic dose response curves with Tango assays and shortened immobility time in the forced swim test. The preliminary mechanism-of-action investigation manifested that the antidepressant activity of compound 18 may be mediated by promoting serotonin (5-HT) and dopamine (DA) levels in the mice brain. Compound 18 also showed favorable pharmacokinetic profiles and low toxicity in vivo. These results suggest that compound 18 could be a potential antidepressant agent.
关键词	BENZOFURAN
DOI	10.1039/d2md00156j
收录类别	SCI
WOS记录号	WOS:000840456300001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/74656
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Li, Tian-Ze,Hu, Jing,Sun, Jin-Jin,et al. Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities[J]. RSC MEDICINAL CHEMISTRY,2022,13(10):1212-1224.
APA	Li, Tian-Ze.,Hu, Jing.,Sun, Jin-Jin.,Huang, Xiao-Yan.,Geng, Chang-An.,...&Chen, Ji-Jun.(2022).Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.RSC MEDICINAL CHEMISTRY,13(10),1212-1224.
MLA	Li, Tian-Ze,et al."Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities".RSC MEDICINAL CHEMISTRY 13.10(2022):1212-1224.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
10.1039_d2md00156j.p（932KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	浏览下载