Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities
文献类型：期刊论文
| 作者 | Li, Tian-Ze; Hu, Jing; Sun, Jin-Jin; Huang, Xiao-Yan; Geng, Chang-An ; Liu, Shu-Bai; Zhang, Xue-Mei; Chen, Ji-Jun
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| 刊名 | RSC MEDICINAL CHEMISTRY
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| 出版日期 | 2022 |
| 卷号 | 13期号:10页码:1212-1224 |
| 关键词 | BENZOFURAN |
| DOI | 10.1039/d2md00156j |
| 英文摘要 | 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. |
| WOS记录号 | WOS:000840456300001 |
| 源URL | [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. |
入库方式： OAI收割
来源：昆明植物研究所
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