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生物碱与香豆素——安全性与药理活性的比较评估

, Alkaloids and Coumarins-A Comparative Assessment of Safety and Pharmacological Activity.

作者信息

Herbet Mariola, Widelski Jarosław, Piątkowska-Chmiel Iwona, Pawłowski Kamil, Dymek Aleksandra, Mroczek Tomasz

机构信息

Department of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 20-090 Lublin, Poland.

Department of Pharmacognosy with the Medicinal Plant Garden, Medical University of Lublin, 20-093 Lublin, Poland.

出版信息

J Clin Med. 2022 Jul 23;11(15):4291. doi: 10.3390/jcm11154291.

DOI:10.3390/jcm11154291
PMID:35893381
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9332316/
Abstract

The study aimed to evaluate the safety and pharmacological activity , alkaloids and coumarins obtained from L., L., L., L. and (Hoffm.) Benth. & Hook.f. ex Franch. & Sav. In the in vivo studies. The influence of the tested compounds on the central nervous system of rats was assessed in behavioral tests (locomotor activity, Y-maze, passive avoidance). In order to investigate the mechanisms of action, biochemical determinations were performed (AChE activity, BChE activity, IL-1β, IL-6 concentration). In order to assess safety, the concentrations of AST, ALT, GGT and urea and creatinine were determined. The results of the conducted studies indicate a high safety profile of the tested compounds. Behavioral tests showed that they significantly improved rodent memory in a passive avoidance test. The results of biochemical studies showed that by reducing the activity of AChE and BChE and lowering the concentration of IL-1β and IL-6, the coumarin-rich extract shows the most promising potential for future therapeutic AD strategies.

摘要

该研究旨在评估从[具体植物名称1]、[具体植物名称2]、[具体植物名称3]、[具体植物名称4]和[具体植物名称5]中获得的生物碱和香豆素在体内研究中的安全性和药理活性。在行为测试(运动活性、Y迷宫、被动回避)中评估了受试化合物对大鼠中枢神经系统的影响。为了研究作用机制,进行了生化测定(乙酰胆碱酯酶活性、丁酰胆碱酯酶活性、白细胞介素-1β、白细胞介素-6浓度)。为了评估安全性,测定了天冬氨酸转氨酶、丙氨酸转氨酶、γ-谷氨酰转移酶以及尿素和肌酐的浓度。所进行研究的结果表明受试化合物具有较高的安全性。行为测试表明,它们在被动回避测试中显著改善了啮齿动物的记忆力。生化研究结果表明,富含香豆素的提取物通过降低乙酰胆碱酯酶和丁酰胆碱酯酶的活性以及降低白细胞介素-1β和白细胞介素-6的浓度,显示出未来治疗阿尔茨海默病策略最有前景的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/3d17cc0d59ef/jcm-11-04291-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/67d56cab4ee1/jcm-11-04291-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/a5155e150c06/jcm-11-04291-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/ad45d53bdf14/jcm-11-04291-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/8d691e17670c/jcm-11-04291-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/3d17cc0d59ef/jcm-11-04291-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/67d56cab4ee1/jcm-11-04291-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/a5155e150c06/jcm-11-04291-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/ad45d53bdf14/jcm-11-04291-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/8d691e17670c/jcm-11-04291-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7742/9332316/3d17cc0d59ef/jcm-11-04291-g005a.jpg

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Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis.乙酰胆碱酯酶抑制剂在神经退行性疾病治疗中的作用及其在发病机制中的作用。
Int J Mol Sci. 2021 Aug 27;22(17):9290. doi: 10.3390/ijms22179290.
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Effects of the Hydroethanolic Extract of L. on Scopolamine-Induced Memory Deficits in Zebrafish.
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Pharmaceuticals (Basel). 2021 Jun 14;14(6):568. doi: 10.3390/ph14060568.
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The Bioassay-Guided Fractionation and Identification of Potent Acetylcholinesterase Inhibitors from Using Optimized Vacuum Liquid Chromatography, High Resolution Mass Spectrometry and Bioautography.采用优化的真空液相色谱、高分辨率质谱和生物自显影法对[来源]中强效乙酰胆碱酯酶抑制剂进行生物测定指导的分级分离和鉴定。
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