Effects of Picrasma quassioides and its active constituents on Alzheimer's disease in vitro and in vivo |
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| Institution: | 1. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China;2. School of Chemistry and Chemical Engineering, Yantai University, Yantai 264005, China;3. State Key Laboratory of Natural Medicine and Traditional Chinese Medicine Injections, Jiangxi Qingfeng Pharmaceutical Co., Ltd., Ganzhou 341000, China;1. Cognitive and Neuroscience Research Center (CNRC), Tehran Medical Sciences Branch, Islamic Azad University, Tehran, Iran;2. Department of Exercise Physiology, School of Physical Education and Sport Sciences, Islamic Azad University, Central Tehran Branch, Tehran, Iran;3. Department of Biology, Faculty of Sciences, University of Zanjan, Zanjan, Iran;4. Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran;5. Iranian National Center for Addiction Studies, Tehran University of Medical Sciences, Tehran, Iran;6. Institute for Cognitive Science Studies (ICSS), Tehran, Iran;1. School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;2. Chinese People''s Liberation Army 210 Hospital, Dalian 116021, China;3. Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China |
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| Abstract: | Alzheimer disease (AD), a prevalent neurodegenerative disorder, is one of the leading causes of dementia. However, there is no effective drug for this disease to date. Picrasma quassioides (D.Don) Benn, a Chinese traditional medicine, was used mainly for the treatment of inflammation, fever, microbial infection and dysentery. In this paper, we reported that the EtOAc extract of Picrasma quassioides stems showed potential neuroprotective activities in l-glutamate-stimulated PC12 and Aβ25-35-stimulated SH-SY5Y cell models, as well as improved memory and cognitive abilities in AD mice induced by amyloid-β peptide. Moreover, it was revealed that the anti-AD mechanism was related to suppressing neuroinflammatory and reducing Aβ1-42 deposition using ELISA assay kits. To clarify the active components of the EtOAc extract of Picrasma quassioides stems, a systematic phytochemistry study led to isolate and identify six β-carboline alkaloids (1–6), seven canthin-6-one alkaloids (7–13), and five quassinoids (14–18). Among them, four β-carbolines (1–3, and 6) and six canthin-6-ones (7–11, and 13) exhibited potential neuroprotective activities in vitro. Based on these date, the structure-activity relationships of alkaloids were discussed. Furthermore, molecular docking experiments showed that compounds 2 and 3 have high affinity for both of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYPKIA) and butyrylcholinesterase (BuChE). |
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| Keywords: | Alkaloids Alzheimer’s disease |
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