New acetylcholinesterase inhibitors isolated from Delphinium uncinatum |
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| Institution: | 1. Department of Chemistry, University of Malakand, Chakdara, Dir (L) 18550, KP, Pakistan;2. Department of Pharmacy, Shaheed Benazir Bhutto University, Sheringal Dir (U) 18000, KP, Pakistan;3. College of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024, China;4. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College Huazhong University of Science and Technology, Wuhan 430030, China;5. Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, Taif University, P.O Box 11099, Taif 21944, Saudi Arabia;6. Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, Bandar, Puncak Alam 42300, Selangor, Malaysia;7. Atta-Ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, Bandar, Puncak Alam 42300, Selangor, Malaysia |
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| Abstract: | The inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is presently the most common pharmacological approach available for Alzheimer’s disease (AD). Despite research on the molecular bases of AD, potent therapeutic agent against its expansion is still needed. In searching for natural cholinesterase inhibitors, the present study was focused on the isolation of three new norditerpenoid alkaloids, uncinatine B-D together with known virescenine from Delphinium uncinatum. Chemical structures for all the isolated norditerpenoids (1–4) were established using latest spectroscopic techniques. The isolated undescribed compounds along with known virescenine were testified for their acetylcholinesterase inhibitory activity supported by docking analyses. Molecular docking simulation showed that the isolated compounds (1–4) were observed to adhered in the active site of AChE with docking scores ? 13.5322 (1), ?11.8173 (2), ?12.4240 (3) and ? 8.9352 (4) respectively. Overall results demonstrated that these natural norditerpenoids compounds were found as selective inhibitors of AChE. This is the first report regarding the use of bioactive ingredients of Delphinium uncinatum in testing against Alzheimer's disease. |
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| Keywords: | Norditerpenoids Uncinatine B-D Alzheimer’s disease (AD) Acetylcholinesterase inhibitory potential Molecular docking |
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