Synthesis and acetylcholinesterase inhibitory activities of tabersonine derivatives |
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| Institution: | 1. Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, Hunan, PR China;2. Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, Hunan, PR China;3. Hunan Vocational College of Science and Technology, Changsha 410004, Hunan, PR China;1. Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan;2. Department of Geology, University of Swabi, Anbar 23561, Khyber Pakhtunkhwa, Pakistan;3. Department of Pharmacy, Abdul Wali Khan University, Mardan 23200, Pakistan;4. Department of Chemistry, University of Malakand, Chakdara, Dir (L), Pakistan;5. Department of Chemistry, Kohat University of Science and Technology, Kohat 26000, Pakistan;6. Department of Biotechnology, Sardar Bahadur Khan Women University, Quetta, Pakistan;1. Division of Polymer Engineering, School of Materials and Mineral Resources Engineering, Universiti Sains Malaysia, Engineering Campus, 14300 Nibong Tebal, Penang, Malaysia;2. Faculty of Engineering Technology, Universiti Malaysia Perlis (UniMAP), P.O Box 77, D/A Pejabat Pos Besar, Kangar, Perlis, 01000, Malaysia;1. Laboratoire de Chimie, Ingénierie Moléculaire et Nanostructures (LCIMN), Université Ferhat Abbas Sétif 1, Sétif 19000, Algeria;2. Leiden Institute of Chemistry, Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands;3. School of Chemistry, University of St Andrews, Fife KY16 9ST, United Kingdom;4. Département de Technologie, Faculté de Technologie, Université 20 Août 1955-Skikda, Skikda 21000, Algeria;5. Science and Engineering Faculty, Queensland University of Technology, GPO Box 2434, Brisbane, Qld 4001, Australia;6. Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;1. Faculty of Chemistry and Chemical Technology, Department of Chemistry, Moldova State University, 60 Mateevici Street, MD 2009 Chisinau, Republic of Moldova;2. Institute of Applied Physics, Academy of Sciences, 5 Academiei Street, MD 2028 Chisinau, Republic of Moldova;1. The Key Laboratory of Biomedical Engineering, Ministry of Education, Zhejiang University, Hangzhou 310027, PR China;2. Shandong University of Traditional Chinese Medicine, Jinan 250355, PR China |
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| Abstract: | Tabersonine, the main alkaloid in Voacanga seeds, was used as a lead compound to semi-synthesize tabersonine derivatives. In total, 13 compounds, containing 10 novel tabersonine derivatives, were synthesized by introducing substituent groups R1–R5. The acetylcholinesterase (AChE) inhibitory activities of tabersnonine derivatives were evaluated using Ellman’s method. Among them, compound (7) showed the highest AChE inhibitory activity with the IC50 value was 5.32 μM. The substituent groups R1–R5 showed different influences on the AChE inhibitory activities of tabersonine derivatives. The AChE inhibitory activities of tabersonine derivatives increased with the introduction of group R1 and/or combined groups R3, R4, while decreased with the introduction of group R5. And the group R2 showed no significant influence on the AChE inhibitory activities of tabersonine derivatives. |
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| Keywords: | Tabersonine derivatives AChE inhibitory activities |
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