Acetylcholinesterase inhibitors and compounds promoting SIRT1 expression from Curcuma xanthorrhiza |
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| Institution: | 1. Department of Natural Product Chemistry, Key Lab of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China;2. Department of Pharmacology, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China;1. Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guangdong University of Technology, Guangzhou, 510006, China;2. School of Chemical and Environment Engineering Wuyi University, Jiangmen, 529020, China;3. Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey,164 Frelinghuysen Road, Piscataway, NJ 08854, USA;4. Allan Conney Biotechnology Company Ltd, Foshan, 528200,China;5. Infinitus (China) Company Ltd, Guangzhou, 510006, China;1. Department of Life and Environmental Sciences, Drug Sciences Section, University of Cagliari, via Ospedale 72, 09124 Cagliari, Italy;2. Department of Life and Environmental Sciences, University of Cagliari, Cittadella di Monserrato SS554, 09042, Monserrato, Cagliari, Italy;3. Dipartimento di Scienze Chimiche, University of Cagliari, Cittadella di Monserrato, 09042, Monserrato, Cagliari, Italy;4. Department of Botany, S. S. G. M. College, IN-423601 Kopargaon, District Ahmednagar, MS, India;5. Dipartimento di Scienze della Salute, Università“Magna Græcia” di Catanzaro, Campus “S. Venuta”, Viale Europa, 88100 Catanzaro, Italy |
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| Abstract: | Curcuma xanthorrhiza is a well-known traditional medicine with anti-inflammatory and anticancer activities, as well as protective effects against neurodegenerative disorders. A previous study revealed the acetylcholinesterase (AChE) inhibitory activity of some sesquiterpenoids from C. xanthorrhiza. In this study, further bioassay-guided isolation led to the identification of nine compounds for the first time from C. xanthorrhiza, including a new Guaiane-type sesquiterpene, zedoaraldehyde (1). Their structures were elucidated using NMR and MS techniques. The AChE inhibitory activities of compounds 1, 3, 4 and 7 were detected as minimum inhibitory quantities of 3, 4, 6 and 1 μg, respectively, using a TLC bioautography assay. Meanwhile, compounds 1, 3, 4 and 8 could promote SIRT1 expression by 1.37-, 1.71-, 1.73- and 1.27-fold, respectively, in HEK293 cell lines exposed to compounds at a concentration of 20 μM for 24 h. SIRT1 is becoming an important drug target for new therapies in the treatment of neurodegenerative diseases. This study indicates the potential of sesquiterpenoids from C. xanthorrhiza for use against Alzheimer's disease. |
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| Keywords: | Zedoaraldehyde Acetylcholinesterase inhibitory activity SIRT1 Alzheimer's disease |
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