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Acetylcholinesterase inhibitors and compounds promoting SIRT1 expression from Curcuma xanthorrhiza

Zhang, Chunmei, Ji, Jianbo, Ji, Mei, Fan, Peihong
Phytochemistry letters 2015 v.12 pp. 215-219
Alzheimer disease, Curcuma zanthorrhiza, acetylcholinesterase, antineoplastic activity, drugs, neurodegenerative diseases, nuclear magnetic resonance spectroscopy, protective effect, sesquiterpenoids, traditional medicine
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 1μg, 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 20μM for 24h. 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.