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AChE inhibitory alkaloids from Coptis chinensis
Yan Lin1, Hong-Cheng Guo2, Yi Kuang2
1State Key Laboratory of Natural and Biomimetic Drugs & Key Laboratory of Molecular Cardiovascular Sciences of Ministry of Education, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China; School of Pharmaceutical Sciences, Guizhou Medical University, University Town, Guian New District, Guizhou 550025, China.
Six new alkaloids were discovered in Coptis chinensis, with seven compounds showing significant acetylcholinesterase (AChE) inhibitory activity, suggesting potential therapeutic applications.
Area of Science:
- Phytochemistry
- Natural Products Chemistry
- Pharmacology
Background:
- Coptis chinensis is a traditional Chinese herbal medicine with a history of medicinal use.
- Alkaloids are a diverse group of natural compounds with significant pharmacological properties.
- Acetylcholinesterase (AChE) is a key enzyme in neurotransmission, and its inhibition is a target for treating neurological disorders.
Purpose of the Study:
- To isolate and characterize new alkaloids from Coptis chinensis.
- To evaluate the AChE inhibitory activities of the isolated compounds.
Main Methods:
- Extraction of alkaloids from Coptis chinensis rhizomes using chloroform.
- Structure elucidation of new compounds using Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS).
- In vitro assessment of AChE inhibitory activity at a concentration of 10 μM.
Main Results:
- Six new alkaloids (coptisine A-F, 1-6) and 26 known alkaloids (7-32) were isolated.
- Compounds 1-3 were identified as α-carbonylated benzylisoquinolines, and 4-6 as berberidic acid type alkaloids.
- Seven compounds (7, 20, 22, 23, 25, 26, 29) demonstrated significant AChE inhibition (>80% at 10 μM).
Conclusions:
- The study successfully identified novel alkaloids from Coptis chinensis.
- Several isolated alkaloids, particularly compounds 7, 20, 22, 23, 25, 26, and 29, show potent AChE inhibitory effects.
- These findings highlight the potential of Coptis chinensis alkaloids as therapeutic agents for conditions related to AChE activity.
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