Abstract
Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of the most general form of dementia, Alzheimer’s Disease (AD). In this study, methanol, dichloromethane and aqueous crude extracts from 80 Traditional Chinese Medical (TCM) plants were tested for their in vitro anti-acetylcholinesterase activity based on Ellman’s colorimetric assay. All three extracts of Berberis bealei (formerly Mahonia bealei), Coptis chinensis and Phellodendron chinense, which contain numerous isoquinoline alkaloids, substantially inhibited AChE. The methanol and aqueous extracts of Coptis chinensis showed IC50 values of 0.031 µg/mL and 2.5 µg/mL, therefore having an up to 100-fold stronger AChE inhibitory activity than the already known AChE inhibitor galantamine (IC50 = 4.33 µg/mL). Combinations of individual alkaloids berberine, coptisine and palmatine resulted in a synergistic enhancement of ACh inhibition. Therefore, the mode of AChE inhibition of crude extracts of Coptis chinensis, Berberis bealei and Phellodendron chinense is probably due to of this synergism of isoquinoline alkaloids. All extracts were also tested for their cytotoxicity in COS7 cells and none of the most active extracts was cytotoxic at the concentrations which inhibit AChE. Based on these results it can be stated that some TCM plants inhibit AChE via synergistic interaction of their secondary metabolites. The possibility to isolate pure lead compounds from the crude extracts or to administer these as nutraceuticals or as cheap alternative to drugs in third world countries make TCM plants a versatile source of natural inhibitors of AChE.
Highlights
With more than 46 million people suffering from Alzheimer’s disease (AD) worldwide [1], this neuro-degenerative disorder is the most common form of dementia in elderly people [2].The progressive degenerative brain syndromes connected to dementia affect memory, thinking, behaviour and emotion
This study investigates the use of plants from Traditional Chinese Medicine (TCM), a complete medical system used to diagnose, treat and prevent illness for thousands of years, as inhibitors of
Of Alzheimer’s already known and widely sold inhibitor galantamine, which might be due to the synergistic. These findings suggest that Traditional Chinese Medical (TCM) plants represent an important source of natural compounds interaction thethe individual in this that of affect activity ofalkaloids
Summary
With more than 46 million people suffering from Alzheimer’s disease (AD) worldwide [1], this neuro-degenerative disorder is the most common form of dementia in elderly people [2]. The progressive degenerative brain syndromes connected to dementia affect memory, thinking, behaviour and emotion. Typical symptoms include loss of memory and difficulties to perform previously routine tasks. Patients have problems with finding the right words or understand what people are saying and they often undergo personality and mood changes [3]. During the progression of AD, the death of nerve cells in the cerebral cortex leads to a shrinkage of the brain. Gaps develop in the temporal lobe and hippocampus, where new information is stored and retrieved
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