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Release Date:2015/8/19 16:04:50

    We have heard a lot of legends about the flower of the other side, which may be sad or fantastic. However, the flower of the other side is not only beautiful and enchanting, but also its rhizome extract has medicinal value. The scientific name of the flower of the other side is Lycoris chinensis, which is beautiful in shape and bright in color. Modern medicine believes that it has an effect on the central nervous system and cardiovascular system. Lycorine is an isoquinoline alkaloid. In recent years, studies have shown that lycorine has many effects, such as anti-inflammatory, anti-virus, anti malaria, cardiovascular protection and inducing tumor apoptosis. amongLycorineThe inhibition of acetylcholinesterase has a certain preventive and therapeutic effect on senile dementia.

    Acetylcholine is a neurotransmitter that transmits information in brain neurons. With this neurotransmitter, brain cells can form sensation and memory. Acetylcholinesterase is a major enzyme in the nervous system that hydrolyzes acetylcholine. Its basic function is to catalyze the hydrolysis of the neurotransmitter acetylcholine. Modern studies have shown that acetylcholine in the brain of patients with Alzheimer's disease is greatly reduced. Therefore, inhibiting the activity of acetylcholinesterase is an important way to treat the disease. The inhibitory effect of lycorine on acetylcholinesterase (AChE) was determined by bioautography. The results showed that lycorine had a weak inhibitory effect on ache (ic50=450 μ m). Through the structural comparison with the analogues of lycorine with the same activity, it was presumed that the ache inhibitory activity of lycorine and its derivatives was related to the two free hydroxyl groups in the molecule.

    The structure-activity relationship of lycorine and its derivatives on AChE inhibition was summarized: the ring opening of D ring in lycorine molecule could improve its AChE inhibition activity and increase its solubility; The substituents on the nitrogen atom in the molecule have a significant effect on the activity. The activity of methyl or butyl substituents on the nitrogen atom is stronger than that of ethyl or propyl substituents. The above studies suggest that through the in-depth study of the structure-activity relationship of lycorine and its derivatives, it is expected to find more effective acetylcholinesterase inhibitors than existing drugs.

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