Club moss alkaloid compound and medicine composition therefore, as well as preparation method and application thereof

A technology of lycopodium alkaloids and compounds, which is applied in the directions of drug combination, organic chemistry method, pharmaceutical formula, etc., can solve the problem of no preparation method and the like

Active Publication Date: 2017-02-15
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there is no report on a class of novel skeleton lycopodium alkaloids phleghenrines A-D and its analogues, its pharmaceutically acceptable salts, nor its preparation method, pharmaceutical compositions and plant extracts containing such compounds , and the application of such compounds and their pharmaceutical compositions and extracts in the preparation of anti-acetylcholinesterase inhibitor drugs, in the preparation of drugs for the treatment of Alzheimer's disease, and in the preparation of drugs for anti-middle-aged and elderly memory and cognitive impairment diseases to report

Method used

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  • Club moss alkaloid compound and medicine composition therefore, as well as preparation method and application thereof
  • Club moss alkaloid compound and medicine composition therefore, as well as preparation method and application thereof
  • Club moss alkaloid compound and medicine composition therefore, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation method and structure identification of lycopodium alkaloids phleghenrines A-D(1-4):

[0041] Get 4.8Kg of dry whole herb of Phlegmariurus henryi (Baker) Ching, grind it and extract it under reflux with 70% industrial ethanol / water mixed solvent (60L), extract three times altogether, the first time is 4 hours, and the last two times each time After 3 hours, the combined extracts were evaporated and concentrated under reduced pressure to remove the organic solvent to obtain a total of 1.2Kg of extract. The lower layer insoluble matter (650g), and then the upper layer aqueous solution was extracted three times with ethyl acetate, 8L each time, to remove most of the non-alkaloid components. The extracted water-soluble part was adjusted to pH 9 with saturated sodium carbonate solution, and then fully extracted with chloroform five times, 8 L each time, to obtain 8.2 g of the total alkaloid extract. The extract was mixed with 50-mesh polyamide (20g), dried and pa...

Embodiment 2

[0054] The phleghenrines A-D (1-4) of the lycopodium alkaloid compound of the present invention shows obvious inhibitory activity in inhibiting acetylcholinesterase. The experimental principles, methods and results are as follows:

[0055] Experimental principle: Acetylcholinesterase can catalyze the degradation of its substrate analogue, thioacetylcholine iodide, to generate thiocholine and acetic acid, and the reaction product reacts with the chromogenic agent DTNB to generate a yellow substance, which has specific light absorption at 405nm. The mixture of compound and acetylcholinesterase reacts at 30°C. If the compound has an inhibitory effect on acetylcholinesterase, the amount of acetylcholinesterase catalyzing the degradation of the substrate analogue thioacetylcholine iodide will decrease, and the corresponding reaction with DTNB will generate The reduction of the yellow compound, that is, the light absorption value at 405nm becomes smaller, so as to screen the compoun...

Embodiment 3

[0067] Compound 1-4 obtained in Example 1 was added with 4% sulfuric acid ethanol solution, pH = 4, filtered and dried to prepare sulfate compound 1-4.

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Abstract

The invention discloses a club moss alkaloid compound or a pharmaceutical salt thereof represented by the structural formula (I) where R1 is hydrogen, aryl, substituted aryl, alkyl or substituted alkyl, R2 is hydrogen, hydroxyl or a halogen atom, R3 is hydrogen, aryl, substituted aryl, alkyl or substituted alkyl, R4 is hydrogen, hydroxyl or a halogen atom, and n is an integer from 0 to 4, as well as a preparation method of the club moss alkaloid compound, a medicine composition containing the compound of the type, a plant extract and application of the compound of the type, the medicine composition of the compound and the extract in preparation of an anticholinesterase inhibitor medicine, preparation of a medicine for treating the alzheimer's disease and preparation of a medicine for treating the memory and cognitive impairment diseases of middle-aged and old people. Club moss alkaloids are diversified natural alkaloids which are of similar and unique structures, separated from fern club moss and relative plants thereof, and have the same biogenesis.

Description

[0001] Technical field: [0002] The invention belongs to the technical field of medicines, and in particular relates to a class of novel skeleton lycopodium alkaloid compounds phleghenrines A-D and their analogs, their pharmaceutically acceptable salts, their preparation methods, pharmaceutical compositions and plant extracts containing such compounds , and the application of the compounds and their pharmaceutical compositions and extracts in the preparation of anti-acetylcholinesterase inhibitor drugs, in the preparation of drugs for the treatment of Alzheimer's disease, and in the preparation of drugs for anti-middle-aged and elderly memory and cognitive impairment diseases. [0003] Background technique: [0004] Alzheimer's disease is a neurodegenerative disease. With the increasing aging of the world's population, the incidence of Alzheimer's disease is also increasing year by year. Alzheimer's disease, also known as Alzheimer's disease (Alzheimer'sDisease, AD), is a main...

Claims

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Application Information

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IPC IPC(8): C07D471/08A61K31/4375A61P25/28A61K36/11
CPCA61K36/11A61K2236/333A61K2236/39C07B2200/07C07D471/08
Inventor 赵勤实董廖斌苏佳彭丽艳吴心德邵立东
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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