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Stemona root alkaloid monomer components and applications thereof

A technology of alkaloids and monomers, applied in drug combinations, digestive system, muscular system diseases, etc.

Inactive Publication Date: 2013-11-13
LANZHOU UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is no report on the inhibitory activity of acetylcholinesterase of the monomer components stenin, neostenine, sessilifoline B and neotuberostemonin of the total alkaloids

Method used

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  • Stemona root alkaloid monomer components and applications thereof
  • Stemona root alkaloid monomer components and applications thereof
  • Stemona root alkaloid monomer components and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Embodiment 1: Separation of Alkaloid Monomer Components

[0011] (1) The preparation of the total alkaloid extract of Herba Melonifolia

[0012] Take 5kg of herbal medicines, crush them, add 10L of 95% ethanol to reflux and extract twice, each time for two hours, combine the extracts, concentrate to dryness, add 3L of distilled water to dissolve, adjust the pH value to 1-2 with 4M concentrated hydrochloric acid, and statically Suction filtration after 12-16h. The filtrate was adjusted to pH 9-11 with concentrated ammonia water or aqueous sodium hydroxide solution, and then extracted twice with 5 L of chloroform, and the extracts were combined and concentrated to dryness to obtain the total alkaloid extract (75 g).

[0013] (2) Separation and identification of effective monomer components in the total alkaloid extracts

[0014] By macroporous resin column chromatography, ethanol-water gradient elution (20%, 30%, 40%, 50%, 60%, 70%, 80%, 90%, 100% %), collected once pe...

Embodiment 2

[0033] Embodiment 2: The improved Ellman method measures the anti-acetylcholinesterase activity of alkaloid monomer components

[0034] The improved Ellman method was used to determine the inhibitory rate of acetylcholinesterase compound 1-4 of the alkaloid monomer component of basilicum alkaloids, and huperzine A was used as the positive control drug. The specific experimental process is as follows:

[0035] Use a 96-well microtiter plate to determine the inhibitory activity of the sample on the enzyme. Add 140 μL of 0.1M phosphate buffer (pH=8.0) to each well of the sample group, and then add 20 μL of the sample. Add 160 μL of phosphate buffer to the blank well without adding For any sample, 20 μL of 0.1 mg / mL physostigmine and 140 μL of phosphate buffer were added to the positive control control group. Add 15 μL of acetylcholinesterase, mix well and incubate at 4°C for 20 min, then add 10 μL of 0.01 mM DTNB (5,5-dithiobis(2-nitrobenzoic acid)) and 10 μL of 0.075 mM ATCI ( ...

Embodiment 3

[0040] Embodiment 3: Morris water maze experiment

[0041] 110 healthy Kunming male mice were randomly divided into 11 groups: normal control group, model control group, compound 1-4 high-dose group (1mg / kg), compound 1-4 low-dose group (0.5mg / kg) and donepezil Control group (0.1 mg / kg). Except the normal control group and the model control group were intraperitoneally injected with the same amount of normal saline, the mice in the other groups were injected intraperitoneally once a day at a fixed time for 5 consecutive days. After 2 days of administration, water maze positioning navigation training was carried out. Except for the normal control group, which was intraperitoneally injected with the same amount of normal saline, the mice in the other groups were intraperitoneally injected with 2 mg / kg of scopolamine before training. Positioning and navigation training was carried out 1 hour after the last administration, and a space exploration test was carried out 24 hours la...

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Abstract

The invention relates to stemona root alkaloid monomer components and applications thereof. The stemona root alkaloid monomer components are stenin, neostenine, sessilifoline B, and neotuberostemonin, and are used for preparing acetylcholinesterase inhibitors. The invention relates to the applications of the stemona root alkaloid monomer components in preparing medicines used for preventing and treating Alzheimer's disease, bowel obstruction, myasthenia gravis, or glaucoma. The stemona root alkaloid monomer components can also be used for preparing medicines used for improving intelligence.

Description

technical field [0001] The present invention relates to the use of alkaloid monomers. Background technique [0002] Alzheimer's disease (AD) is a chronic neurodegenerative disease characterized by memory impairment, cognitive dysfunction, behavioral disturbance and decline in self-care ability, and is the most common disease in senile dementia. The incidence of AD is positively correlated with age. In recent years, clinical studies at home and abroad have shown that acetylcholinesterase inhibitor (actylcholinesterase inhibitor, AChEI) is the most effective drug for the treatment of AD, and it also has a good effect on the treatment of glaucoma, myasthenia gravis, intestinal obstruction, etc. Yu. Pharmacology (Fifth Edition), 2001; 54-55.). Several potent acetylcholinesterase inhibitors, such as huperzine A and galantamine, were originally isolated from herbs, and medicinal plants are a rich resource for finding potential acetylcholinesterase inhibitors. Its medicinal ingr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/16A61P25/28A61P1/00A61P21/04A61P27/06
Inventor 杨中铎赖东海
Owner LANZHOU UNIVERSITY OF TECHNOLOGY
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