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Composition, preparation method and application of composition as acetylcholinesterase inhibitor

A technology of acetylcholine enzyme and composition, which is applied in the field of Chinese medicine extracts, can solve the problems of relative blindness, low sensitivity, and low content of active ingredients, and achieve the effect of reducing difficulty

Inactive Publication Date: 2019-08-20
SHANDONG ANALYSIS & TEST CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The difficulty lies in: the content of active ingredients in natural products is low, it is difficult to enrich; the active ingredients are complex, macromolecules and small molecules, active and inactive substances coexist, especially there are isomers with similar structures, and the separation and purification are difficult
These factors have resulted in long time-consuming, low sensitivity, and relatively blind separation of natural products.

Method used

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  • Composition, preparation method and application of composition as acetylcholinesterase inhibitor
  • Composition, preparation method and application of composition as acetylcholinesterase inhibitor
  • Composition, preparation method and application of composition as acetylcholinesterase inhibitor

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 1 Experimental part

[0047] 1.1 Reagents and materials

[0048] Electric eel AChE was purchased from Sigma; Acetylthiocholine iodide (AChI) was purchased from Fluka; 5,5-Dithiobisnitrobenzoic acid (DTNB) was purchased from Sigma; Tacrine ( tacrine) and physostigmine (galanthamine) were purchased from Sigma; other reagents were imported or domestic analytical grade; experimental water was Milli-Q ultrapure water (18.2MΩ). The samples of Salvia miltiorrhiza used in this experiment were purchased from Zhonglu Hospital of Jinan City and identified by researcher Wang Xiao from Shandong Provincial Analysis and Testing Center.

[0049] 1.2 Instruments and equipment

[0050] Tecan Infinite M200 Multifunctional Microplate Reader (Switzerland TECAN Group Company); MICROTEST TM 96-well ELISA plate (Becton, Dickinson and Company, USA); KQ-400KDE high-power numerically controlled ultrasonic instrument (Kunshan Ultrasonic Instrument Co., Ltd.); R201 rotary evaporator (Shanghai S...

Embodiment 2

[0069] Embodiment 2 extraction solvent selection

[0070] The chemical composition of Danshen is complex and diverse. A large number of studies have shown that the main active ingredients in Danshen are water-soluble salvianolic acid and fat-soluble tanshinone, with large differences in polarity. Therefore, the choice of extraction solvent is of great significance to the subsequent biological activity screening experiments. Using water, 80% ethanol, ethyl acetate and petroleum ether four extraction solvents with different polarities to extract Danshen. Then four different extracts were tested for activity, and the extract with the strongest acetylcholinesterase inhibitory activity was selected for subsequent experiments. The result shows: four kinds of extracts are respectively to the inhibitory rate of acetylcholinesterase: water, 4.84 ± 0.29 (1000mg / L), 4.25 ± 0.06 (50mg / L); 80% (v / v) ethanol, 13.37 ± 0.09 ( 1000mg / L), 3.28±0.26(50mg / L); ethyl acetate, 46.84±0.03(1000mg / L)...

Embodiment 3

[0072] Embodiment 3 chromatographic conditions optimization

[0073] Good resolution of HPLC separation will help to obtain satisfactory screening effect, so the HPLC conditions of the extract were studied in detail.

[0074]First, the separation efficiency of three different types of chromatographic columns (Agilent Eclipse XDB-C18 column, Agilent SB-C18 column and Kromasil 100-5-C18 column) was investigated. The results showed that using Agilent Eclipse XDB-C18 column (4.6× 250mm, 5μm, American Agilent Corporation), can obtain better chromatographic resolution and stable chromatographic peak distribution. On this basis, compared the chromatographic separation effect when methanol-water and acetonitrile-water were used as mobile phases, it was found that the effect of acetonitrile water was significantly better than that of methanol water; considering the complexity of Danshen extract, in isocratic elution mode, The compounds in the ethyl acetate extract of salvia miltiorrhi...

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Abstract

The invention belongs to the field of acetylcholinesterase inhibitor screening, and particularly relates to a composition, a preparation method and an application of the composition as an acetylcholinesterase inhibitor. The existing research shows that danshen roots and danshen root Chinese patent medicine have good anti-Alzheimer disease effect, and the full screening of potential acetylcholinesterase inhibitor in the danshen roots has important significance. The invention provides a method for separating and preparing compounds with anti-acetylcholine activity in the danshen roots by combining ultrafiltration affinity and semi-preparative liquid chromatography, the method screens out six compounds of Oleoyl neocyptotanshinone, dihydrotanshinone I, cryptotanshinone I, tanshinone I, tanshinone II A and Miltirone from an ethyl acetate extract of the danshen roots, and the compounds have good acetylcholinesterase inhibition activity. The method provides technical support for rapidly screening out the acetylcholinesterase inhibitor, and the research result has guiding significance for the development of medicines for treating Alzheimer disease.

Description

technical field [0001] The disclosure belongs to the technical field of traditional Chinese medicine extracts, and in particular relates to a composition isolated from Salvia miltiorrhiza, a preparation method of the composition and its application as an acetylcholinease inhibitor. Background technique [0002] The information disclosed in this Background section is only intended to increase the understanding of the general background of the disclosure, and is not necessarily to be taken as an acknowledgment or any form of suggestion that the information constitutes the prior art that is already known to those skilled in the art. [0003] At present, population aging has become a prominent social problem in the world, and there are more and more age-related degenerative diseases. Among them, Alzheimer's disease, cardiovascular disease, and tumors have become the three major diseases that endanger the health of the elderly. Acetylcholinesterase (AChE) is an important target ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/122A61P25/28
CPCA61K31/58A61K31/122A61P25/28A61K2300/00
Inventor 赵恒强张敏敏王晓刘伟闫慧娇李丽丽赵志国
Owner SHANDONG ANALYSIS & TEST CENT
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