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Application of pentacyclic triterpenoid in preparation of anti-migraine drug

A technology of pentacyclic triterpenoids and migraine, applied in the preparation of anti-migraine drugs, triterpenoids in the field of preparation of anti-migraine drugs, can solve the problems of poor therapeutic effect on migraine, and achieve good anti-migraine activity , good application prospects, widely distributed effect

Active Publication Date: 2020-06-26
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved in the present invention is to solve the problem that the compounds in the prior art have poor therapeutic effect on migraine

Method used

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  • Application of pentacyclic triterpenoid in preparation of anti-migraine drug
  • Application of pentacyclic triterpenoid in preparation of anti-migraine drug
  • Application of pentacyclic triterpenoid in preparation of anti-migraine drug

Examples

Experimental program
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Effect test

preparation example Construction

[0057] The present invention also provides a method for preparing the above-mentioned compound of formula I, the method comprising preparing the compound from a plant of the genus Centella (such as Centella asiatica). Preferably, Asiatic acid and 2α,3β,6β,23α-tetrahydroxy-12-ene-28-ursolic acid are prepared from the roots, stems, leaves, and fruits of Centella asiatica. Preferably, the method has the steps of:

[0058] (1) Extract with solvent after drying and pulverizing Centella asiatica, and combine the extracts;

[0059] (2) concentrating under reduced pressure the extract in (1) to obtain extractum;

[0060] (3) suspending the extract in (2) in water, extracting with sherwood oil, ethyl acetate and n-butanol successively, and then steaming off the solvent with a rotary evaporator to obtain sherwood oil, ethyl acetate and n-butanol respectively. butanol extract;

[0061] (4) The ethyl acetate extract in (3) was separated by silica gel column chromatography, and 10 compo...

Embodiment 1

[0072] Anti-migraine Activity Test of Centella Asiatica Extract

[0073] Source of material: Centella asiatica (Centella asiatica) was collected in Kunming, Yunnan, and was identified as Centella asiatica (L.) Urban by Associate Professor Yang Qingsong, School of Ethnic Medicine, Yunnan University for Nationalities. The specimens are preserved in the Herbarium of the School of Medicine for Nationalities, Yunnan University for Nationalities.

[0074] Preparation of Centella asiatica extract: crush the dried whole herb of Centella asiatica to obtain fragments of Centella asiatica; then extract the fragments of Centella asiatica with 95% ethanol / water reflux for 3 times, each time for 2 hours to obtain Extraction solution; the centella asiatica extract solution was filtered separately and concentrated under reduced pressure with a rotary evaporator to obtain an extract for later use.

[0075]A rat model of migraine induced by nitroglycerin (see scientific literature: Zhang Xiao-...

Embodiment 2

[0081] Further experiments with centella asiatica

[0082] Example 1 was repeated using 95% methanol / water, 70% ethanol / water and 80% acetone / water as extraction solvents respectively. The experimental results show that the 95% methanol extract of Centella asiatica, the 70% ethanol extract of Centella asiatica and the 80 The extract of % acetone / water also has significant anti-migraine effect on rats, so using different concentrations of ethanol / water, methanol / water or acetone / water as the extraction solvent can also obtain the anti-migraine activity in Centella asiatica Element. The results are shown in Table 2.

[0083] Table 2 Effects of different solvent extracts of Centella asiatica on the number of head scratching in migraine rats

[0084]

[0085] n=10

[0086] Note: ## Compared with the blank control group, P# Compared with the blank control group, P** Compared with the negative control group, P* Compared with negative control group, P<0.05.

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Abstract

The invention relates to application of a pentacyclic triterpenoid compound in preparation of an anti-migraine drug. Specifically, the invention relates to application of a pentacyclic triterpenoid compound as shown in a formula I which is described in the specification, and the pentacyclic triterpenoid compound is used for treating migraine. In the formula I, R is H or OH. The pentacyclic triterpenoid compound can be a naturally-existing organic compound or a synthesized organic compound, has strong anti-migraine activity, and can be used as an active component for preparation of an anti-migraine drug or a pharmaceutical composition together with a pharmaceutically acceptable carrier or auxiliary material.

Description

technical field [0001] The present invention relates to the application of a kind of triterpenoids in the preparation of anti-migraine medicines, in particular to the use of triterpenoids which can be isolated from Centella asiatica (such as Centella asiatica) in the preparation of anti-migraine Uses in medicine. Background technique [0002] Migraine is the most common type of headache clinically. Generally, there is no organic lesion. The main clinical manifestation is paroxysmal moderate to severe, throbbing headache, with pain on one or both sides of the head. Migraine is often related to genetics, and people with poor physical fitness, who do not like sports and engage in mental work are more likely to suffer from migraine. Migraine mainly includes three categories: typical migraine, common migraine and cluster migraine. Typical migraine patients are mostly periodic attacks, and women are more common. Before the onset, most patients may experience blurred vision, fla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K36/23A61P25/06
CPCA61K31/56A61K36/23A61P25/06A61K2236/333
Inventor 黄相中于海波李艳红田凯蒋孟圆李育晓李红锐李育逵
Owner YUNNAN MINZU UNIV
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