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Indole group alkaloid of Hainan Gouyahua, and application for preparing drug-breaking medicine

A kind of technology of bermine and bermudagrass, which is applied in the fields of natural medicinal chemistry and medicine

Inactive Publication Date: 2007-02-21
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports on the prevention and treatment of opioid mental and physical dependence and analgesic effects on the above compounds

Method used

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  • Indole group alkaloid of Hainan Gouyahua, and application for preparing drug-breaking medicine
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  • Indole group alkaloid of Hainan Gouyahua, and application for preparing drug-breaking medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 Preparation of Hainan Bermudagrass Total Alkaloids by Alcohol Extraction

[0020] Hainan Bermudagrass dried rhizome 12kg, pulverized, heated and refluxed with 8 times the amount (W / W) of 95% ethanol to extract three times, concentrated the extract under reduced pressure until ethanol-free, and obtained the alcohol extract. After the extract was dissolved with 2000ml of 2% hydrochloric acid, the acid-insoluble matter was filtered off. The acidic water solution was adjusted to pH 8-10 with concentrated ammonia water, and a precipitate was formed, and 500ml of chloroform was added to extract three times. After combining the extracts, the chloroform was removed under reduced pressure to obtain purified total alkaloids of Ervatamia hainanensis alkaloids (tEHA for short).

Embodiment 2

[0021] Example 2 Preparation of Hainan Bermudagrass Alkaloid Monomer by Silica Gel Column Chromatography

[0022] Hainan Bermudagrass total alkaloids 15g, separated by silica gel column chromatography (φ6*80cm, 450g), chloroform-methanol (100:1, 50:1, 25:1, 10:1, 8:1, 5:1) gradient washing Take off, collect every 1000ml, and divide into 1-24 parts. After recovering the solvent under reduced pressure, the crystallization of compound EHA-02, 04, 05 and 07 can be obtained from the 4th, 6th, 9th and 12th parts. The 7th part (2.5g) is separated by silica gel column chromatography (φ4*40cm, 75g ), and petroleum ether-ethyl acetate (20:1, 10:1, 5:1) gradient elution to obtain compounds EHA-01, 03 and 06. The 14th part (1.5g) was separated by silica gel column chromatography (φ2*40cm, 35g), and the compound EHA-08 and 09.

Embodiment 3

[0023] Example 3 The effect on the mental dependence of morphine hydrochloride and its own mental dependence experiment

[0024] 3.1 Materials and methods

[0025] 3.1.1 Animals: Male Sprague-Dawley rats: 160-200 g, purchased from Shanghai Xipuer-Bicai Laboratory Animal Co., Ltd. Male Kunming strain mice (clean grade): 18-22 g, provided by the Department of Experimental Animal Science, Fudan University. The animals were kept in an animal room with natural light, and they had free access to food and water.

[0026] 3.1.2 Drugs and reagents

[0027] Morphine Hydrochloride (Morphine for short, code-named Mor in the table): Physiological saline with a pH of 3.5-4 is used to make an application solution.

[0028] Hainan dog tooth flower alkaloids (Ervatamia hainanensis alkaloids referred to as tEHA): make application solution with physiological saline with pH 3.5-4.0.

[0029] Hydrocortisone: use physiological saline to prepare the application solution.

[0030] 3.2. Administr...

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Abstract

This invention discloses chemical structures and extraction method of indole alkaloids including 3-(2-oxopropyl) ibogamine (EHA05) and 3-(2-oxopropyl) ibogamine hydroxyindolenine (EHA06) from Ervatamia hainanensis Tsiang. This invention also discloses the application of the indole alkaloids and their salts for manufacturing analgsics, drugs or food for treating opioid dependence.

Description

technical field [0001] The present invention relates to the field of natural medicinal chemistry and medicine technology, and relates to the extraction and isolation of new Hainan Bermuda indole alkaloids from Ervatamiahainanensis Tsiang, and Hainan Bermuda indole including the new alkaloids Application of the inole alkaloids in the preparation of drugs for preventing and treating opioid dependence, analgesics or food. Background technique [0002] Ervatamia hainanensis Tsiang is a plant of the genus Ervatamia hainanensis Tsiang, also known as single tree, single tree, mountain pepper tree, mugwort green, chicken claw flower, etc., distributed in Hainan, Guangdong, Guangxi, Yunnan and so on. It has the effects of clearing heat and detoxification, lowering blood pressure, reducing swelling and relieving pain, and is used for the treatment of diseases such as hypertension, sore throat, and rheumatic arthralgia. There are few studies on the chemical constituents of Hainan dog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/22A61K31/439A61P25/04
Inventor 黄矛陈海生张晓冬梁爽陈梅玉金丽郑杰民刘建国谭兴起
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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