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

A technology of dog's tooth flower and alkaloid, which is applied in the field of natural medicinal chemistry and medicine, can solve the problems of no mental dependence, physical dependence and analgesic effect, no report on the chemical composition of fan-shaped dog's tooth flower, etc.

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

We studied the chemical composition and pharmacological activity of the plant, extracted and separated the alkaloid components from the plant and obtained 14 alkaloid monomers. After searching the literature, there was no report on the chemical composition of the dog's tooth flower. There are no reports on its total alkaloids or monomeric alkaloid compounds for the prevention and treatment of opioid mental dependence and physical dependence and analgesic effects

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Preparation of total alkaloids of Bermudagrass fanii by alcohol extraction

[0017] 14 kg of dried rhizomes of Bermudagrass fanii, crushed and extracted three times under reflux with 8 times the amount (W / W) of 95% ethanol, concentrated the extract under reduced pressure until ethanol-free to obtain 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 precipitates were 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 Ervatamia flabelliformis alkaloids (tEFA for short) .

Embodiment 2

[0018] Example 2 Preparation of Bermudagrass alkaloid monomer by silica gel column chromatography

[0019] 15g of total alkaloids of Bermudagrass fanii, separated by silica gel column chromatography (φ6*80cm, 450g), gradient washing with chloroform-methanol (100:1, 50:1, 25:1, 10:1, 8:1, 5:1) Take off, collect every 1000ml, and divide into 1-24 parts. After recovering the solvent under reduced pressure, the crystallization of compound EF-02, 03, 05, 06 and 08 can be obtained from the 5th, 7th, 10th, 13th and 14th parts. The 9th part (2.2 g) was separated by silica gel column chromatography (φ4 *40cm, 80g), petroleum ether-ethyl acetate (20:1, 10:1, 5:1) gradient elution could give compounds EHA-01, 04, 07 and 09. The 16th part (1.8g) was separated by silica gel column chromatography (φ2*40cm, 35g), and the compound EF-10 could be obtained after gradient elution of petroleum ether-ethyl acetate (5:1, 3:1, 1:1). 11 and 12. The eighteenth fraction (1.4g) was separated by silic...

Embodiment 3

[0020] Example 3 The effect on the mental dependence of morphine hydrochloride and its own mental dependence experiment

[0021] 3.1 Materials and methods

[0022] 3.1.1 Animals: Male SD rats: 160-200 g, purchased from Shanghai Xipuer-Bikay Experimental 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.

[0023] 3.1.2 Drugs and reagents

[0024] 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.

[0025] Total Ervatamia flabelliformis alkaloids (total Ervatamia flabelliformis alkaloids referred to as tEFA): Use physiological saline with a pH of 3.5-4 to make an application solution.

[0026] Hydrocortisone: use physiological saline to prepare the application solution.

[0027] ...

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Abstract

This invention discloses chemical structure and extraction method of indole alkaloids including flabelliform dine (EF-14) from Ervatamia flabelliformis 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 invention relates to the field of natural medicinal chemistry and medical technology, and relates to the extraction and separation of new Ervatamiaf labelliformis Tsiang indole alkaloids from Ervatamiaf labelliformis Tsiang, and the new Ervatamiaf labelliformis Tsiang indole alkaloids The application of the indole alkaloids in the preparation of drugs or food for the prevention and treatment of opioid dependence. Background technique [0002] Fan-shaped dogtooth flower (Ervatamia flabelliformis Tsiang) is a common plant in tropical and subtropical Asia. It is wild and cultivated in various provinces and regions in southern my country. All parts of the plant can be used medicinally. It has the effects of clearing away heat and detoxification, lowering blood pressure, reducing swelling and relieving pain. Treatment of hypertension, sore throat, rheumatic arthralgia and other diseases [Editorial Committee of Flora of China, Chinese Academy of Sciences:...

Claims

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Application Information

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IPC IPC(8): C07D471/22A61K31/439A61P25/04
Inventor 陈海生黄矛梁爽张晓冬金丽陈梅玉郑杰民刘建国
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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