Guaiane type sesquiterpenes, preparation and medical use thereof

A technology of guaiacol and sesquiterpenoids is applied in the preparation of medicines for the treatment of acute and chronic inflammation and related diseases. Failure to reveal the material basis of the medicinal effect of Xingxiang rabbit ear wind

Inactive Publication Date: 2008-10-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The relevant pharmacological activity research objects reported in the literature are limited to plant crude extracts. The existing chemical composition research is out of touch with the pharmacodynamic activity screening work, and the pharmacodynamic material basis

Method used

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  • Guaiane type sesquiterpenes, preparation and medical use thereof
  • Guaiane type sesquiterpenes, preparation and medical use thereof
  • Guaiane type sesquiterpenes, preparation and medical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Extraction, separation and structural identification

[0039] (1) Extraction and separation method

[0040] Take 5.5kg of dry Apricot Rabbit Earwind medicinal material, grind it into a coarse powder, reflux extraction with 95% ethanol twice (8 times, 6 times), each time for 2 hours, combine the alcohol extracts, concentrate under reduced pressure to obtain a thick extract, add water Suspend, extract with petroleum ether (60-90°C) and water-saturated n-butanol successively, take the n-butanol part and concentrate it into an extract (160g), add silica gel to mix the sample, load the sample on silica gel (200-300 mesh, 2Kg) column, eluted with chloroform-methanol gradient (95:5-60:40), thin-layer chromatographic detection, combined thin-layer chromatographic spots with the same fractions, sesquiterpene enriched fractions were passed through medium pressure C 18 Column chromatography, preparative high performance liquid chromatography separation and purification,...

Embodiment 2

[0059] Anti-inflammatory pharmacodynamic activity evaluation of the monomer compound of embodiment 2

[0060] 1 Experimental materials and reagents

[0061] 1.1 Animals

[0062] ICR species of mice, half male and half female, with an initial body weight of 18-22 g, were purchased from the Comparative Medicine Center of Yangzhou University, certificate number: SCXK (Su) 2002-0009. SD rats, all male, weighing 180-220 g, were purchased from the Comparative Medicine Center of Yangzhou University, certificate number: SCXK (Su) 2002-0009.

[0063] 1.2 Drugs and preparations

[0064] Drugs under test: Compounds 1, 2, and 3 were provided by the Department of Natural Medicinal Chemistry, China Pharmaceutical University, with dosages of 50 and 100 mg / kg; the positive drug, aspirin, with a dosage of 200 mg / kg; the positive drug, Jingangteng Capsules, Hubei Produced by Furen Pharmaceutical Factory, the content of each g capsule is equivalent to 20g of crude drug; Xylene, analytically p...

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Abstract

The invention belongs to natural medicine field and in particular relates to guaiane sesquiterpenoid with general formulaIwhich is distilled from Chinese herb ainsliaeafragrans; wherein R1 is OH or 0- beta-D-GIc; R2 is OH or H; R3 is alpha-H, beta-CH3 or =CH2. The invention further relates to the preparation method of the compound, the medicine combination with the compound as active component, and the application of the compound and the medicine combination thereof in curing acute or chronic inflammation and relevant diseases, including cervicitis, pelvic inflammation, endometritis, upper respiratory tract infection, quinsy as well as faucitis.

Description

technical field [0001] The invention belongs to the field of natural medicines, and specifically relates to a guaiac-type sesquiterpene compound extracted and separated from the traditional Chinese medicine Xingxiang rabbit ear wind, its preparation method, and the preparation and treatment of acute and chronic inflammation and related diseases of this type of compound. application in medicine. Background technique [0002] Ainsliaea fragrans Champ. is a plant of the genus Ainsliaea fragrans Champ., and its medicinal part is the whole plant. This product has the effects of clearing heat and detoxifying, cooling blood and detoxifying, promoting dampness, and stopping bleeding. It is suitable for treating diseases such as consumptive bone steaming, tuberculosis and hemoptysis, women's metrorrhagia, damp-heat jaundice, edema, carbuncle, swelling and poisoning. It is used in folk prescriptions and clinically. Xingxiang rabbit ear wind treatment of cervical erosion, endometritis...

Claims

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Application Information

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IPC IPC(8): C07D307/93C07H17/04A61K31/7048A61K31/365A61P29/00
Inventor 汪豪熊非刘戈叶文才张陆勇严明江振洲赵守训
Owner CHINA PHARM UNIV
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