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Inula wissmannian extracts, preparation for same, and application of extracts in preparation of anti-inflammatory medicine

A kind of technology of Yangchuan and extract, which is applied in the direction of anti-inflammatory agent, drug combination, antipyretic, etc., can solve the problem that there is no pharmacological activity of chemical constituents of southern Yunnan Yangchuan, and no preparation of southern Yunnan Yangchuan extract is known. methods, uses and other issues to achieve the effect of great clinical application value and social benefits

Inactive Publication Date: 2015-05-27
SHANGHAI JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no literature reports on the chemical constituents and pharmacological activities of S. yunnanensis, and there are no reports related to the preparation method and use of the S. yunnanensis extract in the present invention.

Method used

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  • Inula wissmannian extracts, preparation for same, and application of extracts in preparation of anti-inflammatory medicine
  • Inula wissmannian extracts, preparation for same, and application of extracts in preparation of anti-inflammatory medicine
  • Inula wissmannian extracts, preparation for same, and application of extracts in preparation of anti-inflammatory medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of embodiment 1 southern yunnan fennelide A, B, C, D, E and squirrel

[0039] After drying and pulverizing the whole herb of South Yunnan sheep ear chrysanthemum (10.0kg), it was cold soaked and extracted with 95% ethanol (30L) at room temperature 25°C for 4 times (24, 12, 12, 12h), the solvent was recovered, and concentrated to dryness without water soaking. cream (631.4g); the total extract was suspended in 1.5L water and extracted 3 times with 5L petroleum ether, dichloromethane and ethyl acetate successively, and the solvent was recovered under reduced pressure to obtain petroleum ether fraction (133.2g), dichloromethane Methane fractions (179.6 g) and ethyl acetate fractions (28.1 g).

[0040] Put 120 g of the dichloromethane part of the southern yunnan chrysanthemum on a normal-phase silica gel column, and use dichloromethane-methanol (100% dichloromethane, 100:1, 50:1, 20:1, 10:1, 5: 1 and 100% methanol) gradient elution, the eluent was detected ...

Embodiment 2

[0057] Example 2 Southern Diannan Fructus A, B, C, D, E and Fructus Inhibition of LPS-Induced NO Production Activity of RAW264.7

[0058] (1) Sample configuration

[0059] The southern Yunnan fechinolactones A, B, C, D, and E prepared in Example 1, fecinolactone and the positive control drug aminoguanidine (Sigma-Aldrich, purity>98.0%)) were treated with DMSO (dimethyl Sulfoxide) (Merck) dissolved, added PBS (-) (phosphate buffer saline) to make a 10mM solution, and further diluted to 0, 0.1, 0.5, 5, 20μM samples with gradient concentrations. 10 μg / mL of LPS (Lipopolysaccharides, lipopolysaccharide, sigma, Cat.L-2880) was used as the inducer.

[0060] (2) Experimental method

[0061] Mouse macrophage RAW264.7 (purchased from Cell Resource Center of Shanghai Academy of Biological Sciences) at 37°C, 5% CO 2Routinely cultivated in DMEM medium in the incubator. During the experiment, 1μL / mL LPS (lipopolysaccharide) (dissolved in distilled water) was added to 100mL with a conce...

Embodiment 3

[0068] Example 3 Anti-Xylene-induced Inflammation Activity of Southern Diannan Fructus A, B, C, D, E and Fructus Fructus

[0069] (1) Sample configuration

[0070] The total extract of southern yunnanensis obtained in Example 1, the petroleum ether part, the dichloromethane part, the ethyl acetate part, and the southern dianthenia lactones A, B, C, D, E, and sheep's ear Esters, were prepared with 0.5% Tween-80 (Tween-80) solution to the required concentration of the suspension, set aside. Aspirin tablets (Sigma-Aldrich Company) were prepared into a 200 mg / kg suspension before use as a positive control. The administration volume of each group was 20mL / kg, administered orally.

[0071] (2) Experimental method

[0072] 220 Kunming mice, male, 18-22 g, were randomly divided into 22 groups, 10 in each group. A group of model controls, a group of positive controls and 20 groups of drug administration groups were set up. After the mice were purchased and adapted to the environme...

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Abstract

The invention provides a preparation for inula wissmannian extracts and an application of the extracts in preparation of an anti-inflammatory medicine. The extracts are germacrane sesquiterpene lactone inula wissmannian lactones A, B, C, D and E and inula cappa lactone with the following chemical structural formulas and absolute configurations shown in the specification, wherein the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone generate an inhibition effect on the NO of the RAW264.7 macrophage induced by LPS (lipopolysaccharide); and in an xylene-induced ear swelling mouse model and a Freund complete adjuvant arthritis rat model, the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone are found to be able to obviously inhibit the ear swelling and foot swelling of experimental animals, and the result indicates that the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone are good in anti-inflammatory activity, capable of being used for preparing an anti-inflammatory medicine, and great in application value. The invention provides an extraction and separation method for the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone.

Description

technical field [0001] The present invention relates to natural medicines, in particular to the extraction and separation method and application of the effective components of S. yunnanensis; especially to the extraction and separation method of the gemmane-type sesquiterpene lactones from S. yunnanensis extract and the preparation of anti-inflammatory drugs in the application. Background technique [0002] There are about 100 species of plants of the genus Inula L. in the Compositae family, mainly distributed in the Mediterranean region, and also distributed in other parts of Europe, Africa and Asia. There are more than 20 species and most varieties of this genus in China, more than half of which have medicinal records (Chinese Academy of Sciences Chinese Flora Editorial Committee, Chinese Flora [M], Beijing: Science Press, 1979,75:248-281 ). Scholars at home and abroad have isolated flavonoids, sesquiterpene lactones, terpenoids and other structural types of compounds fr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/93A61K31/365A61P29/00
Inventor 张卫东金慧子成向荣王春辉管斌栾鑫严诗楷单磊苏娟
Owner SHANGHAI JIAOTONG UNIV