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Guaiane type sesquiterpene compound as well as preparation method and application thereof

A technology of guaiacane and sesquiterpene, which is applied in the field of guaiac-type sesquiterpene compounds, can solve the problems of high toxicity and side effects, increase the difficulty of tuberculosis treatment, and easily produce drug resistance, etc., and achieve good activity and excellent Inhibition effect, effect of expanding application range

Active Publication Date: 2021-07-30
CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The commonly used anti-tuberculosis drugs in the world have the disadvantages of high toxicity and side effects, and are prone to drug resistance. In recent years, the emergence of multidrug-resistant strains has increased the difficulty of tuberculosis treatment

Method used

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  • Guaiane type sesquiterpene compound as well as preparation method and application thereof
  • Guaiane type sesquiterpene compound as well as preparation method and application thereof
  • Guaiane type sesquiterpene compound as well as preparation method and application thereof

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preparation example Construction

[0023] The invention provides a preparation method of a guaiac-type sesquiterpene compound, comprising:

[0024] The guaiac-type sesquiterpene compound is formed by extracting the milk mushroom fruiting bodies. Wherein, the milk mushroom fruiting body used can be any one of the milk mushroom fruiting body, the pine milk mushroom fruiting body and the orange red milk mushroom fruiting body or other milky mushroom fruiting bodies containing the guaiane-type sesquiterpene compound .

[0025] First, before the extraction, the milk mushroom fruiting body is pretreated; the milk mushroom fruiting body is placed at a medium temperature for a period of time, then placed at a high temperature for a period of time, and then placed at a low temperature for a period of time Time; for example, put the fresh milk mushroom fruiting bodies at 40-50°C (such as 40°C, 42°C, 44°C, 46°C, 48°C, and 50°C, etc. at any value between 40-50°C) 4-6 hours (for example, 4 hours, 4.5 hours, 5 hours, 5.5 h...

Embodiment 1

[0041] The embodiment of the present invention provides a preparation method of a guaiac-type sesquiterpene compound, comprising:

[0042] (1) Pretreatment: Place the fresh milk mushroom fruiting bodies at 45°C for 6 hours, then place them at 60°C for 3 hours at an oxygen partial pressure of 5%, then place them at 0°C for 24 hours .

[0043] (2) Grind 1.3Kg of the above-mentioned pretreated milk mushroom fruiting bodies with a tissue crusher, and then use acetone (0.5L) to extract 3 times at 25°C for 24 hours each time, collect and combine for 3 times Extraction solution obtained. Next, use methanol:chloroform=1:1 (V:V) The mixed solvent of above-mentioned leaching after extracting the fruiting bodies of Lactaria rufica 2 times, each time for 24 hours, collecting and merging the extract obtained by 2 extractions; after the above-mentioned merging extract and extract are combined, use gauze suction filtration, Organic solvents such as acetone, methanol and chloroform were re...

experiment example

[0053] Acidic Roche medium: The acidic Roche medium base contains L-sodium glutamate, magnesium sulfate, magnesium citrate, potassium dihydrogen phosphate, potato starch, malachite green, etc. Weigh 52.4g of the medium base and dissolve it in 600mL Add 12mL glycerin and 24mL Tween-80 to distilled water and mix well. Boil in a boiling water pot for 30-40min (shaking and stirring constantly) until it becomes a paste. When it cools down to about 50°C, add 1000mL of sterile fresh whole egg liquid , mixed for the preparation of drug-containing medium.

[0054] Preparation of drug-containing medium: dissolve the guaiac-type sesquiterpene compound prepared in Example 1 with DMSO, add it to the above-mentioned acidic Roche medium containing 1.5% Tween-80, and prepare the drug-containing medium The culture medium with a concentration of 9.5 μmol / mL was made into 4.8 μmol / mL, 2.4 μmol / mL, 1.2 μmol / mL, 0.6 μmol / mL, 0.3 μmol / mL and 0.15 μmol / mL by double dilution method, a total of 7 Con...

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Abstract

The invention relates to the technical field of chemical drugs, in particular to a guaiane type sesquiterpene compound as well as a preparation method and application thereof. The structural formula of the guaiane type sesquiterpene compound is shown in the specification, and the guaiane type sesquiterpene compound is extracted from lactarius deliciosus, can well inhibit the activity of tubercle bacillus, and particularly has an excellent inhibition effect on drug-resistant tubercle bacillus or multi-drug-resistant tubercle bacillus. The guaiane type sesquiterpene compound can be used for treating tuberculosis, especially the existing drug-resistant tuberculosis.

Description

technical field [0001] The invention relates to the technical field of chemical medicines, in particular to guaiac-type sesquiterpene compounds, their preparation methods and their applications. Background technique [0002] Due to the increase in population flow and the emergence of antibiotic resistance, tuberculosis has become the biggest killer after AIDS that seriously threatens human health, and it is on the verge of breaking out worldwide. In 2018, WHO pointed out in the "Global Tuberculosis Report" that there were 10 million new cases of tuberculosis in the world, of which about 1.57 million died. The commonly used anti-tuberculosis drugs in the world have the disadvantages of high toxicity and side effects, and are prone to drug resistance. In recent years, the emergence of multi-drug-resistant strains has increased the difficulty of tuberculosis treatment. Therefore, it is urgent to research and develop new anti-tuberculosis drugs, and natural products have unlimi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C47/45C07C45/78C07C45/79C07C45/80A61K31/11A61P31/06
CPCC07C47/45C07C45/78C07C45/79C07C45/80A61P31/06C07C2602/30Y02A50/30
Inventor 任佳丽钟平胜杨亚兰肖臻研贺雅雯杨桥
Owner CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY