Diterpenoids extracted from herba siegesbeckiae, and preparation method and application thereof

An extraction method and a diterpenoid technology are applied in the field of medicine, and can solve the problems of superinfection of fungi, abuse of antimicrobial drugs, adverse reactions and the like, and achieve the effects of low cost, high production efficiency and simple preparation.

Inactive Publication Date: 2016-08-10
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the abuse of antimicrobial drugs is also becoming more and more serious, and the emergence of drug resistance has become an important issue facing the current medical field
The abuse of antimicrobial drugs can easily lead to the production of multidrug-resistant pathogenic bacteria, superinfection of fungi, and adverse reactions

Method used

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  • Diterpenoids extracted from herba siegesbeckiae, and preparation method and application thereof
  • Diterpenoids extracted from herba siegesbeckiae, and preparation method and application thereof
  • Diterpenoids extracted from herba siegesbeckiae, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] This example provides the preparation method of the compound ent-16βH-kaurane-17,19-dicarboxylic acid and the measurement method and results of its antibacterial activity.

[0031] Its chemical structural formula is:

[0032]

[0033] Step 1. Extraction: After pulverizing the weed grass, soak it in absolute ethanol, and extract it by ultrasonic wave three times at 25°C for 15, 30 and 45 minutes respectively, filter, collect the filtrate and put it under reduced pressure or normal pressure. Concentrate down to less than 3% to 5% of the volume of the original solution to obtain a concentrated solution;

[0034] Step 2, degreasing: add 0.5 to 1.5 times the volume of water to dissolve the above concentrated solution, extract with an equal volume of n-hexane or cyclohexane or petroleum ether, discard the extract, and collect the remaining water;

[0035] Step 3, separation: Concentrate the remaining aqueous solution obtained in the previous step to its volume of 1% to 3%...

Embodiment 2

[0044] This example provides the preparation method of the compound ent-16α, 17-dihydroxykaurene-19-carboxylic acid and the measurement method and results of its antibacterial activity.

[0045] Its chemical structure is:

[0046]

[0047] Preparation:

[0048] Step 1. Extraction: After pulverizing the weed grass, heat and reflux at 45-60°C for 2 hours with an ethanol aqueous solution with a concentration of 85-95% by volume, extract 3 times, filter, and collect the filtrate under reduced pressure or normal pressure Concentrate down to less than 3% to 5% of the volume of the original solution to obtain a concentrated solution;

[0049] Step 2, degreasing: add 0.5 to 1.5 times the volume of water to dissolve the above concentrated solution, extract with an equal volume of n-hexane or cyclohexane or petroleum ether, discard the extract, and collect the remaining water;

[0050] Step 3, separation: Concentrate the remaining aqueous solution obtained in the previous step to i...

Embodiment 3

[0059] This example provides the preparation method of the compound ent-16α, 17, 18-trihydroxykaurene-19-carboxylic acid and the measurement method and results of its antibacterial activity.

[0060] Its chemical structure is:

[0061]

[0062] Preparation:

[0063] Step 1. Extraction: After pulverizing the weed grass, heat and reflux with anhydrous methanol solution at 45-60°C for 2 hours, extract 3 times, filter, collect the filtrate and concentrate it to less than the volume of the original solution under reduced pressure or normal pressure 3% to 5%, to obtain a concentrated solution;

[0064] Step 2, degreasing: add 0.5 to 1.5 times the volume of water to dissolve the above concentrated solution, extract with an equal volume of n-hexane or cyclohexane or petroleum ether, discard the extract, and collect the remaining water;

[0065] Step 3, separation: Concentrate the remaining aqueous solution obtained in the previous step to its volume of 1% to 3%, and then carry ou...

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Abstract

The invention relates to a diterpene compound extracted and separated from the traditional Chinese medicine Siberia chinensis, a preparation method and an application thereof. The diterpenoids include all compounds with the following general structural formula; The preparation method of the diterpenoid compound comprises the following steps: pulverizing the weed grass, extracting with an organic solvent, degreasing, and separating and purifying by column chromatography. The diterpenoid compound exhibits a growth inhibitory effect on various microorganisms, especially methicillin-resistant Staphylococcus aureus (MRSA) and fungi, and is a class of compounds with application prospects. When preparing antimicrobial drugs, the diterpenoids can be used alone or in combination to prepare tablets, injections, capsules, granules, powders, suppositories, ointments, sprays, gels, lotions, and films , liniment, foam and other dosage forms. The invention has the advantages of simple preparation, low cost and high production efficiency, and is very suitable for industrialized production.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, to diterpenoids extracted and separated from Siberia chinensis and their application in the preparation of antimicrobial drugs, especially in the preparation of antifungal and Gram-negative bacteria , Gram-positive bacteria drug applications. Background technique [0002] According to the 2015 edition of "Chinese Pharmacopoeia", Siegesbeckia pubescens is the dry aerial part of Siegesbeckia orientalis L., Siegesbeckia pubescens Makino or Siegesbeckia glabrescens Makino of Compositae. Herba Ulusae is pungent in taste, bitter, and cold in nature. Return liver, kidney channel. It has the effects of expelling rheumatism, sharp joints and detoxification. For the treatment of rheumatic arthralgia, weakness of the muscles and bones, weakness of the waist and knees, paralysis of the limbs, hemiplegia, rubella and eczema, etc. Scholars at home and abroad have mainly focused on t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C61/125C07C62/06C07C51/42A61K31/194A61K31/19A61P31/04A61P31/10
CPCC07C61/125C07C51/42C07C62/06
Inventor 余建清杨渊陈惠雷嘉川
Owner WUHAN UNIV
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