Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Method for preparing monoester type aconite total alkaloid and application thereof

A technology of total alkaloids and aconitum, applied in the field of natural medicinal chemistry research, can solve the problems of reduced pharmacological activity, reduced toxicity, and irregularities

Inactive Publication Date: 2018-01-12
JILIN UNIV
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The literature points out that these three diester alkaloids are prone to hydrolysis to produce monoester aconitine and aconitine. The monoester aconitine still has anti-inflammatory and analgesic activity, but its toxicity is greatly reduced
Therefore, it is particularly meaningful to convert diester-type alkaloids into mono-ester-type alkaloids. Traditional Chinese medicine mainly realizes it through the processing of Aconitum, Aconitum or Aconite (including steaming, boiling, sand scalding and adding auxiliary materials, etc.) Convert diester-type alkaloids into mono-ester-type alkaloids, but these methods have poor reproducibility, non-standard, low conversion efficiency, and are easy to further degrade mono-ester-type alkaloids into aconitine to make it pharmacologically active Greatly reduced

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing monoester type aconite total alkaloid and application thereof
  • Method for preparing monoester type aconite total alkaloid and application thereof
  • Method for preparing monoester type aconite total alkaloid and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0009] Take 1 kg of dried Aconitum aconitum powder, put it into a percolation device, extract it by percolation with 10L ethyl acetate (ammonia water 2%) for 32 hours, and recover the ethyl acetate under reduced pressure from the percolation solution to obtain 200ml of concentrated solution, acidify with 0.5% HCl to pH = 2, extracted three times with ethyl acetate, alkalized the aqueous layer with 0.5% NaOH to pH = 12, extracted three times with ethyl acetate, combined the ethyl acetate layers, and concentrated to obtain 6 g of total aconitum alkaloids. Add the total alkaloids of Aconitum to 40% by volume of 1,4-dioxane, heat and reflux for 5 hours, concentrate the hydrolyzate and acidify it to pH=2 with 0.5% HCl, extract with ethyl acetate, water The layer was basified with 0.5% NaOH to pH = 12, extracted with ethyl acetate, the ethyl acetate layers were combined, and the ethyl acetate was recovered under reduced pressure to obtain 3.7 g of total monoester aconitum alkaloids w...

Embodiment 2

[0011] Take 1kg of dried Aconitum aconitum powder, impregnate it with methanol (2.5% ammonia water), put it into a percolation device, use 12L methanol (2.5% ammonia water) for percolation extraction for 32 hours, recover methanol under reduced pressure from the percolation liquid, and obtain 300ml concentrated liquid. Acidify with 1.0% sulfuric acid to pH = 1, extract 3 times with petroleum ether, alkalinize the aqueous layer with 0.8% KOH to pH = 12, extract 3 times with petroleum ether, combine the petroleum ether layers, concentrate to obtain the total organism of Aconitum aconitum Alkali 7g. Add the total alkaloids of Aconitum 50% by volume to 1,4-dioxane, heat and reflux for 5 hours, concentrate the hydrolyzate and acidify it to pH=2 with 0.5% sulfuric acid, extract with petroleum ether, and the water layer Then use 0.5% KOH to alkalinize to pH = 12, extract with petroleum ether, combine petroleum ether, and recover petroleum ether under reduced pressure to obtain 4.5 g...

Embodiment 3

[0013] Take 8kg of dried Aconitum aconitum powder, impregnate the Aconitum aconitum powder with ethanol (containing 2.5% ethylenediamine), put it into a percolation device, extract by percolation with 75L ethanol (containing 2.5% ethylenediamine) for 32 hours, and depressurize the percolation liquid Recover ethanol to obtain 960ml concentrated solution, acidify with 0.5% nitric acid to pH = 1, extract 3 times with cyclohexane, alkalinize the aqueous layer with 0.5% calcium hydroxide to pH = 12, extract 3 times with cyclohexane, and combine The cyclohexane layer was concentrated to obtain 51 g of total aconitum alkaloids. Add the total alkaloids of Aconitum 60% by volume to 1,4-dioxane, heat and reflux for 7 hours, concentrate the hydrolyzate, acidify it with 0.5% nitric acid to pH=1-2, and extract it with cyclohexane , the aqueous layer was basified with 0.5% calcium hydroxide to pH = 11-12, extracted with cyclohexane, the cyclohexane layers were combined, and the cyclohexane ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a method for extracting total alkaloid from common monkshood mother root or kusnezoff monkshood mother root and degrading diester type alkaloid in the extract into monoester type alkaloid and an application thereof. Dried common monkshood mother root or kusnezoff monkshood mother root is ground, ethyl acetate (containing ammonia) is used for percolation extraction, percolates are merged, concentrated and acidified by using 0.5 percent HCl until pH is equal to 1 to 2, ethyl acetate extraction is carried out, the water layer is then basified by using 0.5 percent NaOH until pH is equal to 11 to 12, ethyl acetate extraction is carried out, ethyl acetate layers are merged, and after vacuum recovery, aconite total alkaloid is obtained. The aconite total alkaloid is addedinto aqueous 1,4-dioxane solution, the percentage concentration by volume of which is 40 to 80 percent, and after 5 to 8 hours of heating reflux, monoester type aconite total alkaloid is obtained. Theobtained monoester type aconite total alkaloid has an anti-cancer effect.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry research and relates to a monoester type aconitum [0002] Preparation method of alkaloid and its medicinal use. technical background [0003] Aconitum carmichaelii Debx. is the mother root of Aconitum carmichaelii Debx., Aconitum carmichaelii Debx. is the daughter root of Aconitum carmichaelii Debx., and Aconitum carmichaelii Reichb is the dried root of Aconitum carmichaelii Reichb. Folk medicine has a long history and is often used to treat rheumatism, paralysis, cold hernia, pain and other symptoms. It mainly contains alkaloids, flavonoids and polysaccharides. [0004] Scholars at home and abroad have isolated and identified more than 400 alkaloid compounds from plants of the genus Aconitum, mainly diterpenoid alkaloids, among which aconitine, neoaconitine and hypoaconitine are ubiquitous and high in content. alkali. The results of the study show that these three alkaloids are the ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/714A61K125/00
Inventor 李绪文姜亦甫金永日
Owner JILIN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com