Method for preparing novel mogrol derivatives from momordica grosvenori total saponins

A technology of mogrosides and mogrosanol, which is applied in the field of medicine, can solve the problems of low yield, difficult separation and purification, and difficult industrial production, and achieves the effect of low cost, simple synthesis method, and low cost

Active Publication Date: 2016-08-10
SHENZHEN YINUO BIOPHARM CO LTD
View PDF3 Cites 16 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the literature has reported the preparation of Mogrosin alcohol derivative monomer (3) (Chen X.B., et al; Bioorganic & Medicinal Chemistry 2011,19:5776), but the yield is low, separation and purification are difficult, and it is difficult to industrialize production. In addition, this method ca

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 novel mogrol derivatives from momordica grosvenori total saponins
  • Method for preparing novel mogrol derivatives from momordica grosvenori total saponins
  • Method for preparing novel mogrol derivatives from momordica grosvenori total saponins

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0079] The present invention also provides a method for synthesizing the above composition, which comprises: dissolving the Monk Fruit extract containing total saponins of Monk Fruit in an acidic alcoholic aqueous solution and performing a heating reaction to obtain the composition.

[0080] The alcohol is at least one of methanol, ethanol, n-propanol, isopropanol, butanol; ethylene glycol, propylene glycol, glycerol; polyethylene glycol.

[0081] The preparation method of the acidic alcohol aqueous solution is: adjust the alcohol aqueous solution to be acidic with an acidic substance, preferably, the volume ratio of alcohol to water in the alcohol aqueous solution is 1:10-10:1; preferably 1:3 to 3:1;, more preferably 1:1.

[0082] Preferably, the acidic substance is an inorganic acid or an organic acid; further preferably, the inorganic acid is at least one of hydrochloric acid, sulfuric acid and phosphoric acid; the organic acid is formic acid, acetic acid, haloacetic acid, ...

Embodiment 1

[0111] Example 1: Preparation of Mogrosanol Derivatives Monomers (3) and (4) from the Extract of 98% Mogrosin Total Saponins

[0112] Add 50g of Luo Han Guo extract (98% of the total saponins of Luo Han Guo, containing 55% of Mogroside V, purchased from Guilin Laiyin Biotechnology Co., Ltd.) to 250 mL of ethanol aqueous solution (the volume ratio of ethanol and water is 1:1) (prepared with Hydrochloric acid adjusted to a pH value of 3.0), stirred and dissolved in the reactor, then heated to 120 ° C for 2 hours, cooled to room temperature 25 ° C, the reaction solution was neutralized to a pH value of 7 with 1M NaOH lye, and in Distill the ethanol as much as possible at 90-95°C, add 200mL of distilled water to the remaining concentrated solution, stir thoroughly, cool and let it stand, separate and discard the upper water layer to obtain a brown extract; use 100mL, 50mL, and 50mL of acetic acid respectively Extract the brown extract with ethyl ester for 3 times, combine the 3 ex...

Embodiment 2

[0114] Example 2: Preparation of Mogrosanol Derivative Monomers (3) and (4) from the Extract of 95% Mogrosin Total Saponins

[0115] Add 50g of Luo Han Guo extract (95% of the total saponins of Luo Han Guo, containing 45% of mogroside V, purchased from Guilin Laiyin Biotechnology Co., Ltd.) into 250 mL of methanol aqueous solution (the volume ratio of methanol and water is 3:2) (pre-used Sulfuric acid is adjusted to a pH value of 2.8), stirred and dissolved in the reactor, and then heated to 120°C for 2 hours, cooled to room temperature, and the reaction solution is neutralized with 1M KOH lye to a pH value of 7. Distill the methanol as much as possible at 95°C, add 200mL of distilled water to the remaining concentrated solution, stir thoroughly, cool and let it stand, separate and discard the upper water layer to obtain a brown extract; use 100mL, 50mL, and 50mL ethyl acetate respectively Extract the coffee-colored extract 3 times, combine the 3 extracts, concentrate with a r...

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 provides a synthesis method for a compound containing a mogrol derivative monomer (3) and a mogrol derivative monomer (4). Compared with an existing method for synthesizing the mogrol derivative monomer (3), the synthesis method is simple and low in cost, the novel mogrol derivative monomer (4) can be synthesized, and meanwhile on this basis, the invention further provides a method for preparing the mogrol derivative monomer (3) and the mogrol derivative monomer (4). According to the method, on the basis of the simple column chromatography separation technology, the mogrol derivative monomer (3) and the mogrol derivative monomer (4) can be prepared through low-cost, high-efficiency and large-scale separation, and a foundation is laid for further developing novel related medicines.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a synthesis method of mogrosvenol derivatives. Background technique [0002] In recent years, countries around the world have undergone major changes in their views on cancer and other diseases (including cardiovascular and cerebrovascular diseases, diabetes, mental depression, Alzheimer's disease, etc.), and more and more doctors and researchers are looking for preventable diseases. Or natural medicines that delay the onset of these diseases. At present, natural, high-efficiency, broad-spectrum, and low-toxic clinical research compound drugs for the prevention and treatment of cancer and other diseases, many of which are natural drugs or semi-synthetic products derived from natural raw materials, are currently research and development hotspots in the field of biomedicine. [0003] The latest biomedical research shows that many monomeric active ingredient drugs or multi-component active ...

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
IPC IPC(8): A61K31/575C07J9/00A61P35/00
CPCA61K31/575C07J9/00A61K36/42A61K2300/00
Inventor 余佩华邓跃敏钟牧源
Owner SHENZHEN YINUO BIOPHARM CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap