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

Iridoid ester compounds, and preparation method and application thereof

A technology of iridoid esters and compounds, which is applied in the field of active ingredients of natural medicines, and achieves the effects of low production cost, novel structure and simple operation

Inactive Publication Date: 2015-03-04
ZHEJIANG CHINESE MEDICAL UNIVERSITY
View PDF0 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In terms of the application of iridoid ester compounds of Valeriana genus in the Patriaceae family, most of the literature reports focus on sedation, hypnosis, antidepressant, etc., and there are few reports on its application in cancer treatment.

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
  • Iridoid ester compounds, and preparation method and application thereof
  • Iridoid ester compounds, and preparation method and application thereof
  • Iridoid ester compounds, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation method of two novel iridoid esters in this valerian plant comprises the following steps:

[0043] A. Extraction: powder the medicinal materials of spider incense, and pass through a 40-mesh sieve for later use. Take 2kg of the coarse powder of spider incense, add an appropriate amount of extraction solvent to moisten it, then pack it into a column, add an appropriate amount of 95% ethanol for cold soaking for 24 hours, then extract by percolation, and collect the percolation liquid. The volume of the total solvent for extraction is equivalent to 15 times of the quality of the medicinal material (30 L of 95% ethanol is used in total).

[0044] B. Extraction: Concentrate the percolation liquid obtained in step A to nearly dryness under reduced pressure to obtain 148.4 g of thick extract, add water to suspend to 1 L, and use 1 L of dichloromethane, 1 L of ethyl acetate, and 1 L of n-butanol respectively Extraction, each extraction solvent was extracted thr...

Embodiment 2

[0049] A. Extraction: take 2 kg of the medicinal material of C. chinensis, add 8 times the amount of 95% ethanol, and extract under reflux at 85°C. The extraction time is 2 hours each time. A total of 2 extractions are made, and the two extracts are combined. A total of 32L of 95% ethanol was used.

[0050] B. Extraction: Concentrate the extract obtained in step A to near dryness under reduced pressure to obtain 157.6 g of thick extract, add water to suspend to 1 L, extract with 1 L of dichloromethane and 1 L of ethyl acetate respectively, and extract with each extraction solvent Three times, the extracts of each time were combined to obtain the dichloromethane extract and the ethyl acetate extract respectively. Through TLC inspection, the iridoid esters of spider incense were mainly concentrated in the dichloromethane extract. The solvent was recovered from the methyl chloride extract under reduced pressure to obtain 97.3 g of the dichloromethane extract of the spider incense...

Embodiment 3

[0062] In vitro anti-tumor experiments of two novel iridoid ester compounds:

[0063] Take the human-derived tumor cell lines in the logarithmic growth phase, digest and count them, and divide them into 6~9×10 3 Cells / 100 μL / well were inoculated in a 96-well cell culture plate, cultured for 24 hours, and treated with different concentrations of compounds 1 and 2 prepared in Example 1 after the cells adhered to the wall, and three replicate wells were set in each well. After incubating the drug with the tumor cells for 48 hours, add MTT, continue to incubate at 37°C for 4 hours, stop the culture, gently absorb the culture solution with a pipette gun, add DMSO (150 μL / well), shake evenly, and use a microplate reader to The optical density OD value of each well was measured at 570nm, the OD value of each parallel well was averaged, and the background OD value was subtracted from the OD value of each test well. Calculate the inhibitory rate of drugs on tumor cells.

[0064] Inhi...

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 iridoid ester compounds and a preparation method thereof, and application of the iridoid ester compounds in cancer therapy. The structure of the iridoid ester compounds is disclosed as Formula (I) or Formula (II). The preparation method comprises the following steps: A. extracting a medicinal material by using an extraction solvent to obtain an extracting solution; B. concentrating the extracting solution, adding water for suspension, extracting respectively with organic solvents with gradually increasing polarity to obtain an extract, and concentrating the extract to obtain an iridoid ester crude extract; C. passing the iridoid ester crude extract through a normal-phase column, and eluting with an eluting agent; collecting the eluate, and drying to obtain an extract which is enriched with two novel iridoid ester compounds; and D. carrying out reverse-phase medium-pressure column chromatography and preparative high-efficiency liquid-phase column chromatography on the extract to obtain the two novel iridoid ester compounds. The preparation method is simple to operate and low in production cost; and the obtained product can be used for preparing cancer therapeutic drugs, and has favorable development prospects.

Description

technical field [0001] The invention belongs to the technical field of active ingredients of natural medicines, and relates to the field of extraction, preparation and application of active ingredients from medicinal plants, and in particular to a method for preparing two novel iridoid esters from plants of the genus Valeriana in the Patinaceae family and its application in cancer therapy. Background technique [0002] There are more than 200 species of plants of the genus Valeriana L. in the family Valerianaceae, which are widely distributed in the northern temperate regions of America, Europe and Asia. There are 17 species and 2 varieties in my country, with the most species distributed in the west and southwest. The genus Valeriana is used as a medicinal plant. At present, Valeriana officinalis Linn, Valeriana amurensis Smir.ex Kom, Valeriana jatamansi Jones and Valeriana broadleaf are widely used. officinalis Linn.var.latifolia Miq) and others. This genus of plants ha...

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): C07D311/94A61K31/352A61P35/00
CPCC07D311/94
Inventor 杨波赵华军谷满仓宋会珠
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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