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

Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes

A kind of technology of asterone and aster, applied in hepatitis B virus inhibitor, application in health care products and food, preparation of anti-hepatitis B virus medicine field

Inactive Publication Date: 2013-06-12
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
View PDF2 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The above methods focus on the index component shionone specified in the Pharmacopoeia, but hardly involve other shionone-type triterpenes with strong activity.

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
  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes
  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes
  • Shionone triterpenes as well as pharmaceutical compositions, preparation methods and applications of shionone triterpenes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation and structural identification of new shionone-type triterpenes astatarone C(1), astatarone G(2) and astatarone H(3) from Aster genus:

[0034] Take 50kg of roots and rhizomes of Aster genus Aster, after drying and crushing, soak in 90% industrial methanol for 5 hours, then heat to 65°C for reflux extraction for 3 times (200L×3 times), the first time is 3 hours, For the second time and the third time respectively for 2 hours, the extract was concentrated under reduced pressure to obtain 23kg of methanol extract; ×3 times), the solvent was recovered to obtain 2kg of ethyl acetate, 5L of n-butanol and water; the ethyl acetate was subjected to silica gel (100-200 mesh) column chromatography, and eluted with chloroform to obtain a chloroform segment; The chloroform section was subjected to silica gel (100-200 mesh) column chromatography, eluted with petroleum ether / acetone (100:0-8:1), combined with TLC detection method, and combined into 6 according to the polar...

Embodiment 2

[0047] Experiments on the inhibitory effect of astatarone C (1), astatarone G (2) and astatarone H (3) of the present invention on the secretion of HBsAg and HBeAg from HepG2.2.15 cells and their toxicity to HepG2.2.15 cells. The specific experimental principles, methods and results are as follows:

[0048] Anti-HBV experimental principle: HepG2.2.15 cell line is a transfected cell line established after stably transfecting the whole HBV genome. HepG2.2.15 cells can secrete complete HBV viral DNA and express HBV antigens stably for a long time. It is a good cell model for screening anti-HBV drugs and drug evaluation in vitro, and has been widely used in in vitro research on anti-HBV drugs. . The test compound was co-cultured with HepG2.2.15 cells, and the level of HBsAg and HBeAg secreted by the cells after administration was detected by the HBV antigen detection kit, which can reflect the anti-HBV effect of the compound in vitro.

[0049] Anti-HBV experimental method: (1) C...

Embodiment 3

[0058] Compound 1-3 obtained in Example 1 was added with 5% sodium hydroxide or ammonia solution, pH = 14, filtered, and dried to prepare sodium or ammonium salt compound 1-3.

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 tetracyclic triterpenoids shown as in structural formula (I), i.e., shionone triterpenes including astatarone C (1), astatarone G (2) and astatarone H (3), preparation methods of the shionone triterpenes and applications of the shionone triterpenes to the preparation of drugs for preventing and treating hepatitis B viruses (HBV) and the preparation of liver protection foods and health care products, wherein R in the formula represents anti-HBV drugs taking the shionone triterpenes as active components. Test results prove that the triterpenoids provided by the invention have a better anti-HBV activity and can be used for preparing the anti-HBV drugs. A new source is provided for finding the anti-HBV drugs. An extracting and separating method provided by the invention is good in controllability and repeatability, lower in cost and more convenient to operate.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular, relates to some new shionone-type triterpenes, a pharmaceutical composition containing them as active ingredients, which are used as hepatitis B virus inhibitors, their preparation methods and their application in the preparation of anti-hepatitis B Applications in virus medicine, health care products and food. Background technique: [0002] Hepatitis B virus, referred to as hepatitis B, is a disease caused by hepatitis B virus (HBV) infection of the body. It can be divided into acute and chronic diseases, which seriously endanger human health and affect people's quality of life. Hepatitis B virus is a hepatotropic virus that mainly exists in liver cells and damages liver cells, causing inflammation, necrosis, and fibrosis of liver cells. HBV infection is a worldwide epidemic. About 2 billion people in the world have been infected with HBV, 50 million new infections occur e...

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): C07J63/00A61K31/56A61P31/20A61P1/16A23L1/29A23L33/00
Inventor 谭宁华周文兵曾广智徐会敏
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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