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

Androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone and application thereof

A technology of androsteroids and triketones, applied in steroids, medical preparations containing active ingredients, organic chemistry, etc.

Inactive Publication Date: 2013-05-01
KUNMING UNIV OF SCI & TECH
View PDF3 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The androsta-4,6,8(9),13(14)-tetraene-3,11,16-trione compound provided by the present invention and its use as an immunosuppressive drug have not been reported yet

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
  • Androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone and application thereof
  • Androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Preparation of the compound androst-4,6,8(9),13(14)-tetraen-3,11,16-trione

[0012] Take Simao Vine ( Epigynum auritum ) Whole plant dry powder 8.3kg, extracted with ethanol 3 times, 24 hours each time, filtered to remove slag, concentrated and recovered ethanol to obtain an extract, then suspended the extract in water, first extracted with petroleum ether to remove low polar components , and then extracted with ethyl acetate, collected 150 g of the ethyl acetate extract, crudely separated with macroporous adsorption resin D101, and eluted with ethanol-water solution with a mass percentage concentration of 20%, 35% and 60% respectively, and collected 60% ethanol-water eluent was concentrated to obtain 20 grams of extract, mixed with 200-300 mesh silica gel, dry-packed for column chromatography, and used petroleum ether-acetone (volume ratio 10:1-1: 1) The two-phase system is the mobile phase for gradient elution, detected by thin-layer chromatography (TLC), ...

Embodiment 2

[0021] Example 2: Androst-4,6,8(9),13(14)-tetraene-3,11,16-trione immunosuppressive activity test

[0022] (1) Preparation of splenocyte suspension

[0023] Healthy Balb / c mice were killed by eyeball bleeding, soaked in 75% alcohol and disinfected for 5 minutes, taken out, placed in a sterile tray with the left side up, and in the ultra-clean bench, use sterilized tweezers to pick up the fur in the middle of the abdomen , make an incision, use another set of instruments to cut open the layers of the abdominal wall, use the third set of instruments to take out the spleen, remove fat and connective tissue, put it in PBS (phosphate buffer saline), wash away the floating blood; then the spleen Move the tissue to a plate containing RPMI 1640 incomplete culture medium, cut it into small pieces with scissors, grind the spleen in a 200-mesh stainless steel screen with a sterile syringe core, wash it with a small amount of PBS several times, and filter to obtain a single cell Su...

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 polyene high-oxidation androstane compound, i.e., androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone. The compound is extracted from epigynum auritum plant. Experiments prove that the compound has an obvious suppression effect on Balb / c mouse spleen lymphopoiesis stimulated by ConA (concanavalin) and has activity equivalent to that of the conventional immunosuppression active substances, i.e., triptolide and dexamethasone.

Description

technical field [0001] The present invention relates to a new androster compound, specifically androster-4,6,8(9),13(14)-tetraene-3,11,16-trione compound and its application as an immunosuppressive drug . Background technique [0002] Simao vine ( Epigynum auritum ) is a species of the genus Simao of the oleander family, which is produced in southern Yunnan. According to our previous research results, Simaoteng contains more C with novel structure 21 Steroids and other compounds. Driven by the interest in discovering new drug lead compounds, we conducted a large number of biological activity screening experiments on these new compounds and found that one of the androsteroids with a high polyene oxidation degree [androster-4,6,8(9),13 (14)-tetraene-3,11,16-trione] at a concentration of 10-40 μg / mL has comparable activity to the existing immunosuppressive substances triptolide and dexamethasone. [0003] Immunosuppression refers to the suppression of immune response. Imm...

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): C07J1/00A61K31/568A61P37/06
Inventor 曹建新姚元成徐琳琳蔡圣宝
Owner KUNMING UNIV OF SCI & TECH
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