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
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The androsta-4,6,8(9),13(14)-tetraene-3,11,16-trione compound provided by the pre

Method used

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  • 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
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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...

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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

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Application Information

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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
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