3,16-androstenedione compounds and application thereof

A technology of androstenediones and compounds, applied in the field of 3,16-androstenediones

Active Publication Date: 2018-11-16
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Driven by the interest in discovering new drug lead compounds, pre-biological activity screening found that dotenandrosterone compounds have significant immunosuppressive activity; the dotenandrosterone compounds provided by the present invention and their immunosuppressive drugs have not been reported yet

Method used

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  • 3,16-androstenedione compounds and application thereof
  • 3,16-androstenedione compounds and application thereof
  • 3,16-androstenedione compounds and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: Preparation of 3,16-androstenediones

[0030] Take the plant samples of the genus Simao, dry and crush them, use them, and extract them twice with ethanol solution with a volume concentration of 70%, 3 hours each time, filter to remove the filter residue, combine the extracts, concentrate under reduced pressure, and then use ethyl acetate Extracted 2 times, concentrated to obtain the ethyl acetate layer extract; the ethyl acetate layer extract was roughly separated with macroporous adsorption resin D101, and then purified with pure water, volume percentage 40%, 60%, 80%, 100% A total of 5 fractions (Fr.A, Fr.B, Fr.C, Fr.D, Fr.E) were obtained by eluting with aqueous methanol; 18 The volume concentration of the medium-pressure column is 60%, 70%, 80%, 90% methanol aqueous solution to wash the section, take the 80% methanol water wash section, mix the sample with 100-200 mesh silica gel, and use petroleum ether-acetone two-phase system as The mobile phase w...

Embodiment 2

[0041] Embodiment 2: Immunosuppression detection test

[0042] (1) Preparation of spleen lymphocyte suspension

[0043] Take 18-22g of healthy BABL / c mice and kill them by bloodletting, soak them in 75% alcohol for 5 minutes for disinfection, take them out, put them in a sterile tray with the left side up, and put them in an ultra-clean bench with sterilized Clip the fur in the middle of the abdomen with tweezers, make an incision, use another set of instruments to cut open the layers of the abdominal wall, use a third set of instruments to remove the spleen, remove fat and connective tissue, put it in PBS (phosphate buffer saline), and wash it away. Floating blood; then move the spleen tissue to a plate filled with 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, and use a small amount of PBS several times Rinse, transfer the suspension to a 15mL centrifuge tube wit...

Embodiment 3

[0072] Embodiment 3: in vitro antitumor activity test

[0073] (1) Material

[0074]DMSO (Sigma, USA), fetal bovine serum (HyClone, USA), RPMI-1640 culture medium (HyClone, USA), phosphate buffer (Shanghai beyotime), double antibody (HyClone, USA), CCK-8 (East Asia) Ren Chemical Technology Co., Ltd.), human tumor cells (CCRF-CEM, MOLT-4, K-562, MALME-3M, UACC-62, SNB-75, OVCAR8, EKVX, U0-31, SF-295, NCI-H226 , SK-OV3, MDA_MB-468, Hop92), the compound of the present invention and dexamethasone were prepared with DMSO.

[0075] (2) method

[0076] Take 5 kinds of human tumor cells in the logarithmic growth phase and adjust the cell suspension to a certain concentration and inoculate them in a 96-well culture plate, 90 μl / well, culture for 24 hours, and then add different concentrations of compounds, 10 μl / well, each For each concentration, 3 replicate wells were set. Count the cells and determine the survival rate of the cells using the disc blue staining method, the surviva...

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Abstract

The invention discloses 3,16-androstenedione compounds or pharmaceutically acceptable salts thereof and application of the 3,16-androstenedione compounds or pharmaceutically acceptable salts in preparation of immunosuppressive and anti-tumor drugs. The 3,16-androstenedione compounds are represented in a following formula, are obtained by performing extraction and separation from Epigynum, and havefollowing structural formula, wherein R1 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, carbonyl groups, aliphatic hydrocarbon groups and fatty amino groups, and R2 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, aliphatic hydrocarbon groups and fatty amino groups. It is proven through experiments that the compounds have strong immunosuppressive and anti-tumor activities, and lead compounds are provided for development of immunosuppressants and anti-tumor preparations by the compounds, so that development and utilization of plant medicinal resources are facilitated.

Description

technical field [0001] The present invention relates to a class of 3,16-androstenedione compounds or their medicinal salts and their application in the preparation of immunosuppressive and antitumor drugs. Background technique [0002] The immune response is originally a defense response for the body to protect itself and stabilize itself. Long-term suppression of this response will lead to some serious consequences such as infection and tumor induction, which are also some problems encountered by current immunosuppressants. Immunosuppressants provide effective therapeutic drugs for autoimmune diseases and rejection after organ transplantation in clinic, and are usually used to suppress rejection after organ transplantation, treat graft-versus-host disease after bone marrow transplantation, or treat Rheumatoid arthritis, Crohn's disease and other autoimmune diseases generally use drugs for immunosuppression. [0003] At present, there are about 100 kinds of malignant tumors...

Claims

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Application Information

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IPC IPC(8): C07J1/00A61K31/565A61P37/06A61P35/00
CPCA61P35/00A61P37/06C07J1/0007
Inventor 程桂广杨美莲曹建新高飞万宗姚元成赵天瑞张宏赵燕
Owner KUNMING UNIV OF SCI & TECH
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