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3,16-androstenediones and their applications

A kind of technology of androstenedione and compound, which is applied in the application field of preparing immunosuppressive and antitumor drugs

Active Publication Date: 2021-01-05
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-androstenediones and their applications
  • 3,16-androstenediones and their applications
  • 3,16-androstenediones and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0030] The samples of Simao vines were taken, dried and pulverized, and extracted twice with 70% ethanol solution by volume for 3 h each time. The filter residue was removed by filtration, and the extracts were combined, concentrated under reduced pressure, and then extracted with ethyl acetate. Extracted twice, concentrated to obtain an ethyl acetate layer extract; the ethyl acetate layer extract was roughly divided with macroporous adsorption resin D101, followed by pure water, 40%, 60%, 80%, 100% by volume A total of 5 fractions (Fr.A, Fr.B, Fr.C, Fr.D, Fr.E) were obtained by elution with aqueous methanol; 5 g of fraction D was used with C 18 The medium pressure column was washed with methanol aqueous solutions of 60%, 70%, 80%, and 90% by volume, and the 80% methanol water washed section was used to mix the samples with 100-200 mesh silica gel, and the petroleum ether-acetone two-phase system was used as the The mob...

Embodiment 2

[0041] Example 2: Immunosuppression detection test

[0042] (1) Preparation of spleen lymphocyte suspension

[0043] 18~22g healthy BABL / c mice were sacrificed by exsanguination, soaked in 75% alcohol for 5 minutes, taken out, placed in a sterile tray with the left side up, in a clean bench, and disinfected with sterilized Tweezers pick up the fur in the middle of the abdomen, make an incision, use another set of instruments to cut the layers of the abdominal wall, use a third set of instruments to take out the spleen, remove fat and connective tissue, put it in PBS (phosphate buffered saline), wash away Floating blood; then transfer the spleen tissue to a dish containing RPMI 1640 incomplete culture medium, cut it into small pieces with scissors, use a sterile syringe core to grind the spleen in a 200-mesh stainless steel mesh, and use PBS in small quantities several times Rinse, transfer the suspension to a 15 mL centrifuge tube with a pipette; centrifuge at 1000 r / min for ...

Embodiment 3

[0072] Example 3: In vitro antitumor activity test

[0073] (1) Materials

[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 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 five 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 measure the survival rate of the cells using the disc blue staining method, the survival rate ...

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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 preparing immunosuppressive and antitumor drugs. Background technique [0002] The immune response is a defense response of the body for self-protection and self-stabilization. Long-term inhibition of this response will bring some serious consequences such as infection and tumor induction, which are also some of the problems encountered by the current immunosuppressants. Immunosuppressants provide effective therapeutic drugs for autoimmune diseases and organ transplant rejection in clinical practice. They are usually used to suppress rejection after organ transplantation, treat graft-versus-host disease after bone marrow transplantation, or treat Autoimmune diseases such as rheumatoid arthritis and Crohn's disease are generally immunosuppressed by drugs. [0003] At present, there are about 100 kinds of malignant tumors, and the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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