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Polyenoid androsterone compound and application thereof

A kind of technology of polyene androsterone and compound, applied in the field of polyene androsterone compound

Active Publication Date: 2018-06-22
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The polyene-androsterone compound provided by the present invention and its use as an immunosuppressive drug have not yet been reported

Method used

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  • Polyenoid androsterone compound and application thereof
  • Polyenoid androsterone compound and application thereof
  • Polyenoid androsterone compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of 12β-hydroxyandrost-3,5,14(15)-trien-16-one

[0023] Get 11.0kg dry powder of above-ground parts (stems and leaves) of Laos florida Simao vine plant sample, reflux extraction with 75% ethanol for 3 times, each time for 48h, filter and remove the filter residue after merging the filtrate extracted three times, concentrate under reduced pressure and then use ethyl acetate Extracted 3 times, concentrated the ethyl acetate extract layer and weighed to obtain 352g; the ethyl acetate layer extract was roughly separated by a C18 column, and the volume percentage was 20%, 40%, 50%, 60%, 80%, 100% A total of 6 fractions (Fr.A, Fr.B, Fr.C, Fr.D, Fr.E) were obtained by elution with aqueous methanol solution. Fr.D obtained four parts Fr.B1-B4 by gradient elution with 40%-80% by volume methanol aqueous solution in the preparation liquid phase. Then pass the Fr.B2 through a 200-300 mesh silica gel column, and use chloroform-acetone (volume ratio 20:1-3:1) as...

Embodiment 2

[0027] Example 2: Preparation of 12β-hydroxyandrost-3,5,14(15)-trien-16-one

[0028]Take 11 kg of Yunnan Simao rattan samples after air-drying, crush them and extract them 3 times with methanol reflux, recover the solvent, concentrate to a small volume, then extract 3 times with ethyl acetate, concentrate the ethyl acetate layer, and weigh to obtain 1.2 kg; The ethyl acetate layer was roughly divided with macroporous adsorption resin D101, and eluted with 40%, 60%, 80%, and 100% methanol aqueous solution to obtain a total of 5 fractions (Fr.A, Fr.B , Fr. C, Fr. D, Fr. E). Fr.E (280g) was mixed with 1.5 times the amount of silica gel, mixed with silica gel for routine drying, packed into a column, and carried out gradient elution with chloroform-acetone (0:100-95:5) two-phase system as the mobile phase, according to TLC Check and merge to get three parts Fr.E1-E3. Fr.E2 was eluted with methanol-water gradient on a reverse-phase C18 column with C18 packing to obtain two fracti...

Embodiment 3

[0029] Embodiment 3: Immunosuppression detection test

[0030] (1) Preparation of spleen lymphocyte suspension

[0031] Take 18-22g of healthy BABL / c mice and kill them by bleeding, soak them in 75% alcohol for 5 minutes, take them out, place them in a sterile tray with the left side up, and clamp them with sterilized forceps in a clean bench. Remove 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), and wash away the 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, wash it with a small amount of PBS several times, and Transfer the suspension to a 15mL centrifuge tube with a pipette; centr...

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Abstract

The invention discloses a polyenoid androsterone compound and application thereof. The compound is extracted and separated from an epigynum auritum plant, and the structural formula is as shown in thedescription, wherein R1, R2 and R3 are selected from hydrogen, hydroxyl, methyl, halogen, an aliphatic group and fat amino. The experiment proves that the compound reported in the invention has highImmunosuppressive activity. The compound provided by the invention provides a lead compound for development of an immunosuppressive agent and an anti-tumor preparation, and is favorable for developingand utilizing plant medicinal resources.

Description

technical field [0001] The invention relates to a polyene androsterone compound and its application in the preparation of immunosuppressive and antitumor drugs. Background technique [0002] Steroid drugs are the most commonly used clinical immunosuppressants, such as prednisone, dexamethasone, methylprednisolone and so on. It can effectively inhibit inflammatory factors and reduce various immune cells. 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 Autoimmune diseases such as rheumatoid arthritis and Crohn's disease. [0003] At present, there are about 100 kinds of malignant tumors, and the number of people who die from cancer accounts for about 13% of the world's disease deaths; it is estimated that cancer deaths worldwide will continue to i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00A61P35/00A61P37/06
CPCC07J1/0007
Inventor 曹建新蒋孟君程桂广高飞赵天瑞张宏赵燕
Owner KUNMING UNIV OF SCI & TECH
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