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New immunosuppressive agent extracted from Honghuoma and extraction method and use thereof

An immunosuppressant and weighing technology, which is applied in the field of medical chemical drugs, can solve the problems of short drug action cycle, side effects limit application, and no ideal effective drugs, etc.

Active Publication Date: 2009-11-25
HUAZHONG UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, severe side effects of these drugs limit their application
In recent years, with the deep understanding of the pathogenesis of rheumatoid arthritis at the tissue, cellular and molecular levels, a large number of biological therapeutic agents have been produced, such as various monoclonal antibodies, anti-cytokine antibodies, anti-co-stimulatory molecule antibodies, etc. Although these drugs have achieved certain results in the treatment of rheumatoid arthritis, their application is limited due to antigenicity, short drug action cycle, and repeated withdrawal of the drug. Therefore, there is no ideal effective drug for this type of disease.

Method used

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  • New immunosuppressive agent extracted from Honghuoma and extraction method and use thereof
  • New immunosuppressive agent extracted from Honghuoma and extraction method and use thereof
  • New immunosuppressive agent extracted from Honghuoma and extraction method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Example 1. Extraction and separation of ethyl acetate part of red live hemp

[0086] Weigh the washed and air-dried red live hemp, soak it with 95% ethanol for several times (5-8 times) after crushing, soak the solvent every time to cover the medicinal materials, soak for 3-5 days each time, take the soaking liquid and recover it under reduced pressure To obtain the ethanol extract of Honghuoma, suspend the ethanol extract of Honghuoma in water and then extract with petroleum ether, water-saturated ethyl acetate, water-saturated n-butanol and water, respectively, to obtain petroleum ether extract, ethyl acetate extract, Butanol extract and water extract. The red live hemp used in this example comes from Enshi Autonomous Prefecture, Hubei Province, my country.

Embodiment 2

[0087] Example 2. The extraction and separation of novel immunosuppressant erythromycin

[0088] a. Completely dissolve the extract of the ethyl acetate part with an organic solvent and put it on a silica gel column, and use eluents of different polarities prepared by two solvents, petroleum ether and ethyl acetate, to elute sequentially according to the polarity from small to large, The elution order is: petroleum ether, petroleum ether: ethyl acetate = 50:1, petroleum ether: ethyl acetate = 10:1, petroleum ether: ethyl acetate = 2:1 and water-saturated ethyl acetate. Ether: ethyl acetate = 2: 1 Pale yellow needle-like crystals were precipitated in some fractions, and the mother liquor was changed to a 200-300 mesh silica gel column to continue separation. Petroleum ether: ethyl acetate = 5: 1, petroleum ether: ethyl acetate Esters = 1:1 and ethyl acetate were eluted separately, and light yellow needle crystals also precipitated in the fraction of petroleum ether: ethyl aceta...

Embodiment 3

[0095] Embodiment 3 Preparation of different dosage forms of immunosuppressant erythromycin of the present invention

[0096] There is no clear limitation on the dosage form of the immunosuppressant containing erythromycin in the present invention, and various types of oral or parenteral preparations can be made according to actual clinical conditions. In order to meet the needs of clinical treatment of autoimmune diseases, the invention also provides a clinically suitable dosage form for the novel immunosuppressant.

[0097] 1. Separation and purification of kenafin: take the washed and air-dried red hemp, soak it several times (5 to 8 times) with 95% ethanol after crushing, and make the solvent submerge the medicinal material for each soaking, and soak for 3 to 5 times each time. After taking the soaking liquid and recovering it under reduced pressure, the ethanol extract of Honghuoma was obtained. After suspending the ethanol extract of Honghuoma in water, it was extracted ...

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Abstract

The invention obtains neodicoumarin compound that is 1,3-(6',6'',7',7''-tetramethoxy-8', 8''-dicoumarin)-acetone with immunologic suppression effect, in particular with induced specific immunologic tolerance effect that is extracted and separated from Honghuoma acetic ether extract, wherein the compound produces induced specific immunologic tolerance or achieve new balance effect for unbalanced immune system by inhibiting the multiplication of T lymphocyte, reducing the expression of intracellular transcription factor T-bet of dendritic cell (DC), inducing immature DC and adding the amount of T cells expressing Foxp3 regulation and can be used as an immunosuppressive agent, thereby being used for the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus.

Description

technical field [0001] The present invention relates to medicinal chemicals, in particular to an immunosuppressant and its separation and extraction method and application. technical background [0002] Autoimmune diseases are diseases caused by the body's immune response to self-antigens, resulting in damage to its own tissues. High titer autoantibodies can be detected in the serum of patients. The etiology is still unclear, and it may be related to genetics, infection, drugs and environmental factors. Related, the course of disease is long and occurs alternately repeatedly. Autoimmune diseases mainly include organ-specific autoimmune diseases and systemic autoimmune diseases. The former includes chronic lymphatic thyroiditis, hyperthyroidism, insulin-dependent diabetes mellitus, myasthenia gravis, chronic ulcerative colitis, pernicious anemia with chronic atrophic gastritis, goodpasture syndrome, and multiple sclerosis , acute idiopathic polyneuritis, etc.; the latter in...

Claims

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Application Information

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IPC IPC(8): C07D311/16A61K31/37A61P37/06A61P37/00A61P19/04A61P29/00
Inventor 向明苏志强陈新民
Owner HUAZHONG UNIV OF SCI & TECH
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