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A furan ring derivative and its application in the preparation of drugs with immunosuppressive activity

A technology of immunosuppression, derivatives, applied in the fields of medicine and microbiochemistry

Active Publication Date: 2022-03-15
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its in vitro activity is 5-10 times stronger than cyclosporine, and its in vivo activity is 10 times stronger than cyclosporine, but its toxicity is 100 times that of cyclosporine, which limits the direct application of ISP-1 in clinical practice

Method used

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  • A furan ring derivative and its application in the preparation of drugs with immunosuppressive activity
  • A furan ring derivative and its application in the preparation of drugs with immunosuppressive activity
  • A furan ring derivative and its application in the preparation of drugs with immunosuppressive activity

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1: The compound described in the claims and the description of the invention - a furan ring derivative is obtained as follows:

[0027] Compound separation and purification process:

[0028] Glucose-peptone liquid culture medium is 80L in total, among which glucose (50g), peptone (10g), potato (200g), KH 2 PO 4 (10g), yeast powder (10g), evenly distributed in the conical flask (250mL × 640 bottles, 125mL per bottle), inoculate 5ml of culture medium in each bottle with a concentration of 6 × 10 7 cfu / ml of MHHNU7966-IS bacterial suspension, then cultured on a shaker, cultured and fermented in the dark at a constant temperature of 24°C and rotated at 150rpm for 30 days, and then used a centrifuge to filter 80L of Cordyceps xuefeng liquid into fermentation broth and solid Mycelia, and then utilize rotary evaporator and vacuum pump and low-temperature cooling circulating pump (the same below, decompression concentration device) to distill the filtrate (i.e. "fe...

Embodiment 2

[0037] Example 2: Determination of the immunosuppressive activity of the compound prepared in Example 1 using the non-specific toxicity and proliferation response experiments of mouse lymphocytes

[0038] (1) Preparation of mouse spleen lymphocytes:

[0039] The mice were sacrificed by devertebralization, and their spleens were aseptically removed to prepare a single cell suspension, and the erythrocytes were removed with erythrocyte lysate to adjust the cell concentration.

[0040] (2) Compound concentration processing:

[0041] All test compounds were dissolved in DMSO (dimethyl sulfoxide), and the stock solution concentration was 40 mM. For the detection of cytotoxicity, 200 μM of the test compound was the highest concentration, and 2.5-fold serial dilution was set up with 10 concentrations: 200, 80, 32, 12.8, 5.12, 2.048, 0.82, 0.33, 0.13, 0.05 μM; cyclosporine A ( Cyclosporin A, CsA) 20μM is the highest concentration, 2-fold serial dilution, set 10 concentrations: 20, 1...

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Abstract

The invention relates to the technical field of medicinal microbial chemistry, specifically disclosing a plant of Cordyceps xuefeng ( Ophiocordyceps xuefengensis ) strain of the furan ring derivatives isolated from the liquid fermentation product and its use in the preparation of immunosuppressive drugs, more specifically described the application in the preparation of drugs with significant inhibitory activity on T cell proliferation. The immunosuppressive effect of the furan ring derivatives of the present invention is better than that of cyclosporin A, an immunosuppressant widely used in clinical practice, and is a highly efficient immunosuppressant, which can be used to prepare drugs for organ transplantation and autoimmune diseases. Immunosuppressive drugs.

Description

technical field [0001] The invention relates to the technical fields of medicine and microbial chemistry, in particular to a furan ring derivative derived from Ophiocordyceps xuefengensis and its application in the preparation of drugs with immunosuppressive activity. Background technique [0002] The role of Cordyceps immunoregulatory function on the body is mainly realized by activating cells and lymphocytes, inducing various cytokines and other ways. As the hometown of Cordyceps sinensis, my country's "Medical Chinese Medicine Pharmacology" records that Cordyceps sinensis has the functions of enhancing non-specific immunity, regulating humoral immunity, regulating cellular immunity, enhancing the function of immune organs, enhancing the function of cell system and enhancing natural killer cells. Active and many other immune effects; "Chinese Tibetan Medicine" also recorded the good immune regulation of Cordyceps sinensis. Cordyceps Xuefeng is a new species under the genus...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/46A61P37/06A61P35/00C12P17/16C12R1/645
CPCC07D307/46A61P37/06A61P35/00C12P17/162
Inventor 艾洪莲张娴李正辉冯涛叶可吕晓
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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