Application of carbon-21 steride compound

A technology of steroidal compounds and drugs, applied in the field of medicine, can solve the problems of unreported application and little research on the pharmacological activity of compounds

Inactive Publication Date: 2012-07-18
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since its chemical structure was reported, there have been few studies on the pharmacological activity of this compound, and there has been no report on its application in anti-inflammatory and immunosuppressive drugs by inhibiting the activation of T lymphocytes

Method used

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  • Application of carbon-21 steride compound
  • Application of carbon-21 steride compound
  • Application of carbon-21 steride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Inhibition of STA on T lymphocyte activation in vitro

[0029] 1.1 Experimental method

[0030] 1.1.1 Preparation of mouse spleen cell suspension

[0031] The spleen of the mice was taken aseptically, added with appropriate amount of Hank's solution, and ground, filtered through a 200-mesh stainless steel mesh, centrifuged at 1500 rpm for 5 minutes, discarded the supernatant, red blood cells were removed with red blood cell lysate, and washed twice with Hank's solution. Collect spleen cells, add appropriate amount of RPMI 1640 complete culture medium to suspend, count with 0.4% (mass percentage) trypan blue exclusion method, and the number of viable cells is not less than 95%.

[0032] 1.1.2 T lymphocyte separation

[0033] T cells were separated by nylon wool column method. Take the sterilized nylon wool column and fix it vertically, put it in the ultra-clean table, connect the rubber tube and valve controller at the bottom outlet; flush the balanced column bed with...

Embodiment 2

[0056] Example 2: Inhibition of T lymphocyte activation by STA in vivo

[0057] DTH response is an immune response mediated by sensitized T cells. It is a local reactive inflammation characterized by mononuclear cell infiltration and cell degeneration and necrosis caused by the specific reaction of T cells with antigens, through phagocytes and lymphocytes Gathering in local tissues, causing local damage and increased vascular permeability, such as increased ear swelling. Therefore, we used the DTH response induced by DNFB to observe the effect of STA on the activation of T lymphocytes in vivo.

[0058] 2.1 Experimental method

[0059] 2.1.1 Preparation of drugs

[0060] The drug STA and the positive control CsA are both polished with 0.5% (mass percentage) CMC-Na solution and diluted to the required concentration.

[0061] 2.1.2 Grouping and processing

[0062] Take 50 mice, shave their abdomen, apply 50μl of 1% (mass percentage) DNFB acetone sesame oil (1∶1, volume ratio) solution to ...

Embodiment 3

[0069] tablet:

[0070]

[0071] Preparation method: mix the active ingredient, lactose and starch, evenly moisten it with water, sieve and dry the moistened mixture, then sieve, add magnesium stearate, and then press the mixture into tablets, each weighs 250mg, and the active ingredient content is 10mg .

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Abstract

The invention discloses application of a carbon-21 steride compound STA (stephanthraniline A) in preparation of anti-inflammatory medicines and immunosuppressive agents. The immunosuppressive agents comprise medicines for preventing and treating rejection in organ transplantation, medicines for preventing and treating allergic diseases or medicines for preventing and treating autoimmune diseases. The results of a variety of in-vivo and in-vitro experiments demonstrate that the compound has the effect of T lymphocyte activation suppression and is different from the traditional steride anti-inflammatory medicines in the action mechanism, i.e. the STA acts without virtue of a glucocorticoid receptor.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to the use of a natural or synthetic carbon-21 steroid compound Stephanthraniline A (STA). Background technique [0002] In recent years, immunosuppressants have developed rapidly and have been widely used to control organ transplant rejection, allergic diseases, autoimmune diseases (such as rheumatoid arthritis, lupus erythematosus, nephrotic syndrome, etc.), and infectious inflammation. However, most of the immunosuppressive drugs commonly used clinically have obvious side effects. For example, glucocorticoids can cause diseases such as osteoporosis, diabetes, and glaucoma; cyclophosphamide can cause leukopenia, hemorrhagic cystitis, cardiotoxicity and alopecia; long-term use of azathioprine (Aza) and imidazole Ribin (Mizoribine, MZ) can induce cancer; Cyclosporine (Cyclosporine, CsA), tacrolimus (FK506, Tacrolimus), sirolimus (Sirolimus) has nephrotoxicity, liver toxicity and neurot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00A61K31/565A61P29/00A61P37/06A61P37/08
Inventor 陈峰阳叶益萍李晓誉徐世芳
Owner ZHEJIANG ACAD OF MEDICAL SCI
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