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Application of xanthiazone compound in preparing drug for preventing or treating rheumatoid arthritis

A thiazidedione, rheumatoid technology, applied in the directions of application, drug combination, antipyretics, etc., can solve the problem of no analgesic activity, etc., and achieve the effect of preventing and treating rheumatoid arthritis

Inactive Publication Date: 2018-07-17
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Our previous research found that thiazidione compounds are the anti-inflammatory active ingredients of the traditional Chinese medicine Xanthium n-butanol extract, and 2-hydroxy-Xanthia thiazidediketone glycosides have anti-inflammatory activity, but no analgesic activity

Method used

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  • Application of xanthiazone compound in preparing drug for preventing or treating rheumatoid arthritis
  • Application of xanthiazone compound in preparing drug for preventing or treating rheumatoid arthritis
  • Application of xanthiazone compound in preparing drug for preventing or treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1) Effects of compounds on RAW264.7 inflammatory cells stimulated by LPS

[0034] The basic pathological change of RA is synovitis. As the central cell that initiates the production of inflammatory mediators in the body, the macrophage system plays a leading role in regulating the inflammatory response process, and can produce a large number of cytokines after being activated. RAW264.7 cells, as a kind of macrophages, participate in the immune process of the body, especially after external interference such as lipopolysaccharide (LPS), they can produce a large number of inflammatory mediators. Nitric oxide synthase (NO-synthase, iNOS) catalyzes the reaction of L-arginine and oxygen molecules to generate nitric oxide (nitric oxide, NO). As an important inflammatory mediator in inflammatory response, NO is involved in mediating cellular immunity and inflammatory response. In acute inflammatory sites, inflammatory substances and inflammatory mediators can induce or incre...

Embodiment 2

[0057] 1) Effects of compounds on fibroblast synoviocytes

[0058] Rheumatoid arthritis is mainly manifested as the proliferation of synovial tissue, the most representative of which is fibroblast synoviocytes, so this study starts with fibroblast synoviocytes, by comparing the effects of drugs on cell proliferation, and cell proliferation. The measurement of NO in the supernatant reflects the effect of the drug, wherein NO is a highly reactive cytotoxic free radical and immune active mediator synthesized under the induction of iNOS.

[0059] 2) Pharmacological activity experiment

[0060] (1) The effect of active compounds on the proliferation of fibroblast synoviocytes

[0061] After the membranous cells were digested with 0.25% trypsin in EDTA, DMEM medium was added to adjust the cell concentration to 5×10 4 Cells / mL were inoculated into a 96-well plate at an amount of 100 μl per well. at 5% CO 2 and cultured at 37°C for 24 hours, discarded the supernatant, added variou...

Embodiment 3

[0075] 1) Effects of compounds on the degree of ear swelling caused by xylene

[0076] Xylene can increase the permeability of capillaries. According to the static equilibrium relationship between capillaries and tissues, because the permeability of capillaries increases, the liquid that penetrates into tissues will increase, which is what we see with the naked eye. Inflammatory redness occurs.

[0077] 2) Experimental method

[0078] The male mice were randomly divided into 8 groups according to body weight, 10 in each group, 0.5mL / 20g was administered by intragastric administration 60 minutes before inflammation, and 0.05ml of xylene was dropped in the right ear of the mouse, and the left ear was controlled. After 2 hours, the mice were killed by cervical dislocation, and the two ears were cut off along the baseline of the auricles, and round ear pieces were punched in the same part of the left and right ears with a hole punch with a diameter of 7 mm, and weighed.

[0079]...

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Abstract

The invention relates to the technical field of medicines, in particular to an application of an xanthiazone compound in preparing a drug for preventing or treating rheumatoid arthritis. A formula ofthe xanthiazone compound is shown as follows as shown in the specification. The compound significantly inhibits NO generation for RAW264.7 inflammatory cells and fibroblast-like synoviocytes stimulated by LPS (lipopolysaccharide), and has an obvious inhibiting effect on mouse ear swelling caused by dimethylbenzene and the rheumatoid arthritis induced by collagen, and an obvious swelling diminishing and anti-inflammatory effect on rat toe swelling due to inflammation caused by a Freund adjuvant; and therefore, the compound can be used for preventing and treating the rheumatoid arthritis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a thiazidedione compound in the preparation of drugs for preventing or treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (RA) is one of the most important diseases that endanger human health at present, and is called "the cancer that never dies". RA is a chronic systemic autoimmune inflammatory disease characterized by multi-joint involvement, synovial inflammation, and bone and cartilage destruction. Its pathogenesis has not yet been fully elucidated. Disorders are closely related (Imboden JB. Theimmunopathogenesis of rheumatoid arthritis. Annu RevPathol Mech Dis. 2009, 4:417-434.). In the early stage, the patients have joint redness, swelling, heat pain and dysfunction. In the late stage, the joints may have different degrees of stiffness and deformity, accompanied by bone and skeletal muscle atrophy. From a pathological poi...

Claims

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Application Information

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IPC IPC(8): A61K31/5415A61K31/706C07D279/16C07H15/26A61P29/00A61P19/02A61P1/02A61P19/08A61P19/10A23L33/00
CPCA23V2002/00A61K31/5415A61K31/706A23L33/00C07D279/16C07H15/26A23V2200/30A23V2200/306A23V2200/312
Inventor 蒋益萍韩婷薛黎明辛海量郑承剑张巧艳余璐瑶沈慧叶冰竹
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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