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Small-molecule compound for treating rheumatoid arthritis and application thereof

A small molecular compound, arthritis technology, applied in medical preparations containing active ingredients, plant/algae/fungus/moss components, applications, etc., can solve problems such as increased production of matrix metalloproteinases and destruction of articular cartilage

Inactive Publication Date: 2019-01-04
LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

IL-6 and IL-1 work together to increase the production of matrix metalloproteinases, leading to the destruction of articular cartilage

Method used

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  • Small-molecule compound for treating rheumatoid arthritis and application thereof
  • Small-molecule compound for treating rheumatoid arthritis and application thereof
  • Small-molecule compound for treating rheumatoid arthritis and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example

[0020] 20 clean-grade TNF-Tg mice aged about 3 months were randomly divided into TNF-Tg group and Violet proscurdin group according to body weight, and another 10 wild-type mice (WT) with similar body weight as control group were taken as Control group The proscurdin group was given 5 mg / (kg·d) orally every day, and the control group and the TNF-Tg group were given the same amount of pure water every day. After 12 weeks of continuous gastric gavage, the ankle joints were taken and tested. Micro-CT was used to detect ankle bone mass, and paraffin sections were made for hematoxylin-eosin (HE) staining to observe inflammatory infiltration and joint bone destruction, and Alcian blue-orange G (ABOG) staining to observe articular cartilage destruction. The number of osteoclasts was observed by tartrate acid phosphatase (TRAP) staining.

[0021] 4.1 Perform micro-CT detection.

[0022] After animal ankle joints were taken, they were fixed in 10% paraformaldehyde for 24 hours, transf...

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PUM

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Abstract

The invention relates to a small-molecule compound for treating rheumatoid arthritis. The effective component of the small-molecule compound is nodakenin, the compound serves as a medicine for treating rheumatoid arthritis, and the effective action concentration of the nodakenin is 0.01-1000 micromole / L. The nodakenin and pharmaceutically acceptable pharmaceutical adjuvants are mixed to form powder, paste, pulvis, water aqua, enteric sustained-release preparations or injections. Animal experiments prove that the nodakenin can make the inflammatory infiltration area, bone mass defects and cartilage defects of TNF-Tg rheumatoid arthritis mice reduced, and relieve ankle inflammation injury. The nodakenin can relieve symptoms of rheumatoid arthritis. The invention further discloses applicationof the nodakenin in preparation of medicines or health products for treating rheumatoid arthritis.

Description

technical field [0001] The invention relates to a small molecular compound for treating rheumatoid arthritis, and proposes the application of the compound in preparing various forms of medicines or health food for preventing and treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (Rheumatoid Arthritis, RA) is a chronic, systemic, progressive, autoimmune disease, characterized by extensive persistent synovitis and symmetrical, destructive joint disease. The treatment of RA is very difficult, so far, there is still a lack of safe and effective drugs. Modern medicine is mainly about anti-inflammation and alleviating sequelae. Drugs such as TNFα inhibitors Etanercept, Infliximab and Adalimumab can reduce some objective symptom indicators such as swelling and tender joint counts to 50% in some RA patients, but many patients still have problems in initial treatment. Its non-response, or the failure of the second treatment, an average of about 10% of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P19/02C07H15/26C07H1/08
CPCA23L33/105A61K31/7048C07H1/08C07H15/26A61K36/232A61K36/237A23V2002/00A23V2250/21A23V2200/306
Inventor 梁倩倩王拥军王腾腾贾庆运徐浩施杞王琼王晓赟王怡茹齐晓凤刘洋许崇卿刘利张利李强刘书芬
Owner LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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