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Application of LCA in preparation of drug for treating joint inflammation or cartilago articularis and bone destruction

An inflammation and drug technology, applied in the application field of LCA in the preparation of drugs for the treatment of joint inflammation or articular cartilage and bone destruction, to achieve the effect of broad application prospects

Active Publication Date: 2015-03-25
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

At present, there is no report about the therapeutic effect and mechanism of compound LCA on rheumatoid arthritis.

Method used

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  • Application of LCA in preparation of drug for treating joint inflammation or cartilago articularis and bone destruction
  • Application of LCA in preparation of drug for treating joint inflammation or cartilago articularis and bone destruction
  • Application of LCA in preparation of drug for treating joint inflammation or cartilago articularis and bone destruction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Research on the target of compound LCA

[0021] The target effect of the compound LCA was studied, and the intracellular binding of the compound to MEK1 (RAW264.7 cell) and cathepsin K (Osteoclast) was studied using cellular thermal shift assay (CETSA).

[0022] 1 Experimental method

[0023] 1.1 Osteoclast induction

[0024] Five newborn 3-day-old SD mice were sacrificed, soaked in 75% ethanol solution for 5-10 min, and the tibia of the limbs were removed under the ultra-clean bench, and the bone marrow cells in the bone marrow cavity were absorbed by 1 mL syringe to absorb α-MEM medium. Rinse out, collect the washing liquid, centrifuge at 1200 rpm / min for 10 min, and wash the cells twice with PBS to obtain fresh bone marrow mononuclear cells. The cells were cultured with α-MEM containing 5 ng / mL M-CSF and 10% fetal bovine serum at a cell concentration of 10 7 -10 9 pc / mL, 37℃, 5% CO 2Incubate for 24 h in the incubator. Transfer the unattached cells t...

Embodiment 2

[0033] Example 2 Animal Experiments of Compound LCA in Treating Rheumatoid Arthritis

[0034] 1 Experimental materials

[0035] 1.1 Experimental animals

[0036] Wistar rats, female, 7-8 weeks old, weighing 160-180g, 2 / cage, were reared in separate cages, the rats were free to drink water and eat, the room temperature was 25±1°C, and the animals were adaptively fed for 5 days before the experiment.

[0037] 1.2 Main reagents

[0038] LCA injection: The compound LCA was isolated and obtained according to the prior art. It was formulated into an injection with a concentration of 15 mg / ml in 30% propylene glycol solvent and stored in a 4°C refrigerator for later use.

[0039] MTX injection: specification 5mg / bottle, approval number H20080251, Ebewe Pharma Ges.m.b.H.Nfg.KG.

[0040] Bovine type II collagen was purchased from Chondrex, Inc.; glacial acetic acid was purchased from Beijing Chemical Reagent Company; complete Freund's adjuvant and incomplete Freund's adjuvant were...

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Abstract

The invention relates to an application of LCA (9, 9'-O-bi-(E)-feruloylated-meso-5, 5'-dimethoxy secoisolariciresinol) in preparation of drug for treating arthritis or cartilago articularis and bone destruction. By using a cell heat transfer technology, the compound LCA can be combined with MEK1 protein and cathepsinK protein in cells, animal tests verify that the LCA can improve the symptoms of a rat with rheumatoid arthritis and the research results show that LCA has a double target effects of simultaneously inhibiting immune inflammation and preventing and treating bone destruction and has a board application prospect in clinical treatment of diseases such as rheumatoid arthritis, osteoarthritis, osteoporosis and the like.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, to the natural product 9,9'-O-di-(E)-feruloyl-meso-5,5'-dimethoxysecoisolariciresinol (9,9'-O-di-(E) Application of -feruloyl-meso-5,5'-dimethoxycycloisolaricine resinol, code name LCA) in the preparation of medicines for treating arthritis or articular cartilage and bone destruction. Background technique [0002] Rheumatoid arthritis is a chronic systemic autoimmune disease characterized by joint synovitis. Synovitis is persistent and recurrent, which can lead to the destruction of cartilage and bone in the joint, joint dysfunction, and even disability. Rheumatoid arthritis has no specific therapy so far, and it still stays in the treatment of inflammation and sequelae. Taking comprehensive treatment, most patients can get a certain curative effect. The purpose of current treatment is: 1. control the inflammation of joints and other tissues, relieve symptoms; MEK1 (MAP...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61P19/02A61P19/08A61P29/00A61P19/10A61P37/02
CPCA61K31/216
Inventor 韩婷林兵秦路平张巧艳郑承剑贾敏蒋益萍徐帆陈泠
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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