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Application of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate in preparation of drugs for treating or preventing rheumatoid arthritis

A technology of methoxybenzyl and dimethoxy, applied in the field of proteasome-inhibiting compounds for the prevention and treatment or prevention of rheumatoid arthritis, to achieve the effect of preventing or treating rheumatoid arthritis

Inactive Publication Date: 2014-04-30
NANTONG REPAIR AIR CHEM BIOENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

2. Steroid hormones. Hormones are very good analgesic and anti-inflammatory drugs, but long-term use alone cannot improve the condition, but bring many side effects. Steroids can be used as a transitional second-line slow-acting drug before it takes effect, but the dosage should be limited. small, not too long
Despite this, there are no well-developed proteasome compound inhibitors available for the treatment of rheumatoid arthritis

Method used

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  • Application of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate in preparation of drugs for treating or preventing rheumatoid arthritis

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Immunoprotective effects of proteasome-inhibiting compounds in collagen-induced mouse arthritis animal model

[0022] To construct an animal model of collagen-induced arthritis in mice, and to study the therapeutic effect of proteasome-inhibiting compounds on collagen-induced arthritis (CIA) in mice. Mice were used as experimental animals, 90 SPF grade DBA / 1 mice (provided by Sino-British SIPPR Lab. Animal Ltd, animal production license number: SCXK (Shanghai )2008-0016), male, 7-8 weeks old, weighing 18-22 g, were randomly divided into 6 groups, namely the normal control group, the model control group, and 3 low, middle and high dose groups of the compound (0.4, 0.8, 1.6 mg / kg) and positive drug control group (methotrexate 2 mg / kg). In addition to the normal group, the mouse CIA model was established in each experimental group on day 0 by dissolving chicken cartilage type II collagen (cII) with 0.1 mol / l acetic acid into a 4 mg / ml solution and placing it in a refrige...

Embodiment 2

[0027] In vivo immunoprotective effect of proteasome inhibiting compounds on adjuvanted rat arthritis animal model

[0028] To construct an animal model of adjuvant arthritis in rats, and to study the therapeutic effect of proteasome-inhibiting compounds on Adjuvant arthritis (AA) rats. Rats were used as experimental animals, 90 SPF grade SD rats (provided by Sino-British SIPPR Lab. Animal Ltd, animal production license number: SCXK (Shanghai) 2008 -0016), male, weighing 140 g-160 g, were randomly divided into 6 groups, which were normal control group, model control group, three dose groups of low, medium and high doses of proteasome inhibitory compounds (0.2, 0.4, 0.8 mg / kg) and Positive drug control group (methotrexate 1 mg / kg). In addition to the normal group, on the 0th day, each experimental group established a rat AA model by injecting complete Freund's adjuvant containing inactivated Mycobacterium tuberculosis (H37RA, 10 mg / ml) into the left hindquarters of the rats. ...

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Abstract

The invention relates to the field of drugs, and particularly relates to a compound capable of inhibiting proteasomes and preventing and treating rheumatoid arthritis. The compound has the molecular structure of 3'-methoxy benzyl-4-hydroxy-3,5-dimethoxy-benzoate. The compound has the beneficial effects that the compound can be used for treating rheumatoid arthritis, and has potential new drug development value.

Description

Technical field: [0001] The invention relates to the field of medicine, in particular to proteasome inhibiting compounds for preventing and treating or preventing rheumatoid arthritis. Background technique: [0002] Rheumatoid arthritis (RA) is the most common clinical inflammatory joint disease and one of the main disabling factors. It is about 0.5%-1.0% in the world, and the incidence of RA is about 0.4% in my country. RA can occur at any age, and the incidence rate increases with age. The high-incidence age of women is 45-55 years old, and gender is closely related to the incidence of RA, with a male-to-female ratio of about 1:3. RA is a chronic systemic inflammatory disease of unknown etiology, with chronic, symmetrical, polysynovial arthritis and extra-articular lesions as the main clinical manifestations, and belongs to autoimmune inflammatory disease. Patients often have hand or wrist pain and swelling (especially the swelling on the back of the wrist) as the fi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/235A61P29/00A61P19/02
Inventor 姚炎华朱鹏葛亮刘晓磊奚年英
Owner NANTONG REPAIR AIR CHEM BIOENG
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