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Osteoarthritis-resistant drug containing tripeptide compounds

A peptide compound, osteoarthritis technology, applied in the field of anti-osteoarthritis drugs containing tripeptide compounds, can solve the problems of low biological activity, toxic and side effects, and achieve the effect of avoiding degradation and reducing the release amount

Pending Publication Date: 2017-11-17
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the problem that the existing osteoarthritis drugs have low biological activity and have toxic and side effects which limit clinical application, the present invention provides an anti-osteoarthritis drug whose active ingredient is a tripeptide derivative

Method used

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  • Osteoarthritis-resistant drug containing tripeptide compounds
  • Osteoarthritis-resistant drug containing tripeptide compounds
  • Osteoarthritis-resistant drug containing tripeptide compounds

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Experimental program
Comparison scheme
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Embodiment Construction

[0021] In order to fully understand the technical content of the present invention, the technical solutions of the present invention will be further introduced and illustrated below in conjunction with specific embodiments.

[0022] According to the method recorded in the existing literature, the tripeptide compound of the present invention is synthesized by the method of the synthetic route shown below:

[0023]

[0024]

[0025] In the synthesis route of the above-mentioned tripeptide compound, the structural formulas of the Pybop reagent, LiHMDS, TEA, and TFA are shown below.

[0026]

[0027] The pharmacodynamic related experiments of the tripeptide compound of the present invention as an anti-osteoarthritis drug are as follows: Experiments 1-5.

[0028] The structure of the tripeptide compound (KDPT) described in Tests 1-5 is as follows:

[0029]

[0030] Experiment 1: Cell culture

[0031] The cartilage of postmenopausal female patients (age: over 65 years ...

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Abstract

The invention relates to the technical field of osteoarthritis-resistant drugs, in particular to an osteoarthritis-resistant drug containing tripeptide compounds. These tripeptide compounds contained in the osteoarthritis-resistant drug can significantly reduce the release amount of NO and PGE2 in an osteoarthritis cell model, reduce the expression quantity of COX-2, iNOS, MMP-1 and MMP-13 in cartilage cells and avoid degradation of cartilage matrix protein and type II collagen while resisting the osteoarthritis, and therefore, the osteoarthritis-resistant drug containing tripeptide derivatives has a treatment effect on the osteoarthritis.

Description

technical field [0001] The invention relates to the technical field of anti-osteoarthritis drugs, in particular to an anti-osteoarthritis drug containing a tripeptide compound. Background technique [0002] Osteoarthritis is a slowly progressive degenerative disease of articular cartilage, which is formed by the degeneration of articular cartilage, joint edge and subchondral bone reactive hyperplasia. Therefore, it is called "the number one disease with the highest disability rate" by the World Health Organization. [0003] The incidence of osteoarthritis increases significantly with age. In the Netherlands, the incidence rate of osteoarthritis is 10-20% among the 40-year-old population, and as high as 55% among the 60-70-year-old population, and the incidence rate of women (75%) is higher than that of men. The National Health Interview Survey (NHIS) estimates that the number of people with arthritis in the United States will increase to 670 million by 20301. The aging po...

Claims

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Application Information

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IPC IPC(8): A61K38/06A61P19/02A61P19/08
CPCA61K38/06
Inventor 徐峻李婵娟顾琼
Owner SUN YAT SEN UNIV