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Neutrophilic granulocyte elastase inhibitor

A technology for elastase and neutrophils, which is applied in the field of medicine and achieves effects from a wide range of sources

Active Publication Date: 2012-06-20
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Neutrophilic granulocyte elastase inhibitor
  • Neutrophilic granulocyte elastase inhibitor
  • Neutrophilic granulocyte elastase inhibitor

Examples

Experimental program
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Effect test

Embodiment

[0020] 1.1 Experimental reagents:

[0021] HNE (produced by Innovative Research, USA);

[0022] N-MethoxySuccinyl-Ala-Ala-Pro-Val p-nitroanilide (produced by American sigma-aldrich);

[0023] Trypsin inhibitor (produced by American sigma-aldrich);

[0024] DMSO (produced by American sigma-aldrich);

[0025] 10mM Tris-HCl buffer (pH=7.5);

[0026] Glycyrrhetinic acid, glycyrrhizic acid, betulinic acid, oleanolic acid, ursolic acid and lupeol (purities all greater than 98%, and all provided by Shanghai Standardization Research Center of Traditional Chinese Medicine).

[0027] 1.2 Experimental equipment:

[0028] Synergy HT microplate reader, produced by American Bio-Tek;

[0029] DK-8D type electric heating constant temperature water tank, produced by Shanghai Yiheng Technology Co., Ltd.;

[0030] PB-10pH meter, produced by Germany Sartorius company.

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Abstract

The invention discloses a neutrophilic granulocyte elastase inhibitor of which the active ingredient is a compound with a pentacyclic triterpene structure. The inhibitor can be used for preparing a medicament or health-care food for treating or preventing diseases with neutrophilic granulocyte elastase as an action way. The diseases with the neutrophilic granulocyte elastase as an action way include acute lung injury, acute respiratory distress syndrome, systemic inflammatory response syndrome and cystic fibrosis diseases. As the active ingredient of the neutrophilic granulocyte elastase inhibitor disclosed by the invention, the compound with the pentacyclic triterpene structure can be extracted and separated from a natural product or can be prepared from a natural product through chemical synthesis, and has the advantages of being wide in sources, safe and effective.

Description

technical field [0001] The invention relates to a neutrophil elastase inhibitor, which belongs to the technical field of medicine. Background technique [0002] Neutrophil elastase (HNE) is a kind of neutral protease mainly released by neutrophils, which belongs to the superfamily of serine proteases, and is mainly stored in the azurophilic granules of neutrophils, or expressed in the cells firstly activated by cytokines. Activated cell surface (Clin Sci (Lond). 1983. 64: 119-126; Am J PhysioLung Cell Mol Physiol. 1997, 272: 385-393). The HNE gene ELA2 is located within a 50-bp fragment at the end of the short arm of chromosome 19, and the transcription of this gene is restricted only to the promyelocyte stage and then strictly controlled to the azurophilic granules of neutrophils It is regulated by various endogenous protease inhibitors (Am J Respir Crit Care Med.2001.164:896~904; Cytogenet Cell Gennet.1998.83:104~108). [0003] Under physiological conditions, when tissue...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/704A61P11/00A61P29/00A61P43/00A23L1/30
Inventor 李医明冯丽黄诚张刘强吴迎春郭夫江
Owner SHANGHAI UNIV OF T C M
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