Application of 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives in anti-fibrosis drugs

A technology of andrographolide and myocardial fibrosis, which is applied in the field of medicine, achieves good application and development prospects, improves the effect of organ fibrosis, and expands the effect of selection
CN109730990BActive Publication Date: 2021-07-02ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2021-07-02

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Abstract

The invention belongs to the technical field of medicine, and discloses the application of 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives in the preparation of drugs for preventing and treating human organ or tissue fibrosis. Experiments have proved that these compounds significantly inhibit TGF-β1-induced mesenchymal transition of human alveolar type II epithelial cells A549; significantly inhibit TGF-β1-induced mesenchymal transition of human renal cortical proximal tubule epithelial cells HK-2; inhibit Angiotensin Ⅱ (Ang Ⅱ)-induced proliferation of human primary cardiac fibrosis cells HCFB. Significantly reduce the degree of bleomycin-induced pulmonary fibrosis in mice, significantly reduce the degree of renal fibrosis in rats induced by unilateral ureteral ligation and the degree of myocardial fibrosis in Kunming mice induced by isoproterenol ISO. Using this type of compound as an active ingredient to prepare anti-fibrosis drugs such as kidney, lung, heart, etc., has high efficiency and low toxicity, and provides a new drug approach for the treatment and prevention of diseases related to fibrosis, thereby expanding the choice of clinical medication range, has a good prospect for application development.
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Description

technical field

[0001] The invention relates to the application of andrographolide derivatives as anti-fibrotic drugs for human organs or tissues, in particular to 14-deoxy-11,12-dehydroandrographolide C15 substituted derivatives, belonging to the technical field of medicine. Background technique

[0002] Tissue fibrosis is a chronic disease that occurs mostly in the liver, lung, heart, kidney and other parts. Tissue fibrosis and resulting organ failure are responsible for 1 / 3 of people worldwide. When tissue is injured, a series of cellular reactions occur at the injury site, resulting in excessive deposition of extracellular matrix and tissue fibrosis. It can eventually lead to organ dysfunction and even death. Cardiovascular fibrosis plays an important role in cardiovascular tissue remodeling caused by hypertension and heart failure, and is also the main cause of atherosclerosis. Cardiac fibrosis is characterized by accumulation of extracellular matrix proteins in the ...

Claims

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