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Application of carbonic anhydrase inhibitor to preparation of anti-atherosclerosis drugs

A technology of atherosclerosis and drugs, applied in the field of carbonic anhydrase inhibitors, can solve problems such as the unclear therapeutic effect of carbonic anhydrase inhibitors, and achieve the effect of reducing the content and lowering the comprehensive index of blood lipids

Active Publication Date: 2019-04-05
青岛汇嘉医学科技有限公司
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Problems solved by technology

[0004] Contrary to some laboratories suggesting that CA may play an important role in atherosclerosis, Oksala et al. found that CA2 and CA12 of the CA family are highly expressed in human atherosclerotic plaques and may be associated with monocyte-derived monocytes in advanced atherosclerosis. It is related to osteoclast-like cells, but the relationship between the expression of CA1 and the mineralization of vascular smooth muscle cells and atherosclerosis has not been reported. It is not clear whether carbonic anhydrase inhibitors have a therapeutic effect on aortic atherosclerosis

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  • Application of carbonic anhydrase inhibitor to preparation of anti-atherosclerosis drugs
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  • Application of carbonic anhydrase inhibitor to preparation of anti-atherosclerosis drugs

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Embodiment 1

[0047] 1. Acquisition of Human Atherosclerotic Tissue

[0048] The tissue samples used in this application study were obtained from cardiac surgery patients in Qianfoshan Hospital Affiliated to Shandong University (Jinan, China). Among them, the specimens of the control group were taken from heart transplant donor volunteers (n=7), see Table 1A for details. Atherosclerotic tissue specimens were obtained from patients with aortic aneurysm and aortic dissection (n=7) with atherosclerotic conditions. Most of the patients had hypertension, and imaging tests showed aortic calcification, as shown in Table 1B. The samples were immediately stored in a -80°C refrigerator after being collected from relevant tissues for subsequent experiments. All tissue samples were collected with informed consent signed by the patients. All medical research involving human subjects (including human specimens and human data) follows the "Declaration of Helsinki", and animal experiments strictly abide...

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Abstract

The invention belongs to the field of anti-arteriosclerosis drugs, and particularly relates to application of a carbonic anhydrase inhibitor to preparation of the anti-arteriosclerosis drugs. The study finds for the first time that carbonic anhydrase 1 (CA1) is highly expressed in arteriosclerosis calcified tissue, and CA1 is related to vascular smooth muscle calcification and affects cell proliferation and apoptosis. Methazolamide, the inhibitor of CA1, can significantly reduce the progression of atherosclerosis and inhibit atherosclerotic inflammatory factors. The results suggest that calcification plays an important role in atherosclerosis, and CA1-dominated calcification promotes the course of the atherosclerosis. Methazolamide has a potential therapeutic effect on the atherosclerosisby inhibiting expression of CA1. The findings not only further explain the close relationship between the atherosclerosis and the calcification, but also explore the calcification mechanism of the atherosclerosis, and further prove that inhibition of the calcification is a key point in the treatment of the atherosclerosis. The application of the carbonic anhydrase inhibitor to the preparation of the anti-arteriosclerosis drugs provides new ideas for the treatment of the atherosclerosis.

Description

technical field [0001] The invention relates to the field of anti-atherosclerosis drugs, in particular to the preventive and therapeutic effects of carbonic anhydrase inhibitors, methazolamide and acetazolamide on vascular smooth cell calcification and atherosclerosis. Background technique [0002] Atherosclerosis (AS) is a common vascular system disease characterized by chronic inflammatory response, and is an important risk factor for cardiovascular disease, mainly involving the intima of large and medium-sized vessels. The damage of vascular endothelial cells is its initial link, followed by massive blood lipid deposition, monocyte aggregation and foam cell formation, vascular endothelial cell dysfunction and smooth muscle cell proliferation, and finally leads to atherosclerotic lesions. Vascular calcification is a common pathological manifestation in atherosclerosis, hypertension, diabetes, vascular injury, chronic kidney disease and aging, and is an adaptive process of ...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/433A61P9/10A61P29/00A61P3/06G01N33/15A23L33/10
CPCA61P3/06A61P9/10A61P29/00A23L33/10G01N33/15A61K31/433A23V2002/00A61K2300/00A23V2200/326A23V2200/3262
Inventor 常晓天
Owner 青岛汇嘉医学科技有限公司
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