CN-122005580-A - Application of adefovir in preparing medicine for preventing and treating atherosclerosis

Abstract

The invention relates to application of adefovir in preparing medicines for preventing and treating atherosclerosis. The application of the Ruidexivir in preparing the medicine for preventing and treating atherosclerosis comprises one or more of (1) inhibiting the formation of atherosclerosis plaques, (2) inhibiting vascular endothelial activation by the Ruidexivir, (3) reducing the mRNA and protein expression levels of ox-LDL-mediated VCAM-1 and ICAM-1, (4) reducing the immunofluorescence expression of ox-LDL-mediated endothelial cells VCAM-1 and ICAM-1 and (5) reducing the adhesion of ox-LDL-mediated THP1 cells on the surface of endothelial cells by the Ruidexivir. The invention provides a new application of adefovir, namely an application of adefovir or pharmaceutically acceptable salts, esters and hydrates thereof in preparing medicines for preventing and treating atherosclerosis diseases. Provides an effective novel potential alternative medicine for preventing and treating atherosclerosis, expands the indication of the Ruidexivir and improves the application potential and market prospect of the Ruidexivir.

Inventors

• ZHANG CHENGHU
• ZHANG HANNING
• WU ZONGYIN
• REN CHANGJIE
• HUO QIANQIAN
• LI LI
• LI RURU

Assignees

• 济宁市第一人民医院(济宁市医学科学研究院)

Dates

Publication Date

20260512

Application Date

20241108

Claims (6)

1. 1. Application of adefovir in preparing medicine for preventing and treating atherosclerosis is provided.
2. 2. The use according to claim 1, wherein said adefovir comprises one or more of the following actions: (1) The adefovir has an inhibitory effect on the formation of atherosclerotic plaques; (2) The adefovir has an inhibitory effect on vascular endothelial activation; (3) The adefovir has a reduced effect on ox-LDL mediated mRNA and protein expression levels of VCAM-1 and ICAM-1; (4) The adefovir has a reduced effect on ox-LDL mediated immunofluorescence expression of endothelial cells VCAM-1 and ICAM-1; (5) The adefovir has a reduced effect on ox-LDL mediated adhesion of THP1 cells to the surface of endothelial cells.
3. 3. The medicine for preventing and treating atherosclerosis is characterized by comprising adefovir or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein the carrier comprises one or more of diluents, buffers, suspensions, emulsions, granules, encapsulating agents, excipients, fillers, adhesives, spraying agents, transdermal absorbents, wetting agents, disintegrating agents, absorption promoters, surfactants, colorants, flavoring agents or adsorption carriers.
4. 4. An agent for preventing and treating atherosclerosis according to claim 3, wherein the effective dose of said adefovir in the agent is 900mg every two days when the adult weight standard is set to 60 kg.
5. 5. A medicament for preventing and treating atherosclerosis according to claim 3, which is in the form of oral or injectable administration, including one of powder, tablet, granule, capsule, oral liquid, emulsion or suspension.
6. 6. A medicament for preventing and treating atherosclerosis according to claim 3, characterized in that the adefovir dipivoxil medicament further comprises other excipients.

Description

Application of adefovir in preparing medicine for preventing and treating atherosclerosis Technical Field The invention relates to the technical field of medicines, in particular to application of adefovir in preparing medicines for preventing and treating atherosclerosis. Background Atherosclerosis is a common cardiovascular disease characterized primarily by plaque formation in the intima of the artery, which is composed of lipids, fibrous tissue, necrotic material, cells, etc., and may lead to stiffening of the vessel wall and lumen narrowing. Atherosclerosis is the main cause of cardiovascular diseases and cerebral apoplexy, and its pathological mechanism is vascular endothelial dysfunction, and thus mediates complex pathological processes such as inflammatory reaction. The treatment of atherosclerosis is a comprehensive process, and aims to slow down the progress of diseases, relieve symptoms, prevent complications and improve the life quality of patients; The existing drug treatment comprises lipid-lowering drugs, antiplatelet drugs, antihypertensive drugs, hypoglycemic drugs and the like. Lipid lowering drugs, statins are commonly used lipid lowering drugs which can lower the level of Low Density Lipoprotein (LDL), reduce plaque formation and stabilize existing plaque, antiplatelet drugs, such as aspirin, can prevent platelet aggregation and reduce the risk of thrombosis, antihypertensive drugs, which are required to be taken by patients suffering from hypertension to control blood pressure and reduce damage to blood vessel walls, and hypoglycemic drugs, which are required to control blood glucose level to reduce damage to blood vessel walls for diabetics. Rede-Sivir (Remdesivir,L-Alanine,N-[(S)-hydroxyphenoxyphosphinyl]-,2-ethylbutyl ester,6-ester with2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-D-altrononitri le) is a prodrug of an adenosine nucleotide analogue, and the action mechanism of the prodrug is to inhibit RNA-dependent RNA polymerase, and is mainly used for treating Ebola virus and is known for its broad-spectrum antiviral activity. Early small amounts of data indicate that during the COVID-19 pandemic period, adefovir shows efficacy in inhibiting SARS-CoV-2 replication, shortening patient hospitalization period, but later large amounts of clinical trial data indicate that its anti-neocrown efficacy is not quite significant. However, it was found that adefovir has potential therapeutic effects on non-viral inflammation-related diseases. It is unclear whether adefovir is effective in treating atherosclerosis. Therefore, the research focuses on the new application of Redexi-vir in regulating and controlling the vascular endothelial cell function and treating atherosclerosis, provides a new therapeutic scheme for treating atherosclerosis cardiovascular diseases. Therefore, the application of the adefovir in preparing the medicines for preventing and treating atherosclerosis is designed, and the problems are solved. Disclosure of Invention The invention aims to overcome the defects and provides the application of the adefovir in preparing the medicines for preventing and treating atherosclerosis. Further, the adefovir includes one or more of the following effects: (1) The adefovir has an inhibitory effect on the formation of atherosclerotic plaques; (2) The adefovir has an inhibitory effect on vascular endothelial activation; (3) The adefovir has a reduced effect on ox-LDL mediated mRNA and protein expression levels of VCAM-1 and ICAM-1; (4) The adefovir has a reduced effect on ox-LDL mediated immunofluorescence expression of endothelial cells VCAM-1 and ICAM-1; (5) The adefovir has a reduced effect on ox-LDL mediated adhesion of THP1 cells to the surface of endothelial cells. Further, the medicament for preventing and treating atherosclerosis comprises adefovir or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein the carrier comprises one or more of diluents, buffers, suspensions, emulsions, granules, encapsulating agents, excipients, fillers, binders, sprays, transdermal absorbents, wetting agents, disintegrants, absorption promoters, surfactants, colorants, flavoring agents or adsorption carriers. Further, the effective dose of the adefovir in the medicine is that the adult weight standard is set to be 60kg, and the effective dose of the adefovir is 900mg every two days. Further, the composition is in an oral or injection administration form, wherein the oral or injection administration form comprises one of powder, tablets, granules, capsules, oral liquid, emulsion or suspension. Furthermore, the adefovir dipivoxil medicament also comprises other auxiliary materials. The beneficial effects of the invention are as follows: the application of the adefovir in preparing the medicine for preventing and treating atherosclerosis comprises the following actions: (1) The adefovir has an inhibitory effect on the formation of atherosclerotic pl