Application of entacapone to prevention or treatment of obesity and other metabolic syndrome

A technology of entacapone and its composition, which is applied in the field of medicine, can solve the problems that the upstream and downstream action elements and regulatory mechanisms of FTO protein have not been reported, and the mechanism of action of FTO protein is unclear.

Active Publication Date: 2014-06-11
NAT INST OF BIOLOGICAL SCI BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

11,12 However, the mechanism of action of FTO protein is still unclear, especially the upstream a

Method used

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  • Application of entacapone to prevention or treatment of obesity and other metabolic syndrome
  • Application of entacapone to prevention or treatment of obesity and other metabolic syndrome
  • Application of entacapone to prevention or treatment of obesity and other metabolic syndrome

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Experimental program
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Effect test

Embodiment 1

[0083] Structure-Based Virtual Screening . We screened 1323 FDA-approved drugs for the substrate-binding site of FTO protein, and according to some criteria based on physicochemical definitions, such as the number of hydrogen bonds, the number of embedded carbon atoms and hydrophobic interactions, delete Go to some unreasonable conformation. The remaining conformations were subjected to further conformational optimization and recalculation of relative binding free energies. According to binding conformation and energy, one of the top-ranked compounds is entacapone ( figure 1) .

[0084] Enzyme activity inhibition test . We determined the inhibitory activity of entacapone on FTO protein by demethylation assay. We used a 100μl reaction system containing 50mM HEPES buffer (pH=7.0), 100μM a-KG, 100μM (NH 4 ) 2 Fe(SO 4 ) 2 , 1mM L-ascorbic acid, 50μg / ml BSA, 0.5μM ssDNA with N 6 -mA(5'-ATTGTCA(m 6 A) CAGCAGA-3'), and 0.1 μM FTO protein. The reaction system was incub...

Embodiment 2

[0090] Embodiment 2 co-packaging or co-preparation embodiment

[0091] 1. Entacapone / orlistat are jointly made into tablets at 1000mg / 120mg or 2000mg / 120mg.

[0092] 2. Entacapone / sibutramine are jointly made into tablets at 1000mg / 10mg or 2000mg / 10mg.

[0093] 3. Entacapone / Greencaserin are jointly made into tablets at 1000mg / 10mg or 2000mg / 10mg.

[0094] 4. Entacapone / rimonabant is jointly made into tablets at 1000mg / 20mg or 2000mg / 20mg.

[0095] 5. Entacapone / Metformin are jointly made into tablets at 1000mg / 500mg or 2000mg / 500mg.

[0096] 6. Entacapone / Exenatide: 1000mg or 2000mg per tablet / 250mg / mL solution co-packed

[0097] 7. Entacapone / Exenatide: 1000mg or 2000mg per tablet / suspension ER 2mg (Bydureon), co-packaged

[0098] 8. Entacapone / pramlintide: 1000mg or 2000mg per tablet / 600mg / mL), co-packaged.

[0099] 9. Entacapone / phentermine is jointly made into tablets at 1000mg / 10mg or 2000mg / 10mg.

[0100] 10. Entacapone / atorvastatin are jointly made into tablets a...

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PUM

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Abstract

The invention discloses application of entacapone to prevention or treatment of obesity and other metabolic syndromes. Specifically, the invention discloses application of entacapone as shown in the formula I or a pharmaceutically acceptable salt thereof to preparation of medicaments for the prevention and / or treatment of metabolic diseases, cardiovascular and cerebrovascular diseases, as well as liver, kidney and thyroid diseases induced therefrom. The metabolic disease is selected from obesity, diabetes and hyperlipidemia; the cardiovascular and cerebrovascular disease is selected from hypertension, coronary heart disease, and atherosclerosis. The prevention and / or treatment of obesity refers to inhibition of body weight increase or promotion of weight loss. The blood lipid is selected from the group consisting of low density lipoprotein, low density lipoprotein-cholesterol, cholesterol and triglyceride. The renal disease is selected from diabetic nephropathy. (img file = 'DDA00002485677700011.TIF' wi = '1113' he = '654' /).

Description

technical field [0001] The present invention relates to the application of entacapone in preventing or treating obesity and other metabolic syndromes. Belonging to the field of medical technology Background technique [0002] Worldwide, obesity has become a huge threat to human health. Factors leading to obesity, a chronic disease, include environmental and genetic factors. Recently, people use genome-wide association studies (GWAS, genome-wide association studies) method to analyze the single nucleotide polymorphism (SNP) of obese patients, and found that a single gene FTO (fat mass and obesity) gene is associated with obesity Phenotypes were significantly correlated. 1-4 Moreover, the relationship between FTO gene and obesity has been further confirmed in transgenic animal models. Specifically, mice with complete knockout of the FTO gene and neuron-specific knockout mice had significantly lower body weight than wild-type mice, while mice with high expression of the FTO...

Claims

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Application Information

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IPC IPC(8): A61K31/277A61P3/00A61P9/00A61P1/16A61P13/12A61P3/04A61P3/10A61P3/06A61P9/12A61P9/10
CPCA61K31/277A61K45/06C12Q1/6883C12Q2600/156A61P1/16A61P13/12A61P3/00A61P3/04A61P3/06A61P9/00A61P9/10A61P9/12A61P3/10A61K2300/00
Inventor 黄牛智刚柴继杰彭士明侯楠楠
Owner NAT INST OF BIOLOGICAL SCI BEIJING
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