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Composition for prevention or treatment of hyperlipidemia and related diseases containing rebamipide as an active ingredient

A technology for rebamipide and hyperlipidemia, applied in the field of rebamipide, can solve side effects and other problems, and achieve the effect of improving fatty liver, stabilizing effect, and inhibiting activity

Active Publication Date: 2018-04-13
THE CATHOLIC UNIV OF KOREA IND ACADEMIC COOP FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among these, lovastatin, simvastatin, pravastatin, etc. are the most well-known cholesterol-lowering agents that inhibit HMG-CoA reductase in the early stage of cholesterol biosynthesis, but also inhibit the synthesis of steroid hormones and dolichols , thus causing serious side effects (Havel, R.L. et al., Ann. Internal Med., 107:609-615, 1987; Illingworth, D.R. and Bacon, S. Am. J. Cardiolopy 60: 33-42, 1987)

Method used

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  • Composition for prevention or treatment of hyperlipidemia and related diseases containing rebamipide as an active ingredient
  • Composition for prevention or treatment of hyperlipidemia and related diseases containing rebamipide as an active ingredient
  • Composition for prevention or treatment of hyperlipidemia and related diseases containing rebamipide as an active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Inflammatory cytokines based on rebamipide treatment of macrophages (inflammatory cytokines) generation inhibitory effect

[0097] In order to ascertain the effect of rebamipide on macrophages, the inventors of the present application pre-treated mouse (Mouse) macrophages with rebamipide, and utilized LPS (lipopolysaccharide; lipopolysaccharide) to stimulate, Thus, the inflammatory cytokines TNF-a (tumor necrosis factor-α; tumor necrosis factor-alpha), IL-6 (interleukin-6; interleukin-6) and IL-1β (interleukin-1β; The degree of production of interleukin-1β) was assessed by ELISA (enzyme linked immunosorbent assay) analysis.

[0098] Cell culture

[0099] RAW 264.7 cells, which are mouse macrophage cell lines, were distributed from the Korean Cell Line Bank (KCLB), and for cell culture, a culture medium containing 10% FBS and 1% penicillin-streptomycin (penicillin-streptomycin) was used. DMEM (Dulbeccos Modified Eagle Medium) medium. At 37°C, 5% CO 2 cells were...

Embodiment 2

[0106] Toxicity determination of rebamipide to cells

[0107] In order to examine the cytotoxicity of rebamipide against RAW 264.7, which is a mouse macrophage, an MTT assay (MTT assay) was performed.

[0108] This method measures the conversion of MTT (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide; thiazolium blue) to formazan (Formazan) in a 96-well Packed in the plate 1×10 4 The cells / well (cells / well) of RAW 264.7 cells were treated with rebamipide according to the concentration (20, 100, 500, 1000, 5000 μM) for 18 hours. Add 100 μl of MTT solution to each well (well), so that at 37 ° C, 5% CO 2 The reaction was carried out in an incubator for 4 hours, and then the change in absorbance was measured at 570 nm using a microplate reader (VERSAmax, Molecular Devices, USA).

[0109] As a result, such as figure 2 As shown, the cytotoxicity is weak at concentrations of 20 μM, 100 μM and above, which are effective concentrations, and thus it can be seen that th...

Embodiment 3

[0111] Inhibitory effect of rebamipide-based treatment on vascular etiological cells

[0112] In this experiment, it was examined whether the generation of vascular etiogenic cells could be really inhibited when rebamipide treatment was performed in the vascular etiogenic cells. The "vascular etiological cell" refers to a foam cell (Foam cell) that forms a precursor cell of an arteriosclerotic plaque that causes arteriosclerosis, and is considered to be a cell that causes arteriosclerosis. In the invention, it is arbitrarily named as vascular etiological cell.

[0113] Inhibitory effect of rebamipide-based treatment on vascular etiological cells

[0114] In order to carry out this experiment, THP1 cells, a human macrophage cell line, were treated with PMA (phorbol 12'-myristate 13'-acetate; 12'-myristate-13'-acetate phorbol) at a concentration of 160nM to activate the cells , and then PAF (platelet-activating factor; platelet-activating factor) was treated with 10ug / ml,...

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Abstract

The present invention relates to a pharmaceutical use of rebamipide used in the prevention or treatment of hyperlipidemia and diseases related thereto, in particular to hyperlipidemia containing rebamipide as an active ingredient and its combination with Compositions for the prevention or treatment of related diseases. The rebamipide compound according to the present invention inhibits the production of TNF-a, IL-6 and IL-1b as hyperlipidemia-induced inflammatory cytokines secreted in macrophages; and inhibits the formation of atherosclerotic plaque ( Artherosclerotic plaque) precursor cell foam cell (Foam cell) generation; reduce blood total-cholesterol, LDL-cholesterol and neutral fat value to improve blood lipids; improve fatty liver; inhibit B cell activity; make accelerated arteries The expression of Th17, which is responsible for the formation of sclerotic plaques, is reduced, while the expression of Treg cells, which can control the inflammatory response, is increased. Accordingly, the rebamipide compound can be advantageously used as a pharmaceutical composition capable of preventing or treating hyperlipidemia and associated arteriosclerosis, heart failure, and hypertensive heart disease through various mechanisms as described above . In addition, there is no toxicity and side effects as a drug, so it can be used safely even if taken for a long time, and it has a stable effect in the body.

Description

technical field [0001] The present invention relates to the pharmaceutical use of Rebamipide used in the prevention or treatment of hyperlipidemia and diseases related thereto, and in particular to the high content of Rebamipide contained as an active ingredient. Composition for prevention or treatment of lipemia and related diseases. Background technique [0002] Modern people's excessive intake of saturated fat and cholesterol due to the pursuit of Western European diet and lifestyle changes and the requirements of the era of convenience is considered to cause cardiovascular diseases such as obesity, hyperlipidemia, arteriosclerosis, and myocardial infarction. Systemic diseases, and lipid peroxides cause degenerative processes in organisms and promote cancer and aging, and change or destroy biofilms. Cholesterol in the blood has been proven to be a risk factor for ischemic cerebrovascular disease and coronary artery disease, and has been proven to be the cause of aging su...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4704A61P3/06A61P3/00
CPCA61K31/4704A61P3/00A61P3/06A61P9/00A61P9/04A61P9/06A61P9/10A61P9/12A61P43/00
Inventor 曹美罗闵俊基田周燕边财耿任艺彬金恩敬杨恩智郑静禧
Owner THE CATHOLIC UNIV OF KOREA IND ACADEMIC COOP FOUND
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