Compositions containing monoacetyldiacylglycerol compound as an active ingredient for preventing or treating rheumatoid arthritis

a technology of monoacetyldiacylglycerol and monoacetyldiacylglycerol, which is applied in the direction of biocide, drug composition, immunodeficiency disorder, etc., can solve the problems of limited treatment, ineffective treatment methods, and inability to prevent rheumatoid arthritis, so as to prevent, treat or improve rheumatoid arthritis, inhibit the effect of phosphorylation

Inactive Publication Date: 2016-07-14
ENZYCHEM LIFESCI CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention is about a compound called monoacetyldiacylglycerol, which can reduce the phosphorylation of a protein called STAT-3, which is associated with rheumatoid arthritis. This compound is effective without causing any harmful side effects, making it a promising treatment for the condition. It can be used to prevent, treat, or improve rheumatoid arthritis.

Problems solved by technology

To date, known methods for treating or preventing rheumatoid arthritis are not effective and better treatments are needed.
However, because the use of the hormone medications is not a fundamental treatment and can cause several side effects, the treatment is limited.
Arthritis, especially rheumatoid arthritis, causes severe pain so that the patient must take anti-inflammatory agents.
However, the harmful effect of aspirine on stomach makes it difficult to take a sufficient amount of aspirine necessary for the treatment of arthritis continuously.
Drugs currently used for the treatment of arthritis have several limitations including side effects preventing long-term use of the drugs, the absence of anti-inflammatory effect and the lack of efficacy for treating the arthritis that has already occurred.
Especially, because it is necessary to take medications for a long period of time for the treatment of rheumatoid arthritis, it is very important and urgent problem to develop a novel pharmaceutic agent with low side effect.
However, the effect of the monoacetyldiacylglycerol compounds including EC-18 on rheumatoid arthritis is not known or disclosed in the prior art.

Method used

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  • Compositions containing monoacetyldiacylglycerol compound as an active ingredient for preventing or treating rheumatoid arthritis
  • Compositions containing monoacetyldiacylglycerol compound as an active ingredient for preventing or treating rheumatoid arthritis
  • Compositions containing monoacetyldiacylglycerol compound as an active ingredient for preventing or treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

examples

[0043]The following examples are provided for better understanding of this invention. However, the present invention is not limited by the examples.

experimental example 1

Inhibitory Effect of EC-18 on STAT-3 Phosphorylation in U937 Cells

[0045]Cells treated in EC-18 and IL-6 cytokines were lysed with cold SDS lysis buffer [(50 mM HEPES, 150 mM NaCl, 0.2 mM EDTA, 0.5% NP-40, 0.1% SDS, 1 mM Na3VO4, 10 mM NaF, and complete Protein Inhibitor Cocktail (Roche)] for 30 minutes on ice. After cell lysis, the aqueous solution was separated from the insoluble precipitate by centrifuging the cell lysates for 30 minutes at 13,000 rpm in a high-speed centrifuge. After protein quantification, the aqueous solution was separated in 10 to 12% SDS-PAGE by electrophoresis. Proteins separated in the gel were transferred into PVDF membrane (Millipore, Billerica, Mass., USA) at 100V for 2 hours.

[0046]To measure the amount of phosphorylated STAT-3, the membrane was incubated with poly rabbit-anti-(STAT1, STAT3) or poly rabbit-anti-phospho (STAT1, STAT3) antibody (Cell Signaling Technology, USA (1:1000) as a primary antibody for 60 minutes at room temperature. The membrane wa...

experimental example 2

Inhibitory Effect of EC-18 on STAT-3 Phosphorylation in NK-92 Cells

[0048]Cells treated in EC-18 and PMA (Phobol 12-myristate 13-acetate) were lysed with cold SDS lysis buffer [(50 mM HEPES, 150 mM NaCl, 0.2 mM EDTA, 0.5% NP-40, 0.1% SDS, 1 mM Na3VO4, 10 mM NaF, and complete Protein Inhibitor Cocktail (Roche)] for 30 minutes on ice. After cell lysis, the aqueous solution was separated from the insoluble precipitate by centrifuging the cell lysates for 30 minutes at 13,000 rpm in a high-speed centrifuge. After protein quantification, the aqueous solution was separated in 10 to 12% SDS-PAGE by electrophoresis. Proteins separated in the gel were transferred into PVDF membrane (Millipore, Billerica, Mass., USA) at 100V for 2 hours.

[0049]To measure the amount of phosphorylated STAT-3 and STAT-1, the membrane was incubated with poly rabbit-anti-STAT3, poly rabbit-anti-STAT1, or poly rabbit-anti-phospho-STAT3 antibody (Cell Signaling Technology, USA (1:1000) as a primary antibody for 60 min...

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Abstract

The invention relates to pharmaceutical compositions, as well as health functional food compositions and quasi-drug compositions, for preventing, treating, or improving rheumatoid arthritis, comprising a monoacetyldiacylglycerol compound as an active ingredient. The monoacetyldiacylglycerol of the invention is effective in inhibiting the phosphorylation of STAT-3 known to be a therapeutic target for rheumatoid arthritis. As the monoacetyldiacylglycerol is an effective therapeutic agent without toxicity, the monoacetyldiacylglycerol can overcome the side effects of the medicines currently used in the treatment of rheumatoid arthritis. Thus, the monoacetyldiacylglycerol can be used for preventing, treating or improving rheumatoid arthritis.

Description

FIELD OF THE INVENTION[0001]The present invention relates to pharmaceutical compositions, as well as health functional food compositions and quasi-drug compositions, for preventing, treating, or improving rheumatoid arthritis, comprising a monoacetyldiacylglycerol compound as an active ingredient.BACKGROUND OF THE INVENTION[0002]Rheumatoid arthritis is a chronic autoimmune disease that causes inflammation by attacking joints or other parts of the body. Rheumatoid arthritis causes a painful swelling of fingers, hands, feet, wrists, ankles, knees and sometimes can affect other organs of the body such as muscle, skin, lungs and eyes. The underlying cause of rheumatoid arthritis remains unclear and has been investigated continuously. To date, known methods for treating or preventing rheumatoid arthritis are not effective and better treatments are needed. Many hormone medications such as steroids have been widely used to treat arthritis. However, because the use of the hormone medication...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/231A61K9/48A61K9/00
CPCA61K31/231A61K9/4825A61K9/0053A61K31/23A61P19/00A61P19/02A61P29/00A61P37/04A61P43/00A61K31/22A61K2121/00
InventorKIM, JAE WHAOH, SEI RYANGAHN, KYUNG SEOPKANG, HO BUMPARK, BEOM SULEE, TAE SUKKANG, JONG KOOJUNG, YOUNG SIKHAN, YONG-HAESOHN, KI-YOUNG
OwnerENZYCHEM LIFESCI CORP