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Application of evodiamine in preparation of anti-inflammatory drugs and/or immunosuppressor drugs

An immunosuppressant, evodigoside technology, applied in the field of pharmaceuticals, can solve the problems of unclear active ingredients and complex composition of rheumatoid arthritis

Active Publication Date: 2022-04-15
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the total glycosides extract of pterygium is a mixture of various components, and its composition is complex, and the active components for treating rheumatoid arthritis are not clear

Method used

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  • Application of evodiamine in preparation of anti-inflammatory drugs and/or immunosuppressor drugs
  • Application of evodiamine in preparation of anti-inflammatory drugs and/or immunosuppressor drugs
  • Application of evodiamine in preparation of anti-inflammatory drugs and/or immunosuppressor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 Anti-inflammatory activity test of evodigoside

[0050] (1) Experimental method

[0051] 2×10 4 RAW 264.7 cells per well (mouse mononuclear macrophage leukemia cells) were attached to the wall overnight in a 96-well plate, and 10, 20, and 40 μM concentrations of rutadiel were added to act on the cells for 4 hours, and then LPS ( Lipopolysaccharide) solution, so that the final concentration was 1 μg / ml, and after 24 hours, TNF-α, IL-1β and IL-6 in the cell culture supernatant were detected with mouse TNF-α, IL-1β and IL-6 detection kits. 6 content.

[0052] (2) Experimental results

[0053] The results showed that evodiside at concentrations of 10, 20, and 40 μM could effectively inhibit LPS-induced RAW 264.7 cells to produce TNF-α, IL-1β and IL-6 three inflammatory factors ( figure 1 ).

[0054] The above experiments proved that evodiside can effectively reduce the inflammatory response of RAW264.7 cells induced by LPS.

Embodiment 2

[0055] Example 2 Effect of Evodigoside on the Inflammatory Response of HFLS-RA Cells

[0056] 1. Effect of evodigoside on NO content in HFLS-RA cells

[0057] (1) Experimental method

[0058] 2×10 4 After the HFLS-RA cells (rheumatoid arthritis fibroblast-like synoviocytes) per well were attached to the wall overnight in a 96-well plate, 10, 20, and 40 μM concentrations of evodielin solutions were added to act on the cells for 4 hours, and then LPS solution was added to make the final concentration 1 μg / ml, and the NO content in the cell culture supernatant was detected 24 hours later with a NO detection kit.

[0059] (2) Experimental results

[0060] The results showed that compared with the LPS-induced group, 10, 20, and 40 μM evodiside could effectively inhibit the increase of NO content induced by LPS ( figure 2 ).

[0061] 2. Effect of evodigoside on the content of IL-1β in HFLS-RA cells

[0062] (1) Experimental method

[0063] 2×10 4 After the HFLS-RA cells per...

Embodiment 3

[0097] Example 3 Effect of Evodigoside on Mitochondrial Function of HFLS-RA Cells

[0098] 1. Effect of evodigoside on the swelling degree of isolated mitochondria

[0099] (1) Experimental method

[0100] Take the brain tissue of Kunming mice, shred it in 10 times the volume of pre-cooled mitochondrial separation buffer, wash once with PBS, homogenize in ice bath, and immediately centrifuge the homogenate at 2000g / min for 3min at 4°C; take the supernatant again Centrifuge at 2000g / min for 3min, discard the supernatant, resuspend the pellet with pre-cooled mitochondrial isolation buffer, then centrifuge at 12000g / min for 8min, and resuspend the obtained brown precipitate with pre-cooled mitochondrial isolation buffer to obtain purified mitochondria. The resulting mitochondria were quantified for mitochondrial protein content using the BCA protein assay. The isolated mitochondria were diluted with 25°C swelling buffer to contain 100mg protein per ml solution. Add the corresp...

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Abstract

The invention discloses application of evodiamine in preparation of anti-inflammatory drugs and / or immunosuppressor drugs, and belongs to the field of pharmacy. It is found for the first time that the evodiamine can significantly inhibit inflammatory response of rheumatoid arthritis fibroblast-like synovial cells, promote cell mitochondrial dysfunction, promote cell apoptosis and inhibit cell migration. The evodiamine is derived from a natural plant pterocephalus hookeri heck, and is low in cytotoxicity and high in safety. The evodiamine has a wide clinical application prospect in preparation of immunosuppressor drugs and anti-inflammatory drugs for preventing and / or treating autoimmune diseases such as rheumatoid arthritis and the like.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to the use of a natural plant component evodigoside in the preparation of anti-inflammatory drugs and / or immunosuppressant drugs. Background technique [0002] Autoimmune diseases refer to diseases caused by the body's immune response to self-antigens, resulting in damage to its own tissues or organs. Autoimmune disease is a common clinical disease, including systemic lupus erythematosus, rheumatoid arthritis, idiopathic thrombocytopenic purpura, dermatophytosis, membranous glomerulonephritis, inflammatory bowel disease, autoimmune hemolytic anemia And more than 40 kinds of diseases. [0003] Rheumatoid arthritis is a chronic autoimmune disease, and its final outcome often leads to joint destruction. Studies have reported that T cells, macrophages and their respective cytokines play a key role in the course of rheumatoid arthritis. It has also been reported that in the long-term course of...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K36/185A61P29/00A61P37/06A61P19/02A61P7/00A61P17/00A61P31/10A61P13/12A61P1/00A61P7/06
CPCA61K31/7048A61K36/185A61P29/00A61P37/06A61P19/02A61P7/00A61P17/00A61P31/10A61P13/12A61P1/00A61P7/06Y02A50/30
Inventor 唐策张艺孟宪丽柏金容
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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