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Coumarether compound and use of its composition

A technology of coumarin and compounds, applied in the field of coumarin compounds, can solve the problems of untreated autoimmune liver disease and viral hepatitis, coordination dysfunction, increased antibody production, etc.

Inactive Publication Date: 2008-07-23
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

During the pathogenesis of chronic viral hepatitis, the virus continues to replicate in the liver cells, causing the liver cells to be continuously immune damaged, and due to the abnormal metabolism of the liver cells, the quality and quantity of the immunoregulatory factors formed in the liver undergo changes, resulting in Immunoregulatory dysfunction, coordination dysfunction between T-B lymphocytes and T cell subgroups, increased production of autoantibodies, through antibody-dependent cytotoxicity or antibody-mediated complement-dependent cytolysis, resulting in autoimmunity Liver damage; or more serious and persistent damage to the liver or other tissues and organs due to the formation of a large number of antigen-antibody complexes
[0021] In summary, the liver injury caused by autoimmune liver disease and viral hepatitis is closely related to the activation of T lymphocytes. However, so far, there is no effective method for the treatment of autoimmune liver disease and viral hepatitis.

Method used

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  • Coumarether compound and use of its composition
  • Coumarether compound and use of its composition
  • Coumarether compound and use of its composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123]The compound wedelolide extracted from Eclipta alba

[0124] (1) soaking and filtering

[0125] Eclipta whole grass 300kg, fully immersed in 0.75 tons of ethanol (concentration 95%)→soak overnight (10 hours)→coarse filtration, thereby removing the whole grass residue (retention)→net filtration (suction filtration) or high-speed centrifugation (10000rpm, 10 minutes), thereby removing dust and fine residue → green clarified filtrate.

[0126] (2) Ethanol recovery

[0127] Recover ethanol by distillation, the temperature does not exceed 60°C → distill for 2 hours each time, remove the extract in the reaction kettle to the collection bucket (the extract is dark dark green, slightly viscous) → repeat the above steps until all ethanol is recovered .

[0128] (3) Second soaking and back distillation

[0129] Recover 0.75 tons of ethanol, re-soak the whole herb residue → soak overnight, the requirements for coarse filtration, net filtration and distillation recovery are the ...

Embodiment 2

[0142] experimental method:

[0143] 1. The mice (male SPF-grade KM mice, purchased from Shanghai Slack Experimental Animal Co., Ltd.) were sacrificed by devertebrate, and their spleens were removed under aseptic conditions. Grind the spleen with a ground glass piece, pass through the membrane, centrifuge at 300g for 5 minutes, and discard the supernatant. Add 1ml of erythrocyte lysate to the precipitate, mix well, let stand for 1 minute, add PBS solution, and centrifuge. After washing the cells 1-2 times, adjust the cell concentration to 4×10 with RPMI-1640 medium containing 10% calf serum 6 / ml;

[0144] 2. Inoculate the cell suspension into a 96-well cell culture plate, 100 μl per well, and place in a cell culture incubator (37°C, 5% CO 2 ) after culturing for 24 hours, AP-150 μl (final concentrations were 5 μM, 10 μM, 25 μM, 50 μM, 100 μM) and 50 μl of ConA (final concentration was 5 μg / ml) diluted in cell culture medium were added to each well of the drug group; Add 5...

Embodiment 3

[0156] Protective effect of wedelolide on ConA-induced immune liver injury in mice

[0157] In 1992, Tiegs et al. successfully induced specific liver injury in mice with concanavalin A (ConA). In recent years, it has gradually developed into the main experimental model for studying immune cell-mediated liver injury.

[0158] Concanavalin (Concanavalin, ConA is a plant lectin, has a mitogenic effect, and acts as a mitogen to stimulate T lymphocytes to express various cytokines TNF-α, IFN-γ, IL-2 to mediate liver damage, ConA induces T lymphocytes The pathology of dependent liver injury is similar to that of human autoimmune liver disease and acute and chronic viral hepatitis, and can be alleviated by immunosuppressants.

[0159] Eight hours after the administration of ConA, plasma ALT, AST, and LDH were significantly increased, and a large number of T lymphocytes infiltrated in the liver, and some lymphocytes in the portal area showed "sleeve" changes, and a large number of liv...

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PUM

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Abstract

The invention discloses a coumaric grass ethers extracted from compositae plants, or a salt or an ester accepted in pharmacy, or the application of the plant extracts of the compound for the preparation of medicine for curing autoimmune liver disease and viral hepatitis. As shown by the vitro and vivo experiments to the animal body, the coumaric grass ethers extracted from compositae plants, or a salt or an ester accepted in pharmacy has the advantages of effective therapy and improvement of the symptoms of autoimmune liver disease and viral hepatitis.

Description

technical field [0001] The invention relates to plant extracts, in particular to a coumarin compound extracted from Compositae plants, or the use of a pharmaceutical composition containing the compound. Background technique [0002] Eclipta prostrata Linn. is a traditional Chinese medicinal material. It is the whole herb of Eclipta prostrata Linn., which was first recorded in "Tang Materia Medica". Traditional Chinese medicine believes that Eclipta is sweet and sour in nature, cool, enters the liver and kidney meridians, has the effect of nourishing the liver and blood, cooling blood and stopping bleeding, and is mainly used for vomiting blood, coughing up blood, premature graying of beard and hair, turbid stranguria, and leukorrhea. [0003] According to reports, the whole herb of Eclipta contains saponins, flavonoids, Ecliptine, tannins, vitamins, nicotine, and various thiophene compounds; Methyl wedelolide and desmethyl wedelolide-7-glucoside. [0004] In 1956, Govindac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61K31/366A61K36/28A61P31/12A61P1/16
CPCY02A50/30
Inventor 俞强
Owner XIANGBEI WELMAN PHARMA CO LTD
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