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Application of artemisinin derivative in preparation of medicaments for treating Crohn disease

A technology of artemisinin derivatives and Crohn's disease, applied in the field of biomedicine, can solve the problems of large side effects and unsatisfactory effects of Crohn's disease, and achieve the effect of less side effects, mild side effects and effective treatment

Inactive Publication Date: 2011-05-11
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] The object of the present invention is to provide an application of artemisinin derivatives in the preparation of medicines for treating Crohn's disease, said artemisinin and artemisinin derivatives should solve the problem of drug treatment of Crohn's disease in the prior art. The technical problem of en disease with large side effects and unsatisfactory effect

Method used

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  • Application of artemisinin derivative in preparation of medicaments for treating Crohn disease
  • Application of artemisinin derivative in preparation of medicaments for treating Crohn disease
  • Application of artemisinin derivative in preparation of medicaments for treating Crohn disease

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1: Animal grouping and establishment of colitis model

[0033] C57BL / 6 mice (supplied by Shanghai Experimental Animal Center, Chinese Academy of Sciences) were randomly divided into 3 groups, namely, ethanol control group, trinitrobenzenesulfonic acid model group and artesunate treatment group, with 6 mice in each group. Establishment of the mouse colitis model in the trinitrobenzenesulfonic acid group and the artesunate treatment group: After the mice were lightly anesthetized, the flexible tube was inserted into the anus about 4cm, and 0.1ml of trinitrobenzenesulfonic acid / ethanol solution was slowly injected; ethanol control The group was injected with 0.1ml of ethanol solution, inverted for about 60s, and put back into the cage. About 8 hours after the enema, the mice in the artesunate treatment group were intraperitoneally injected with artesunate 150 mg / kg / day (Guangxi Guilin Pharmaceutical Co., Ltd.), and the ethanol control group and the trinitrobenze...

Embodiment 2

[0036] Example 2: Histological examination

[0037] On the eighth day of the experiment, the mice were sacrificed, and the serum was collected and stored in a -70°C refrigerator; laparotomy was performed, and the intestines were collected and stored in liquid nitrogen. Colonic changes were observed with the naked eye and a general score was made. The criteria were: colon ulcer, colon and peritoneal adhesions, colon wall thickening, and mucosal edema. The severity of each parameter ranged from normal (0 points) to the most severe (4 points) points 4 The general score is the average of the four parameter scores. Colon tissues with the most obvious lesions were taken and fixed in 10% formalin solution, routinely embedded in paraffin, sectioned, stained with hematoxylin-eosin, observed histological changes with a light microscope and scored, and the standard was: 0 points: no inflammation; 1 point : mild inflammation of the colon; 2 points: a small amount of inflammatory cells su...

Embodiment 3

[0038] Example 3 Immunohistochemical staining and result judgment

[0039] The SP method was used for nuclear factor-κBp65 immunohistochemical staining, and the specific operation steps were carried out according to the instructions of the nuclear factor-κBp65 SP immunohistochemical staining kit (Fujian Maixin Biotechnology Development Co., Ltd.). The result judgment includes two aspects: (1) Positive staining intensity grading: level 0 is negative, no cell staining; level 1 is weakly positive, scattered yellow particles appear in the cells; level 2 is moderately positive, a small amount of brown-yellow cells appear Particles; grade 3: a large number of brown-yellow particles appear in the cells. (2) Grading of the number of positive cells: Grade 0 is negative, no cell staining; Grade 1 is the number of positive cells ≤ 10%; Grade 2 is the number of positive cells 11% to 50%; Grade 3 is the number of positive cells 51% to 80% ; Grade 4 is the number of positive cells > 80%. ...

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Abstract

The invention discloses an application of an artemisinin derivative in preparation of medicament for treating Crohn disease, and the artemisinin derivative is selected from artesunate or artemether or styrene monomer 905 (SM905). The artemisinin derivative can be used for achieving the purpose of treating the Crohn disease by inhibiting Th1 / Th17 immune response and inhibiting nuclear factor-kB activation. Compared with the existing medicaments, the artemisinin derivative has less and light side effects, in one year of following visits for the treatment of rheumatoid arthritis, transient reticulocyte decline and hepatic dysfunction only occur in individual cases, and the health can be restored by liver protection treatment without medicament withdrawal. Therefore, the artemisinin derivative can be taken by patients for a long time, the treatment can be maintained, and the purpose of effective treatment can be achieved.

Description

Technical field: [0001] The present invention relates to the field of biomedicine, in particular to an artemisinin derivative, especially an application of an artemisinin derivative in preparing a medicine for treating Crohn's disease. Background technique: [0002] In the prior art, drugs for treating Crohn's disease include glucocorticoids, 5-aminosalicylic acid, immunosuppressants such as azathioprine, anti-tumor necrosis factor-α monoclonal antibodies, and the like. The current goal of treatment is to relieve symptoms and maintain remission. [0003] 5-aminosalicylic acid: recommended for mild to moderate patients, can maintain treatment, relatively minimal side effects, but poorly controlled symptoms of most patients. [0004] Glucocorticoids: For moderate to severe patients whose 5-aminosalicylic acid cannot be controlled, it can relieve symptoms, but cannot heal mucosal ulcers, relatively many side effects, and has no maintenance remission effect. [0005] Immunosup...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P1/00A61P37/06
Inventor 杨川华
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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