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Application of norisoboldine in preparing medicament for treating autoimmune disease

A technology of norisoboldine and autoimmunity, which is applied in the field of medicine and can solve the problems of no biological activity or clinical application of norisoboldine.

Inactive Publication Date: 2009-03-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are no reports on the biological activity or clinical application of noribordine except for the in vitro antioxidant effect [Acta Pharmacina Sinica 200641(10):956-962]

Method used

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  • Application of norisoboldine in preparing medicament for treating autoimmune disease
  • Application of norisoboldine in preparing medicament for treating autoimmune disease
  • Application of norisoboldine in preparing medicament for treating autoimmune disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Preparation of norisoboldine: dry 3 kg of root tuber powder, reflux extraction with 95% ethanol for 3 times, 2 hours each time, concentrate under reduced pressure to obtain extract, add 2% hydrochloric acid to dissolve, and filter. The filtrate was chromatographed on a strongly acidic cation exchange resin column, washed with water, and the pH was adjusted to 8.5 with ammonia water, then the exchange resin was transferred to a Soxhlet extractor, and ether was refluxed for extraction. Ether was evaporated to obtain 4.8 g of dark brown extract. The extract was separated by silica gel column chromatography repeatedly, eluted repeatedly with chloroform-methanol (7:3) to obtain the crude compound I, and after repeated recrystallization, 0.76 g of brown powder Compound I was obtained. Co-silica gel thin layer chromatography with reference substance, R f The value is consistent, and the mixing melting point does not decrease, so the identification compound I is norisoboldine....

Embodiment 2

[0018] Effects of Noribordine on Type II Collagen-Induced Arthritis in Mice

[0019] 1 The effect of noribordine on the body weight of mice with collagen arthritis

[0020] Add chicken type II collagen into 0.1M acetic acid, stir at 4°C until fully dissolved, and make the concentration 2mg / ml, overnight at 4°C, mix with an equal volume of complete Freund's adjuvant (containing 2mg / ml hot water) in an ice bath Inactivated Mycobacterium tuberculosis) were mixed and fully emulsified to obtain type II collagen emulsion. Male ICR mice were sensitized by intradermal injection of 100 μl type II collagen emulsion at the base of the tail, and the day of injection was recorded as d 0. On the 21st day, 100 μl of type II collagen emulsion was injected again at the same site to attack, and the mice were randomly divided into 6 groups (n=7-8): 1) normal group; 2) model group; 3) norisobolidine ( 10 mg / kg); 4) Noripordine (20 mg / kg); 5) Noripordine (40 mg / kg); 6) Dexamethasone (DEX, 1 mg / k...

Embodiment 3

[0038] Effect of Noribordine on Experimental Autoimmune Encephalomyelitis (EAE) in Rats

[0039] The guinea pig spinal cord was collected under aseptic conditions, made into a 50% homogenate, and fully mixed with the same amount of complete Freund's adjuvant to prepare the immunogen. Rats were injected with 0.1 mL of immunogenic emulsion in each of the two hind foot pads, and at the same time, subcutaneously injected pertussis vaccine (5.5×10 10 mL -1 ) 0.2 mL. The guinea pig spinal cord homogenate in the immunogen of the control group was replaced with an equal amount of normal saline, and the administration group was administered from the day of immunization for 18 consecutive days.

[0040] After immunization, the body weight of the rats was weighed every day, the condition was observed, and the neurological dysfunction score was performed. The scoring standard of neurological dysfunction adopts a 5-point scoring method: 0 points, no obvious abnormality; 1 point, tail we...

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Abstract

The invention relates to the medicine filed, in particular to a medicinal purpose of norisoboldine. The medicinal purpose is characterized in that the norisoboldine can be used in the application of preparing drugs for the treatment of autoimmune diseases. The autoimmune diseases are: rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, multiple sclerosis, type-I diabetes, psoriasis, ulcerative colitis, Sjogren syndrome, scleroderma, polymyositis, chronic active hepatitis, mixed connective tissue disease, primary biliary cirrhosis, autoimmune hemolytic anemia and other diseases.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the medical application of norisoboldine. Background technique [0002] Autoimmune disease is a common clinical disease caused by abnormal immune response, including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type I diabetes, psoriasis, ulcerative colitis, etc. disease. Among them, rheumatoid arthritis is a disease dominated by non-suppurative inflammation of multiple joints with peripheral symmetry, often accompanied by inflammation of the synovial membrane of the joint cavity, hyperplasia of synovial tissue, formation of granuloma, destruction of cartilage and bone tissue, and finally joint deformation. ,Loss of function. Multiple sclerosis is an autoimmune disease characterized by inflammatory demyelinating lesions of the central nervous system. Drugs for the treatment of rheumatoid arthritis mainly include non-steroidal anti-inflammatory drugs (diclofen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/473A61P37/02
Inventor 戴岳夏玉凤刘美侴桂新王峥涛
Owner CHINA PHARM UNIV
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