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Preparation method and new application of artemisinin B

A technology of artemisinin and extract, applied in the field of preparation of artemisinin B, can solve the problems of complex immunosuppressive effect and the like

Active Publication Date: 2012-04-11
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Experiments and clinical studies in the past ten years have confirmed that various active ingredients in Artemisia annua have immunosuppressive activity, and have shown varying degrees of therapeutic or protective effects on autoimmune diseases such as rheumatoid arthritis and lupus erythematosus. Inflammation and more complex immunosuppressive effects, but no related reports on artemisinin B

Method used

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  • Preparation method and new application of artemisinin B
  • Preparation method and new application of artemisinin B
  • Preparation method and new application of artemisinin B

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0024] 1. Experimental materials

[0025] 1.1 Animals: 8-10 weeks old female Wistar rats.

[0026] 1.2 Main reagents: Ficoll-Paque (Amersham Biosciences), LPS (E.coli 0111:B4; Sigma; 1ng / mL), ELISA kit (R&D Systems, Minneapolis, MN). Medium: RPMI-1640 medium (Sigma-Aldrich), containing 10% calf serum, 2m ML-glutamine, 50μg / ml gentamicin and 5 damycin -5M 2-mercaptoethanol (purchased from Sigma), the medium was freshly prepared before cell culture, and the cells were cultured for 37 hours in 5% CO 2 to cultivate.

[0027] 1.3 The test drug is a series of compounds AA1-AA7 extracted from Artemisia annua L., wherein AA2 is artemisinin B (artemisinin B).

[0028] 2. Experimental method

[0029] 2.1 Acquisition of rat peritoneal cells: 5-10 rats per cage (transparent plastic mouse cage), fed in a standard animal room. Lighting: 6:00-18:00; Temperature: 22-24°C. After the broken vertebrae were killed, 16ml of normal saline was injected into the abdominal cavity to wash the per...

Embodiment 1

[0051] Artemisia annua leaves 1kg dried, crushed, soaked in 5L 95% ethanol for 24 hours, percolated with 50L 95% ethanol, collected percolation liquid, recovered solvent under reduced pressure below 50°C to obtain extract, dissolved in ethyl acetate, mixed with 2 times The column chromatography silica gel of extract weight is mixed, and after drying, it is added to the top of the chromatography column that 30 times of extract weight column chromatography silica gel is housed, with sherwood oil-ethyl acetate (1: 0 → 5: 5) Gradient elution, using thin layer chromatography to detect the eluent components, collecting the fractions containing artemisinin B, recovering the solvent to a small volume, leaving it to precipitate crude crystals, and then recrystallizing and purifying from acetone to obtain artemisinin B .

Embodiment 2

[0053] After drying 1 kg of Artemisia annua leaves, crush them, soak them in 4L of ethyl acetate for 50 hours, percolate with 45L of ethyl acetate, collect the percolation liquid, recover the solvent under reduced pressure below 55°C to obtain an extract, dissolve it in ethyl acetate, Mix with the column chromatography silica gel of 3 times of extract weight, dry, add the top of the column chromatography that 25 times of extract weight column chromatography silica gel is housed and carry out silica gel column chromatography separation, use sherwood oil-ethyl acetate (1: 0 → 5:5) mixed solvent gradient elution, detect the eluent components by thin layer chromatography, collect the fractions containing artemisinin B, recover the solvent to a small volume, leave it to precipitate crude crystals, and then pass through ethyl acetate Repeated recrystallization purification, that is.

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Abstract

The invention discloses a preparation method and new application of artemisinin B. The extraction and separation method of artemisinin B comprises the following steps: drying sweet wormwood leaves, grinding, percolating / soaking with an organic solvent for extraction, recycling the solvent at 60 DEG C under reduced pressure, mixing with silica gel for column chromatography, airing, performing silica gel column chromatography to separate, performing gradient elution by use of a petroleum ether-ethyl acetate or petroleum ether-acetone mixed solvent, adopting the thin layer chromatography to detect the components of the eluent, collecting the component flow with artemisinin B, recycling the solvent to ensure that the solution has small volume, standing the solution to separate out coarse crystals, and repeatedly recrystallizing and purifying the coarse crystals by using an organic solvent such as acetone and ethanol to obtain artemisinin B. The artemisinin B is used for preparing immunosuppressive drugs, has obvious immunosuppressive activity, and can be used for preparing drugs for preventing and treating autoimmune diseases and inflammatory diseases and be used in clinic.

Description

technical field [0001] The present invention relates to a preparation method of artemisinin B (artemisinin B) and its new application, in particular to the preparation of artemisinin B (artemisinin B) in the preparation of drugs for preventing and treating autoimmune diseases and inflammatory diseases. application. Background technique [0002] In recent years, with the gradual improvement of the degree of social industrialization, autoimmune diseases, hypersensitivity diseases and other diseases caused by excessive immune response are also increasing. It has become a worldwide task to find high-efficiency and low-toxicity immunosuppressants. research hotspots. Evidence shows that traditional Chinese medicine immunosuppressants have special curative effects of high efficiency and low toxicity, but the difficulty in controlling the quality of preparations and clarifying the mechanism of action limits their wide application in clinical practice. Using modern extraction and s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/10A61K31/365A61P37/00A61P37/06A61P29/00
Inventor 朱晓新杨岚李玉洁陈颖杨庆翁小刚张东
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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