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Preparation method and new application of artemisinin B

A compound and volume technology that can be used in antipyretics, organic chemistry, non-central analgesics, etc., to solve problems such as complex immunosuppression

Inactive Publication Date: 2014-07-16
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

[0025] 1. Experimental materials

[0026] 1.1 Animals: Female Wistar rats aged 8-10 weeks.

[0027] 1.2 Main reagents: Ficoll-Paque (Amersham Biosciences), LPS (E.coli0111: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 -5 M2-Mercaptoethanol (purchased from Sigma), the medium is freshly prepared before cell culture, 37 cells culture, 5% CO 2 to cultivate.

[0028] 1.3 The test drug is a series of compounds AA1-AA7 extracted from Artemisia annua L., where AA2 is artemisinin B.

[0029] 2. Experimental method

[0030] 2.1 Obtaining of rat abdominal cavity cells: 5-10 rats in a cage (transparent plastic mouse cage), fed in a standard animal room. Light: 6 to 18 o'clock; temperature: 22-24 ℃. After the vertebrae were sacrificed, 16ml of normal saline was injected into the abdominal cavity to wash the abdominal cavity cells with a concentration of 2×10 6 100...

Embodiment 1

[0052] After 1kg of Artemisia annua leaves are dried, crushed, add 5L of 95% ethanol to soak for 24 hours, percolate with 50L of 95% ethanol, collect the percolate, and recover the solvent under reduced pressure below 50℃ to obtain the extract. Mix the column chromatography silica gel with the weight of the extract, dry it, add it to the top of the column chromatography silica gel with 30 times the weight of the extract, use petroleum ether-ethyl acetate (1:0→5:5) Gradient elution, the components of the eluent were detected by thin-layer chromatography, the fractions containing artemisinin B were collected, the solvent was recovered to a small volume, and the crude crystals were separated out, and then purified by acetone recrystallization to obtain artemisinin B .

Embodiment 2

[0054] After 1kg of Artemisia annua leaves are dried, crushed, soaked in 4L of ethyl acetate for 50 hours, percolated with 45L of ethyl acetate, collected the percolate, and recovered the solvent under reduced pressure below 55°C to obtain the extract. After dissolving with ethyl acetate, Mix with column chromatography silica gel of 3 times the weight of the extract, dry, and add 25 times the weight of the extract to the top of the column chromatography silica gel for silica gel column chromatography. Use petroleum ether-ethyl acetate (1: 0→5:5) Gradient elution of mixed solvents, the components of the eluent are detected by thin layer chromatography, the fractions containing artemisinin B are collected, the solvent is recovered to a small volume, the crude crystals are precipitated out, and then subjected to ethyl acetate Repeated recrystallization and purification, that is.

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Abstract

The invention discloses a preparation method of artemisinin B and an application in immune field. 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 invention relates to a preparation method of artemisinin B (artemisinin B) and new uses thereof, and particularly relates to a preparation method of artemisinin B (artemisinin B) in the preparation of medicines for preventing and treating autoimmune diseases and inflammatory diseases application. Background technique [0002] In recent years, with the gradual increase in the degree of social industrialization, autoimmune diseases, hypersensitivity diseases and other diseases caused by excessive immune response are also increasing. The search for highly effective and low-toxic immunosuppressants has become a worldwide Research hotspots. There is evidence that traditional Chinese medicine immunosuppressants have special effects with high efficiency and low toxicity. However, the quality of preparations is difficult to control and the mechanism of action is difficult to clarify, which limits its wide clinical application. The use of modern extraction and...

Claims

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Application Information

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Patent Type & Authority Patents(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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