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Hetisin type diterpenoid alkaloid and preparation method and application thereof

A kind of technology of diterpene alkaloid and anti-inflammatory drug, which is applied in the field of haitiform diterpene alkaloid

Inactive Publication Date: 2011-07-20
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There is no report on diterpene alkaloids as shown in structural formula (I) extracted and isolated from Ranunculaceae Aconitum aconitum

Method used

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  • Hetisin type diterpenoid alkaloid and preparation method and application thereof
  • Hetisin type diterpenoid alkaloid and preparation method and application thereof
  • Hetisin type diterpenoid alkaloid and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Take the dried aconite, crush it, cold-soak it with pH 2 hydrochloric acid aqueous solution for 1 day, repeat the extraction three times, combine the extracts, filter off the precipitate, then add ammonia water to alkalinize the acid water extract to pH 9, and then extract it three times with ethyl acetate , the extract was washed with water to neutrality, and dried with anhydrous sodium sulfate, then concentrated under reduced pressure to obtain the total alkaloids extract, the total alkaloids were subjected to silica gel H short column chromatography, respectively with different proportions of petroleum ether-acetone Gradient elution to obtain the compound of the present invention.

Embodiment 2

[0028] Take the dried aconite, crush it, soak it coldly with pH 1 sulfuric acid aqueous solution for 1 day, repeat the extraction three times, combine the extracts, filter off the precipitate, then add sodium hydroxide to alkalinize the acid water extract to pH 10, and then extract it three times with chloroform , the extract was washed with water to neutrality, and dried with anhydrous sodium sulfate, then concentrated under reduced pressure to obtain the total alkaloid extract, the total alkaloids were subjected to silica gel H short column chromatography, and ethyl acetate in different proportions- Gradient elution with acetone gives the compound of the present invention.

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Abstract

The invention discloses hetisin type diterpenoid alkaloid and a preparation method thereof and application of the alkaloid as anti-inflammatory medicaments. The diterpenoid alkaloid is prepared from buttercup aconitum plant monkshood serving as a raw material by the steps of acid water extraction, alkalization, organic solvent extraction, silica gel short column chromatography and elution. According to authentication by a chromatographic method, the compound is novel hetisin type diterpenoid alkaloid carmichaeline A. An animal test shows that the new compound has certain anti-inflammatory activity on a mouse inflammation model caused by various inflammatory agents.

Description

technical field [0001] The invention relates to a hytigenous diterpene alkaloid extracted and separated from aconite of Ranunculaceae Aconitum and its specific preparation method and application. Background technique [0002] Aconitum is mainly produced in Sichuan and other places, and its subgenus is called aconite, which is a commonly used traditional Chinese medicine. Modern pharmacological research shows that its main active ingredient is C 19 Type diterpene alkaloids have various activities such as anti-inflammatory and analgesic. The 3-deoxyaconitine contained in it has been developed into an original new drug in my country. Aconite is currently mainly used for dispelling rheumatism and other diseases, and has analgesic and anti-inflammatory effects. [0003] There is no report on diterpene alkaloids as shown in structural formula (I) extracted and isolated from Aconitum aconitum of Ranunculaceae at present. Contents of the invention [0004] The object of the pre...

Claims

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Application Information

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IPC IPC(8): C07D221/22A61K31/439A61P29/00
Inventor 苟小军陈封政李书华刘嵬宋芹颜军
Owner CHENGDU UNIV
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