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1'-acetoxy chavicol acetic ester

A technology of acetoxypiperol acetate and carbon dioxide, which is applied in the field of preparation of Mycobacterium tuberculosis inhibitors by 1'-acetoxypiperol acetate, can solve problems such as unseen

Inactive Publication Date: 2007-08-22
HONGYI SCI & TECH CO LTD NANCHANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are also research reports showing that 1'-acetoxypiperol acetate has antitumor properties (Moffatt J, A, et al. [J]. Carcinogenesis, 2000, 21: 2151-2157; zheng Q et al. [J] .J Cancer Res Clin Oncol, 2002, 128:539~546), antibacterial (Janssen A M, [J].planta Med, 1985(6):507~511), antifungal (Ficker C E, etal.[J] .J Ethnophamacal, 2003, 85:589~593), anti-ulcer (Mitsuis, etal.[J].Chem Pham Bull, 1976,24:2377~2382), antioxidant (Kubota K, etal.[J].Spec Publ R Soc Chem, 2001, 274: 601~607), anti-inflammatory (NakamuraY, [J]. Cancer Res, 1998, 58: 4832~4839) and other biological activities, but no supercritical carbon dioxide extraction and silica gel column layer Analysis of the production method The research report on the extraction and purification of 1'-acetoxypiperol acetate from the dry rhizome of Alpiniagalanga Willd. of Zingiberaceae, Alpiniagalanga Willd., and no 1'-acetoxypiperol acetate Application of Phenyl Acetate in Preparation of Inhibitors of Mycobacterium Tuberculosis

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0018] Take the dried rhizome galanga of Zingiberaceae plant Alpinia galanga Willd., dry it to a moisture content of 5.6%, grind it into 18 mesh fine powder, put it in a supercritical carbon dioxide extractor, and the temperature of the extraction kettle is 33°C. The pressure is 15Mpa; the temperature of the separation column is 45°C and the pressure is 10Mpa; the temperature of the desorption kettle is 36°C and the pressure is 8MPa; the instantaneous flow rate of carbon dioxide is 200L / hour; the extraction and separation time is 4 hours. Take the above-mentioned extract separation liquid and pass it through a silica gel chromatography column, elute and refine it with 10:1 n-hexane-ethyl acetate, collect the eluted refined liquid, and dry it under reduced pressure to obtain the compound 1 (1'-acetoxypiperol B esters). The compound (1'-acetoxypiperol acetate) is made into soft capsules, tablets, capsules, pills, granules and injections by conventional preparation methods and us...

Embodiment 2

[0020] Take the dried rhizome galanga of Zingiberaceae plant Alpinia galanga Willd., dry it to a moisture content of 8.2%, grind it into 20 mesh fine powder, put it in a supercritical carbon dioxide extractor, and the temperature of the extraction kettle is 38°C. The pressure is 20Mpa; the temperature of the separation column is 41°C and the pressure is 12Mpa; the temperature of the desorption kettle is 32°C and the pressure is 10MPa; the instantaneous flow rate of carbon dioxide is 250L / hour; the extraction and separation time is 5 hours. Take the above-mentioned extract separation liquid and pass it through a silica gel chromatography column, elute and refine it with 10:1 n-hexane-ethyl acetate, collect the eluted refined liquid, and dry it under reduced pressure to obtain compound 2 (1'-acetoxypiperol B esters). The compound (1'-acetoxypiperol acetate) is made into soft capsules, tablets, capsules, pills, granules and injections by conventional preparation methods and used ...

Embodiment 3

[0022] Take the dried rhizome galanga of Zingiberaceae plant Alpinia galanga Willd., dry it to a moisture content of 7.1%, pulverize it into a 14-mesh fine powder, put it in a supercritical carbon dioxide extractor, and the temperature of the extraction kettle is 40°C. The pressure is 10Mpa; the temperature of the separation column is 50°C and the pressure is 18Mpa; the temperature of the desorption kettle is 45°C and the pressure is 15MPa; the instantaneous flow rate of carbon dioxide is 150L / hour; the extraction and separation time is 6 hours. Take the above-mentioned extract separation liquid and pass it through a silica gel chromatography column, elute and refine it with 10:1 n-hexane-ethyl acetate, collect the eluted refined liquid, and dry it under reduced pressure to obtain compound 3(1'-acetoxypiperolol B esters). The compound (1'-acetoxypiperol acetate) is made into soft capsules, tablets, capsules, pills, granules and injections by conventional preparation methods an...

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Abstract

The present invention discloses a supercritical CO2 extraction and silica gel column chromatographic process for extracting, separating and refining 1'-acetoxy chavicol acetic ester with activity of resisting tubercle bacillus infection from dried galangal rhizome as one kind of Zingiberaceae plant.

Description

technical field [0001] The invention relates to a production method of supercritical carbon dioxide extraction and silica gel column chromatography to extract, separate and refine 1'-acetoxy piperonol B from the dry rhizome of Alpinia galanga Willd. Application of esters in the preparation of Mycobacterium tuberculosis inhibitors. Background technique [0002] The English name of 1’-acetoxychavicol acetate is 1’-acetoxychavicol acetate, and its molecular formula is C 13 h 14 o 4 , the molecular weight is 234.25, and the structural formula is On August 10, 2006, Japanese Patent JP2006206541 disclosed a chemical synthesis method of 1'-acetoxypiperol acetate. On July 7, 2005, Japanese Patent JP2005179201 disclosed that 1'-acetoxypiperol acetate isolated from the methanol extract of Galanga galanga fruit can inhibit the replication of HIV-1NL43 in MT-4 cells , but has no effect on the survival of MT-4 cells, showing high safety and the characteristics of inhibiting the ext...

Claims

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Application Information

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IPC IPC(8): C07C67/48C07C69/16A61K31/20A61P31/04A61K36/9062
CPCY02P20/54
Inventor 刘孝乐
Owner HONGYI SCI & TECH CO LTD NANCHANG
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