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Compounds with anti-tumor activity in chloranthus japonicus as well as effective parts and purpose thereof

A technology of anti-tumor activity and effective parts, which is applied in the direction of anti-tumor drugs, medical preparations containing active ingredients, organic active ingredients, etc., and can solve the problems of ineffective development and utilization of plants

Active Publication Date: 2010-09-08
匡海学
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, the plant has hardly been effectively developed and utilized

Method used

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  • Compounds with anti-tumor activity in chloranthus japonicus as well as effective parts and purpose thereof
  • Compounds with anti-tumor activity in chloranthus japonicus as well as effective parts and purpose thereof
  • Compounds with anti-tumor activity in chloranthus japonicus as well as effective parts and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026]Weigh 15kg of dry whole herb of Silvertraceae, add 10 times volume ratio of 95% ethanol to reflux extraction, extract 2 times altogether, each time for 2 hours, combine the extracts, reclaim EtOH, and obtain 1208g of EtOH extract thick paste; The thick paste of the extract is suspended with 18 times the volume ratio of water to obtain a water suspension; it is successively extracted with petroleum ether, chloroform, ethyl acetate, and n-butanol in an amount equal to the volume of the water suspension, and each The solvent was extracted three times respectively, and the solvent was recovered to obtain five components of petroleum ether, chloroform, ethyl acetate, n-butanol, and water; the activity tracking and screening results proved that the ethyl acetate component was an effective antitumor component. The ethyl acetate fraction was then subjected to silica gel column chromatography, ODS reversed-phase column chromatography, and preparative HPLC to obtain a total of 12 m...

Embodiment 2

[0031] Weigh 25kg of dry whole herb of Silvertraceae, add 95% ethanol with 10 times volume ratio to reflux extraction, extract 2 times altogether, each 2 hours, combine extracts, reclaim EtOH, obtain EtOH extract thick paste 2150g, then The thick paste of the extract was degreased with petroleum ether and carried out AB-8 type macroporous resin column chromatography, followed by H 2 O, 50% EtOH, 95% EtOH were eluted to obtain petroleum ether, H 2 O, 50% EtOH, 95% EtOH four parts. The pharmacodynamic activity tracking experiment proves that the 50% EtOH part is the effective part. Continue to use silica gel column chromatography, ODS reversed-phase column chromatography and HPLC to separate this part, and analyze chemical analysis and various spectral data. A total of 5 arachnolactone-type sesquiterpenoids were separated and identified. Chemical structures of monomeric compounds, including novel compounds: silver thread grass A, silver thread grass B, silver thread grass C. ...

Embodiment 3

[0032] The preparation of embodiment 3 slow-release tablet, dropping pill

[0033] Take silvertrimidin A, silvertrimidin B, and silvertrimidin C monomer compounds, and form the main drug according to any combination of the three, or directly use the effective parts of silver thread grass as the main drug composition, Add appropriate amount of auxiliary materials such as slow-release agent, diluent, disintegrant, etc., mix well, make granules, dry, compress into tablets, coat or spray film-coat to get it; or add a suitable base, drop into slow-release drop pill , for antitumor therapeutic purposes.

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PUM

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Abstract

The invention discloses compounds with anti-tumor activity in chloranthus japonicus as well as effective parts and the purpose thereof. In the invention, three novel compounds with stronger anti-tumor activity are separated from the chloranthus japonicus which is a traditional Chinese medicine, i.e. a chloranthus japonicus element A, a chloranthus japonicus element B and a chloranthus japonicus element C. The method for separating the compounds comprises the following steps of: sequentially extracting a chloranthus japonicus extractive obtained by refluxing with 95% ethanol by using petroleum ether, ethyl acetate and n-butyl alcohol, and collecting the part obtained by ethyl acetate extraction; or degreasing the chloranthus japonicus extractive obtained by refluxing with 95% ethanol by using petroleum ether, carrying out macroporous resin column chromatograph, and eluting by using H2O, 50% alcohol and 95% alcohol sequentially; and carrying out silicagel column chromatography and ODS column chromatography on the ethyl acetate extracting part and the 50% alcohol component, and separating a prepared liquid phase to obtain the three compounds. Proved by in vitro anti-tumor activity research, the three compounds can remarkably restrain common tumor cells, have remarkable anti-tumor activity and can be used for developing novel anti-tumor harmfulless medicaments prepared from natural traditional Chinese medicines.

Description

technical field [0001] The present invention relates to three new compounds of a class of sesquiterpenoids, in particular to three kinds of antitumor active sesquiterpenoids isolated from the traditional Chinese medicine silvertraceae and a preparation method thereof. It further relates to the extract of effective anti-tumor parts of Silverwort and its preparation method. The present invention also relates to the medical use of the sesquiterpenoids and the extract of effective parts of Silvertraceae in the preparation of anti-tumor drugs, which belongs to the traditional Chinese medicine silver thread Field of grass extracts. Background technique [0002] After the 1980s, the incidence of malignant tumors increased at an average annual rate of 3% to 5%, and now ranks as the leading cause of death, which greatly endangers people's physical and mental health, and also restricts national economic construction and social development. It has caused a heavy burden to individuals,...

Claims

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Application Information

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IPC IPC(8): C07D307/77C07D493/06A61K31/365A61K36/898A61P35/00
Inventor 匡海学杨炳友夏永刚王秋红吕邵娃孙光日谷文倩
Owner 匡海学
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