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The method and application of extracting strychnine nitrogen oxides from Strychnis chinensis

A technology of nitrogen oxides and strychnine, which is applied in the direction of medical preparations containing active ingredients, drug combinations, organic chemistry, etc., can solve the differences between batches of compounds, potential effects to be developed, and few people to study the application, etc. problem, to achieve the effect of small reagent consumption, good development potential and good operability

Active Publication Date: 2019-02-12
正源堂(天津)生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The current separation and extraction of strychnine nitrogen oxides is limited by the non-mechanized operation of traditional Chinese medicine. The steps are cumbersome, time-consuming, and labor-intensive. The amount of the compound obtained is small and the difference between batches is large, making it difficult to conduct clinical research.
[0005] In addition, for strychnine nitrogen oxide, its application is rarely studied, so its potential role remains to be developed

Method used

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  • The method and application of extracting strychnine nitrogen oxides from Strychnis chinensis
  • The method and application of extracting strychnine nitrogen oxides from Strychnis chinensis
  • The method and application of extracting strychnine nitrogen oxides from Strychnis chinensis

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Embodiment 1

[0036] Embodiment 1: Extraction of strychnine nitrogen oxides in Nuxychnium chinensis

[0037] Use the fruiting bodies of Nuxyche as the raw material, grind them into powder, then reflux extract with ethanol for 1.5h, filter, take the precipitate and repeat the extraction twice, combine the obtained filtrates, spin evaporate to obtain dry coarse powder of Nuxe nux, weigh 10g, dissolve In 100mL of 55% methanol-water (0.1% acetic acid) solution, the Nuxychia seed extract solution was prepared with a concentration of 100mg / mL, passed through a 0.45μm microporous membrane, and prepared by one-dimensional liquid chromatography. One-dimensional liquid chromatography adopts Innovel C18 150×250mm, 10μm, The mobile phase is a mixture of binary liquid phases, in which phase A of the binary liquid phase is water (containing 0.1% acetic acid), and phase B is methanol. % isocratic for 20 minutes, phase B concentration 100% isocratic for 10 minutes. Adopt ultraviolet detector, select 210...

Embodiment 2

[0040] Embodiment 2: Extraction of strychnine nitrogen oxides in Semen Nuxtrix

[0041] Use the fruiting body of Nuxyche as the raw material, grind it into powder, extract it with ethanol under reflux for 2 hours, filter, take the precipitate and repeat the extraction twice, combine the obtained filtrate, spin evaporate to obtain dry coarse powder of Nuxe officinalis, weigh 15g, dissolve in 100mL of 50% methanol-water (0.1% acetic acid) solution was used to prepare a Nuxychia seed extract solution with a concentration of 150mg / mL, passed through a 0.45μm microporous membrane, and prepared by one-dimensional liquid chromatography. One-dimensional liquid chromatography adopts Innovel C18 150×250m, 10μm, The mobile phase is a mixture of binary liquid phases, in which the binary liquid phase A is water (0.1% acetic acid), and B phase is methanol, and the elution method: the concentration of phase B is 25% isocratic for 10 minutes, and the concentration of phase B is 35% Isocrati...

Embodiment 3

[0044] Embodiment 3: Extraction of strychnine nitrogen oxides in Nuxychnium chinensis

[0045] Use the fruiting body of Nuxyche as the raw material, grind it into powder, soak it in ethanol for 2 hours, filter, take the precipitate and repeat twice, combine the obtained filtrates, spin evaporate to obtain dry coarse powder of Nuxe officinalis, weigh 5g, dissolve in 100mL 60 % methanol-water (0.1% acetic acid) solution to prepare a Nuxebra chinensis extract solution with a concentration of 50 mg / mL, pass through a 0.45 μm microporous membrane, and prepare by one-dimensional liquid chromatography. One-dimensional liquid chromatography adopts Innovel C18 150×250mm, 10μm, The mobile phase is a mixture of binary liquid phases, in which the binary liquid phase A is water (0.1% acetic acid), and B phase is methanol, and the elution method: the concentration of phase B is 25% isocratic for 10 minutes, and the concentration of phase B is 35% Isocratic for 20 minutes, B phase concentr...

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Abstract

The invention provides a method for extracting strychnine N-oxides from semen strychni, which comprises the following steps: a) grinding the semen strychni into powder, and soaking or reflux-extracting the powder in ethanol, evaporate-drying a filtrate and dissolving the obtained powder in a methanol-water solution; b) performing one-dimensional liquid-phase separation with a C18 chromatographic column through a binary liquid phase with water as an A phase and methanol as a B phase, wherein elution includes: isocratic elution with 25% B phase for 10 min, isocratic elution with 35% B phase for 20 min and isocratic elution with 100% B phase for 10 min, collecting an eluent in 11.5-13.5 min, evaporate-drying the eluent, and dissolving the eluent in the methanol-water solution; and c) performing two-dimensional liquid-phase separation with a C18 chromatographic column through a binary liquid-phase mixture with water as an A phase and methanol as a B phase, wherein elution includes: isocratic elution with 30% B phase for 15-30 min, collecting an eluent in 9.7-10.5 min, and evaporate-drying the eluent to obtain the monomer compound of the strychnine N-oxides. The method is used for separating the monomer compound, which has strong antitumor activities, for preparation of an antitumor medicine.

Description

technical field [0001] The invention relates to the technical field of extracting traditional Chinese medicines, in particular to a method for extracting strychnine nitrogen oxides from Nuxychnium chinensis and the application of the compound in preparing anti-liver cancer and anti-lung cancer drugs. Background technique [0002] Strychnine nitrogen oxide is a compound with anticancer activity in the traditional Chinese medicine Strychnis chinensis, and its structural formula is as follows: [0003] [0004] The current separation and extraction of strychnine nitrogen oxides is limited by the non-mechanized operation of traditional Chinese medicine. The steps are cumbersome, time-consuming, and labor-intensive. The amount of the compound obtained is small and the difference between batches is large, making it difficult to conduct clinical research. [0005] In addition, for strychnine nitrogen oxide, its application is rarely studied, so its potential role remains to be d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/22A61K31/439A61K36/56A61P35/00
CPCA61K31/439A61K36/56C07D493/22
Inventor 张耀洲李上文
Owner 正源堂(天津)生物科技有限公司
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