Prepn process of peonol as active anticancer component

A technology for paeonol derivatives and anticancer activity is applied in the field of preparation of anticancer active components paeonol derivatives, which can solve the problems of unsatisfactory anticancer drugs and unsatisfactory treatment effects, and achieve anticancer effects. activity-enhancing effect

Inactive Publication Date: 2006-05-17
THE CHINESE TRADITIONAL HERB MEDICINE RES INST HENAN PROV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, the anti-cancer drugs used by humans are not satisfactory, and their therapeutic effects are still not satisfactory to people.

Method used

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  • Prepn process of peonol as active anticancer component

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Embodiment 1

[0024] The preparation method of the present invention is prepared according to the following steps:

[0025] The first step, take 500g of p-aminophenylarsine acid, dissolve it in 5L of hydrochloric acid solution with a concentration of 0.5Mol / L, slowly add 20ml of sodium nitrite solution with a concentration of 10% at 0°C, and dissolve it at 0°C. Stir for 3 hours at ℃, filter, and wash the precipitate with dilute hydrochloric acid and water successively, and set aside;

[0026] The second step, take by weighing paeonol 200g and the precipitate that the first step makes and be dissolved in 4L concentration and be 2%, in the sodium hydroxide solution of W / V, stir at 0 ℃; Regulate pH value to 8, at 0 Stir at ℃ for 6 hours, add dilute hydrochloric acid to adjust the pH value to 1, and place at 0℃ for 6 hours;

[0027] The third step is to filter the result of the second step, wash the precipitate with dilute hydrochloric acid and water in turn, separate the precipitate, add a 2%...

Embodiment 2

[0029] The preparation method of the present invention is prepared according to the following steps:

[0030] The first step, take by weighing p-aminophenylarsine 500g, be dissolved in the hydrochloric acid solution that 30L concentration is 1.2Mol / L, add 500ml concentration slowly at 3 ℃ and be 30%, the sodium nitrite solution of W / V, in 3 Stir for 1 hour at ℃, filter, and wash the precipitate with dilute hydrochloric acid and water successively, and set aside;

[0031] The second step, take paeonol 300g and the precipitate that the first step makes and be dissolved in 12L concentration and be 6%, in the sodium hydroxide solution of W / V, stir at 3 ℃; Regulate pH value to 11, at 3 Stir at ℃ for 2 hours, add dilute hydrochloric acid to adjust the pH value to 2, and place at 3℃ for 1 hour;

[0032] The third step is to filter the result of the second step, wash the precipitate with dilute hydrochloric acid and water successively, separate the precipitate, add 6% sodium hydroxid...

Embodiment 3

[0034] The preparation method of the present invention is prepared according to the following steps:

[0035]The first step, weigh 500g of p-aminophenylarsine acid, dissolve in 50L of hydrochloric acid solution with a concentration of 2Mol / L, slowly add 1000ml of 45% W / V sodium nitrite solution at 5°C, Stir for 10 minutes, filter, and the precipitate is washed with dilute hydrochloric acid and water successively, and set aside;

[0036] The second step, take by weighing paeonol 400g and the precipitate that the first step makes and be dissolved in 20L concentration and be 10%, in the sodium hydroxide solution of W / V, stir at 5 ℃; Regulate pH value to 14, at 5 Stir at ℃ for 0.5 hours, add dilute hydrochloric acid to adjust the pH value to 3, and place at 5℃ for 0.5 hours;

[0037] The third step is to filter the result of the second step, wash the precipitate with dilute hydrochloric acid and water in turn, separate the precipitate, add 10% sodium hydroxide solution to dissolv...

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Abstract

The present invention discloses the preparation process of peonol derivative as active anticancer component. The preparation process includes the following steps: 1. dissolving atoxylic acid in hydrochloric acid solution, adding sodium nitrite solution slowly at 0-5 deg.c, stirring, filtering, and washing the precipitate with dilute hydrochloric acid and water successively; 2. dissolving peonol and the obtained precipitate in sodium hydroxide solution at 0-5 deg.c, stirring, regulating pH value to 8-14, stirring, regulating pH value to 1-3 with dilute hydrochloric acid and setting at 0-5 deg.c; and 3. filtering the product obtained in the step 2, washing the precipitate with dilute hydrochloric acid and water successively, dissolving in sodium hydroxide, filtering, dropping dilute hydrochloric acid to regulate pH value to 1-3, setting at 0-5 deg.c, filtering, drying the precipitate, and re-crystallizing to obtain the product peonol diazo arsonate, which can inhibit the growth of human cancer cells in large intestine, liver and stomach effectively.

Description

technical field [0001] The invention relates to an anticancer drug, in particular to a preparation method of paeonol derivatives as an anticancer active ingredient. Background technique [0002] Cancer has become one of the main killers faced by human beings in modern society. Due to environmental pollution, bad living habits and various pressures, human beings have to fight unremittingly against various cancers. But so far, the anti-cancer drugs used by humans are not satisfactory, and their therapeutic effects are still not satisfactory to people. According to literature reports, currently recognized drug paclitaxel with strong anticancer activity has obvious inhibitory effect on gastric cancer cell line SGC-7901 cells, and with the increase of paclitaxel concentration in the medium and the prolongation of culture time, the inhibitory effect is gradually enhanced. The growth inhibition rate of SCG-7901 cells currently ranges from 34.7% to 63.0%. Contents of the inventio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/72A61P35/00
Inventor 张留记屠万倩侯惠鸣李向阳
Owner THE CHINESE TRADITIONAL HERB MEDICINE RES INST HENAN PROV
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