Ilicis routundae cortex derivants and application thereof in preparing medicament capable of resisting tumors

An anti-tumor drug and a salvage acid technology, which is applied in the field of preparation of salvage acid derivatives, can solve the problems of no discovery of salvage acid and salvage acid derivatives, such as reports on the application of anti-tumor drugs

Inactive Publication Date: 2011-07-20
赵全成
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Before the completion of the present invention, there was no bibliographical report that the derivatives of basic acid and basic acid have the effect of inhibitin

Method used

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  • Ilicis routundae cortex derivants and application thereof in preparing medicament capable of resisting tumors
  • Ilicis routundae cortex derivants and application thereof in preparing medicament capable of resisting tumors
  • Ilicis routundae cortex derivants and application thereof in preparing medicament capable of resisting tumors

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0038] Preparation of 3β,19α,24-trihydroxy-ursane-12-ene-28-carboxylic acid (compound 1):

[0039] The medicinal materials are refluxed with 70% ethanol for 3 times, 2 hours each time, the extracts are combined, and the volume of the extract is 2% medicinal activated carbon, filtered, and the filtrate is concentrated to contain 1g medicinal materials per 1ml; add 1mol / l sodium hydroxide 2 times the amount of the solution, hydrolyze at 100°C for 4 hours, let it cool, adjust the pH to 3 with hydrochloric acid, filter, discard the hydrolysate, wash the filter cake with deionized water until it is neutral, and then heat it with 85% ethanol to boiling. Add 1% of the medicinal liquid volume of medicinal activated carbon, filter while hot, the filtrate is concentrated under reduced pressure and recovered to no alcohol, add water to 1g of medicinal materials per 1ml, place, filter, wash, dry, and recrystallize twice to get Compound 1 (Molecular Formula C 30 H 48 O 5 , The molecular weigh...

example 2

[0041] Preparation of 3β,19α-Diacetoxy-24-hydroxy-ursane-12-ene-28-carboxylic acid (compound 2):

[0042] Take 5g of compound 1, add 200ml of pyridine, 100ml of acetic anhydride, stir at 80℃, check the end of the reaction by TLC, after the reaction is complete, recover the reaction solvent, add water to 250ml, adjust the pH to 5 with dilute hydrochloric acid, filter, and wash the filter cake with water To colorless, dissolve with 250ml ethyl acetate, wash twice with water, 100ml each time, and then wash 3 times with 10% sodium carbonate, 100ml each time, then wash once with 100ml 1mol / l hydrochloric acid, and finally wash 2 times with water Each time, 100ml each time, recover the ethyl acetate to dryness, add 300ml of ethanol to heat to dissolve, add 1g of activated carbon, stir evenly, filter, and the filtrate to recover ethanol to 50ml, place, crystallize and filter to obtain compound 2 (molecular formula C 34 H 52 O 7 , The molecular weight is 572.74). The solid is 4.1 g. Whi...

example 3

[0044] Preparation of 3β,19α-Disuccinyloxy-24-hydroxy-ursane-12-ene-28-carboxylic acid (compound 4):

[0045] Take 5g of compound 1, 8g of succinic anhydride, 100ml of pyridine, stir to dissolve, slowly heat to 110°C, stir the reaction, check the end of the reaction by TLC, after the reaction is completed, put it to room temperature, add 100ml of ice water, use hydrochloric acid ice water mixture Adjust the PH value, filter, wash the filter residue with water until it is colorless, heat it with 300ml ethanol to dissolve it, add water to 1000ml, filter, and then heat the filter residue with 500ml 95% ethanol to dissolve, add 2g activated carbon, stir evenly, filter, and recover ethanol to 200ml from the filtrate , Add 200ml of water, concentrate, place, crystallize, and filter to obtain compound 4 (molecular formula C 38 H 56 O 11 , The molecular weight is 688.80). The solid is 7.1 g. White powder, mp: 244.4~246.4℃; IR(KBr)cm -1 : 1169, 1216~1273, 1714; NMR: characteristic chemic...

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Abstract

The invention discloses Ilicis routundae cortex derivants and an application thereof in preparing a medicament capable of resisting tumors. Ilicis routundae cortex acid is obtained by extracting, separating and purifying traditional Chinese medicine Ilicis routundae cortex to serve as a lead compound; the lead compound is subjected to corresponding chemical reaction to prepare a series of derivants. The pharmacological test proves that the Ilicis routundae cortex derivants have the function of resisting tumor activity and have inhibition action on prostatic cancer cells, lung cancer cells, liver cancer cells, cervical cancer cells and gastric cancer cells; and the inhibiting effects on the tumor cells by the derivants are superior to that of parent nucleus Ilicis routundae cortex.

Description

Technical field [0001] The invention relates to a method for preparing a derivative of salvage acid obtained from natural Chinese medicine. To be precise, a series of derivatives are prepared with chemical components extracted from traditional Chinese medicine as the lead compound, and the structure is structured with anti-tumor activity as an indicator Modification belongs to the field of medicine. Background technique [0002] Salvage acid is a pentacyclic triterpenoid compound obtained from the traditional Chinese medicine Ilicis routundae cortex through extraction, purification, separation, and alkali degradation. Our research has proved that salvage acid has the pharmacological activity of preventing and treating cardiovascular and cerebrovascular diseases (patent publication number: CN101856357A), and also has pharmacological effects such as lowering blood lipids (patent publication number: CN101849950A). According to literature reports, some pentacyclic triterpenoids, suc...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P35/00
Inventor 赫玉芳赵全成南敏伦王化录马吉胜赵昱玮王莲萍
Owner 赵全成
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