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Process for the separation and preparation of 4'-demethyl podophyllic acid

A technology for demethylation of epipodophyllin and substrates, applied in the field of biopharmaceuticals, can solve problems such as poor selectivity, easy pollution of the environment, and low reaction yield, and achieve the effects of simple operation, environmental friendliness, and simple separation methods

Inactive Publication Date: 2009-07-29
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the problems of poor selectivity, low reaction yield and easy pollution of the environment in the process of preparing 4'-desmethyl epipodophyllic acid in the prior art, and to provide a new 4' -The preparation and separation method of demethyl epipodophyllotoxin, the method uses 4'-demethyl epipodophyllotoxin as a reaction substrate, and obtains 4'-demethyl epipodophyllotoxin through a biotransformation method, the present invention The method is simple to operate, has strong reaction selectivity, is environmentally friendly, and has low production cost

Method used

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  • Process for the separation and preparation of 4'-demethyl podophyllic acid
  • Process for the separation and preparation of 4'-demethyl podophyllic acid
  • Process for the separation and preparation of 4'-demethyl podophyllic acid

Examples

Experimental program
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Effect test

Embodiment 1

[0044] 1. Cultivation of Clostridium:

[0045] Slope culture: culture medium: glucose 2%, beef extract 0.3%, peptone 0.5%, sodium chloride 0.5%, agar 2%, pH value 7.0, sterilized at 115 degrees Celsius for 30 minutes, cooled after sterilization, and prepared Inclined surface, inoculated with Clostridium sp., cultured at 37°C for 6 hours;

[0046] Liquid seed culture: medium: yeast powder 0.5%, peptone 0.5%, sodium chloride 0.5%, pH value 7.0, liquid volume is 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes, cooled, and inoculated on the slant Bacteria, cultivated at 37 degrees Celsius and 180 rpm for 4 hours, as liquid seeds;

[0047] Preparation of fermentation broth: medium is 1% sucrose, 0.5% yeast powder, 0.5% peptone, 0.5% sodium chloride, pH value is 7.0, liquid volume is 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes , cooled, inoculated with liquid seeds, the inoculum size was 10%, and cultivated for 3 hours at 3...

Embodiment 2

[0053] 1. Culture of Pseudomonas aeruginosa

[0054] Inclined surface strain culture: culture medium: beef extract 0.3%, peptone 0.5%, sodium chloride 0.5%, agar 2%, pH value 7.0, sterilized at 115 degrees Celsius for 30 minutes, cooled, made into inclined surface, and inoculated with Pseudomonas aeruginosa Bacterial strains, cultivated at 37 degrees Celsius for 12 hours;

[0055] Liquid seed culture: medium: beef extract 0.3%, peptone 0.5%, sodium chloride 0.5%, pH value 7, liquid volume 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes, cooled after sterilization, Inoculate the slant bacteria, cultivate for 10 hours at 37 degrees Celsius and 200 rpm, as liquid seeds;

[0056] Fermentation culture: medium: beef extract 0.3%, peptone 0.5%, sodium chloride 0.5%, pH value 7, liquid volume 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes, cooled and inoculated after sterilization Liquid seeds, inoculum size 10%, cultivated for ...

Embodiment 3

[0062] 1. Cultivation of Rhodococcus erythropolis:

[0063] Slope culture: medium: beef extract 0.3%, peptone 1.0%, sodium chloride 0.5%, agar 1.5%, pH value 7.0, sterilized at 115 degrees Celsius for 30 minutes, cooled after sterilization, made into a slope, inoculated with red Rhodococcus strains, cultivated at 30 degrees Celsius for 12 hours;

[0064] Liquid seed culture: medium: beef extract 0.3%, peptone 1.0%, sodium chloride 0.5%, pH value 7.0, liquid volume 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes, cooled after sterilization, Inoculate the slant seeds, and cultivate them for 10 hours at 30 degrees Celsius and 180 rpm, as liquid seeds;

[0065] Fermentation culture: beef extract 0.3%, peptone 1.0%, sodium chloride 0.5%, pH value 7.0, liquid volume 50 ml / 250 ml shake flask, sterilized at 115 degrees Celsius for 30 minutes, cooled after sterilization, and inoculated with liquid seeds, The inoculum was 2%, cultured at 30°C, 180 rpm for 10...

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Abstract

The invention discloses a method for converting 4'- demethylpodophyllotoxin to 4'- demethylation epipodophyllic acid, comprising the following steps: the 4'- demethylpodophyllotoxin solution is added during the fermentation process of microorganism clostridium, pseudomonas aeruginosa, rhodococcus erythropolis, corynebacterium pekinense, hay bacillus, erwinia uredovora, bacillus or bending pseudomonas for carrying out biotransformation reaction, thus obtaining biotransformation matrix with the 4'-demethylation epipodophyllic acid. The invention also discloses a method for separating the 4'-demethylation epipodophyllic acid from the biotransformation matrix, comprising the following steps: the macroporous absorbent resin column is adopted to carry out initial separation on the biotransformation matrix and gel column chromatography is adopted to carry out fine separation, thus obtaining 4'-demethylation epipodophyllic acid. In the invention, modification is carried out on the 4'- demethylpodophyllotoxin structure by biotransformation, thus obtaining 4'-demethylation epipodophyllic acid, in addition, the reaction selectivity is high, the operation is easy, the reaction conditions are moderate, the generated waste is little, the separation process is simple and the yield is high.

Description

technical field [0001] The present invention relates to the preparation method of podophylloid lignans, in particular to a method for converting 4'-demethylepipodophyllotoxin into 4'-demethylepipodophylloic acid. The invention discloses a method for separating 4'-desmethyl epipodophyllic acid from a biotransformation matrix, belonging to the field of biopharmaceuticals. Background technique [0002] 4'-Demethylated epipodophyllotoxin is a derivative obtained by demethylating the E-4' position of podophyllotoxin. It is different from podophyllotoxin by destroying tubulin assembly and microtubule formation during cell mitosis. 4'- Demethyl epipodophyllotoxin exerts anti-tumor effect by inhibiting the activity of DNA topoisomerase II, and its activity is significantly stronger than that of podophyllotoxin. Because of its similar structure to conventional chemotherapy drugs etoposide and teniposide, their derivatives are more likely to become drugs with significant anti-tumor a...

Claims

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Application Information

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IPC IPC(8): C12P17/04C07D493/04C12R1/145C12R1/385C12R1/01C12R1/125C12R1/15C12R1/07C12R1/18
Inventor 汤亚杰徐小玲李冬生
Owner HUBEI UNIV OF TECH
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