Method for converting podophyllinic acid lactone into podophyllic acid and picropodophyllin

A technology for podophyllotoxin and picropodophyllin, which is applied in biochemical equipment and methods, microorganism-based methods, organic chemistry and other directions, can solve the problems of easily polluted environment and low product yield, and achieves environmental friendliness and product yield. The effect of high rate and mild reaction conditions
CN101492704BInactive Publication Date: 2011-09-21HUBEI UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HUBEI UNIV OF TECH
Publication Date
2011-09-21
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for converting podophyllotoxin to podophyllic acid and picropodophyllin, comprising the following steps: the substrate podophyllotoxin solution is added during the fermentation process of microorganism pseudomonas aeruginosa, bacillus, rhodococcus erythropolis, clostridium, corynebacterium pekinense, hay bacillus, erwinia uredovora or bending pseudomonas for carrying out biotransformation reaction, thus obtaining biotransformation matrix with the podophyllic acid and picropodophyllin. The invention also discloses a method for separating the podophyllic acid and picropodophyllin from the obtained 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 respectively obtaining the picropodophyllin and the podophyllic acid. In the invention, modification is carried outon the picropodophyllin structure by microbiological transformation, thus obtaining the picropodophyllin and the podophyllic acid, in addition, the conversion rate of the substrate 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.
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Description

Technical field

[0001] The present invention relates to a method for preparing podophyllophyll lignans, in particular to a method for converting podophyllotoxin into podophyllic acid and picropodophyllin. The present invention also relates to the separation of podophyllophyllic acid and podophyllin from a biotransformation matrix The bitterness method belongs to the field of biopharmaceuticals. Background technique

[0002] Podophyllotoxin (Podophyllotoxin) is a natural active lead compound isolated from podophyllum plants with anti-tumor effect. It has a unique molecular structure, with four chiral centers, a trans-lactone ring and C-1 position. Axial contiguous aryl substituent groups. Podophyllotoxin disrupts the formation of tubulin and microtubules in mitotic cells, stops cell mitosis in M ​​phase, inhibits normal division of tumor cells, and exerts anti-tumor effects. However, it has strong side effects, such as water solubility. Poor sex and low bioavailability limit its...

Claims

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