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Process for preparing genistein

A technology of genistein and genistein, applied in the field of medicine, can solve problems such as affecting purity or yield, unsuitable use, adding steps of degreasing and recovering alcohol, etc.

Active Publication Date: 2019-03-08
西安蓝绿卓生物科技有限公司
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Problems solved by technology

[0007] 3. Genistein and cancer
[0016] Considering that genistein has extremely high clinical application value, its preparation process has become a hot research direction in this field. For example, Chinese patent ZL02123450.7 discloses a preparation process of genistein, which solves the problem of preparing a large number of high-purity dyes. The difficult problem of lignin makes the wide application of genistein possible; but it has the following technical defects: (1) the process "firstly, the plant meal is extracted with alcohol reflux", and alcohol is also extracted when extracting sophorin Fat is added, and the steps of degreasing and alcohol recovery are added. In addition, the relative cost of alcohol extraction is high; (2) the process "Secondly, concentrate and recover alcohol to prepare extract, add water to precipitate, wash away the water-soluble impurities in the precipitate, and collect Precipitation", the extract is difficult to dissolve, and it needs to be dissolved in heated water. If it is not handled properly, the purity or yield will be affected; (3) the process "Then, the precipitate is refluxed with an organic solvent to degrease, and the precipitate is washed with water, and crystallized with alcohol , collect precipitation ", " the organic solvent of reflux degreasing is chloroform or ether or its mixture, preferred chloroform "
According to the International Conference on Harmonization of Technical Requirements for Registration of Drugs for Human Use (ICH) common organic solvent classification and residue limit standards, chloroform is a second-class solvent (referring to solvents that are non-genotoxic but carcinogenic to animals), and should not be used in pharmaceuticals. Although it can be used Ethyl acetate instead, but the residues in the genistein API must be tested
The extensive use of chloroform also affects environmental protection (environmental protection requirements were established when the pharmaceutical factory was built), and the organic solvent reflux degreasing technology has affected the application of genistein raw materials
In addition, alcohol extraction and organic solvent degreasing also increase the production cost

Method used

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Experimental program
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preparation example Construction

[0078] The preparation process of genistein (taking Sophora japonicus as an example):

[0079] Sophoside is connected with a glucose at the 4' position of genistein to form glucoside, so it is also called genistein-4-glucoside. The English name is Sophoricoside. Because it has one more glucose than genistein, its water solubility is larger than that of genistein.

[0080] In the extraction of sophorin, in order to prevent a large amount of plant protein from being extracted and affect the subsequent separation in the original process, high-alcohol extraction is used to denature the protein, but there will be a large amount of lipids in the high-alcohol extraction, which needs to be degreased. Affecting environmental protection, now we use the characteristics of genistin to be easily soluble in alkaline hot water to extract genistin with pH 6-9.5 alkaline water thermal reflux, and according to the characteristics of poor water solubility of sophorin and genistein, water is used...

Embodiment 1

[0085] Example 1. An improved process for preparing genistein by acid hydrolysis after extraction of sophorin and purification (flow chart see figure 1 )

[0086] One, the preparation of sophorin:

[0087] 1. Screening and processing of Huaijiao to obtain Huaijiao and beans;

[0088] Sophora japonicus washing and drying: Sieve the collected sophora japonicus, pick out the branches and other sundries, quickly rinse with water to remove the sediment, and dry (80°C-90°C).

[0089] 2. Weigh 200g Sophora japonica, add distilled water according to the ratio of material to liquid (weight to volume ratio) 1:4, adjust the pH to 9 with 3mol sodium hydroxide, and carry out reflux extraction; the temperature is 96°C-99°C, and the extraction time is 2.5 hours. The final volume is 195ml, and the specific gravity is 1.04g / ml by density meter.

[0090] The second reflux extraction was carried out according to the ratio of solid to liquid 1:3; the temperature was 96°C-99°C, the extraction t...

Embodiment 2

[0101] Example 2. Factory-level experimental research on the improved process of extracting sophorin and preparing genistein by acid hydrolysis after purification

[0102] One, the preparation of sophorin:

[0103] 1. Purchase 500 kilograms of Sophora japonica treated, feed 200 kilograms, and use plant extraction tank 3T (manufactured by Hongda Phytoextraction Factory, Sanyuan County, Shaanxi Province) in the factory, and the extraction scheme is carried out according to the scheme in Example 1.

[0104] 2. Combine about 1.5 tons of the three extracts, and measure the specific gravity to 1.02g / ml.

[0105]3. Take 100 kg of the above extract and dilute it at a volume ratio of 1:5, adjust the pH to about 4.5, let it settle naturally and pour the supernatant, collect 700 g of the precipitate by centrifugation in the factory, dry 357 g, and detect it as genistein and sophora japonicus by HPLC Glycoside mixture, wherein sophorin is 9.83%, and genistein is 86.63%. HPLC analysis ch...

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Abstract

The invention relates to a process for preparing genistein. The process is characterized by: directly using an inorganic solvent to extract dye wood glucoside (sophoricoside), and performing acid hydrolysis after precipitation and purification to generate genistein or using the inorganic solvent to extract a sophoricoside mixture, then directly performing acid hydrolysis to generate genistein, andpurifying. Two improving processes are characterized in that steps of alcohol extraction and degreasing through organic solvents like trichloromethane (chloroform), ethyl ether and ethyl acetate areomitted, so that environment protection is facilitated, the steps are simplified, cost is saved, yield is increased, and the process is suitable for mass production. The genistein prepared by the process can be applied in preventing and treating osteoporosis, female climacteric syndrome, tumor and cardiovascular and cerebrovascular disease and resisting radiation and belongs to the field of drum preparation and drug treatment.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to a process for preparing genistein. Background technique [0002] Research literature shows that genistein can bidirectionally regulate estrogen levels in the body and selectively bind to estrogen receptors. Clinical pharmacological application research mainly includes: [0003] 1. Genistein and cardiovascular disease [0004] Genistein plays a very important role in reducing the incidence of cardiovascular diseases. Low-density lipoprotein cholesterol in the blood is high and easily oxidized, which can cause atherosclerosis. Genistein can effectively reduce cholesterol through anti-oxidation, inhibit the oxidation of low-density lipoprotein cholesterol (LDL), and make LDL in the blood Keep the level low, improve the abnormal state of peroxidation in the body caused by high fat, and alleviate the peroxidation damage to the body. Genistein can up-regulate LDL recep...

Claims

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Application Information

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IPC IPC(8): C07D311/36
CPCC07D311/36
Inventor 王增禄李涛刘永艳
Owner 西安蓝绿卓生物科技有限公司
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