Method for obtaining anhydroicaritin from icariin by adopting naringinase

A technology of icariin and icariin, which is applied in the field of obtaining icariin by naringinase reaction, can solve the problems of low aglycone content and low yield, and achieve the improvement of pharmacological activity, Improve the conversion rate and reduce the effect of difficulty

Inactive Publication Date: 2015-04-29
山东大学(威海)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the content of aglycone or low aglycone i

Method used

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  • Method for obtaining anhydroicaritin from icariin by adopting naringinase
  • Method for obtaining anhydroicaritin from icariin by adopting naringinase
  • Method for obtaining anhydroicaritin from icariin by adopting naringinase

Examples

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Example Embodiment

[0021] Example 1: In a 1000mL conical flask, add 10mg icariin standard substance and 400ml 30% ethanol aqueous solution, adjust the pH value to 4.0 with 1M NaOH solution, the system reaches a certain temperature of 50 ° C, and then add 0.5g naringinase (standard activity). 475AGUPg), and finally, the reaction was stirred for 30 hours at 50°C, 200 rpm. After the reaction, extract with the same volume of ethyl acetate to remove the impurities of carbohydrates and enzymes and proteins. The extract was developed with G silica gel plate (100mm×25mm), chloroform:methanol=8:2 as the mobile phase, under 245nm ultraviolet light. The following observation and qualitative analysis were carried out by TLC, and the results were as follows figure 1 shown (1.R f淫羊藿苷标准品 =0.50,

[0022] 2. R f反应产物 = 0.8), the reaction product R f The value 0.8 is much larger than the standard R f A value of 0.5 indicates that icariin, which is less polar than icariin, is produced by an enzymatic reaction,...

Example Embodiment

[0025] Example 2: In a 1000ml conical flask, add 10mg icariin standard substance and 400ml 40% ethanol aqueous solution, adjust the pH value to 4.0 with 1M NaOH solution, the system reaches a certain temperature of 50 ° C, and then add 0.5g naringinase (standard activity). 475AGUPg), and finally, the reaction was stirred for 30 hours at 50°C, 200 rpm. After the reaction, extract with the same volume of ethyl acetate to remove impurities of carbohydrates and enzymes and proteins. The extract was developed with G silica gel plate (100mm×25mm), chloroform:methanol:water=7.5:2.5:0.25 as mobile phase, Observation under 245nm ultraviolet light and qualitative analysis by TLC, the results are as follows figure 2 shown (R f淫羊藿苷标准品 =0.42, 2.R f反应产物 ==0.8) Reaction product R f The value 0.8 is much larger than the standard R f A value of 0.42 indicates that icariin, which is less polar than icariin, is produced by an enzymatic reaction, and the reaction mechanism is the same as in ...

Example Embodiment

[0026] Example 3: In a 1000ml conical flask, add 10mg icariin standard substance and 400ml 30% ethanol aqueous solution, adjust the pH value to 6.0 with 1M NaOH solution, the system reaches a certain temperature of 60°C, and then add 0.5g naringinase (standard activity). 475AGUPg), and finally, the reaction was stirred for 30 hours at 60°C, 200 rpm. After the reaction, extract with the same volume of ethyl acetate to remove impurities of carbohydrates and enzymes and proteins. The extract was developed with G silica gel plate (100mm×25mm), chloroform:methanol:water=7.5:2.5:0.25 as mobile phase, Observation under 245nm ultraviolet light and qualitative analysis by TLC, the results are as follows figure 2 shown (R f淫羊藿苷标准品 =0.42, 2.R f反应产物 =0.8) Reaction product R f The value 0.8 is much larger than the standard R f A value of 0.42 indicates that icariin, which is less polar than icariin, is produced by an enzymatic reaction, and the reaction mechanism is the same as in Exa...

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Abstract

The invention relates to a method for converting icariin to anhydroicaritin by biological enzyme reaction so as to improve the biological activity. Under the action of naringinase, the reaction is performed in an ethanol water solution with the concentration of 30%-70%. The reaction temperature is 40-70 DEG C, and the reaction time is 1-30h. A glycosyl group on a hydroxyl group of icariin is cut off, and then icariin is converted to anhydroicaritin with higher pharmacological activity. By adopting the method provided by the invention, the processability of icariin is improved, and meanwhile, the actual application range can be expanded.

Description

technical field [0001] The invention relates to a method for converting icariin into icariin, in particular to a method for obtaining icariin by naringinase reaction. Background technique [0002] Icariin (Icratin) molecular formula is C 33 h 40 o 15 , the chemical structure is as shown. Pale yellow needle crystal. [0003] [0004] Icariin is derived from natural products. The natural active substances icariin and icariin have great development value. At present, icariin and icariin are mostly used in the clinical treatment of cardiovascular diseases. [0005] Icariin can significantly inhibit myocardial contractility and reduce the rate of increase of left ventricular pressure, indicating that it can reduce myocardial oxygen consumption, while reducing peripheral resistance, reducing cardiac afterload, and has therapeutic effects on cardiovascular diseases such as myocardial ischemia and arrhythmia. Improvement effect. [0006] Icariin has obvious effects on t...

Claims

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Application Information

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IPC IPC(8): C12P17/18
Inventor 许明淑陆波卢珊
Owner 山东大学(威海)
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