Method of preparing anhydroicaritin from icariin by using naringinase

A technology of icariin and icariin is applied in the field of obtaining icariin by naringinase reaction, which can solve the problems of low yield and low content of low glycoside, and achieves the improvement of conversion rate and high Pharmacological activity, effect of expanding processability and practical application range

Inactive Publication Date: 2012-05-16
许明淑 +2
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  • 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 of preparing anhydroicaritin from icariin by using naringinase
  • Method of preparing anhydroicaritin from icariin by using naringinase
  • Method of preparing anhydroicaritin from icariin by using naringinase

Examples

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example 1

[0024] Example 1: In 1000mL Erlenmeyer flask, add 10mg icariin standard substance and 400ml30% ethanol aqueous solution, adjust pH value to 4.0 with 1M NaOH solution, system reaches certain temperature 50 ℃, then add 0.5g naringinase (standard activity 475AGUPg), and finally, at 50° C. and 200 rpm, the reaction was stirred for 30 hours. After the reaction was completed, extract with the same volume of ethyl acetate to remove carbohydrates and enzyme protein impurities. The extract was developed on a G silica gel plate (100mm×25mm), with chloroform:methanol=8:2 as the mobile phase, and developed under 245nm ultraviolet light Observed below and carried out qualitative analysis with TLC, the results are as follows figure 1 Shown (1.R f淫羊藿苷标准品 =0.50, 2.R f淫羊藿苷元 =0.8), the reaction product R f The value 0.8 is much larger than the standard R f A value of 0.5 shows that the polarity of icariin less than icariin has been produced by the enzymatic reaction, and the reaction mecha...

example 2

[0027] Example 2: In a 1000ml Erlenmeyer flask, add 10mg icariin standard substance and 400ml40% ethanol aqueous solution, adjust the pH value to 4.0 with 1M NaOH solution, and the system reaches a certain temperature of 50°C, then add 0.5g naringinase (standard activity 475AGUPg), and finally, at 50° C. and 200 rpm, the reaction was stirred for 30 hours. After the reaction, extract with the same volume of ethyl acetate to remove carbohydrates and enzyme protein impurities. The extract is developed on a G silica gel plate (100mm×25mm), and chloroform:methanol:water=7.5:2.5:0.25 is the mobile phase. Observe under 245nm ultraviolet light and carry out qualitative analysis with TLC, the result is as follows figure 2 Shown (R f淫羊藿苷标准品 =0.42, 2.R f淫羊藿苷元 =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 the enzymatic reaction, and the reaction mechanism is the sa...

example 3

[0028] Example 3: In a 1000ml Erlenmeyer flask, add 10mg icariin standard substance and 400ml30% ethanol aqueous solution, adjust the pH value to 6.0 with 1M NaOH solution, and the system reaches a certain temperature of 60°C, then add 0.5g naringinase (standard activity 475AGUPg), and finally, at 60° C. and 200 rpm, the reaction was stirred for 30 hours. After the reaction, extract with the same volume of ethyl acetate to remove carbohydrates and enzyme protein impurities. The extract is developed on a G silica gel plate (100mm×25mm), and chloroform:methanol:water=7.5:2.5:0.25 is the mobile phase. Observe under 245nm ultraviolet light and carry out qualitative analysis with TLC, the result is as follows figure 2 Shown (R f淫羊藿苷标准品 =0.42, 2.R f淫羊藿苷元 =0.8) Reaction product R f The value 0.8 is much larger than the standard R f A value of 0.42 shows that icariin, which is less polar than icariin, has been produced by the enzymatic reaction, and the reaction mechanism is the ...

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Abstract

The invention provides a method of converting icariin into anhydroicaritin by using a biological enzyme reaction so as to improve biological activity of icariin. According to the invention, under the action of naringinase, a reaction is carried out in an ethanol aqueous solution with a concentration of 30% to 70%, wherein, reaction temperature is 40 to 70 DEG C and reaction time is 1 to 30 h; glycosyl groups on hydroxy groups of icariin are cut off, and icariin is converted into anhydroicaritin with higher pharmacological activity; furthermore, machinability of icariin is improved, and the practical application scope of icariin can be enlarged.

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] The molecular formula of icariin is C 33 h 40 o 15 , the chemical structural formula is as shown in formula I. Pale yellow needle crystal. [0003] [0004] (Formula I) [0005] 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. [0006] 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. ...

Claims

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Application Information

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IPC IPC(8): C12P17/06
Inventor 许明淑赵无恙张丽娟
Owner 许明淑
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