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Process for preparing kaempferol derivatives

A technology of kaempferol and derivatives, which is applied in the field of preparing kaempferol derivatives, and can solve the problems of high production cost

Inactive Publication Date: 2005-06-22
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The raw material used in the existing preparation method is Hefei safflower whose appearance and properties of the medicinal material meet the requirements of the Pharmacopoeia (see the invention patent with application number 02137548.8 for details), but in the raw material, kaempferol-3-O-rutinoside, kaempferol-3-O- The content of glucoside is on the low side, and the total yield of both is no more than 0.5%, so the production cost is higher
According to the Pharmacopoeia, the safflower medicinal material "is the dried flower of Carthamus tinctorius L. of Compositae, which is picked when it changes from yellow to red in summer, and dried in the shade or in the sun" (see the 2000 edition of "The Pharmacopoeia of the People's Republic of China" for details). It can be seen that the flower color is The white or light yellow flowers of Compositae safflower have not been used as safflower medicinal materials. In fact, so far, there have been no reports of using them as raw materials to extract kaempferol derivatives

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0006] Example 1 Preparation of kaempferol derivatives kaempferol-3-O-glucoside and / or kaempferol-3-O-rutinoside using white flowers.

[0007] Take 1.8 kg of dry white flowers of safflower of Compositae, infiltrate it with 9L of 70% ethanol for 12 hours and then percolate and extract. Collect 30 times the amount of percolate, which is the extract; the extract is used to recover the ethanol under reduced pressure with a rotating film concentrator After that, it is the upper column sample liquid; the sample liquid is passed into a chromatographic column equipped with a macroporous resin (SIP-905, Shanghai Institute of Pharmaceutical Industry) according to 0.3 times the column volume of the sample, and 8 times the amount is used in turn Elute with water, 6 times the amount of 30% ethanol, 10 times the amount of 95% ethanol; collect the 30% ethanol elution fraction; the 30% ethanol eluate is concentrated under reduced pressure until there is no alcohol smell, stand for 12 hours, and f...

Embodiment 2

[0012] Example 2 Kaempferol-3-O-rutinoside and / or kaempferol-3-O-glucoside were prepared from pale yellow flowers.

[0013] Take 2.0 kg of dry light yellow flowers of safflower of Compositae, heat and extract with 20L of 70% ethanol for 3 hours, filter, collect the filtrate, add the remaining residue to 20L of 70% ethanol, heat to extract, filter, and collect the filtrate; combine the 2 filtrates , It is the extract; the extract is applied to the rotating thin film concentrator to recover the ethanol under reduced pressure, and then it is the upper column sample solution. The sample solution is passed into the sample solution containing polyamide powder (30-60 mesh, 30-60 mesh, 0.3 times the column volume). The chromatographic column of Luqiao Sijia Biochemical Plastic Factory, Taizhou City, was eluted with 10 times the amount of water, 20 times the amount of 5% ethanol, 15 times the amount of 50% ethanol, and 10 times the amount of 95% ethanol in sequence. Collect 20 times the 5%...

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PUM

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Abstract

The invention provides a novel process for preparing Kacmpferol derivative, i.e. Kacmpferol-3-0-rutinose glycoside and Kacmpferol-3-0-glucose glycoside monomer or their mixture by using the white flowers or light-yellow flowers of Carthamus tinctorius L. as raw material, extracting with water or water-containing ethanol, and isolating and purifying through microporous resin and silica gel column chromatography.

Description

Technical field [0001] The present invention relates to the technical field of medicine, in particular to a new method for preparing kaempferol derivatives. The kaempferol derivatives mentioned here refer to kaempferol-3-O-rutinoside and kaempferol-3-O-glucoside. Background technique [0002] Kaempferol derivatives kaempferol-3-O-rutinoside and kaempferol-3-O-glucoside are effective ingredients for the prevention and treatment of cardiovascular and cerebrovascular diseases. According to reports, kaempferol derivatives can also relieve pain, promote skin pigmentation, Anti-allergic and other activities. The raw material used in the existing preparation method is Hefei safflower whose appearance and properties meet the requirements of the pharmacopoeia (see the invention patent application number 02137548.8 for details), but the raw material contains kaempferol-3-O-rutinoside and kaempferol-3-O- The content of glucoside is low, and the total yield of b...

Claims

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Application Information

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IPC IPC(8): C07H1/08C07H17/07
Inventor 郭美丽张戈
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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