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Method for preparing catalpol and derivative thereof based on radix rehmanniae praeparata and application

A derivative, the technology of catalpol, applied in the field of medicine, can solve the problems of acid resistance, poor alkalinity, unstable chemical properties and limitations of catalpol, and achieve the effect of less drug dosage, good analgesic effect and good analgesic effect

Pending Publication Date: 2021-01-08
河北仁心药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Catalpol has extremely unstable chemical properties, and its resistance to acid and alkali is poor, and heat can decompose catalpol, so its application is limited.

Method used

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  • Method for preparing catalpol and derivative thereof based on radix rehmanniae praeparata and application
  • Method for preparing catalpol and derivative thereof based on radix rehmanniae praeparata and application
  • Method for preparing catalpol and derivative thereof based on radix rehmanniae praeparata and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] A preparation method of catalpol derivatives,

[0045] Preparation of Rehmannia glutinosa: Soak rehmannia glutinosa in distilled water at 25°C for 1 hour, transfer to a pressure cooker, steam for 0.5 hour at a pressure of 0.22 MPa and a temperature of 120°C, and dry to obtain Rehmannia glutinosa.

[0046] Catalpol extraction: Add Rehmannia glutinosa to ethanol solution, crush the homogenate in a homogenizer, stir at 30°C for 1 hour, filter with four layers of gauze, squeeze dry, extract the residue twice under the same conditions, and combine the extracts , to remove ethanol by rotary evaporation to obtain the crude extract of rehmannia glutinosa; separate and purify the crude extract of rehmannia glutinosa on macroporous adsorption resin and silica gel column to obtain a catalpol solution, and crystallize through methanol-ethanol to obtain solid catalpol powder; The addition amount is 200wt% of the ethanol solution, and the mass fraction of the ethanol solution is 95wt...

Embodiment 2

[0057] A preparation method of catalpol derivatives,

[0058] Preparation of Rehmannia glutinosa: Soak rehmannia glutinosa in distilled water at 25°C for 1 hour, transfer to a pressure cooker, steam for 0.5 hour at a pressure of 0.22 MPa and a temperature of 120°C, and dry to obtain Rehmannia glutinosa.

[0059] Catalpol extraction: Add Rehmannia glutinosa to ethanol solution, crush the homogenate in a homogenizer, stir at 30°C for 1 hour, filter with four layers of gauze, squeeze dry, extract the residue twice under the same conditions, and combine the extracts , to remove ethanol by rotary evaporation to obtain the crude extract of rehmannia glutinosa; separate and purify the crude extract of rehmannia glutinosa on macroporous adsorption resin and silica gel column to obtain a catalpol solution, and crystallize through methanol-ethanol to obtain solid catalpol powder; The addition amount is 200wt% of the ethanol solution, and the mass fraction of the ethanol solution is 95wt...

Embodiment 3

[0070] A kind of preparation method of caffeamide (threonine) compound,

[0071] Preparation of caffeamide compound: under nitrogen protection, mix caffeic acid and tetrahydrofuran, add N-methylmorpholine and isobutyl chloroformate at 0°C for 30 minutes, add silk amino acid, add 4-di-n-propylaminopiperidine Pyridine was also kept at a temperature of 0°C for 2 hours, and then reacted at a temperature of 30°C for 9 hours. After the reaction was completed, it was concentrated under reduced pressure, extracted with ethyl acetate, washed with citric acid solution, and then washed with sodium chloride solution. Drying over sodium sulfate in water, and finally obtain caffeamide (threonine) compound (yield 56.28%) through silica gel column chromatography and rotary evaporation; the addition of tetrahydrofuran is 1.5wt% of caffeic acid, and the addition of N-methylmorpholine Amount is 0.9wt% of caffeic acid, the addition of isobutyl chloroformate is 1.3wt% of caffeic acid, the addition...

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Abstract

The invention discloses a method for preparing catalpol and a derivative thereof based on radix rehmanniae praeparata and application, and belongs to the technical field of medicines. According to themethod, the catalpol derivative is prepared by reacting a caffeic imide compound with the catalpol in anhydrous acetonitrile, wherein the caffeic imide compound is obtained by reacting caffeic acid with amino acids; and the amino acids include serine and threonine. The catalpol derivative obtained by the method has a blood sugar reducing effect, and the dosage of the catalpol derivative is smallwhile the same blood sugar reducing effect is achieved; moreover, the catalpol derivative has no toxicity to cells, and does not influence cell proliferation; moreover, the catalpol derivative has theeffect of improving the activity of tyrosinase, so that the activity of the tyrosinase at least reaches 140%; and the catalpol derivative also has a good analgesic effect, and the minimum mechanicalretraction threshold value reaches 35g.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method and application for preparing catalpol and its derivatives based on rehmannia glutinosa. Background technique [0002] The chemical composition of Rehmannia glutinosa is mainly glycosides, among which iridoid glycosides such as catalpol are the main ones. Glycosides that have been isolated and identified from fresh rehmannia and dried rehmannia include: catalpol, dihydrocatalpol, acetyl catalpol, motherwort glycoside, aucubin, monomelite glycoside, melitrol glycoside, dehydroxygardenia Glycosides, Glycosides, Echinitin, Rehmanthin A, B, C, D, and carotene, etc. [0003] Catalpol has strong pharmacological activity. Studies have shown that it has anti-tumor, anti-apoptosis, and anti-diabetic effects. It can pass through the blood-brain barrier and has various neuroprotective effects such as anti-inflammation and anti-oxidation on the central nervous system. ...

Claims

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Application Information

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IPC IPC(8): C07H17/04C07H1/00A61P3/10A61P29/00
CPCC07H17/04C07H1/00A61P3/10A61P29/00
Inventor 解伟松邢鹏程李炜
Owner 河北仁心药业有限公司
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