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Novel scutellarin compounds and uses thereof

A technology of scutellarin and compounds, which is applied in the field of medicine, can solve the problems of reducing the efficacy of scutellarin, many adverse reactions, and poor water solubility of scutellarin

Inactive Publication Date: 2008-07-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to aim at the defects and deficiencies in the above-mentioned prior art, and to provide a method that can overcome the disadvantages of poor water solubility of scutellarin, difficulty in making injections by conventional methods, and many adverse reactions, without reducing the risk of scutellarin A new drug with the efficacy of B

Method used

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  • Novel scutellarin compounds and uses thereof
  • Novel scutellarin compounds and uses thereof
  • Novel scutellarin compounds and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: The preparation method of 4'-hydroxyethyl scutellarin

[0022] At 50°C, 10g of scutellarin, 10ml of water, and 0.86g of sodium hydroxide were added to the reaction flask, and nitrogen was introduced to remove oxygen; then, ethylene oxide was introduced to react for 5 hours. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl scutellarin. Dissolve the crude product of hydroxyethyl scutellarin in water, absorb it through a macroporous adsorption resin chromatographic column, and elute it with water, collect the water-eluted part, check it by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and wash with ethanol Dissolve, add activated carbon to decolorize, and recover the solvent. The content of 4'-hydroxyethyl scutellarin detected by HPLC was 75%.

Embodiment 2

[0023] Embodiment 2: the method for preparing 6-hydroxyethyl scutellarin

[0024] At 60°C, 10g of scutellarin, 10ml of water, and 0.9g of sodium hydroxide were added to the reaction flask, and nitrogen was introduced to remove oxygen; then, ethylene oxide was introduced to react for 5 hours. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl scutellarin. Dissolve the crude product of hydroxyethyl scutellarin in water, absorb it through a macroporous adsorption resin chromatographic column, and elute it with water, collect the water-eluted part, check it by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and wash with ethanol Dissolve, add activated carbon to decolorize, and recover the solvent. The content of 6-hydroxyethyl scutellarin detected by HPLC was 70%.

Embodiment 3

[0025] Embodiment 3: the method for preparing 4', 6-dihydroxyethyl scutellarin

[0026] At 65°C, add 10g of scutellarin, 10ml of water, and 1.6g of sodium hydroxide into the reaction flask, pass through nitrogen to remove oxygen; then pass through ethylene oxide, and react for 8 hours. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl scutellarin. Dissolve the crude product of hydroxyethyl scutellarin in water, absorb it through a macroporous adsorption resin chromatographic column, and elute it with water, collect the water-eluted part, check it by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and wash with ethanol Dissolve, add activated carbon to decolorize, and recover the solvent. The content of 4', 6-hydroxyethyl scutellarin detected by HPLC was 80%.

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Abstract

The invention belongs to a medicine technology field, relates to a new scutellarin compound and the application of the new scutellarin. The invention precisely relates to the new scutellarin compound for treating cardiocerebral vascular diseases. The general formula of the hydroxyethyl (hydroxypropyl or hydroxybutyl) scutellarin compound in the invention is (I), in which R4 is H or Alkyl; R1, R2 and R3 are hydroxyethyl (hydroxypropyl or hydroxybutyl) or H, among which at least one of R1, R2 and R3 is the hydroxyethyl (hydroxypropyl or hydroxybutyl). The new scutellarin compound is substantially used in the prevention and treatment of cardiocerebral vascular diseases, Alzheimer diseases, cerebral infarction, cerebral ischemia and other varied diseases caused by the cerebral ischemi, etc.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to new scutellarin compounds and applications thereof, in particular to new hydroxyethyl (propyl, butyl) scutellarin compounds and their effects in the prevention and treatment of cardiovascular and cerebrovascular diseases, senile dementia, and brain diseases. Infarction, cerebral ischemia and other various diseases caused by cerebral ischemia. Background technique [0002] Modern pharmacological studies have shown that scutellarin (the main ingredient is breviscapine) can reduce peripheral resistance, reduce myocardial oxygen consumption, promote collateral circulation, inhibit platelet aggregation, improve cardiovascular and cerebrovascular circulation, and increase cardiovascular and cerebrovascular blood flow. Clinically, it is mainly used to treat cerebral thrombosis, sequelae of cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease, angina pe...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61K31/7048A61P9/00A61P25/28A61P9/10
Inventor 裴月湖华会明白皎李占林苏兰
Owner SHENYANG PHARMA UNIVERSITY
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