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Novel scutellaria glycosides compounds and uses thereof

A technology of baicalin and compounds, which is applied in the field of medicine, can solve the problems of limited drug efficacy, low oral bioavailability of baicalin, and difficulty in injection, and achieve good water solubility

Inactive Publication Date: 2012-10-17
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the oral bioavailability of baicalin is low, and because of its low solubility in water, it is difficult to make injections, which limits its efficacy.

Method used

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  • Novel scutellaria glycosides compounds and uses thereof
  • Novel scutellaria glycosides compounds and uses thereof
  • Novel scutellaria glycosides compounds and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation method of 6-hydroxyethyl baicalin

[0021] At 80°C, add 111.5g of baicalin, 300ml of water, and 1.0g of sodium hydroxide into the reaction kettle, pass through nitrogen to remove oxygen; then pass through ethylene oxide, react for 12.0 hours, stop passing through ethylene oxide alkyl. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl baicalin. Dissolve the crude product of hydroxyethyl baicalin in water, after being adsorbed by a macroporous adsorption resin chromatographic column, elute with water, collect the water-eluted part, check by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and dissolve in ethanol , add activated carbon for decolorization, and recover the solvent. The content of 6-hydroxyethyl baicalin detected by HPLC was 50.3%.

Embodiment 2

[0022] Embodiment 2: the preparation method of 6-hydroxyethyl baicalin

[0023] At 80°C, add 111.5g of baicalin, 300ml of water, and 1.0g of sodium hydroxide into the reaction kettle, pass through nitrogen to remove oxygen; then pass through ethylene oxide, react for 10.0 hours, stop passing through ethylene oxide alkyl. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl baicalin. Dissolve the crude product of hydroxyethyl baicalin in water, after being adsorbed by a macroporous adsorption resin chromatographic column, elute with water, collect the water-eluted part, check by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and dissolve in ethanol , add activated carbon for decolorization, and recover the solvent. The content of 6-hydroxyethyl baicalin detected by HPLC was 63.4%.

Embodiment 3

[0024] Embodiment 3: the preparation method of 6-hydroxyethyl baicalin

[0025] At 70°C, add 111.5g of baicalin, 300ml of water, and 1.0g of sodium hydroxide into the reaction kettle, pass through nitrogen to remove oxygen; then pass through ethylene oxide, react for 10.0 hours, stop passing through ethylene oxide alkyl. Cool, filter, and concentrate the filtrate under reduced pressure to obtain the crude product of hydroxyethyl baicalin. Dissolve the crude product of hydroxyethyl baicalin in water, after being adsorbed by a macroporous adsorption resin chromatographic column, elute with water, collect the water-eluted part, check by thin-layer chromatography, combine the same fractions, concentrate to dryness under reduced pressure, and dissolve in ethanol , add activated carbon for decolorization, and recover the solvent. The content of 6-hydroxyethyl baicalin detected by HPLC was 64.2%.

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Abstract

The invention belongs to the medicine technology field, relates to a new baicalin compound and the application of the new baicalin compound, which precisely relates to the new baicalin compound of general formula (I) for treating cardiocerebral vascular diseases. The compound has excellent water solubility and can be conveniently made into water soluble injection or lyophilized powder for injection combining with acceptable carriers in the pharmacy, which is substantially used in the prevention and treatment of cardiocerebral vascular diseases, Alzheimer diseases, cerebral infarction, cerebral ischemia and other varied diseases caused by cerebral ischemia and so on. In the formula, R3 is H or Alkyl; R1 and R2 are hydroxyethyl (hydroxypropyl or hydroxybutyl) or H, among which at least one of R1 and R2 is the hydroxyethyl (hydroxypropyl or hydroxybutyl).

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a new baicalin compound and its application, in particular to a new baicalin compound used for preventing and treating cardiovascular and cerebrovascular diseases, senile dementia, cerebral infarction, cerebral ischemia and other diseases caused by cerebral ischemia Hydroxyethyl (propyl, butyl) baicalin compounds. Background technique [0002] Modern pharmacological studies have shown that baicalin has the functions of scavenging oxygen free radicals, anti-arrhythmia, dilating cardiovascular and cerebrovascular, reducing ischemia-reperfusion injury of heart and brain tissue, anti-isoproterenol-induced acute myocardial injury, and hypoxia-glucose-induced myocardial cell injury. And protect brain nerve cells, as well as antibacterial, anti-inflammatory, anti-tumor effects. Clinically, it is mainly used for the treatment of acute, chronic persistent and chronic active hepatitis, immune ...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61K31/7048A61P9/00A61P25/28
Inventor 裴月湖华会明高慧媛李占林刘英学
Owner SHENYANG PHARMA UNIVERSITY