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
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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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