2,3,5,4'-tetrahydroxy diphenyl ethylene-2-1-beta-d-glucoside

A technology of tetrahydroxystilbene and glucoside, which is applied in the field of natural compounds and can solve problems such as expensive processes and unfavorable mass production

Inactive Publication Date: 2004-10-27
广州中医药大学热带医学研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main component of Polygonum multiflorum is 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside. In the prior art, Polygonum multiflorum is extracted with ethanol, and the alcohol extract is extracted with ethyl acetate to obtain acetic acid The ethyl ester extraction part was preliminarily separated by dry column chromatography, and the eluent was ethyl acetate-methanol (8:2), and then refined by vacuum chromatography to obtain 2,3,5,4'-tetrahydroxyl Stilbene-2-O-β-D-glucoside, the process is relatively expensive, which is not conducive to safe mass production
In the prior art, there are no public reports of pharmacological experiments and clinical applications related to the treatment of hyperlipidemia for this component monomer

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1: Preparation of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (method 1)

[0014] Take slices of medicinal material, add water to decoct 3 times (each 2h, 1h, 1h), filter, combine the filtrates, concentrate, add 95% ethanol to make the alcohol content 60%, let stand overnight, and filter. Add 70% ethanol to the precipitate, heat and wash in a 70°C water bath, filter, combine the filtrate and the previous filtrate, recover ethanol under reduced pressure until there is no ethanol smell, add chloroform to extract twice to remove fat-soluble impurities, take the water layer, and extract completely with n-butanol ( Detected by TLC, the developer is chloroform-methanol (80:20), 10% ethanol sulfate for color development, or 254nm ultraviolet light for inspection), the n-butanol layers were combined, and evaporated to dryness under reduced pressure. Obtain the extract containing stilbene glycoside as the main component. The yield is 3%-7%.

[0015] Dissolve the ex...

Embodiment 2

[0018] Example 2: Preparation of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (method 2)

[0019] Take slices of medicinal materials, add water to decoct 3 times (each 2h, 1h, 1h), filter, combine the filtrates, concentrate, add 95% ethanol to make the alcohol content 60%, let stand overnight, and filter. Add 70% ethanol to the precipitate, heat and wash in a 70°C water bath, filter, combine the filtrate and the previous filtrate, recover the ethanol under reduced pressure until there is no ethanol smell, add chloroform to extract twice to remove fat-soluble impurities, take the water layer, evaporate the chloroform, add water to dilute, Filter, and the filtrate is passed through the D101 macroporous adsorption resin that has been processed, successively rinsed with water and an aqueous solution containing 30% ethanol until the target component is completely eluted (detected by TLC), and the eluent containing the component is combined (by 30% ethanol). -50% eluent), evapora...

Embodiment 3

[0021] Example 3: Effects on serum lipids of experimental animals with hypercholesterolemia [1]

[0022] Male SD rats were randomly divided into normal group, model group, positive drug (fenofibrate) control group, test drug (2,3,5,4′-tetrahydroxystilbene-2-O-β- D-glucoside) low-dose group, test drug (2,3,5,4′-tetrahydroxystilbene-2-O-β-D-glucoside) high-dose group (the same below). Except the normal group, the other 4 groups were administered with fat emulsion for 3 consecutive weeks. From the second week onwards, different treatments were given to each group: the normal group and the model group were given intragastric administration of normal saline (2ml / day), the control group were given intragastric administration of fenofibrate (100mg / kg·day), and the low-dose drug group was given intragastric administration. Oral administration of 80 mg / kg·day, and 160 mg / kg·day of the test drug group were administered by intragastric administration for 2 consecutive weeks.

[0023] S...

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PUM

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Abstract

A 2,3,5,4'-tetrahydroxy distyrene-2-O-beta-D-glucoside used for hypoglycemic medicine is prepared from the decoction of fleece flower root through extracting, separating and purifying. It can suppress the increasement of serum cholesterol, decrease low-density serum lipoprotein cholesterol and improve activity of liver esterase.

Description

Technical field [0001] The present invention relates to a natural compound with medicinal value, especially a stilbene glycoside compound 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucose with hypolipidemic effect Glycosides. Background technique [0002] A large number of epidemiological surveys and research data show that hyperlipidemia is an important risk factor for many diseases such as atherosclerosis, coronary heart disease, hypertension, diabetes, and cholelithiasis. The prevention and treatment of hyperlipidemia is the focus of current medical research. The current blood lipid lowering (regulating) drugs mainly include phenoxyacetic acid represented by fenofibrate, statin synthetic drugs represented by simvastatin, and compound Chinese medicine preparations such as evening primrose and special red yeast rice (Xuezhikang) . The Chinese Pharmacopoeia has recorded blood lipid-lowering traditional Chinese medicine prescriptions such as Xuezhining containing Polygonum mul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/16A61K9/20A61K9/48A61K31/7034A61P3/06C07H15/20
Inventor 胡英杰符林春高瑄卢元嫒
Owner 广州中医药大学热带医学研究所
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