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Isoquercetin and derivative and application and preparation methods thereof

A technology of isoquercetin and derivatives, applied in the directions of sugar derivatives, preparations for skin care, medical preparations containing active ingredients, etc., can solve the problems of small production scale, low purity, environmental pollution, etc. Utilization, solving the effect of decomposition and absorption

Inactive Publication Date: 2019-03-08
FOSHAN GOLDEN HEALTH TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention uses glycosidase to catalyze the hydrolysis of rutin into isoquercetin and glycosyltransferase to catalyze quercetin and isoquercetin into polysaccharide-based quercetin, which not only solves the problem of chemical preparation of isoquercetin and polysaccharide-based isoquercetin The problems of low purity, small production scale, serious environmental pollution and high cost can be realized in industrialized production

Method used

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  • Isoquercetin and derivative and application and preparation methods thereof
  • Isoquercetin and derivative and application and preparation methods thereof
  • Isoquercetin and derivative and application and preparation methods thereof

Examples

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Effect test

Embodiment 1

[0019] Rutin is used as a raw material, the reaction buffer is disodium hydrogen phosphate-sodium citrate buffer with a mass fraction of 0.5%, the pH of the buffer is 6, the reaction temperature is 45°C, and the reaction time is controlled for 24 hours. Add rhamnosidase to the reaction system, and the mass fraction of the enzyme is 25% of the input rutin. In this reaction system, the molar yield of isoquercetin is 98.8%.

Embodiment 2

[0021] Rutin is used as a raw material, the reaction buffer is disodium hydrogen phosphate-sodium citrate buffer with a mass fraction of 0.5%, the pH of the buffer is 6.1, the reaction temperature is 55° C., and the reaction time is controlled for 12 to 15 hours. Adding rhamnosidase, glucosidase or naringinase into the reaction system, the mass fraction of the total enzyme is 20-30% of the input rutin. In this reaction system, the molar yield of quercetin was 101.6%.

Embodiment 3

[0023] Quercetin is used as a raw material, the reaction buffer is 1% disodium hydrogen phosphate-sodium citrate buffer, the pH of the buffer is 3.5, the reaction temperature is 40-45°C, and the reaction time is controlled for 10-12 hours. Add glucosidase:glucosyltransferase=10:90 to the reaction system, and the mass fraction of the total enzyme is 35-40% of the input rutin. In this reaction system, the molar yield of isoquercetin is 97.2%.

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Abstract

The invention provides an isoquercetin and derivative. The structural formula of the isoquercetin and derivative is shown as the formula I, wherein n=1-9, and R is selected from Glu, Rha, Gal, Xyl orAll. The isoquercetin and derivative solves the problem of poor solubility of rutin and quercetin as well as in vivo digestion and absorption of rutin, improves the bioavailability of isoquercetin andpolysaccharide isoquercetin and achieves significant therapeutic effects on prevention and treatment of osteoporosis and hyperlipidemia.

Description

technical field [0001] The invention relates to the application and preparation method of isoquercetin and its derivatives. Background technique [0002] Rutin, also known as rutin, is a class of flavonoids and one of the raw materials of Chinese herbal medicines in my country's pharmaceutical industry. Isoquercitrin (Quercetin-3-glucose) is a derivative of rutin, which has only one rhamnosyl group less than rutin in structure, and is also called quercetin glucoside. Although rutin is widely distributed in plant resources (for example, the content of rutin in Sophora japonica can reach up to 28%), isoquercitrin is less distributed in nature, and its content is only tens of thousands or even ten percent. A few ten thousandths (Journal of Dalian Institute of Light Industry, 2007,26(2): 112~115). Due to the multiple active phenolic hydroxyl groups in its own structural formula, the cost of chemically synthesizing isoquercitrin by traditional methods is high, so the preparatio...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61K31/7048C12P17/06A23L33/105A61P19/10A61P39/06A61P29/00A61P35/00A61P9/12A61P9/14A61P3/06A61P31/04A61P31/10A61K8/60A61Q19/00
CPCA23L33/105A23V2002/00A61K8/602A61K2800/10A61K2800/805A61P3/06A61P9/12A61P9/14A61P19/10A61P29/00A61P31/04A61P31/10A61P35/00A61P39/06A61Q19/00C07H17/07C12P17/06A23V2250/2116A23V2200/30
Inventor 郭晓路周金林卢宇靖黄宝华林丽薇李慧灵
Owner FOSHAN GOLDEN HEALTH TECH CO LTD
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