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Application of glycosylated puerarin derivate and its combination for preventing and treating cardiovascular and cerebrovascular disease

A technology of puerarin and compounds, applied in the field of medicine, can solve the problems of poor stability of preparations, increased water solubility, and fast elimination rate, etc.

Inactive Publication Date: 2009-11-25
NANJING NORMAL UNIVERSITY +1
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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 provide a new class of puerarin derivatives and pharmaceutically acceptable salts thereof, which not only increase their water solubility, but also overcome the shortcomings of fast elimination rate in vivo and poor preparation stability

Method used

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  • Application of glycosylated puerarin derivate and its combination for preventing and treating cardiovascular and cerebrovascular disease
  • Application of glycosylated puerarin derivate and its combination for preventing and treating cardiovascular and cerebrovascular disease
  • Application of glycosylated puerarin derivate and its combination for preventing and treating cardiovascular and cerebrovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Put 150mL of LB medium into a 500mL Erlenmeyer flask, a total of 1L of medium. After high-pressure steam sterilization at 121°C, insert Microbacterium oxydans CGMCC1788 seed solution, 30°C, 220rpm shaking culture for 12 hours, stop fermentation, collect bacterial cells by centrifugation, put them into a 500mL Erlenmeyer flask, add 150mL containing 0.02% puerarin -2% maltose 1 / 15mol / L phosphate buffer solution (pH8.0), 30°C, 200rpm shaking aeration to carry out the transformation reaction of puerarin glycosylation resting cells, after 48h, stop the transformation reaction, centrifuge to remove the bacteria, and The supernatant liquid was separated by C18 preparative high-performance liquid chromatography to obtain puerarin-7-O-glucoside and puerarin-7-O-isomaltoside components respectively, and concentrated to an appropriate volume with a vacuum film, and placed at 4°C When the crystals are separated out, the crystals are collected, washed and dried to obtain the product...

Embodiment 2

[0062] Insert the Microbacterium oxydans CGMCC1788 strain into a 1L Erlenmeyer flask containing 300mL of sterilized LB medium, 30°C, 220rpm shaking culture for 24 hours, then put it into a fermenter containing 3LLB medium, 30°C, 3L / min aeration After culturing for 18 hours, the bacteria were collected by centrifugation, resuspended with 200 mL of water, and the cells were crushed by Franch Press at 1800 psi to extract glycosyltransferase, and 160 mL of the enzyme extract was collected by centrifugation, and two 40 ml enzyme extracts were taken respectively. Add to two 3L 1 / 15mol / L PBS buffer solution (pH8.0) containing 4% sucrose-0.2% puerarin, 30 DEG C, 400rpm. Under the condition of agitation, transform for 72 hours and then stop the reaction. Heat at 100°C for 5 minutes to precipitate the protein, and centrifuge at 10,000 rpm for 15 minutes to remove the precipitate. The supernatant is adsorbed with a 35cm × 2.5cm macroporous resin column, after the column is washed with di...

Embodiment 3

[0064] Put 150mL of LB medium into a 500mL Erlenmeyer flask, a total of 1L of medium. After high-pressure steam sterilization at 121°C, insert Microbacterium oxydans CGMCC1788 seed solution, 30°C, 220rpm shaking culture for 12 hours, stop fermentation, collect bacterial cells by centrifugation, put them into a 500mL Erlenmeyer flask, add 150mL containing 0.02% puerarin -4% maltose 1 / 15mol / L phosphate buffer solution (pH8.0), 30°C, 200rpm shaking aeration to carry out the transformation reaction of puerarin glycosylation resting cells, after 72h, stop the transformation reaction, centrifuge to remove the bacteria, heat Concentrate 10 times, add 95% ethanol to adjust the concentration to 20%, centrifuge or filter to remove the bacteria, the supernatant is passed through a macroporous resin column, and after the impurities are eluted with water, it is eluted with 60% ethanol solution, and the eluate is collected. After the vacuum film is concentrated to an appropriate volume, the...

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Abstract

The invention relates to a glycosylated puerarin derivate shown in the general formula (I) and its pharmaceutically acceptable salt. In the formula, R is described as the text. A preparation method and a medicament combination containing the compound shown in the general formula (I) of the effective dose are also provided. The combination is used for treating and preventing the cardiovascular and cerebrovascular diseases, diabetic nephropathy and osteoporosis.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new puerarin derivative and its pharmaceutical composition used in the preparation and treatment of cardiovascular and cerebrovascular diseases; prevention and treatment of atherosclerosis, lowering blood fat, diabetic nephropathy, insulin resistance, and bone resistance loose application. Background technique [0002] Puerarin is an active ingredient extracted from Radix Puerariae. It is a commonly used natural medicine and is recorded in the national drug standards. It is mainly used for coronary heart disease, angina pectoris, myocardial infarction, ischemic cerebrovascular disease, Retinal arteriovenous thrombosis, sudden deafness, etc. Puerarin preparations include injections, freeze-dried powder injections, and eye drops. The actual use is mainly based on the clinical application of injection administration. With the prolongation of clinical use time, some adverse reactions appe...

Claims

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Application Information

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IPC IPC(8): C07H17/07C12P19/60A61K31/7048A61P9/00A61P3/06A61P3/10A61P19/10C12R1/01
Inventor 袁生蒋洁蓉丁娟芳丛晓东朱守创戴亦军叶辉
Owner NANJING NORMAL UNIVERSITY
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