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11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use

A technology of use, medicine, applied in the field of medicine

Inactive Publication Date: 2015-09-02
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no relevant report about the application of triterpenoid acids in Ganoderma lucidum to 11β-hydroxysteroid dehydrogenase inhibitors. The present invention is a new discovery of its medicinal use

Method used

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  • 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use
  • 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use
  • 11 beta-hydroxysteroid dehydrogenase inhibitor and its pharmaceutical composition and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] 11β-HSD inhibitory activity test

[0028] 1. Experimental materials

[0029] Reagents: Ganoderma lucidum triterpene acid, all self-made by our research group, with a purity greater than 95%; cortisone, hydrocortisone, prednisone acetate and nicotinamide adenine dinucleotide phosphate (NADPH) were purchased from Bailingwei Reagent Company; HPLC uses methanol as chromatographically pure, and the rest of the reagents are analytical grade domestic reagents.

[0030] Animals: Wistar rats, weighing 240-300 g, were bred and raised by the animal room of Tianjin Institute of Pharmaceutical Research.

[0031] Instruments: 515 type high performance liquid chromatography pump (Waters Company), 717plus autosampler (Waters Company), 2487 type ultraviolet detector (Waters Company).

[0032]2. Experimental method:

[0033] 2.1 Enzyme activity inhibition experiment

[0034] Preparation of liver microsomes and analysis of 11β-HSD1 activity: several rats were taken, anesthetized with ...

Embodiment 2

[0046] Grind and dry 6 kg of Chizhi fruiting body, heat and reflux extract with 70% ethanol for 3 times, each time for 2 hours, combine the extracts and concentrate under reduced pressure until there is no alcohol smell, disperse with a small amount of water, add 3 times the amount of acetone to stir, let stand, and filter , and the filtrate was concentrated under reduced pressure to obtain 120 g of liquid extract. Transfer to methanol, mix the sample with 60-100 mesh silica gel, carry out silica gel column chromatography (1200g), and use dichloromethane alcohol-methanol system (100:0~3:1) gradient elution, and collect and wash each 500ml. The liquid was removed, and the same components were combined for TLC detection to obtain 21 components.

[0047] Components 10 and 11 were concentrated to obtain 19.4g. Weighed 19.4g of sample mixing silica gel (60-100 mesh), dissolved the sample in methanol and mixed the sample, and weighed the silicon dichloromethane-methanol system (100:...

Embodiment 3

[0055] Take 10 g of compound No. 8, add 30 g of lactose-microcrystalline cellulose (4:1), 1% magnesium stearate, granulate with 70% ethanol, and compress into tablets to obtain 1000 tablets. Specification 10mg / tablet.

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PUM

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Abstract

The invention provides a novel use of a ganoderic acid component with a structure shown in the general formula I as a 11 beta-HSD inhibitor. The ganoderic acid component as a 11 beta-hydroxysteroid dehydrogenase inhibitor with a novel structure has a certain selective inhibition effect on 11 beta-HSD1 and can be used for preparation of drugs for adjusting lipid metabolism and treating diabetes, adiposis and cardiovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to ganoderma triterpenoid components with inhibitory effect on 11β-hydroxysteroid dehydrogenase, its pharmaceutical composition and its new medical application. Background technique [0002] Glucocorticoids play an important role in glucose, protein, fat, water and salt metabolism and stress response. Excessive or insufficient glucocorticoids will bring abnormalities to the body. 11β-Hydroxysteroid dehydrogenase (11β-HSD) is a metabolic enzyme of glucocorticoids, which catalyzes the redox reaction between the ketone group and the hydroxyl group at the C11 position of glucocorticoids, so that the biologically active cortisol (cortisol) and Inactive cortisone (cortisone) interconverts, thereby regulating the level of glucocorticoids in local tissues and organs. It has two isozymes, namely 11β-HSD1 and 11β-HSD2. 11β-HSD1 is widely expressed in liver, adipose tissue, pla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P3/10A61P3/00A61P3/04A61P3/08A61P5/50A61P3/06A61P9/12A61P9/00A61P13/12A61P19/10A61P25/28A61P25/22A61P25/24A61P37/02
Inventor 赵娜夏韩英梅
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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