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

A technology of drugs, compounds, 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

[0026] 11β-HSD inhibitory activity test

[0027] 1. Experimental materials

[0028] Reagents: Ganoderma lucidum triterpene acids, all made by our research group, with a purity of greater than 95%; cortisone, hydrocortisone, prednisone acetate and nicotinamide adenine dinucleotide phosphate (NADPH) were purchased from Bailingwei Reagent Company; The methanol used in HPLC is chromatographically pure, and the rest of the reagents are analytical grade domestic reagent.

[0029] Animals: Wistar rats, weighing 240-300g, were bred and raised in the animal room of Tianjin Pharmaceutical Research Institute.

[0030] Instruments: 515 type high performance liquid chromatography pump (Waters company), 717plus autosampler (Waters company), 2487 type ultraviolet detector (Waters company).

[0031] 2. Experimental method:

[0032] 2.1 Enzyme activity inhibition experiment

[0033] Preparation of liver microsomes and analysis of 11β-HSD1 activity: Take several rats, anesthetize with ether and heparinize...

Embodiment 2

[0044] Crushed and dried Ganoderma lucidum fruiting body 6kg, heated and refluxed with 70% ethanol for 3 times, 2h each time, the combined extracts were concentrated under reduced pressure until no alcohol taste, dispersed with a small amount of water, stirred with 3 times the amount of acetone, allowed to stand, and filtered , The filtrate was concentrated under reduced pressure to obtain 120g of liquid extract. Dissolve in methanol, mix the sample with 60-100 mesh silica gel, perform silica gel column chromatography (1200g), elution with a gradient of dichloromethane-methanol system (100:0~3:1), collect and elute every 500ml Liquid, TLC detection combined the same components to obtain 21 components.

[0045] Component 16 was chromatographed on a silica gel column and eluted with a petroleum ether-acetone system (100:0~1:1) to obtain 28.3mg of ganoderiol A, 25mg of ganodermatriol and 25mg of ganodermatriol. Ganodermanontriol (ganodermanontriol) 17.2mg.

[0046] Ganoderma lucidum...

Embodiment 3

[0050] Take 10g of No. 8 compound, add 30g lactose-microcrystalline cellulose (4:1) and 1% magnesium stearate, granulate with 70% ethanol and press 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-hydroxysteroid dehydrogenase 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 specifically relates to ganoderma triterpenoids with 11β-hydroxysteroid dehydrogenase inhibitory effect, its pharmaceutical composition and its new medical application. Background technique [0002] Glucocorticoids play an important role in sugar, protein, fat, water and salt metabolism and stress response. Excessive or lack of glucocorticoids can bring abnormalities to the body. 11β-Hydroxysteroid dehydrogenase (11β-HSD) is a metabolic enzyme of glucocorticoids. It catalyzes the redox reaction between the ketone group at the C11 position of glucocorticoids and the hydroxyl group to make the biologically active cortisol (cortisol) and Inactive cortisone (cortisone) is converted into each other, thereby regulating the level of glucocorticoid in local tissues and organs. It has two isozymes, 11β-HSD1 type and 11β-HSD2 type. 11β-HSD1 is widely expressed in liver, fat, placental tissue, and brain ...

Claims

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Application Information

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