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Mastic tetracyclic triterpenoid components with 11 beta-hydroxysteroid dehydrogenase 1 inhibitory activity, composition of mastic tetracyclic triterpenoid components and application

A technology of hydroxysteroids and dehydrogenase inhibitors, applied in the field of medicine

Inactive Publication Date: 2017-01-04
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no relevant report about the application of the tetracyclic triterpenes of frankincense to 11β-hydroxysteroid dehydrogenase inhibitors. The present invention is a new discovery of its medical use

Method used

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  • Mastic tetracyclic triterpenoid components with 11 beta-hydroxysteroid dehydrogenase 1 inhibitory activity, composition of mastic tetracyclic triterpenoid components and application
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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 11β-HSD inhibitory activity test

[0044] 1. Experimental materials

[0045] Reagents: Boswellia tetracyclic triterpenes, 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 ; Methanol is chromatographically pure for HPLC, and the rest of the reagents are analytical grade domestic reagents.

[0046] Animals: Wistar rats, weighing 240-300 g, were bred and raised by the animal room of Tianjin Institute of Pharmaceutical Research.

[0047] Instruments: 515 type high performance liquid chromatography pump (Waters Company), 717plus autosampler (Waters Company), 2487 type ultraviolet detector (Waters Company).

[0048] 2. Experimental method:

[0049] 2.1 Enzyme activity inhibition experiment

[0050] Preparation of liver microsomes and analysis of 11β-HSD1 activity: several rats were taken, anesthetized with...

Embodiment 2

[0062] Take 300g of frankincense medicinal material, put it in a 2L round bottom flask, add 1.5L of 95% ethanol, heat and reflux for extraction for 2hr, 1.5hr, 1.5hr. The extracts were filtered and combined. Concentrate the extract under reduced pressure until there is no alcohol smell to obtain liquid extract. Disperse it in 400mL water, adjust the pH value to 9-10 with 2% NaOH solution, extract with ethyl acetate, and separate the organic layer; continue to adjust the pH value of the aqueous layer to 3-4 with dilute hydrochloric acid, extract three times with ethyl acetate, and combine The organic layer was washed with water until neutral, dehydrated with anhydrous sodium sulfate, and concentrated under reduced pressure to obtain 56.8 g of liquid extract.

[0063] Dissolve the above liquid extract with a small amount of methanol, mix the sample with coarse silica gel, and load the sample on a 500g column chromatography silica gel column. Gradient elution with petroleum eth...

Embodiment 3

[0068] Take 300g of frankincense medicinal material, put it in a 2L round bottom flask, add 1.5L of 95% ethanol, heat and reflux for extraction for 2hr, 1.5hr, 1.5hr. The extracts were filtered and combined. Concentrate the extract under reduced pressure until there is no alcohol smell to obtain liquid extract. Disperse it in 400mL water, adjust the pH value to 9-10 with 2% NaOH solution, extract with ethyl acetate, and separate the organic layer; continue to adjust the pH value of the aqueous layer to 3-4 with dilute hydrochloric acid, extract three times with ethyl acetate, and combine The organic layer was washed with water until neutral, dehydrated with anhydrous sodium sulfate, and concentrated under reduced pressure to obtain 56.8 g of liquid extract.

[0069] Dissolve the above liquid extract with a small amount of methanol, mix the sample with coarse silica gel, and load the sample on a 500g column chromatography silica gel column. Gradient elution with petroleum eth...

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Abstract

The invention provides mastic tetracyclic triterpenoid components with 11 beta-hydroxysteroid dehydrogenase 1 inhibitory activity, a composition of the mastic tetracyclic triterpenoid components and application, and novel application of mastic tetracyclic triterpenoid components with structures of the general formulas I-IV as 11 beta-HDS inhibitors. As a class of 11 beta-HSD inhibitors in novel structure types, the mastic tetracyclic triterpenoid components have certain selective inhibition effects on 11 beta-HSD1 and are expected to be developed into medicine for regulating lipid metabolism and treating diabetes, obesity, cardiovascular diseases and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to boswellia tetracyclic triterpenoid components with 11β-hydroxysteroid dehydrogenase inhibitory effect, 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 The inactive corticosterone (cortisone) is interconverted, 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 live...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P3/10A61P3/00A61P3/04A61P5/50A61P3/06A61P3/08A61P9/12A61P19/10A61P13/12A61P25/28A61P25/24A61P25/22A61P37/02A61P25/00
Inventor 赵娜夏韩英梅
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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