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Diterpenoid compound in fir and preparation method and application thereof in pharmacy

A technology of compounds and diterpenoids, applied in the separation/purification of carboxylic acid compounds, separation/purification of hydroxyl compounds, separation/purification of carbonyl compounds, etc., can solve the diterpenoid components and pharmacological activities, and there is no report And other issues

Active Publication Date: 2020-08-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Douglas fir is produced in Yunnan, Sichuan, Guizhou, Hubei, Hunan and other places, and is born at an altitude of 800-1200 meters. At present, there is only one Chinese literature on its chemical composition that reports 6 flavonoids (Yi Jinhai et al., Acta Pharmaceutica Sinica , 2002,37:352-354), and diterpenoid components and pharmacological activity have not seen any report

Method used

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  • Diterpenoid compound in fir and preparation method and application thereof in pharmacy
  • Diterpenoid compound in fir and preparation method and application thereof in pharmacy
  • Diterpenoid compound in fir and preparation method and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of diterpenoids derived from Douglas fir

[0023] Take 30kg of Douglas fir pine needles and twigs, crush them and extract them by cold immersion in 90% methanol at room temperature for 5 times, combine the extracts and concentrate under reduced pressure to obtain 3.1kg of extract. The extract was dispersed with water and extracted with petroleum ether, ethyl acetate and n-butanol in sequence, and the ethyl acetate extract was concentrated under reduced pressure to obtain 500 g of extract. The extract was subjected to 100-200 mesh silica gel column chromatography, and was eluted with a gradient of petroleum ether: ethyl acetate 50:1-0:1 and ethyl acetate: methanol 10:1-0:1 to obtain 10 components ( Fr.1-Fr.10). cis-communic acid (25.0 mg) crystallized from subfraction Fr.2. Subcomponent Fr.9 was successively subjected to MCI microporous resin column chromatography (eluted with a gradient of 50%-100% methanol), silica gel column chromatography (20...

Embodiment 2

[0027] Example 2: Determination of ATP-citrate lyase inhibitory activity

[0028] Experimental method: In this experiment, the ATP-dependent citrate lyase ACL can catalyze the conversion of citric acid into acetyl-CoA, and then produce the precursor molecule of fatty acid synthesis - malonyl-CoA. This reaction is accompanied by the consumption of ATP, so ADP-Glo ​​and kinase detection kits can be used to detect changes in ATP to indirectly reflect the inhibitory effect of compounds on ACL enzyme activity. Specifically, the percent inhibition rate of ACL enzyme activity was investigated when the concentration of the compound was selected as 20 μg / ml in the preliminary screening, and the test results showed that pseudosinin E, cis-communic acid and 4β, 15-dihydroxy-19-norabieta-8 ,11,13-trien-7-one inhibition rates were higher than 61%, 110% and 59%. Further determination of IC 50 Value: The sample is dissolved in DMSO to make a suitable concentration before use, 3-fold diluti...

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Abstract

The invention belongs to the technical field of medicines, and relates to a 90% methanol extract prepared from branches and leaves of Pseudotsuga sinensis, labdane and abietane diterpenoid compounds separated from the methanol extract, a preparation method of the compounds and application of the compounds in pharmacy. A biological activity test shows that the compound remarkably inhibits ATP-citrate lyase (ACL); the compound can be used for preparing medicines or lead compounds of the medicines for preventing or treating ACL-mediated glycolipid metabolism disorder related diseases, such as hyperlipemia, atherosclerosis, non-alcoholic fatty liver disease, type 2 diabetes mellitus and obesity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to diterpenoids in Douglas fir, in particular to a class of diterpenoids prepared from the branches and leaves of Pseudotsuga sinensis and its 90% methanol extract and isolated therefrom. terpenes. The present invention also relates to the preparation method and the application in pharmacy of the compound. The biological activity test of the present invention shows that this type of compound significantly inhibits ATP-citrate lyase (ACL), and can be used to prepare, prevent or treat ACL-mediated diseases related to glucose and lipid metabolism disorders (such as hyperlipidemia, atherosclerosis, Non-alcoholic fatty liver, type 2 diabetes and obesity) drugs or lead compounds of such drugs. Background technique [0002] The prior art discloses that adenosine triphosphate (ATP)-citrate lyase [adenosine triphosphate(ATP)-citrate lyase, ACL] is a key enzyme in sugar metabolism and fatty ...

Claims

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Application Information

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IPC IPC(8): C07C33/14C07C61/35C07C49/737C07C29/76C07C51/42C07C45/78A61P3/06A61P1/16A61P9/10A61P3/10A61P35/00A61K31/047A61K31/19A61K31/122
CPCC07C33/14C07C61/35C07C49/737A61P3/06A61P1/16A61P9/10A61P3/10A61P35/00C07C2602/28C07C2603/26
Inventor 熊娟黄婷胡金锋
Owner FUDAN UNIV
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