Application of natural coumarin compound in preparation of ATP (adenosine triphosphate) citrate lyase inhibitor

A technology of citrate lyase and coumarin, which is applied in the field of medicine and can solve problems such as chemical composition research that has not been reported in the literature

Inactive Publication Date: 2022-07-15
TAIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no literature report on the research on the phytochemical constituents of Maoshan Xiaoju

Method used

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  • Application of natural coumarin compound in preparation of ATP (adenosine triphosphate) citrate lyase inhibitor
  • Application of natural coumarin compound in preparation of ATP (adenosine triphosphate) citrate lyase inhibitor
  • Application of natural coumarin compound in preparation of ATP (adenosine triphosphate) citrate lyase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of compound fraxidin

[0028]Take 10.0kg of fresh branches and leaves of Maoshan small orange to dry, pulverize it into coarse powder, soak it with 95% ethanol for 3 times, the solvent volume is 20.0, 15.0 and 15.0L in turn, soak for 1 week each time, combine the soaking liquid, and concentrate under reduced pressure to obtain total extract. The total extract was dispersed in warm water, and then extracted with petroleum ether and ethyl acetate, respectively. After the solvent was recovered under reduced pressure, petroleum ether extraction fraction (69.0 g) and ethyl acetate extraction fraction (90.0 g) were obtained. The petroleum ether fraction was firstly chromatographed on a silica gel column, analyzed by TLC, and merged into 5 groups through a petroleum ether-ethyl acetate gradient (80:20→70:30→60:40→50:50→0:100). points (Fr.1-Fr.5). Component Fr.4 (Petroleum ether-EtOAc, 50:50) was purified by Sephadex LH-20 (CHCl) 3 -MeOH) and semi-prep...

Embodiment 2

[0031] Example 2: Testing of ACL Inhibitory Activity of Compounds in the Application

[0032] Experimental method: In this experiment, the ATP-dependent citrate lyase ACL can catalyze the conversion of citrate 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 the change of ATP. When the inhibitor exists, the catalytic reaction of ACL cannot occur, and the enzymatic activity inhibition of ACL by the compound can be indirectly reflected according to the change of ATP. effect.

[0033] Specifically, the percentage inhibition rate of ACL enzyme activity was investigated when the concentration of the selected compound was 20 μg / ml, and the test results showed that the inhibition rate of fraxidin was 85.7%.

[0034] Further determination of IC 50 Value: before use, the sample was dissolved in DMSO to make a suitable conc...

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Abstract

The invention discloses application of a natural coumarin compound in preparation of an ATP (adenosine triphosphate) citrate lyase inhibitor. The structural formula of the natural coumarin compound is as shown in formula (1). The compound fraxidin is separated from 95% ethanol extract of branches and leaves of glycosmis mollissima for the first time. Multiple pharmacological test studies show that the compound has shown ACL inhibitory activity, and can be used for preparing drugs for treating ACL-mediated diseases or used as a lead compound of the drugs.

Description

technical field [0001] The present application belongs to the field of medical technology, and specifically relates to the preparation of the compound fraxidin for preventing or preventing ATP-citrate lyase (ATP-citrate lyase, ACL)-mediated diseases related to glucose and lipid metabolism disorders (such as hyperlipidemia, atherosclerosis Cirrhosis, non-alcoholic fatty liver, type II diabetes and obesity, etc.) drugs or the use in the leading compounds of such drugs. Background technique [0002] ATP-citrate lyase (ACL) is a key enzyme in glucose metabolism and fatty acid and cholesterol biosynthesis. Its substrates and products are key intermediates in glucose metabolism and can be used as substrates for fatty acid synthesis. . Human ACL enzyme protein is a homotetramer composed of 4 identical 120KDa subunits, each polypeptide chain contains 1101 amino residues (Singh et al, J. Biol. Chem. 1976, 251, 5254-5250) . ACL is a cytoplasmic enzyme that catalyzes the conversion ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366A61P3/06A61P9/10A61P1/16A61P3/10A61P3/04
CPCA61K31/366A61P3/06A61P9/10A61P1/16A61P3/10A61P3/04
Inventor 周戚吴寿远姜春筱梅迪
Owner TAIZHOU UNIV
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