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Preparation of flavonolignans in milk thistle and application thereof

A technology of lignans and milk thistle, applied in the field of natural medicinal chemistry, can solve the problems of unreported anti-diabetic activity and the like

Inactive Publication Date: 2019-11-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, due to its potential preventive and therapeutic effects on diabetes, more and more attention has been paid to it, but there have been no reports on the anti-diabetic activity and mechanism of action of flavonoid lignans in this plant based on the PTP1B target.

Method used

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  • Preparation of flavonolignans in milk thistle and application thereof
  • Preparation of flavonolignans in milk thistle and application thereof
  • Preparation of flavonolignans in milk thistle and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: Separation, purification and preparation of flavonoid lignans 1-11

[0017] 1 Experimental method

[0018] Use petroleum ether to heat and reflux the pulverized milk thistle seeds for 3 times, each time for 2 hours, to obtain 1.6 L of fatty oil, then continue to heat the residue with 95% ethanol for 3 times, each time for 2.5 hours, and combine the three extractions solution, filtered and then rotary evaporated to obtain 2.0Kg of extract. A part of the extract was taken and prepared at a concentration of 1.0 mg / mL for the PTP1B enzyme inhibitory activity test, and the inhibition rate was as high as 73.1%. The extract was uniformly dispersed with water, and then extracted with equal volumes of dichloromethane, ethyl acetate and n-butanol to obtain a dichloromethane layer, ethyl acetate layer, n-butanol layer and a water layer. Different extraction layer samples were prepared to a concentration of 1.0mg / mL for the PTP1B enzyme inhibition activity test, the in...

Embodiment 2

[0021] Example 2: Inhibition of flavonoid lignans to PTP1B, TCPTP, VHR, SHP-1, SHP-2

[0022] 1 Experimental method

[0023] Preparation of PTP1B and VHR buffer: Take 0.06M sodium citrate (pH 6.0), 0.1M sodium chloride, 1mM EDTA, and 1mMDTT to prepare a buffer solution with a pH of 7.

[0024] Preparation of TCPTP, SHP-1, and SHP-2 buffer: Take 25mM Tris / HCl, 50mM NaCl, 2mM EDTA, 5mMDTT, 0.01% Brij35, 1mg / mL bovine serum albumin to prepare a buffer solution with a pH of 7.

[0025] Preparation of positive control and samples to be tested: Dissolve 1.142mg of oleanolic acid in DMSO and dilute to 2.5mL as a stock solution, and then dilute it with buffer solution to form 500, 100, 50, 10μM serial solutions. Take the corresponding mass of the compound to be tested, dissolve it in DMSO to make 1mM stock solution, and then dilute it with buffer solution to make 500, 100, 50, 10, 5μM serial solutions.

[0026] Preparation of PTP1B enzyme: 0.1 μL enzyme was dissolved in 80 μL buffer...

Embodiment 3

[0031] Example 3: Molecular simulation docking of flavonoid lignans and PTP1B

[0032] 1 Experimental method

[0033] Find the crystal structure of the target protein PTP1B (PDB: 2QBP) through the RCSB protein database (PDB) with a resolution of Prepare protein through software DS 3.0, including hydrogenation, dehydration, loop completion, protein plus polar hydrogen. The flavonoid lignans were prepared by drawing the relevant structures with ChemDraw 14.0, importing them into DS 3.0, and converting them into mol2 structures. And use sybyl 2.0 to optimize the relevant structure, the relevant parameters are as follows: select Tripos force field in the Force Field option menu; select Gasteiger-Huckel charge in the Charges option menu; increase the maximum number of repetitions (Max.Iterations) to 1000; reduce the Gradient to 0.005 ;Small molecule plus all hydrogen and other parameters default.

[0034] Import the prepared protein and flavonoid lignans into Autodock4.2, deter...

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Abstract

The invention relates to the field of natural medicinal chemistry, a preparation of a crude extract and flavonolignans compounds in milk thistle and an application thereof, and in particular to the activity-oriented separation and purification preparation as well as antidiabetic activity of the flavonolignans compounds in traditional Chinese medicine milk thistle. The invention also discloses theisolation and preparation of the compounds, the inhibitory activity on PTP1B enzyme, the evaluation of molecular simulation docking with PTP1B enzyme, the evaluation of enzyme kinetics of PTP1B, and the selective evaluation of homologous enzymes. The test results show that the crude extract from an ethyl acetate extraction layer of milk thistle and the flavonolignan compounds play better PTP1B enzyme inhibitory activity; and the flavonolignans compounds can inhibit the activity through a hydrogen bond with strong binding to a catalytically active region of PTP1B enzyme.

Description

technical field [0001] The present invention relates to the field of natural medicinal chemistry, the preparation and application of crude extracts and flavonoid lignans in milk thistle, in particular to the activity-oriented separation and purification preparation of flavonoid lignans in traditional Chinese medicine silybum Diabetic activity. The invention also discloses the separation and preparation of these compounds, the inhibitory activity to PTP1B enzyme, the molecular simulation docking evaluation with PTP1B enzyme, the enzyme kinetic evaluation of PTP1B and the selectivity evaluation to homologous enzymes. Background technique [0002] Diabetes mellitus (DM) is a serious chronic endocrine metabolic disorder accompanied by hyperglycemia symptoms for a long time. It is mostly due to insufficient insulin secretion or the inability of the body to effectively use insulin, resulting in elevated blood sugar concentration and metabolic abnormalities. It can lead to adverse...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/28A61K31/357A61K31/352A61K31/365C07D407/04A61P3/10
CPCA61K31/352A61K31/357A61K31/365A61K36/28A61P3/10C07D407/04
Inventor 华会明秦宁波李达翃李占林胡旭李佳
Owner SHENYANG PHARMA UNIVERSITY
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