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Compound extracted from broussometia kaempferi and application thereof in pharmacy

A technology of compounds and extracts, applied in the field of medicine, can solve the problems of unreported chemical composition and biological activity, etc.

Active Publication Date: 2020-03-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Rattan (Broussonetia kaempferi Sieb.var.australis Suzuki) is distributed in many provinces and regions in southern my country and is rich in resources. There are no reports on its chemical composition and biological activity.

Method used

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  • Compound extracted from broussometia kaempferi and application thereof in pharmacy
  • Compound extracted from broussometia kaempferi and application thereof in pharmacy

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Embodiment 1 extracts compound of the present invention from rattan structure

[0017] (1) Extraction: after pulverizing 3.3 kg of rattan stems and branches, extract by percolation with 60 liters of 95% ethanol, collect the percolation liquid, concentrate under reduced pressure to obtain 100 grams of extract. The extract was dissolved in water and extracted with ethyl acetate, and the recovered solvent was concentrated to dryness to obtain 74 grams of ethyl acetate extract;

[0018] (2) Separation: 74 grams of ethyl acetate extract was subjected to MCI gel CHP-20P column chromatography, and methanol-water (50:50→60:40→70:30→80:20→90:10→100: 0) Gradient elution, the amount of each gradient is 15 liters, and the fractions are collected; wherein the methanol-water 90:10 fraction (8 grams) is subjected to silica gel column chromatography, and petroleum ether-acetone (30:1~1:1) Gradient elution, 2 liters of each gradient solvent consumption, thin-layer chromatography detect...

Embodiment 2

[0020] Example 2 Determination of the inhibitory activity of the compound (I) of the present invention to protein tyrosine phosphatase 1B (protein tyrosinephosphatase 1B, PTP1B)

[0021] (1) Preparation of protein tyrosine phosphatase 1B protein

[0022]The recombinant plasmid containing the PTP1B catalytic domain was transformed into Escherichia coli BL21-CodonPlus (DE3) for expression; the BL21-CodonPlus (DE3) cells containing the recombinant plasmid were inoculated in Luria-Bertani containing ampicillin (ampicillin) 100mg / l On (LB) medium, shake culture at 37°C, add isopropylthiogalactopyranoside (IPTG) to 500nM to induce protein expression when the cell concentration reaches the absorbance value at 600nm between 0.4-0.6; use GSTrap FF column was used for protein sample purification; 10% polyacrylamide gel electrophoresis was used for protein analysis, and the protein concentration was determined by the Coomassie brilliant blue method (Bradford), with bovine serum albumin (...

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PUM

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Abstract

The invention belongs to the technical field of pharmacy and relates to an isopentenyl flavone compound having the structure of the formula (I) and an application thereof, and particularly relates tothe compound 8-(3,4-dihydroxybenzene)-5-hydroxy-7-methoxy-2-hydroxymethyl-2-methyl-10-(3-methyl-2-butenyl)-2H,6H-benzo[1,2-b:5,4-b']dipyran-6-one and an application thereof in preparation of a protein-tyrosine-phosphatase 1B inhibitor. The compound is extracted from broussometia kaempferi. Experiment result proves that the compound has excellent inhibition activity on the protein-tyrosine-phosphatase 1B and can be used as a protein-tyrosine-phosphatase 1B inhibitor and for researching a new lead compound for preventing or treating diabetes type II. The compound also can be used for preparing medicines for preventing or treating diabetes type II which is common clinically.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a prenyl flavonoid compound isolated from rattan and its application in the preparation of protein tyrosine phosphatase 1B inhibitors. Background technique [0002] The prior art discloses that diabetes is a chronic metabolic disease, and the main manifestation of the disease is hyperglycemia. Sustained hyperglycemia will lead to several complications, such as retinal, renal, nervous system and microvascular complications. According to statistics, type 2 diabetes accounts for more than 90% of diabetic patients in my country. Studies have shown that type 2 diabetes is characterized by abnormal metabolism of glucose and lipids, leading to insulin resistance and β-cell insulin secretion dysfunction, resulting in an imbalance of energy metabolism in the body. Commonly used drugs currently used clinically for the treatment of type 2 diabetes, such as biguanides, sulfonylureas, dipept...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61P3/10
CPCC07D493/04A61P3/10
Inventor 侯爱君雷春俞媚华薛静静李亚楠
Owner FUDAN UNIV
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