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A compound extracted from rattan and its use in pharmacy

A compound, prenylflavone technology, applied in the field of medicine, can solve problems such as chemical composition and biological activity that have not been reported

Active Publication Date: 2022-03-22
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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  • A compound extracted from rattan and its use in pharmacy
  • A compound extracted from rattan and its use in pharmacy

Examples

Experimental program
Comparison scheme
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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Abstract

The invention belongs to the technical field of medicine, and relates to a prenylflavonoid compound with a structure of formula (I) and its application. Specifically related to said compound 8-(3,4-dihydroxybenzene)-5-hydroxy-7-methoxy-2-hydroxymethyl-2-methyl-10-(3-methyl-2-butene Base)-2H, 6H-benzo[1,2-b:5,4-b']dipyran-6-one and its use in the preparation of protein tyrosine phosphatase 1B inhibitors. The compound is extracted from rattan. Experiments have confirmed that the compound has a strong inhibitory activity on protein tyrosine phosphatase 1B, and can be used as a protein tyrosine phosphatase 1B inhibitor and to develop new drugs for preventing or treating type 2 diabetes The lead compound of the invention can also be used for the preparation of drugs for preventing or treating type 2 diabetes which is commonly seen in clinical practice.

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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Patent Type & Authority Patents(China)
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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