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Application of isopentenyl flavonoid compounds in preparation of antidiabetic drugs

A technology of prenyl flavonoids and compounds, applied in the field of medicine, to achieve the effect of strong inhibitory activity

Inactive Publication Date: 2020-03-24
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] A class of prenyl flavonoids with structures as shown in the general formula (I) are all isolated from the stems and branches of the mulberry tree, and there is no report about its inhibition of the activity of protein tyrosine phosphatase 1B

Method used

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  • Application of isopentenyl flavonoid compounds in preparation of antidiabetic drugs
  • Application of isopentenyl flavonoid compounds in preparation of antidiabetic drugs
  • Application of isopentenyl flavonoid compounds in preparation of antidiabetic drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Embodiment 1 extracts the compound of the present invention from mulberry

[0031] (1) Extraction: after pulverizing 10 kilograms of stems and branches of the tree, extract by percolation with 200 liters of 95% aqueous ethanol, collect the percolation liquid, and concentrate under reduced pressure to obtain 380 grams of extract. The extract was dissolved in water and extracted with chloroform, and the recovered solvent was concentrated to dryness to obtain 140 g of chloroform extract;

[0032] (2) Separation: 140 grams of chloroform 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, each gradient consumption 10 liters, collect fraction; Wherein methanol-water 70: 30 fraction (6.3 grams) and 80: 20 fraction (4.4 grams) carry out Sephadex LH-20 gel column chromatography separation respectively, Eluted with methanol, and combined by thin layer chromatography to obtain 17 fractions: 1-1...

Embodiment 2

[0038] Example 2 Determination of the inhibitory activity of the compound (I) of the present invention on protein tyrosine phosphatase 1B (protein tyrosinephosphatase 1B, PTP1B)

[0039] (1) Preparation of protein tyrosine phosphatase 1B protein

[0040] The recombinant plasmid containing PTP1B catalytic domain was transformed into Escherichia coli BL21-CodonPlus (DE3) for expression. Inoculate the BL21-CodonPlus (DE3) cells containing the recombinant plasmid on the Luria-Bertani (LB) medium containing 100 mg / l ampicillin, culture with shaking at 37 °C, and when the cell concentration reaches 600 nm, the absorbance value is 0.4 Between -0.6, add isopropylthiogalactoside (IPTG) to 500nM to induce the expression of protein; carry out the purification of protein sample with GSTrap FF column, carry out protein analysis with 10% polyacrylamide gel electrophoresis, protein The 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 application of isopentenyl flavonoid compounds. The compounds have a structure in a general formula (I). The compounds are (E)-2-(3,4-dihydroxyphenyl)-8-(3,7-dimethyl-2,6-octadienyl)-5,7-dihydroxy-3-methoxy-4H-benzopyranyl-4-one (1), 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3-methoxy-8-(3-methyl-2-butenyl)-4H-benzopyranyl-4-one(2), 2-[3,4-dihydroxy-5-(3-methyl-2-butenyl)phenyl]-3,5,7-trihydroxy-8-(3-methyl-2-butenyl)-4H-benzopyranyl-4-one (3), 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3-methoxy-6,8-bis(3-methyl-2-butenyl)-4H-benzopyranyl-4-one (4) and 2-[3,4-dihydroxy-2,6-bis(3-methyl-2-butenyl)phenyl]-3,5,7-trihydroxy-8-(3-methyl-2-butenyl)-4H-benzopyranyl-4-one (5). It is confirmed through experiments that the compounds have high inhibitory activity on protein tyrosine phosphatase 1B, protein tyrosine phosphatase 1B inhibitors can be prepared, and drugs for prevention and treatment of type 2 diabetes can be prepared further.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to new medicinal uses of natural compounds, in particular to the use of prenyl flavonoids in mulberry trees in the preparation of antidiabetic drugs. Background technique [0002] The prior art discloses that type 2 diabetes is a chronic metabolic disease, also known as non-insulin-dependent diabetes mellitus, which is caused by insulin secretion disorder and tissue and organ resistance to insulin. Statistics show that currently type 2 diabetes patients account for more than 90% of the diabetic population, seriously endangering human health. Commonly used clinically for the treatment of type 2 diabetes are biguanides, sulfonylureas, dipeptidyl peptidase-4 inhibitors, peroxisome proliferator-activated receptor gamma agonists, alpha-glucosidase inhibitors, Glucagon-like peptide-1 analogues, etc. Treatment practice shows that the above-mentioned drugs have certain hypoglycemic effects,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P3/10C07D311/30C07D311/40
CPCA61K31/352A61P3/10C07D311/30C07D311/40
Inventor 雷春侯爱君俞媚华苏诗韵
Owner FUDAN UNIV