Application of neuraminidase and neuraminidase inhibitors to preparation of medicines for inhibiting hepatic gluconeogenesis

A neuraminidase and inhibitor technology, applied in the field of biomedicine, can solve the problem of undiscovered neuraminidase correlation and other issues

Active Publication Date: 2018-03-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] In subsequent studies, the applicant also found that neuraminidase is related to various diseases. After searching, no prior art has been found to disclose the relationship between neuraminidase and these diseases

Method used

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  • Application of neuraminidase and neuraminidase inhibitors to preparation of medicines for inhibiting hepatic gluconeogenesis
  • Application of neuraminidase and neuraminidase inhibitors to preparation of medicines for inhibiting hepatic gluconeogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Fifty Kunming mice were randomly divided into 5 groups according to body weight and gender: control group and zanamivir, oseltamivir phosphate, coptisine, salvianolic acid B administration group. The mice in the administration group were given 0.2mg / kg / d zanamivir (i.v.), 5mg / kg / d oseltamivir phosphate (p.o.), 40mg / kg / d coptisine (p.o.), 40mg / kg / d salvianolic acid B (p.o.), the control group was given an equal volume of vehicle 0.5% CMC-Na by intragastric administration for 4 weeks. Take 7 rats from each group to measure the rate of gluconeogenesis. The specific method is: after fasting for 12 hours after the last gavage, take blood from the tail vein to measure the fasting blood sugar, which is recorded as the blood sugar value at 0 min; After injecting L-a-alanine, the eyeballs were removed 1 hour later to collect blood, and the blood glucose level was measured at 60 minutes. The gluconeogenesis rate (%) was calculated according to the blood glucose values ​​at 0 mi...

Embodiment 2

[0032] The commercially available neuraminidase inhibitor screening kit P0309 (Beyotime, Beyotime) was used to test the inhibitory activity of salvianolic acid B in vitro, and the positive control drug was oseltamivir phosphate. Add 70 μL of buffer solution and 10 μL of neuraminidase solution to each well of a 96-well plate, then add 10 μL of different concentrations of the test solution, shake and mix, incubate at 37°C for 5 minutes, add 10 μL of the solution containing the fluorescent substrate, shake and mix Homogenize, incubate at 37°C for 30min, and perform fluorescence measurement, wherein the excitation wavelength is 322nm and the emission wavelength is 450nm. The inhibition rates of different test solutions were calculated according to the fluorescence readings, and the IC50 values ​​of the positive control drugs oseltamivir phosphate and salvianolic acid B were further obtained. The results are shown in the table below.

[0033]

Oseltamivir Phosphate

...

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Abstract

The invention discloses application of neuraminidase and neuraminidase inhibitors to preparation of medicines for inhibiting hepatic gluconeogenesis. Zanamivir and oseltamivir phosphate are effectiveinhibitors of the neuraminidase; the inhibition effect of coptisine on neuraminidase is also disclosed in the previous patent application of the applicant. The applicant also discovers that salvanic acid B is capable of inhibiting the activity of the neuraminidase in vitro and is used as an inhibitor of the neuraminidase. In-vivo test proves that the several neuraminidase inhibitors are capable ofeffectively inhibiting the activity of the neuraminidase in the liver and then inhibiting hepatic gluconeogenesis. Therefore, the neuraminidase and the neuraminidase inhibitors can be used for preparing the medicines for inhibiting hepatic gluconeogenesis and can also be used for treating diabetes, obesity and non-alcoholic fatty liver disease.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the application of enzymes and enzyme inhibitors, in particular to the application of neuraminidase and its inhibitors in the preparation of drugs for inhibiting liver gluconeogenesis. Background technique [0002] Neuraminic acid is a class of natural sugar and acid compounds widely present in organisms. It is now confirmed that there are more than 50 natural derivatives of neuraminic acid, and N-acetylneuraminic acid and N-glycolylneuraminic acid are the more common ones. Neuraminic acid is usually linked to the end of glycoconjugates such as glycoproteins and glycolipids in the form of short chain residues. Neuraminic acid is an important biological information transfer molecule, and the neuraminidative modification of cell surface glycoproteins and glycolipids plays a vital role in many biological processes, including cell adhesion, antigen recognition and signal transduction. [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/47A61K45/00A61K31/4375A61K31/343A61K31/351A61K31/215A61P3/10A61P3/04A61P1/16
CPCA61K31/215A61K31/343A61K31/351A61K31/4375A61K38/47A61K45/00C12Y302/01018
Inventor 齐炼文刘群张蕾
Owner CHINA PHARM UNIV
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