Application of neuraminidase and inhibitors in preparing anti-thrombotic medicine

A technology of neuraminidase and inhibitor, which is applied in the field of biomedicine and can solve the problems of undiscovered neuraminidase correlation

Active Publication Date: 2018-04-24
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 inhibitors in preparing anti-thrombotic medicine

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 1. Experimental method

[0020] Get clean-grade male SD rats, weighing 250-300g, and randomly divide them into 5 groups, namely the sham operation group (control group), the model group, and give zanamivir, oseltamivir phosphate, coptisine, and salvianolic acid B. Medicine group, 10 rats in each group. Rats 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 and the model group were administered intragastrically with an equal volume of 0.5% CMC-Na for 2 weeks.

[0021] 6 rats in each group were anesthetized with 3% pentobarbital sodium 1 hour after the last administration, and the abdominal cavity was opened through a midline abdominal incision, the inferior vena cava was separated, ligated with thin silk thread, and the abdominal cavity was sutured. After 4 hours of ligation, the rats were sacrificed , open the abdominal cavity, c...

Embodiment 2

[0028] 1. Experimental method

[0029] The human umbilical vein endothelial cell line (HUVEC-c) was cultured in high-glucose DMEM medium with 10% fetal bovine serum and 1% double antibody at 37°C and 5% CO 2 . The medium was changed every other day, after being digested and passaged with 0.25% trypsin, they were replanted in culture dishes according to different conditioned media, and were divided into blank control group, model group, zanamivir group, oseltamivir phosphate group, Coptidis rhizome Alkaline group, salvianolic acid B group. The conditioned medium was prepared according to the experimental groups as follows:

[0030] ①Blank control group: normal medium containing serum;

[0031] ② Model group: normal culture medium containing serum and 1 μg / ml LPS;

[0032] ③Zanamivir group: 20nmol / L zanamivir was added to the culture medium of the model group;

[0033] ④Oseltamivir phosphate group: 20nmol / L oseltamivir phosphate was added to the culture medium of the model ...

Embodiment 3

[0043] 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 Table 3.

[0044] Table 3 IC50 values ​​of positive control drug...

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Abstract

The invention discloses application of neuraminidase and inhibitors in preparing anti-thrombotic medicine. As known, zanamivir and oseltamivir phosphate are effective inhibitors of the neuraminidase,an inhibition effect of coptisine on the neuraminidase also has been disclosed in precious patent application of an applicant, and the applicant also proves that salvianolic acid B is capable of inhibiting the activity of the neuraminidase in vitro and is the inhibitor of the neuraminidase; an in-vivo experiment proves that the inhibitors of the neuraminidase are capable of effectively inhibitingthe activity of the neuraminidase in vascular endothelial cells and playing an anti-thrombotic effect; as a consequence, the neuraminidase and the inhibitors thereof can be used for preparing the anti-thrombotic medicine and can be used for treating cerebral apoplexy or coronary heart 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 inhibitors in the preparation of antithrombotic drugs. 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. [0003] In organisms, neuramin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/47A61K45/00A61K31/351A61K31/215A61K31/343A61K31/4375A61P7/02A61P9/10
CPCA61K31/215A61K31/343A61K31/351A61K31/4375A61K38/47A61K45/00C12Y302/01018
Inventor 李萍齐炼文张蕾
Owner CHINA PHARM UNIV
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