Application of scutellarein to preparing medicine for preventing and/or treating thrombotic diseases

A technology for thrombotic diseases and scutellarin, which is applied in the field of medicine and can solve problems that do not involve anti-platelet adhesion, activation, release and/or aggregation, etc.

Inactive Publication Date: 2014-05-07
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] Scutellarein belongs to flavonoids, and many pharmacological studies related to cardiovascular aspects have begun to focus on scutellarein, but it has not yet involved anti-platelet adhesion, activation, release and / or aggregation, especially anti-platelet aggregation Aspects of research
So far, there is still no report about scutellarein as an active ingredient of antiplatelet drugs for the treatment of thrombotic diseases

Method used

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  • Application of scutellarein to preparing medicine for preventing and/or treating thrombotic diseases
  • Application of scutellarein to preparing medicine for preventing and/or treating thrombotic diseases
  • Application of scutellarein to preparing medicine for preventing and/or treating thrombotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Effect of scutellarein on platelet aggregation induced by agonist ADP

[0054] Experimental method: healthy SD male rats (200-220g) were anesthetized with 10% chloral hydrate. ACD (38mM citric acid, 75mM sodium citrate, 124mM glucose) was anticoagulated, and blood was collected through the abdominal aorta of rats. The obtained blood was centrifuged at room temperature, 200×g, for 10 minutes. The platelet-rich plasma (PRP) was centrifuged again at 800×g for 10 minutes. Finally, the platelets were resuspended in buffer solution A (130mM NaCl, 10mM sodium citrate, 9mM NaHCO 3 , 6mM Glucose, 0.9mM MgCl 2 , 0.81 mM KH 2 PO 4 , 10mM Tris-base). Using a transparent 96-well plate, add 100 μL of platelets (approximately 10 7 platelets), the drug group was added with different concentrations of scutellarein 50 μL, and the control group was added with 50 μL buffer solution A. At this time, the volume of each well solution was 150 μL. Put the 96-well plate into a multifunct...

Embodiment 2

[0061] Effects of scutellarein on platelet cAMP level induced by agonist ADP

[0062] Experimental method: platelet extraction is the same as in Example 1. Platelets (100 μL / 10 7 50 μL of scutellarein at different concentrations were added to each platelet of the positive drug group, forskolin was added to each unit of platelets in the positive drug group to a final concentration of 10 μM, 50 μL of buffer solution A was added to each unit of platelets in the control group, 37 ° C, 100 rpm, and incubated 10 minutes. Then add 2 mM CaCl to each unit of platelets 220μM ADP induces platelet activation, and the activation time lasts for 8 minutes. After adding an equal volume of 0.1M HCl to each group of platelets to stop the reaction, mediate and shake until the platelets are fully lysed. Finally, the platelets were centrifuged (1500×g, 10 minutes), the supernatant was taken, and the cAMP content was determined by enzyme-linked immunosorbent assay (ELISA, product of ENZO life s...

Embodiment 3

[0068] Scutellarein on ADP-induced platelet [Ca 2+ ]i level effect

[0069] Experimental method: Platelets were loaded with Fluo-3 / AM for 30 minutes, and then added different concentrations of scutellarein, positive drug u73122 (as the positive drug group), and buffer solution A (as the control group), incubated for 15 minutes, and then centrifuged at room temperature. 800 x g, 10 minutes. Platelets were resuspended, the agonist ADP (15 μM) was added to induce platelet activation, and the relative fluorescence value of platelets was measured in real time.

[0070] Table 3 Effect of scutellarein on platelet [Ca2+] i levels induced by agonist ADP

[0071]

[0072] X±SD vs control group, *P<0.05, **P<0.01

[0073] (Note: Resting is the experimental group not induced by ADP and is the blank group.)

[0074] In the experiment of the present invention, purified rat platelets were used to incubate with different concentrations of scutellarein for 10 minutes. After being induce...

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Abstract

The invention relates to an application of scutellarein to preparing a medicine for preventing and / or treating thrombotic diseases. The invention further provides a kit containing scutellarein.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to the use of scutellarein in the preparation of drugs for the prevention and / or treatment of thrombotic diseases, in particular to the use of scutellarein in the preparation of anti-platelet adhesion, activation, release and / or Aggregation, especially the application of anti-platelet aggregation drugs. Background technique [0002] Thrombotic diseases refer to diseases caused by two pathological processes of thrombosis and thromboembolism. Thrombotic disease is a serious threat to human life and health, and its incidence rate ranks first among various diseases, and it has gradually increased in recent years. It is one of the focuses and hotspots of contemporary medical research. Thrombosis refers to the pathological process in which formed components of blood form embolisms in blood vessels (mostly small blood vessels) under certain conditions, resulting in partial or complete bl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P7/02A61P9/10A61P3/10A61P11/00A61P3/06
Inventor 朱彦常连赢高秀梅刘二伟王志龙张砚
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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