Application of 3,4,7-trihydroxyisoflavone or 3-methoxydaidin in the preparation of drugs for inhibiting platelet aggregation and thrombus

A technology of trihydroxyisoflavone and platelet aggregation, applied in the field of biomedicine, can solve the problems of increased bleeding risk, weakened drug efficacy, and impact on the life and health of patients in clinical use.

Active Publication Date: 2020-08-28
KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the drugs used clinically for the prevention and treatment of thrombotic diseases mainly include anticoagulant drugs, thrombolytic drugs and anti-platelet aggregation drugs, but common antithrombotic drugs such as aspirin and clopidogrel often produce drug effects Side effects such as weakening, gastrointestinal irritation, and neutropenia. In addition, aspirin, clopidogrel and other drugs can also increase the risk of bleeding, which seriously affects clinical use and the life and health of patients.

Method used

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  • Application of 3,4,7-trihydroxyisoflavone or 3-methoxydaidin in the preparation of drugs for inhibiting platelet aggregation and thrombus
  • Application of 3,4,7-trihydroxyisoflavone or 3-methoxydaidin in the preparation of drugs for inhibiting platelet aggregation and thrombus
  • Application of 3,4,7-trihydroxyisoflavone or 3-methoxydaidin in the preparation of drugs for inhibiting platelet aggregation and thrombus

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preparation example Construction

[0041]The present invention also provides the preparation method of the oral preparation, which comprises the following components in mass percent: 5-20% active ingredient, 2-10% disintegrant, 0.2-2% lubricant, 0.1-1.5% % of glidant, 0-0.5% of additives, and the balance of fillers are mixed to make an oral agent; the active ingredient is 3,4,7-trihydroxy isoflavone or 3-methoxydaidin.

[0042] In the present invention, the administration frequency of the oral agent is once a day, and 3-7 days is a course of treatment.

Embodiment 1

[0045] Platelets from healthy people were diluted with plasma to 2.5×10 8 individual / mL. Take 300 μL of plasma-rich platelets, add different concentrations of samples and incubate at 37°C for 5 minutes, then add 70 μmol / L ADP to induce aggregation, and draw the aggregation curve within 5 minutes on a platelet aggregometer. Platelet aggregation without sample treatment was used as a control.

[0046] Detection of collagen-induced platelet aggregation using washed human platelets. Such as figure 1 As shown, 3,4,7-trihydroxyisoflavone and its analogs inhibit platelet aggregation induced by 0.6 μg / mL collagen in a gradient-dependent manner. 20μM 3-methoxydaidin can inhibit about 50% of platelet aggregation, while 20μM 3,4,7-trihydroxyisoflavone can completely inhibit platelet aggregation. The platelet washing method is as follows:

[0047] a. Each 1.5mLEP tube was filled with 1.4mL platelets (platelet-concentrated plasma), centrifuged at 400g for 5min at room temperature, and...

Embodiment 2

[0054] Rat tail thrombosis model induced by carrageenan

[0055] Male Kunming mice, weighing 20-25 g, were used as experimental animals. After feeding for one week, they were randomly divided into groups (n=10). The first group is the normal saline control group, the sample group is administered with 3,4,7-trihydroxy isoflavone and 3-methoxydaidin at concentrations of 33, 100, and 300 μmol / kg, respectively, and the positive control is administered with 300 μmol / kg clopidogrel Gray gavages. After intragastric administration for 30 minutes, the mice were intraperitoneally injected with carrageenan (carrageenan, type I, Sigma) at a dose of 40 mg / kg. Since the thrombus formation rate was >90% in a low temperature environment, the feeding temperature used was 18°C. After 24 hours, the average length of thrombus was determined according to the change of tail skin color. Oral administration of 3,4,7-trihydroxyisoflavone and 3-methoxydaidin has a greater inhibitory rate on thrombus ...

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Abstract

A use of 3,4,7-trihydroxyisoflavone or 3-methoxydaidzein is provided for implementation in preparation of a drug for inhibiting platelet aggregation. The 3,4,7-trihydroxyisoflavone or 3-methoxydaidzein has a significant inhibition effect on platelet aggregation, and bleeding test conducted with these embodiments show that all of the mice administrated with 3,4,7-trihydroxyisoflavone and 3-methoxydaidzein did not show any significant hemorrhagic activity, while the control group, i.e., the group administrated with the same concentration of clopidogrel showed very significant hemorrhagic activity. Thus, the use of such a drug of the present invention is useful in inhibiting platelet aggregation, and the use of such a drug can reduce the risk of bleeding, is safe for use, and expands the clinical and medical applications thereof.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to the application of 3,4,7-trihydroxy isoflavone or 3-methoxydaidin in the preparation of drugs for inhibiting platelet aggregation and thrombus. Background technique [0002] A thrombus is a small clotted plaque formed by blood flow on the surface of a peeled or repaired vessel in the cardiovascular system. In the physiological process of coagulation, thrombus is the final product of the cascade reaction of the coagulation system, which is mainly composed of deposited platelets, insoluble fibrin, accumulated white blood cells and red blood cells. Platelet aggregation is one of the initial steps in the hemostasis process and one of the important factors of thrombus formation. The formation of thrombus in the blood vessel will hinder the flow of blood flow, and even lead to the complete occlusion of the blood vessel. The thrombus peels off and detaches from the inner wall of t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P7/02
CPCA61K31/352A61K9/0053A61P7/02
Inventor 赖仞申传斌吕秋敏刘明
Owner KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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