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Application of vanillic acid in preparation of antiplatelet and antithrombotic drugs

An anti-platelet and vanillic acid technology, applied in the field of medicine, can solve problems such as no reports on the effect, and achieve the effects of reducing the level of plasma calcium ions, reducing the area of ​​cerebral infarction, and reducing cerebral edema

Inactive Publication Date: 2020-10-16
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In recent years, there have been reports on vanillic acid's antioxidant, hypotensive, hepatoprotective and anti-apoptotic effects, but its role in the preparation of antiplatelet and / or thrombosis drugs has not been reported

Method used

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  • Application of vanillic acid in preparation of antiplatelet and antithrombotic drugs
  • Application of vanillic acid in preparation of antiplatelet and antithrombotic drugs
  • Application of vanillic acid in preparation of antiplatelet and antithrombotic drugs

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0040] Experimental example 1. Effect of vanillic acid on platelet aggregation in vitro.

[0041] Male SD rats with a body weight of 200-220 g were selected for the experiment, anesthetized with chloral hydrate, blood was taken from the abdominal aorta, and 3.8% sodium citrate solution 1:9 (anticoagulant: blood) was added for anticoagulation, 1200rpm, room temperature ( 23°C) for 10 minutes. After the centrifugation, carefully absorb the upper layer with a pipette gun to avoid sucking blood cells. The upper layer obtained is PRP (platelet-rich), and the remaining lower layer is centrifuged again at 3000 rpm at room temperature (23°C) for 10 minutes. Pipette the upper layer carefully, resulting in PPP (platelet-poor). Take PRP and centrifuge at room temperature (23°C), 1800rpm, 10min, discard the supernatant, obtain platelet assay, add platelet resuspension (7.7772mg / mL NaCl, 0.048mg / mL NaCl 2 HPO 4 , 0.217mg / mL KCL, 1.008mg / mL NaHCO 3 , 0.9mg / mL Glucose, 0.095mg / mL MgCl 2 ...

experiment example 2

[0042] Experimental example 2. Effect of vanillic acid on platelet aggregation in vivo.

[0043] Male SD rats, weighing 200-220g, were randomly divided into 6 groups, with 5 rats in each group. The blank control group was given 0.5% CMC-Na (100g / mL), once in the morning and once in the evening, and the aspirin group: 100mg / kg in the morning and evening. Each time, clopidogrel group: 30mg / kg, once in the morning and evening, low-dose vanillic acid group: 10mg / kg, once in the morning and evening, medium-dose vanillic acid group: 30mg / kg, once in the morning and evening, high-dose vanillic acid group: 100mg / kg, once in the morning and once in the evening, after 5 days of continuous administration, platelet aggregation was measured on the 6th day. Prepare PRP and PPP according to the above-mentioned experimental method, and use the turbidimetric method to measure the platelet aggregation rate under the condition of 37 ° C by LG-PABER-I semi-automatic coagulation analyzer (Beijing ...

experiment example 3

[0044] Experimental example 3. Effects of vanillic acid on four items of blood coagulation in rats.

[0045] Male SD rats, 210-230g, were randomly divided into 6 groups, 5 rats in each group. The blank control group was given 0.5% CMC-Na (100g / mL), once in the morning and evening. Aspirin group: 100mg / kg, once in the morning and evening. Clopidogrel group: 30mg / kg, once in the morning and evening, vanillic acid group: 100mg / kg (with the optimal dose determined by the above-mentioned in vivo experiment), after continuous administration for 5 days, on the sixth day the rats were anesthetized with chloral hydrate, Take blood from the abdominal aorta, add 3.8% sodium citrate solution 1:9 (anticoagulant: blood) for anticoagulation, centrifuge at 3000rpm, room temperature (23°C) for 10min, after centrifugation, carefully draw with a pipette The upper layer is used for the detection of four coagulation items. The results show (attached image 3 ), vanillic acid has no significant e...

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Abstract

The invention discloses application of vanillic acid in preparation of antiplatelet and antithrombotic drugs. The invention discloses in-vitro and in-vivo action mechanisms of vanillic acid in antiplatelet aggregation and antithrombosis, and it is discovered that the vanillic acid can relieve encephaledema and infarct volumes caused by cerebral ischemia, significantly reduce platelet aggregation caused by adenosine diphosphate (ADP) and arachidonic acid (AA), inhibit the concentration of calcium ions, and reduce P-selectin overexpression caused by cerebral ischemia. The vanillic acid can be used for preparing the antiplatelet and antithrombotic drugs, adverse reactions are reduced, and a safe, effective and economical solution is provided for treatment and prevention of diseases.

Description

technical field [0001] The invention relates to a new application of vanillic acid in the preparation of medicines, mainly relates to the application of vanillic acid in the preparation of medicines against platelet and thrombosis, and belongs to the technical field of medicine. Background technique [0002] Platelets play an important role in the process of pathological thrombosis. Ischemic disease caused by thrombosis is the main cause of death in middle-aged and elderly people in my country. With the increasing trend of population aging, it has a great impact on human life, health and quality of life. serious threat. Antiplatelet therapy targeting platelet aggregation has become one of the important directions in the treatment of thrombotic diseases. [0003] Existing antiplatelet drugs have their corresponding limitations. Including the weak inhibitory effect on platelet function, such as aspirin, which only blocks one pathway of platelet aggregation signal transduction...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P7/02A61P9/10A61P11/00A61P9/14
CPCA61K31/192A61P7/02A61P9/10A61P11/00A61P9/14
Inventor 杜冠华王海港孔令雷王睿陈燕霞杨时伦赵晓悦周启蒙
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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