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A platelet inhibitor and its application in the preparation of anti-platelet disease drugs

A platelet inhibitor and anti-platelet disease technology, applied in the preparation of anti-platelet disease drugs, in the field of platelet inhibitors, can solve the problems of obstructing physiological hemostasis, bleeding complications, unavoidable thrombotic events, etc.

Active Publication Date: 2017-08-11
SHENYANG SUNSHINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since aspirin, clopidogrel, and cilostazol can only inhibit the 2 , ADP or cAMP-mediated platelet activation, so some patients still cannot avoid the occurrence of thrombotic events; although GPⅡb / Ⅲa receptor antagonists can block the final pathway of platelet aggregation, they also hinder the process of physiological hemostasis. May cause bleeding complications

Method used

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  • A platelet inhibitor and its application in the preparation of anti-platelet disease drugs
  • A platelet inhibitor and its application in the preparation of anti-platelet disease drugs
  • A platelet inhibitor and its application in the preparation of anti-platelet disease drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 KIF inhibits platelet aggregation

[0026] Wash human platelets (3*10 8 / ml) Incubate with concentration gradient KIF (1.25, 2.5 and 5μM) or dimethyl sulfoxide (DMSO) at 37°C for 10 minutes, then use the polymerizer collagen (Collagen) 2μg / ml and thrombin (Thrombin) 0.02u / ml stimulation, record the aggregation curve with a platelet aggregation meter. Attached figure 1 The aggregation curve of platelets incubated with a KIF concentration gradient after stimulation with aggregating agent indicates that KIF can inhibit platelet aggregation caused by a variety of aggregating agents.

Embodiment 2

[0027] Example 2 KIF drug safety study

[0028] Platelet resuspension solution (2.5*10 8 / mL) Incubate with KIF (5, 10, 20μM) at 37°C for 10 minutes, then each group is incubated with AlamarBlue reagent 10μl (1:10) at 37°C for 4h, and the fluorescence intensity is monitored by the microplate reader at 570nm and 585nm wavelengths. Observe whether the platelets survive. Attached figure 2 In order to use the AlamarBlue assay to determine the histogram of the toxicity of KIF on platelets at different concentrations, it was observed that KIF was basically non-toxic to platelets.

[0029] Platelet suspension (2×10 7 / mL) 100μl, incubate with KIF 5, 10, 20μM at 37°C for 10 minutes, add 100μl Binding Buffer, and treat with Annexin V-FITC 1μl. Place in a dark room at room temperature for 15 minutes, and immediately perform quantitative detection of Annexin by flow cytometry The percentage of V-positive cells. Attached image 3 For platelets treated with KIF concentration gradient, the fl...

Embodiment 3

[0030] Example 3 KIF inhibits the "internal-external" signal pathway of platelets

[0031] Platelets (2.0X10 7 / mL) 200μl pretreated with KIF 5μM 37°C for 10 minutes, and then treated with thrombin (Thrombin) 0.05u, while adding 1μl of PE-CD62P and FITC-Fibrinogen antibody, let stand at room temperature for 30 minutes in a dark room, then add 200μl of PBS to resuspend , Detect the fluorescence intensity with a flow cytometer. Attached Figure 4 For the flow cytometry of KIF's influence on thrombin (Thrombin)-induced platelet activation, it was observed that the platelet activation rate incubated with KIF was low, indicating that KIF significantly inhibited the platelet "inside-outside" signal pathway.

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Abstract

The invention belongs to the technical field of medicine, and in particular relates to a platelet inhibitor and its application in the preparation of anti-platelet disease medicines; the KIF disclosed in the invention can inhibit the activation and aggregation of platelets induced by various aggregating agents, and more effectively inhibit the activation and aggregation of platelets. The formation of thrombus does not affect the physiological hemostasis process, and the risk of bleeding is small, thus showing the prevention and treatment of thrombotic cardiovascular and cerebrovascular diseases.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to a platelet inhibitor and its application in the preparation of antiplatelet disease drugs. Background technique [0002] In recent years, cardiovascular and cerebrovascular diseases have posed a serious threat to human health. According to WHO statistics, an average of 17 million people die from cardiovascular and cerebrovascular diseases each year, accounting for about 1 / 3 of the total deaths worldwide. Cardiovascular and cerebrovascular diseases in my country are also on the rise. It is estimated that 2 million new strokes and 500,000 myocardial infarctions occur every year; 2.5 million people die from cardiovascular and cerebrovascular diseases, including cardiovascular and cerebrovascular diseases. Half and half. Cardiovascular and cerebrovascular diseases are most common with thromboembolism. Intimal damage, blood flow slowing, and blood coagulation increase can caus...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/275A61P7/02A61P9/10
Inventor 曹碧茵郝亚南孔岩徐耑毛新良
Owner SHENYANG SUNSHINE PHARMA
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