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Application of montelukast in preparation of medicine for preventing and treating thrombotic diseases

A technology for thrombotic diseases and drugs, applied in the field of medicine, can solve the problem of not finding montelukast anti-thrombotic diseases, etc., and achieve the effects of reducing clinical trial time, preventing deep vein thrombosis, and saving research and development costs.

Inactive Publication Date: 2021-01-29
FUZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, no relevant reports about montelukast antithrombotic diseases have been found

Method used

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  • Application of montelukast in preparation of medicine for preventing and treating thrombotic diseases
  • Application of montelukast in preparation of medicine for preventing and treating thrombotic diseases
  • Application of montelukast in preparation of medicine for preventing and treating thrombotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Determination of the inhibitory effect of montelukast on FXIa and its homologous serine protease activity

[0022] experimental method:

[0023] The activity of FXIa and nine homologous serine proteases was determined by the reported chemiluminescence method (Chromogenicassay), which was specifically performed in a 100 μL reaction system (containing 20 mM Tris-HCl pH 7.4, 150 mM NaCl, 0.1% BSA), FXIa or homologous serine protease at a final concentration of 10 nM was pre-incubated with montelukast at a final concentration of 0-100 μM for 15 minutes, and then a luminescent substrate (manufactured by Chromogenix, each protease at a final concentration of 200 μM) was added. The corresponding luminescent substrates are shown in Table 1), and immediately put into the BioTek Synergy 4 microplate reader after mixing, and the absorbance was detected at 405 nm, and the detection time was 30 s / read for 30 min. Each test was repeated at least 3 times. Montelukast IC w...

Embodiment 2

[0028] Embodiment 2: In vitro thrombolysis experiment of montelukast

[0029] experimental method:

[0030] Clot lysis experiments were performed in 96-well clear plates and human plasma was collected from healthy donors, collected in sodium citrate vacutainer tubes and centrifuged to obtain clear plasma. Pre-incubate 20 nM recombinant FXIa with 0-25 μM montelukast in 37 °C buffer (containing 50 mM Tris-HCl pH 7.4, 150 mM NaCl, 1% DMSO) for 15 min, then add 25% (v / v) plasma, and by immediately adding 10 mM CaCl 2 cause blood clotting. Then, the absorbance at 405 nm was measured with a microplate reader at 37° C., and the formation and dissolution of blood clots were monitored in real time. Finally, the clot coagulation curve was drawn using GraphPad Prism 5 software.

[0031] Experimental results:

[0032] Such as figure 2 As shown, the plasma in the sodium citrate vacuum blood collection tube was added with 10 mM CaCl 2After coagulation occurs, fibrin is produced and...

Embodiment 3

[0033] Example 3: Effect of Montelukast on Electrically Induced Arterial Thrombosis

[0034] experimental method:

[0035] ICR mice were randomly divided into six groups, and each group contained 6 mice. Firstly, montelukast and apixaban were administered in two gradients of 2 mg / kg and 10 mg / kg, respectively. Administration, warfarin administration dose was 4 mg / kg, normal saline administration group served as control. Three hours after administration, mice were anesthetized (1.5% pentobarbital sodium, 30 mg / kg, intraperitoneal injection) and the left common carotid artery was exposed, stimulated with a 0.1 mA current to destroy the vessel wall, thereby passing through YLS-14B animals The thrombus forming instrument forms mixed thrombus in the blood vessel, records the occlusion rate of carotid blood flow every 4 seconds through the infrared detector, and records the average time for forming occlusive thrombus in the carotid artery (occlusion rate reaches 95%).

[0036] Exp...

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Abstract

The invention discloses an application of montelukast in preparation of a medicine for preventing and treating thrombotic diseases. It is found for the first time that montelukast has blood coagulation factor XIa (FXIa) inhibitory activity, and therefore montelukast can be used for preparing and developing medicine for treating or preventing thrombotic diseases and has wide application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of montelukast in the preparation of medicines for preventing and treating thrombotic diseases. Background technique [0002] Thrombotic cardiovascular and cerebrovascular diseases are a major cause of death worldwide. Thrombotic diseases are mainly divided into venous thrombosis (VT) and arterial thrombosis (ArT). Globally, a quarter of all in-hospital deaths are reported to be related to thrombotic disorders, and globally, a patient presents with a VT-related disorder every 16 seconds and a patient dies from a VT-related disorder every 37 seconds . [0003] Thrombotic diseases are the result of the imbalance of procoagulant, anticoagulant and fibrinolytic processes. Currently, the clinical drugs used to prevent and treat thrombotic diseases include anticoagulant drugs, antiplatelet drugs and thrombolytic drugs, among which anticoagulant drugs Majo...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61P7/02
CPCA61K31/47A61P7/02
Inventor 李金宇徐芃王栋周阳齐迎迎黄明东
Owner FUZHOU UNIVERSITY
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