Application of evodiamine in preparation of antiplatelet drugs

An anti-platelet drug, the technology of evodiamine, applied in the field of medicine and biology, can solve the problems of low decoction rate, resistance, anti-platelet and anti-thrombotic effects that have not been reported, and achieve the effect of inhibiting the retraction of blood clots

Inactive Publication Date: 2020-09-22
FIRST AFFILIATED HOSPITAL OF KUNMING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, many antiplatelet therapies have been widely used in the prevention and treatment of thrombotic diseases such as acute myocardial infarction and cerebral embolism. Response phenomenon, and adverse ischemic events still occur (Kopaleishvili L.A.,2014(236):105-10)
On the one hand, these drugs have a single mechanism of action, and the antiplatelet effect has certain limitations: for example, aspirin irreversibly blocks the synthesis of cyclooxygenase, thereby inhibiting platelet activation and aggregation (Halvorsen S., 2014,64(3):319- 27); Abciximab, tirofiban, and eptifibatide all belong to α Ⅱb beta 3 receptor antagonist ( -Lozano A., 2013,7(4):197-213)
Studies have found that the content of evodiamine in Evodia rutaecarpa only accounts for about 0.1%, and the decoction rate in the decoction process of clinical medication is very low, only about 10% ("Determination of evodiamine and evodiamine in Evodia rutaecarpa by one test and multiple evaluation methods") and the content of evodiamine, Song Yafang, 2009(21):96-100)
On the other hand, the pharmacological effects of evodiamine have not been fully elucidated, for example: anti-platelet and anti-thrombotic effects have not been reported

Method used

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  • Application of evodiamine in preparation of antiplatelet drugs
  • Application of evodiamine in preparation of antiplatelet drugs
  • Application of evodiamine in preparation of antiplatelet drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Evodiamine inhibits collagen-induced human platelet aggregation in vitro

[0019] (1) Source of experimental human platelets

[0020] Healthy volunteers signed informed consent for blood donation and were given certain nutritional subsidies. Venous whole blood was collected, apheresis platelets were separated by Kunming Blood Center, and apheresis platelets were collected in the Hematology Department of the First Affiliated Hospital of Kunming Medical University.

specific Embodiment approach

[0022] Step 1, using DMSO to dissolve and adjust the concentration of evodiamine to 5 mM and 25 mM.

[0023] Step 2, washing the platelets. Take 1 mL of human apheresis platelets stored at 25°C with constant temperature and shaking in a 1.5 mL centrifuge tube, add EDTA at a final concentration of 5 mM and 0.1 U / mL Apyrase (prepared with normal saline to prevent platelet aggregation during centrifugation), and centrifuge at 400 g for 10 Minutes; discard the supernatant of human apheresis platelets after centrifugation, add 1mL Tyrode's BufferB (137mM NaCl, 27mM KCl, 1mM MgCl 2 ,0.42mM NaH 2 PO 4 , 5.5mM Glucose, 5.55mM HEPES, 0.25% Bovine SerumAlbumin, pH 6.5), 5mM EDTA, 0.1UApyrase, blow gently, centrifuge again at 400g room temperature for 10 minutes; 2 ,0.42mM NaH 2 PO 4,5.5mM Glucose,5.55mM HEPES,0.25%Bovine Serum Albumin,pH7.4) resuspend the centrifuged platelets, adjust the platelet count to 150-250x 10 9 / L. Store with shaking at 70 rpm at 25°C, and use the washed...

Embodiment 2

[0027] Evodiamine inhibits platelet clot retraction

[0028] (1) The source of experimental human platelets is the same as Example 1.

[0029] (2) The specific implementation method is as follows:

[0030] Platelet-rich plasma was diluted with Tyrode's BufferA and quantified 500x 10 9 / L, put 200 μL of platelet-rich plasma into a siliconized transparent glass tube, and incubate at 37°C for 20 minutes. DMSO was used to dissolve evodiamine, and the concentration was adjusted to 250 mM. The experimental groups were: positive control group (Thrombin 0.2U / mL), negative control group (Control) and evodiamine experimental group. Add evodiamine with a final concentration of 250 μM to the experimental group, add DMSO equal to the volume of the experimental group to the positive control group and negative control group, and incubate at 37° C. for 20 minutes. After incubation, add thrombin at a final concentration of 0.2 U / mL to the positive control group and evodiamine test tubes, m...

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PUM

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Abstract

The invention relates to an application of evodiamine in preparation of antiplatelet drugs. The antiplatelet effect is resisting collagen-induced platelet aggregation or resisting thrombin-induced platelet blood clot retraction. An optical turbidimetry detection result shows that the sensitivity is high, the evodiamine has a remarkable inhibition effect on collagen-induced human platelet aggregation and thrombin-induced platelet blood clot retraction, the evodiamine is not limited to inhibition of collagen-induced platelet aggregation, can be used for exploring influences of the evodiamine andother platelet activators (collagen, arachidonic acid, ADP, epinephrine, restomycin and the like) on effects and related functions of platelets, and can also be used for monitoring existing antiplatelet treatment.

Description

technical field [0001] The invention relates to the field of medical biotechnology, in particular to the application of evodiamine as an antiplatelet drug. Background technique [0002] Thrombotic diseases mainly include arterial thrombotic diseases (myocardial infarction, cerebral infarction, pulmonary infarction) and venous thrombotic diseases (lower extremity venous thrombosis), which seriously threaten human health and life, and are the first cause of death for Chinese residents (Chen Weiwei, " Summary of China Cardiovascular Disease Report 2017, 2018). Platelets are small pieces of cytoplasm shed from mature megakaryocytes in the bone marrow, without nuclei. Platelets not only play a key role in the physiological hemostasis process, but also participate in pathological processes such as thrombus formation and tissue repair; platelet activation is an important initiating factor in the occurrence and development of thrombotic diseases (George J.N., 2000, 355 (9214 ): 15...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K36/754A61P7/02
CPCA61K31/519A61K36/754A61P7/02
Inventor 孟照辉叶雨佳石少卿
Owner FIRST AFFILIATED HOSPITAL OF KUNMING MEDICAL UNIV
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