Apelin-17-containing pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of pharmaceutical compositions containing Apelin-17, can solve the problems of Apelin-17 and platelet function and thrombosis that have not yet been reported, and achieve the effects of preventing platelet aggregation and thrombosis.

Pending Publication Date: 2018-11-13
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the research on APJ ligand subtype Apelin-17 mainly focuses on angiogenesis, myocardial contraction and hemodynamics, but there is no report on the relationship between Apelin-17 and platelet function and thrombus formation.

Method used

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  • Apelin-17-containing pharmaceutical composition and application thereof
  • Apelin-17-containing pharmaceutical composition and application thereof
  • Apelin-17-containing pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Determination of the Effect of Apelin-17 on Platelet Aggregation in New Zealand Rabbits

[0027] The platelet aggregation rate was measured with a platelet aggregation coagulation factor analyzer (LG-PABER-I, Beijing Shidi Scientific Instrument Company). This instrument uses photoelectric turbidimetry to test platelet aggregation: platelet poor plasma (platelet poor plasma, PPP) is used as the substrate, and platelet rich plasma (platelet rich plasma, PRP) is used for measurement. Under the stirring of the magnetic beads, the inducer is added to the PRP, the platelets aggregate, and the transmittance of the PRP increases or the turbidity decreases. The change of light and turbidity is converted into the change of electrical signal, so as to calculate the aggregation rate of platelets.

[0028] Aggregation rate = (measured voltage value - PPP photoelectric voltage value) / (PRP photoelectric voltage value - PPP photoelectric voltage value) * 100%

[0029] 1. ...

Embodiment 2

[0035] Example 2 Measuring the impact of Apelin-17 on thrombus formation in vitro

[0036]The thrombus model in vitro was established with a thrombus detector (LMK-12, Zhengzhou Mingju Technology Co., Ltd.). This instrument uses the chandler method: blood is injected into a rotating ring outside the body to simulate the blood flow state in the body to form thrombus.

[0037] 1. Determination of the effect of different concentrations (1*10-7-1*100μmol / L) of Apelin-17 on thrombus formation in vitro

[0038] Blood collection from the middle artery of New Zealand rabbit ears (without any anticoagulant, 1ml of venous blood was taken directly, and the bubbles in the syringe should be removed, and treated with different concentrations of Apelin-17 (0.001, 0.01, 0.1, 1μmol / L) , fill the ring with blood sample, slowly inject 1m1 blood sample into the tube along the tube wall at one end of the plastic ring, connect it into a ring at any time, and place it in the corresponding turntable....

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Abstract

The invention relates to an endogenous ligand Apelin-17, wherein the endogenous ligand acts on an APJ receptor to promote platelet aggregation and thrombosis, and can cooperate with the promotion of platelet aggregation and thrombosis induced by a platelet activator thrombin; an APJ receptor blocker F13A can inhibit the platelet aggregation of New Zealand rabbits induced by Apelin-17. In the fundamental research on hemorrhagic disease, the Apelin-17 can be served as a novel drug for promoting platelet aggregation and thrombosis.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing Apelin-17 and its application. Apelin-17 can promote platelet aggregation and promote thrombus formation in vitro; APJ receptor blocker F13A inhibits platelet aggregation and thrombus formation induced by Apelin-17; and found that Apelin-17 has a synergistic effect on platelet aggregation induced by platelet activator thrombin . Background technique [0002] Apelin is the endogenous ligand of the transmembrane G protein-coupled receptor APJ, which is widely distributed in tissues and expressed in cardiovascular, kidney, nervous and brain systems. Apelin / APJ system has various biological effects such as enhancing myocardial contractility, lowering blood pressure, promoting blood vessel growth, regulating insulin secretion, pituitary hormone release and body fluid balance. Apelin precursor peptide consists of 77 amino acid residues, which are then cleaved into fragments of different amino...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61P7/04A61P7/02
CPCA61K38/1709A61P7/02A61P7/04
Inventor 陈临溪刘梅青罗旭灵李兰芳蒋进勇徐金周群
Owner NANHUA UNIV
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