Pharmaceutical composition containing Apelin-12 and application of pharmaceutical composition

A composition and drug technology, applied in the field of pharmaceutical compositions containing Apelin-12, can solve the problems of Apelin-12 and platelet function and thrombosis without any reports, and achieve the effect of preventing platelet aggregation and preventing thrombosis

Pending Publication Date: 2019-03-01
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-12 mainly focuses on myocardial contraction, myocardial protection and hemodynamics, but there is no report on the relationship between Apelin-12 and platelet function and thrombus formation.

Method used

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  • Pharmaceutical composition containing Apelin-12 and application of pharmaceutical composition
  • Pharmaceutical composition containing Apelin-12 and application of pharmaceutical composition
  • Pharmaceutical composition containing Apelin-12 and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0023] Test its function, as shown in the following example. The following implementations are used to illustrate the present invention, but should not be used to limit the scope of the present invention.

Embodiment 1

[0024] Example 1 Determination of the Effect of Apelin-12 on Platelet Aggregation in New Zealand Rabbits

[0025] 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.

[0026] Aggregation rate = (measured voltage value - PPP photoelectric voltage value) / (PRP photoelectric voltage value - PPP photoelectric voltage value) * 100%

[0027] 1. ...

Embodiment 2

[0033] Example 2 Measuring the impact of Apelin-12 on thrombus formation in vitro

[0034] 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.

[0035] 1. Determination of the effect of different concentrations (1*10-7-1*100μmol / L) of Apelin-12 on thrombus formation in vitro

[0036]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-12 (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-12. The endogenous ligand can promote platelet aggregation and thrombosis by acting on an APJ receptor and can cooperate ADP and collagen induced platelet aggregation and thrombosis promoting functions. The Apelin-12 is used as a novel drug for promoting platelet aggregation and thrombosis in fundamental research of hemorrhagic diseases.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing Apelin-12 and its application. Apelin-12 itself can promote platelet aggregation through the APJ receptor, and also has synergistic effects on promoting platelet aggregation and external thrombus formation induced by ADP and collagen. Background technique [0002] APJ receptor is a G protein-coupled receptor with high homology to angiotensin type Ⅰ receptor, and Apelin is its endogenous ligand. The human Apelin gene is located on the q25-26 segment of the X chromosome, and its encoded product is a precursor peptide containing 77 amino acids, which is subsequently cleaved into fragments of different amino acid lengths, including: Apelin-12, Apelin-13, Apelin-17 and Apelin- 36 etc. The Apelin / APJ system is widely distributed in tissues and has rich physiological and pathological functions. It plays an important role in the regulation of cardiovascular function, energy metabolism, humoral ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/10A61P7/04A61P7/02
CPCA61K38/10A61P7/02A61P7/04
Inventor 李兰芳陈临溪刘梅青陈哲黄仕芳胡昊良
Owner NANHUA UNIV
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