Application of cobicistat as anti-HIV drug in preparing antithrombotic drug

An antithrombotic drug and drug technology, which are used in drug combinations, medical preparations containing active ingredients, blood diseases, etc.

Active Publication Date: 2018-10-26
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on whether cobistat has new targets and functions; whether it will partic

Method used

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  • Application of cobicistat as anti-HIV drug in preparing antithrombotic drug
  • Application of cobicistat as anti-HIV drug in preparing antithrombotic drug
  • Application of cobicistat as anti-HIV drug in preparing antithrombotic drug

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 impact of cobistat on platelet aggregation

[0025] The platelet aggregation rate was measured with a platelet aggregation coagulation factor analyzer (LG-PABER-I, Beijing Shidi Scientific Instrument Company). The instrument adopts photoelectric turbidimetry to test platelet aggregation: platelet poor plasma (PPP) is used as the substrate, and 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. Determination of the effect of different concentrations of cobistat...

Embodiment 2

[0033] Example 2 Measuring the Effect of Cobistat on Thrombosis 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 cobistat on inhibiting the thrombus formation of artificial blood vessels induced by the coagulant ADP in vitro

[0036] New Zealand rabbit ear middle artery blood collection (without any anticoagulant, 1ml of venous blood was taken directly, and the bubble in the syringe should be removed, and different concentrations (0.001, 0.01, 0.1, 1 μmol / ml) of cobistat and After being treated with 10μmol / ml coagulant ADP, the blood sample is filled into the ring, and 1m1 blood sample is slowly injected into the tube along one end of the plastic ring, and connected to form a ring at any tim...

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Abstract

The invention discloses application of cobicistat as an anti-HIV drug in preparing an antithrombotic drug. The drug can effectively inhibit platelet aggregation and vitro thrombus formation of artificial blood vessels. The invention relates to the cobicistat as the anti-HIV drug. The cobicistat has the effects of inhibiting New Zealand rabbit platelet aggregation induced by a platelet inducer ADPand the vitro thrombus formation of the artificial blood vessels and can effectively inhibit New Zealand rabbit platelet aggregation induced by Elabela, Apelin-12, Apelin-13 and Apelin-36 as APJ endogenous ligands. The cobicistat is taken as a novel drug for resisting platelet aggregation and thrombosis formation in basic study of thrombotic diseases.

Description

technical field [0001] The invention relates to the drug cobistat, which itself can effectively inhibit platelet aggregation and in vitro thrombus formation induced by the procoagulant ADP; it also inhibits the platelet-promoting effect of APJ endogenous ligands Elabela, Apelin-12, Apelin-17 and Apelin-36 Aggregation, in vitro thrombosis. Background technique [0002] APJ receptor is a transmembrane 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 can be cleaved into active fragments of different amino acid lengths by peptidases: Apelin-12, Apelin-17, and Apelin-36. The Apelin / APJ system is widely distributed in tissues and expressed in cardiovascular, brain and kidney systems. ELABELA is a new endogenous ligand of APJ receptor discovered in 2013. The mat...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61P7/02
CPCA61P7/02A61K31/5377Y02A50/30
Inventor 陈临溪李兰芳胡昊良何璐伍乐乐刘佳琪
Owner NANHUA UNIV
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