Application of GPR31 inhibitor in pharmacy

An inhibitor and a technology for preparing drugs, applied in the field of biomedicine, can solve the problems of increasing the incidence of sudden death, increasing myocardial oxygen consumption, reducing myocardial compliance and the like

Active Publication Date: 2017-11-21
武汉惠康达科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although early myocardial hypertrophy is conducive to maintaining normal heart function, but because myocardial hypertrophy itself can increase myocardial oxygen consumption and reduce myocardial compliance, it will lead to heart failure and increase the incidence of sudden death for a long time

Method used

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  • Application of GPR31 inhibitor in pharmacy
  • Application of GPR31 inhibitor in pharmacy
  • Application of GPR31 inhibitor in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0185] Example 1 GPR31 expression changes in liver tissue at different times of ischemia

[0186] The C57 mice were randomly divided into 6 groups, namely the Sham group and the operation group (divided into 5 different time points: ischemia 5min, 10min, 20min, 40min, 60min), and the liver tissues of the mice in the operation group and the Sham group were collected. , Western blot detection of GPR31 protein content changes in liver tissue of each group (3 independent repeated experiments). The primary antibody used for WB is: Anti-GPCR GPR31antibody (ab75579; Abcam), and the secondary antibody is: PeroxidaseAffiniPure goat anti-rabbit-IgG (H+L) (#111-035-003; JacksonLaboratory). GAPDH was used as the control standard for expression detection.

[0187] The result is as figure 1 As shown, the GPR31 band was almost invisible in the WB results of the Sham group, and the GPR31 protein band became more and more obvious in the operation group with the prolongation of ischemia time....

Embodiment 2

[0188] Example 2 Effect of GPR31 overexpression on H / R treatment-induced L02 cell injury and inflammatory response

[0189] L02 cells were divided into 4 groups: GFP control group, GPR31 control group, GFP H / R group, and GPR31H / R group. Adherent L02 cells were transiently transfected with corresponding plasmids, and then treated with H / R (hypoxia for 6 hours and reoxygenation for 6 hours) after 24 hours. After the plasmid transfection was completed, the total protein of the cells was extracted, and the overexpression of GPR31 was detected by Western blot (3 independent repeated experiments, each with 3 repetitions). After H / R treatment, the release of LDH in the medium was detected (6 replicates per group) to evaluate the effect of GPR31 overexpression on H / R-induced hepatocyte injury; RNA was extracted for RT-PCR analysis (2 independent The experiment was repeated, with 3 repetitions each time), and the changes in mRNA levels of inflammation-related cytokines and chemokines ...

Embodiment 3

[0195] Example 3 Effect of GPR31 overexpression on the activity of H9C2 cells induced by H / R treatment

[0196] H9C2 cells were divided into 4 groups: GFP control group, GPR31 control group, GFP H / R group, and GPR31H / R group. The corresponding recombinant lentivirus liquids were used to infect the cultured H9C2 cells, and H / R treatment was performed after 24 hours (hypoxia for 1 hour and reoxygenation for 6 hours). After the plasmid transfection was completed, the total protein of the cells was extracted, and the overexpression of GPR31 was detected by Western blot (3 independent repeated experiments). Cell viability was detected after H / R was completed (6 replicates per group). Taking the detection result of the GFP control group as 1, the ratios of the other groups compared with this group were calculated.

[0197] WB test results such as Figure 5 As shown, compared with the GFP group, the GPR31 overexpression histone band was significantly enhanced, that is, the GPR31 o...

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Abstract

Experiment researches find that the expression quantity of GPR31 protein is gradually increased along with the prolonging of tissue ischemia time, and a positively related relationship exists between the expression quantity of GPR31 protein and tissue ischemia reperfusion injury severity. The overexpression of GPR31 can increase the activity of liver cells, cardiac muscle cells and kidney cells caused by H/R treatment. Moreover, the decrease of GPR31 expression in the liver cells can inhibit cellular lipid accumulation caused by palmitate and oleic acid stimulation. The overexpression of GPR31 in the cardiac muscle cells can increase cardiac hypertrophy caused by Angiotensin II. Therefore, the GPR31 inhibitor can be used for preparing drugs, and the drugs can be used for curing related diseases of ischemia reperfusion injury, cardiac hypertrophy and related diseases and liver metabolism diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to the use of GPR31 inhibitors in the preparation of medicines, and the medicines are used to treat ischemia-reperfusion injury and related diseases, myocardial hypertrophy and related diseases, inflammatory diseases of the heart, fat Metabolic abnormalities and related diseases, etc. Background technique [0002] G protein-coupled receptors (GPCRs) are a class of membrane proteins with seven transmembrane structures, with more than 800 family members, and are the largest class of membrane proteins in mammalian genomes. In the human body, GPCRs are widely expressed in the cardiovascular system, immune system, nervous system and other tissues and organs, and participate in growth and development and various pathophysiological processes. Due to its wide distribution and diverse functions, GPCR family molecules are regarded as the most potential drug development targets...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P9/10A61P9/00A61P3/06A61P3/00A61P3/04A61P3/10A61P1/16A61P13/12C12N15/85C12N15/867A61K31/7105
CPCA61K31/7105A61K45/00A61P9/10C12N15/113C12N15/86C12N2310/14C12N2740/15043A61K45/06C12N15/85
Inventor 李红良张晓晶
Owner 武汉惠康达科技有限公司
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