Novel application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide and medicine thereof

A technology of phenylethyl and formamide, applied in the field of medicine, can solve the problems of aggravating acute lung injury, edema, and increased permeability of pulmonary vascular endothelial cells, etc.

Active Publication Date: 2021-04-30
ANHUI MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved by the present invention is to solve the problem that HIF-1α promotes the production of inflammatory cytokines, induces the generation of inflammatory storm in acute lung injury; and induces the increase of permeability of pulmonary vascular endothelial cells to cause edema and aggravate acute lung injury.

Method used

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  • Novel application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide and medicine thereof
  • Novel application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide and medicine thereof
  • Novel application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide and medicine thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] The test of compound N-(2-phenylethyl)-5-phenyl-pyridine-2-carboxamide on LPS-induced RAW264.7 macrophages:

[0078] (1) MTT method: RAW264.7 macrophages were seeded in a 96-well plate at a seeding density of about 4000 cells / well. Cultivate for 24 hours, add different concentrations of compound N-(2-phenylethyl)-5-phenyl-pyridine-2-carboxamide and solvent control DMSO in groups, respectively control group (Control), drug group with different concentrations (compound The concentration of N-(2-phenylethyl)-5-phenyl-pyridine-2-carboxamide is 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM), DMSO solvent control group. Continue to cultivate for 24h. Add 5g·L to each well after culturing -1 20 μL of MTT solution and continue to incubate for 4 h. Aspirate the medium, add 150 μL of DMSO to each well, shake and mix well. Measure the OD value of each well at 492nm with a microplate reader, and record the results. Cell viability was plotted against dose. Result c...

Embodiment 2

[0087] Compound N-(2-phenylethyl)-5-phenyl-pyridine-2-carboxamide was tested on animal model of acute lung injury:

[0088] Male SD rats weighing 200g-250g were adaptively cultured for 1-2 days, and divided into normal group (Control), model group (LPS5mg / kg), low-dose group (LPS5mg / kg+25mg / kg), middle-dose group (LPS5mg / kg+50mg / kg), high-dose group (LPS5mg / kg+100mg / kg), positive drug control group (LPS5mg / kg+2mg / kgYC-1) 6-10 in each group. The SD rats were intraperitoneally injected with the above-mentioned doses of drugs for 3 days, and the normal group was injected with the same volume of solvent as control. On the 4th day, the model was established by instilling LPS into the trachea. To establish the ALI model, the rats were anesthetized by intraperitoneal injection of pentobarbital sodium (50 mg / kg), then intratracheal injection of LPS (5 mg / kg, 200 ul), and the rats in the control group were given 200 ul of normal saline in the trachea. Rats were sacrificed twenty-four...

Embodiment 3

[0091] The obtained total inflammatory cell mass was resuspended with incomplete medium RPMI1640 by pipetting, divided into 15ml centrifuge tubes, and centrifuged at 1500rpm×10min, and the supernatant was discarded. Count cells according to 5 x 10 5 Inoculate 6-well plates. The cells were suspended in RPMI1640 medium with 10% FBS, and cultured in an incubator for 2 hours. Aspirate the cell suspension, wash with RPMI1640 medium, remove unattached cells, and add complete medium RPMI1640. After thorough mixing, incubate for 24 hours in a cell culture incubator at 37°C, 5% CO2, and saturated humidity to make the macrophages adhere to the wall. Shake the flask to suspend non-adherent cells and aspirate the cell suspension. Wash with PBS three times to remove unattached cells. The macrophages were washed three times with RPMI1640 culture medium, and the cells were suspended in RPMI1640 medium containing 10% FBS to obtain purified primary alveolar macrophages. Cell identificatio...

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Abstract

The invention discloses a novel application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide. The novel application of the medicine provided by the invention is the application of N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide in preparing the medicine for treating / preventing lung injury of mammals. Research finds that N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide has a certain prevention and treatment effect on rat ALI caused by LPS and has an effect of inhibiting inflammatory reaction on RAW264.7 macrophages stimulated by LPS, and the action mechanism can regulate expression of IL-6 and IL-1beta, and is also related to inhibition of hypoxia inducible factor HIF-1alpha by N-(2-phenylethyl)-5-phenyl-pyridine-2-formamide and glycolysis and activation of an acid-sensitive ion channel ASIC1a; researches show that N-(2-phenylethyl)-5-phenyl-pyridine-2-formyl can relieve lung tissue injury caused by LPS, improve respiratory metabolism functions of rats with lung injury, improve pulmonary edema of the rats with lung injury, relieve inflammatory response and inhibit inflammatory diseases related to ASIC1a.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the new application of N-(2-phenylethyl)-5-phenyl-pyridine-2-carboxamide and its medicine. Background technique [0002] In recent years, the morbidity and mortality of pneumonia have been increasing. At present, the drugs used to treat lung injury mainly include glucocorticoids, drugs that inhibit inflammatory factors, anti-inflammatory drugs, and antioxidants. Although there are many types of therapeutic drugs, specific drugs and specific treatment methods have not yet been developed, and commonly used glucocorticoids and anti-inflammatory drugs have obvious side effects. Therefore, there is an urgent need to develop drugs for preventing and treating lung injury with low side effects to reduce lung injury mortality and improve prognosis. [0003] Lung injury is a thoracic surgical disease, including severe chest trauma, inhalation of substances harmful to the lungs (toxic ga...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61P11/00A61P29/00A61P31/00
CPCA61K31/44A61P11/00A61P29/00A61P31/00
Inventor 黄艳刘明明杜娜王媛媛胡成穆徐涛吴文勇臧洪梅孟晓明吴繁荣朱月琴潘学胜
Owner ANHUI MEDICAL UNIV
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