Application of Apelin in preparation of medicine for treating silicosis

A drug and pharmaceutical technology, applied in the field of pharmaceutically active peptides, achieves the effects of good safety, alleviating fibrosis symptoms, and reducing expression levels

Pending Publication Date: 2022-03-01
广东省职业病防治院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] It is known that a variety of lung-related diseases may cause pulmonary fibrosis, but the pathogenesis and pathogenesis of different lung-related diseases are different. Although Apelin can improve the pulmonary fibrosis caused by BPD, but Whether it also works well for other types of lung disease is unknown

Method used

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  • Application of Apelin in preparation of medicine for treating silicosis
  • Application of Apelin in preparation of medicine for treating silicosis
  • Application of Apelin in preparation of medicine for treating silicosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: Therapeutic effect of Apelin on mouse silicosis

[0027] SPF grade C57BL / 6 male mice (6-8 weeks old, body weight 18-25g) were selected, randomly divided into 3 groups (15 mice in each group), and the control group, silicosis group and silicosis + Apelin treatment were respectively set up by the following methods Group.

[0028] Control group: Inject 20 μL of normal saline through the mouse trachea;

[0029] Silicosis group: Inject 20 μL of 250 g / L silica suspension through the trachea of ​​mice by tracheal exposure method;

[0030] Silicosis + Apelin treatment group: Inject 20 μL of 250 g / L silica suspension through the trachea of ​​mice by the tracheal exposure method. From the 3rd day after modeling, mice in this treatment group were intraperitoneally injected with 500 μg / kg of Apelin-13 trifluoroacetate (purchased from Germany sigma company).

[0031] After the above-mentioned groups were set up, conventional animal feeding was carried out; 5 mice in...

Embodiment 2

[0037] Embodiment 2: the influence of different concentrations of Apelin on A549 cytotoxicity

[0038] Control group: A549 cells (human lung cancer cells) were cultured in serum-free GIBCO DMEM high-glucose medium (purchased from Thermo Scientific, USA);

[0039]Apelin administration group: A549 cells (human lung cancer cells) were cultured in serum-free GIBCO DMEM high-glucose medium containing Apelin (Apelin-13 trifluoroacetate) at concentrations of 1, 0.1, 0.01, 0.001, and 0.0001 μM middle.

[0040] After the control group and the Apelin-administered group were placed in a constant temperature incubator for 48 hours, the toxic effects of Apelin at various concentrations on A549 were detected using the CCK-8 kit. Test results such as image 3 Shown: Compared with the control group, Apelin at 0.0001, 0.001, 0.01, and 0.1 μM has no obvious toxic effect on A549 cells.

Embodiment 3

[0041] Example 3: Effect of Apelin on expression level of epithelial-mesenchymal transition (EMT) marker protein regulated by silicon dioxide Control group: A549 cells (human lung cancer cells) were cultured in serum-free medium;

[0042] Silica exposure group: A549 cells (human lung cancer cells) were cultured in serum-free medium containing silica at a concentration of 100 μg / mL;

[0043] Apelin+silica exposure group: A549 cells (human lung cancer cells) were cultured in serum-free GIBCODMEM containing 100 μg / mL silica and 0.1, 1 μM Apelin (Apelin-13 trifluoroacetate) in high glucose medium.

[0044] The above groups were placed in a constant temperature incubator for 48 hours, and the changes in the protein levels of epithelial-mesenchymal transition (EMT) markers were detected by Western blotting. The detection results were as follows: Figure 4 shown.

[0045] Figure 4 The results showed that: compared with the control group, the protein expression of the epithelial m...

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Abstract

The invention belongs to the technical field of active peptides of medicines, and discloses application of Apelin in preparation of medicines for treating silicosis. Tests show that Apelin has a good curative effect on relieving diseases of silicosis, has a good medicinal value prospect, and can be developed into a novel medicine for treating silicosis.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutically active peptides, and in particular relates to the application of Apelin in the preparation of medicines for treating silicosis. Background technique [0002] Apelin (Apelin / APLN) is a biologically active peptide, which was first isolated, extracted, purified and named from the gastric secretion of cattle in 1998. The human Apelin gene is located on the X chromosome, and its precursor peptide consists of 77 active amino acid residues, which can be cut into active peptide molecular fragments of different lengths by proteolytic enzymes, among which Apelin-13 and [Pyr1]Apelin- 13 is the most common subtype in human plasma, and its receptor is G protein-coupled receptor-angiotensin Ⅰ type 1 receptor-related protein. [0003] In recent years, it has been found that injection of Apelin can reduce the bronchopulmonary dysplasia and pulmonary fibrosis of neonatal rats exposed to hyperoxia, reduce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/10A61P11/00
CPCA61K38/10A61P11/00
Inventor 赵娜黄永顺瞿红鹰
Owner 广东省职业病防治院
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