Novel application of aurantiamide alcohol ester as MMP-9 inhibitor

A golden amido alcohol ester, MMP-9 technology, applied in medical preparations containing active ingredients, organic active ingredients, bone diseases, etc., can solve problems such as unclear new targeting mechanism, and achieve the effect of great clinical application value

Pending Publication Date: 2020-08-04
YUNNAN AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, other pharmacological activities and possible new targeting mechanisms of AA are still un...

Method used

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  • Novel application of aurantiamide alcohol ester as MMP-9 inhibitor
  • Novel application of aurantiamide alcohol ester as MMP-9 inhibitor
  • Novel application of aurantiamide alcohol ester as MMP-9 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Molecular docking binding experiment of golden amido alcohol ester and MMP-9 protein

[0034] Such as figure 1 As shown, a computer-assisted molecular docking experiment between the drug ligand and the protein receptor was carried out on the golden amido alcohol ester and the MMP-9 protein to further analyze the ligand-receptor interaction mechanism; the binding energy and interaction energy were calculated, and Binding pattern analysis was performed.

[0035] After molecular docking and binding energy calculation, compared with the original ligand inhibitor, the key site of docking is consistent, and the binding energy is -72.0206kcal / mol. The results show that golden amido alcohol ester and MMP-9 protein have better drug-protein Molecular docking binding capacity.

Embodiment 2

[0036] The action activity of embodiment 2 in vitro golden amido alcohol ester

[0037] 1. In vitro osteoclastogenesis assay

[0038] RAW 264.7 cells use DMEM medium, containing 10% fetal bovine serum, 5% penicillin-streptomycin, temperature 37°C, CO 2 The culture was carried out under the condition of 5%. To induce osteoclasts, RAW264.7 cells were cultured on 96-well plates in the presence of RANKL concentration of 50 ng / mL and 5, 10, 25 μM gold amidoalcohol ester. On the 7th day, the cells were fixed, and then TRAP activity was stained according to the protocol of the kit. TRAP-positive multinucleated cells with more than 3 nuclei were considered osteoclasts using a light microscope (IX71; Olympus).

[0039] 2. Western blot analysis

[0040] Western blot was used to determine the level of protein expression. RAW 264.7 cells were seeded into 60mm dishes, 5×10 5 Cells / dish were incubated overnight and then treated with RANKL (50 ng / mL) for 48 hours in the absence or pres...

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Abstract

The invention discloses a new application of aurantiamide alcohol ester as an MMP-9 inhibitor. Under the condition that the aurantiamide alcohol ester has no cytotoxicity to osteoclast precursor cellsRAW 264.7, the capability of differentiation of RAW 264.7 cells induced by RANKL into osteoclasts is remarkably inhibited, and a certain concentration dependence is shown; follow-up research finds that the aurantiamide alcohol ester significantly reduces the expression of MMP-9 in the osteoclast formation process, thereby inhibiting osteoclast differentiation and formation. The invention discloses the application of the aurantiamide alcohol ester in preventing and treating osteolytic diseases, wherein the aurantiamide alcohol ester can be used for preventing and treating osteolytic diseases including bone destruction, osteoporosis and the like together with a medicine prepared from a conventional medicinal carrier. The invention provides a new medicine for preventing and treating osteoporosis, and has a great clinical application value.

Description

technical field [0001] The invention belongs to the technical field of biomedicine extraction. More specifically, it relates to the novel use of golden amido alcohol esters as MMP-9 inhibitors. Background technique [0002] Osteolytic disease refers to a systemic bone disease in which bone density and bone quality decrease and bone microstructure is destroyed due to the increase in the number and activity of osteoclasts, resulting in increased bone fragility and prone to fracture. At present, a large number of literatures have shown that the functional filling of osteoclasts mediated by RANKL is closely related to various types of pathological osteolysis, such as: bone destruction caused by tumors, inflammatory osteolysis, aseptic osteolysis after artificial joint replacement, etc. Sexual prosthesis loosening, postmenopausal osteoporosis, Page's disease, psoriatic arthritis and ankylosing spondylitis, etc. As the global aging population increases, the proportion of osteopo...

Claims

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Application Information

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IPC IPC(8): A61K31/221A61P19/10A61P19/08
CPCA61K31/221A61P19/10A61P19/08
Inventor 杨扬盛军田洋代佳和史崇颖贺水莲
Owner YUNNAN AGRICULTURAL UNIVERSITY
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