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Application of erianin in preparation of osteoclast differentiation inhibitor

A technology for osteoclast differentiation inhibition, applied in anti-inflammatory agents, bone diseases, non-central analgesics, etc., can solve problems such as lack of osteoclast differentiation inhibition

Active Publication Date: 2021-08-24
SOUTHERN MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no research on its use in the inhibition of osteoclast differentiation

Method used

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  • Application of erianin in preparation of osteoclast differentiation inhibitor
  • Application of erianin in preparation of osteoclast differentiation inhibitor
  • Application of erianin in preparation of osteoclast differentiation inhibitor

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0041] Experimental example 1. The effect of erianin on the cell survival of RAW264.7 cells and mouse bone marrow macrophages (BMMs):

[0042] RAW264.7 or BMMs cells in good growth state were inoculated in 96-well plates. After overnight attachment, the negative control group (Control group) was not added with Erianin, and the drug group was added with 1.95–250nM Erianin. After culturing in a 5% CO2 incubator for 24h, 48h, and 72h, discard the medium, add 100 μl / well MTT solution (0.5mg / ml), and incubate for 4h. Add 150 μl / well DMSO, mix thoroughly with a micro-oscillator at low speed for 10 minutes, and measure the OD value at 570 nm with a TECAN GENios Pro multifunctional microplate reader. The result is as figure 1 , figure 2 .

[0043] Depend on figure 1 , figure 2 It can be seen that within 72 hours, erianin with an in vitro concentration of ≤250nM has no significant effect on the survival of RAW264.7 cells and BMMCs.

experiment example 2

[0044] Experimental Example 2. Effect of Erianin on RANKL-induced differentiation of mouse bone marrow macrophages (BMMs) into osteoclasts:

[0045] BMMs were seeded in 96-well plates, and after adhering to the wall overnight, in addition to the negative control group (Blank group), the positive control group (RANKL group) and the drug group were added with M-CSF and RANKL (the final concentration of M-CSF was 30ng / ml, The final concentration of RANKL was 50ng / ml), and the drug group was simultaneously added with erianin concentrations of 62.5nM, 125nM, and 250nM, and each group had three replicate wells. Change the medium every 2 days. On the 4th day of induction, TRAP staining was observed, photographed under a microscope, and counted as osteoclasts that were positive for TRAP and had more than 3 nuclei (osteoclasts were purplish red and multiple cells fused together). The result is as image 3 , Figure 4 .

[0046] Combined with the results of the cell survival experim...

experiment example 3

[0047] Experimental Example 3. Effect of Erianin on RANKL-induced osteoclast activity:

[0048] Inoculate BMMs cells with the same protocol of osteoclast generation in Experimental Example 2 above and culture them on the Osteo Assay 96-well plate coated with artificial bone slices. On the 7th day of induction, the cells were washed away, observed and photographed with an inverted optical microscope, and photographed through Image- Pro Plus software calculates the percentage of bone resorption area in each well. The result is as Figure 5 , Image 6 .

[0049] The experimental results prove that erianin with concentrations of 62.5nM, 125nM, and 250nM can significantly reduce the area of ​​bone depressions formed by osteoclasts on bone slices, and have an inhibitory effect on the bone resorption activity of osteoclasts.

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Abstract

The invention relates to application of erianin in preparation of an osteoclast differentiation inhibitor. Experiments prove that low-dose erianin can significantly inhibit RANKL and breast cancer induced mouse osteoclast generation and bone resorption activity; meanwhile, low-dose erianin can inhibit osteoclast precursor cells of a patient with breast cancer bone metastasis from generating polykaryotic osteoclasts, so that erianin can be used as an osteoclast differentiation inhibitor drug for treating diseases by an osteoclast differentiation inhibitor. The invention provides a new application of erianin, and also provides a new thought for treating bone destruction related diseases, tumor-induced bone destruction and other diseases.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new medicine application of erianin. Background technique [0002] In the process of maintaining bone remodeling, a dynamic balance is maintained between bone resorption mediated by osteoclasts (OCs) and bone formation mediated by osteoblasts (OBs). However, factors such as estrogen deficiency, elevated inflammatory factors, and tumor cell metastasis to bone will lead to excessive activation of osteoclasts in the body, resulting in osteoporosis, rheumatoid arthritis, osteomyelitis, periodontitis, tumor bone metastasis, etc. Exacerbation of bone destruction. [0003] The population of osteoclast-related bone destruction is very large, and there are hundreds of millions of patients in the world with osteoporosis and rheumatoid arthritis alone. In recent years, with the arrival of population aging, the population base of osteoporosis patients has become larger and larger, and the morbidi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61P19/10A61P35/04A61P29/00
CPCA61K31/09A61P19/10A61P35/04A61P29/00
Inventor 李晓娟郑洁煌邹斌华邓文德
Owner SOUTHERN MEDICAL UNIVERSITY
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