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Application of epoxidized diene as osteoclast differentiation inhibitor

A technology of epoxydiene and chemical formula, applied in the application field of epoxydiene as osteoclast differentiation inhibitor, can solve the problems of unreported physiological activity of osteoporosis and the like

Inactive Publication Date: 2013-12-25
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound epoxydiene was first reported in 1999 (Cai et al., Tetrahedron Letters, 1999, 40, 1479-1482). It was isolated from the fermentation broth of a rare fungus OS-F66617, but the literature did not report that it has Physiological activity for treating osteoporosis

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  • Application of epoxidized diene as osteoclast differentiation inhibitor
  • Application of epoxidized diene as osteoclast differentiation inhibitor
  • Application of epoxidized diene as osteoclast differentiation inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1, epoxy diene cytotoxicity experiment

[0024] Detection of Cytotoxicity of Epoxydiene Using MTT Assay

[0025] The test method is as follows:

[0026] Mouse C57 / BL6 bone marrow-derived macrophages (7×10 3 Cells / well) were inserted into 96-well culture plate and cultured overnight. The next day, different concentrations of MED (0.5, 1, 5, 10 μmol / L) were added for 72 hours, and then MTT was added to a final concentration of 0.5 mg / ml for 4 hours. The absorbance at 560nm (OD 560 ).

[0027] The MTT assay method can reflect the growth of the cells, so by comparing the OD 560 Value to judge whether MED has cytotoxicity to bone marrow-derived macrophages.

[0028] The test results are as follows:

[0029] For the results of the MTT method, see figure 1 . The test results show that epoxydiene has no cytotoxicity to bone marrow-derived macrophages in the concentration range of 0.5-10 μmol / L.

Embodiment 2

[0030] Example 2, the effect of epoxydiene in inhibiting the differentiation of osteoclasts

[0031] The present invention detects the role of MED in the osteoclast differentiation process through the tartrate-resistant acid phosphatase (TRAP) staining experiment technique.

[0032] The test method is as follows:

[0033] 1) MED concentration gradient:

[0034] Mouse C57 / BL6 bone marrow-derived macrophages (2×10 4 cells / well) into a 48-well culture plate, after culturing overnight, RANKL was added to a final concentration of 50ng / mL, and different concentrations of MED (1, 2.5, 5μmol / L) were added at the same time, and the effect of MED on osteoclasts was observed after stimulation for 96h The impact of differentiation.

[0035] 2) MED action time:

[0036] Mouse C57 / BL6 bone marrow-derived macrophages (2×10 4Cells / well) were inserted into 48-well culture plate, after culturing overnight, RANKL was added to a final concentration of 50ng / ml, 5μmol / LMED was added after RANK...

Embodiment 3

[0039] Example 3. Epoxydiene inhibits the expression level of osteoclast characteristic gene mRNA

[0040] The test method is as follows:

[0041] Mouse C57 / BL6 bone marrow-derived macrophages (2×10 5 Cells / well) were inserted into 6-well culture plate, after overnight culture, RANKL was added to a final concentration of 50ng / mL, and MED (5μmol / L, DMSO was used as blank control) was added to stimulate 96h, and the cellular RNA was extracted and detected by real-time fluorescence Quantitative PCR was used to detect the mRNA expression levels of osteoclast differentiation characteristic genes such as tartrate-resistant acid phosphatase (TRAP), cathepsin K (Cathepsin K) and calcitonin receptor (Calcitonin Receptor).

[0042] The test results are as follows:

[0043] The test result of embodiment 3 sees Figure 6-8 . The test results show that MED can inhibit the mRNA expression levels of osteoclast differentiation characteristic genes such as osteoclast TRAP, Cathepsin K, and...

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Abstract

An application of epoxidized diene as an osteoclast differentiation inhibitor relates to an epoxidized diene compound. The invention provides the application of epoxidized diene as the osteoclast differentiation inhibitor in preparation of drugs for treating osteoporosis, especially for treating osteoporosis caused by estrogen deficiency. The compound can be separated and obtained from fungi fermentation products and also can be obtained by chemical synthesis. It is confirmed by pharmacological experiments that epoxidized diene can inhibit nuclear factor kappa B receptor activator ligand (RANKL) induced differentiation of osteoclasts, and inhibits the expression of tartrate-resistant acid phosphatase (TRAP), cathepsin K (Cathepsin K), calcitonin receptor (Calcitonin Receptor) and other osteoclast differentiation characteristic genes by inhibiting the expression of osteoclast key integration factor activated T cells nuclear factor c1 (NFATc1).

Description

technical field [0001] The invention relates to an epoxy diene compound, in particular to the application of an epoxy diene as an inhibitor of osteoclast differentiation. Background technique [0002] Osteoporosis is a systemic degenerative disease of skeletal structure characterized by low bone mass and degeneration of bone tissue microarchitecture, which increases bone fragility and is prone to fractures, including primary and secondary osteoporosis. Typical bone characteristics of osteoporosis are thin cortical bone, increased voids, sparse trabecular bone, and disorderly arrangement. Factors causing osteoporosis include endocrine factors, nutritional factors, physical factors, immune factors, genetic factors and so on. Among them, postmenopausal osteoporosis in women is mainly due to the decrease of cancellous bone mass caused by estrogen deficiency, which accelerates bone remodeling and causes brittle bone structure. Therefore, the currently commonly used osteoporosis...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61P19/10
Inventor 俞春东朱敬伟陈强赵扬莫萍丽沈月毛
Owner XIAMEN UNIV
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