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Use of crataegolic acid and derivatives thereof in preparation of therapeutic and/or preventive medicines for inhibiting osteoclast differentiation and function

A technology for inhibiting osteoclast and cell differentiation, which is applied in the application field of maslinic acid and its derivatives in the preparation of therapeutic and/or preventive medicines for inhibiting the differentiation and function of osteoclasts, and can solve the problem that no maslinic acid inhibits osteoclast differentiation. and function, no maslinic acid osteoporosis drug and other issues

Active Publication Date: 2011-10-12
BIORAY LABORATORIES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report about maslinic acid inhibiting osteoclast differentiation and function so far, and there is no report of maslinic acid as a drug for the preparation of osteoporosis

Method used

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  • Use of crataegolic acid and derivatives thereof in preparation of therapeutic and/or preventive medicines for inhibiting osteoclast differentiation and function
  • Use of crataegolic acid and derivatives thereof in preparation of therapeutic and/or preventive medicines for inhibiting osteoclast differentiation and function
  • Use of crataegolic acid and derivatives thereof in preparation of therapeutic and/or preventive medicines for inhibiting osteoclast differentiation and function

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: cytotoxicity test

[0022] Experimental principle: In living cells, NADPH dehydrogenase in mitochondria converts MTS tetrazolium salt into a colored substance soluble in cell culture fluid. The more living cells, the more colored salts will be produced. Therefore, under certain conditions, the number of living cells is directly proportional to the amount of the substance produced. Therefore, the number of living cells can be indirectly reflected by detecting the absorption value of the substance at 490nm. This method can be used to evaluate the effect of drugs on the proliferation ability of cells.

[0023] Methods: Osteoclast precursor cells were inoculated into 96-well culture plate, 3000 cells / well, and control group and drug-dosed group were set up. When the cells are attached to the wall, add different concentrations of drugs for treatment. After 72 hours, add 20 microliters of cellTiter96 Aqueous cell proliferation detection reagent, incubate for 1...

Embodiment 2

[0025] Example 2: Maslinic acid inhibits differentiation of osteoclast precursor cells

[0026] Principle: Under the induction of differentiation cytokines (such as RANKL, M-CSF), mononuclear osteoclast precursor cells can gradually fuse and differentiate into multinucleated mature osteoclasts. Osteoclast precursor cells do not have the ability to dissolve osteolysis, only differentiated mature osteoclasts have the ability to dissolve stubborn cells, therefore, the differentiation level of osteoclasts can reflect their osteolytic ability.

[0027] Methods: Osteoclast precursor cell lines or primary isolated and cultured mouse osteoclast precursor cells were inoculated into 48-well culture plates, 3000 cells / well. Set up a control group, a single-dosing group and a double-dosing group. After the cells adhered to the wall overnight, different doses of maslinic acid and / or 50 ng / ml RANKL were added, and the culture continued for 3 to 5 days. After the cells with single addition...

Embodiment 3

[0029] Example 3: Maslinic acid inhibits osteoclast bone resorption test (pits assay)

[0030] Principle: Mature osteoclasts can dissolve and resorb bone, leaving imprints on the surface of bone. The degree of damage to the bone surface directly reflects the ability of osteoclasts to resorb bone. The principle of this experiment is to use this feature to differentiate osteoclast precursors on the surface of bone slices, and to detect and analyze the ability of these differentiated cells to dissolve bone slices.

[0031]Method: Osteoclasts were inoculated on the bone slices placed in a 48-well plate (3000 / piece / well). After the cells adhered to the wall overnight, different doses of maslinic acid and 50ng / ml RANKL were added to induce cell differentiation. control group. After 3 to 4 days, wait until the cells in the RANKL group are fully differentiated and mature into multinucleated cells, and after another 6 to 12 hours, remove the cells on the surface of the bone slices, s...

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Abstract

The invention provides use of crataegolic acid and derivatives thereof in preparation of medicines for inhibiting osteoclast differentiation and function and osteoclast activity associated diseases. The invention also provides the use of a composition, which contains an effective dose of crataegolic acid of formula (I) and derivatives thereof and pharmaceutically acceptable ingredients, in the preparation of medicines for inhibiting osteoclast differentiation and function.

Description

technical field [0001] The present invention relates to a medicine for inhibiting osteoclast differentiation and its application, in particular to the application of maslinic acid and its derivatives in the preparation of osteoporosis medicine related to the increase of osteoclast activity. Background technique [0002] Osteoporosis (osteoporosis) is a chronic systemic bone disease caused by multiple factors, which is characterized by decreased bone mass and destruction of bone microstructure. Before the fracture occurs, there are usually no special clinical manifestations. The disease is more common in women than in men and is common in postmenopausal women and the elderly. With the increase of the elderly population in my country, the incidence of osteoporosis is on the rise, and it is a health problem worthy of attention in my country and even in the world. The etiology of osteoporosis is not particularly clear. Previous studies have shown that osteoclasts play an impo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P19/10A61P19/02A61P19/04A61P29/00A61P1/02A61P19/08
Inventor 罗剑刘明耀李成海杨正峰仇文卫汤杰
Owner BIORAY LABORATORIES INC
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