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Application of acrylophenone amide derivates to preparation of anti-osteoporosis medicine

A phenyrolactone ester amide, anti-osteoporosis technology, applied in the direction of drug combination, bone disease, pharmaceutical formulations, etc., can solve the problem of not being able to reduce the risk of atypical fractures, and achieve the purpose of inhibiting osteoclast differentiation, structural Simple, easy-to-composite effects

Active Publication Date: 2017-06-13
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention discovers new anti-osteoporosis drugs based on the new target RANKL signaling pathway, in order to overcome the problem that existing osteoporosis treatment drugs cannot reduce the risk of atypical fractures, and provides a class of phenyllactyl enyl ester amide derivatives in Application in the preparation of anti-osteoporosis drugs

Method used

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  • Application of acrylophenone amide derivates to preparation of anti-osteoporosis medicine
  • Application of acrylophenone amide derivates to preparation of anti-osteoporosis medicine
  • Application of acrylophenone amide derivates to preparation of anti-osteoporosis medicine

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Experimental program
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Effect test

Embodiment 1

[0039] Embodiment 1: computer drug screening

[0040] Compound library preprocessing: The compound library is a self-prepared compound database. The compound library is processed as follows: removing ions and complexing water molecules, adding charges, protonating, and generating three-dimensional conformations. These processes are completed in the drug design software package DiscoveryStudio 2.5. Wherein the protonation is carried out under the condition of pH 6.5-8.5. Prepare small molecule libraries for virtual screening.

[0041] A three-dimensional similarity search was performed with known anti-osteoporosis drugs and osteoclast differentiation inhibitors to find compounds with a similarity higher than 80%. In the present invention, the computer drug screening program is the independent research and development program WEGA of the laboratory, and it is predicted that there are 44 potentially active compounds in the compound reserve library of the laboratory. The 44 co...

Embodiment 2

[0042] Example 2: Toxicity assay of compound cells

[0043] S1. Cell culture.

[0044] RAW264.7 cells were cultured in vitro. DMEM high-glucose medium containing 10% fetal bovine serum was used for routine maintenance and passage at 37°C and 5% carbon dioxide concentration.

[0045] S2. Compound intervention.

[0046] Collect logarithmic phase cells and make the cell suspension concentration 1×10 5 cells / ml, added to 96-well cell culture plate. After culturing in a carbon dioxide incubator for 24 hours, the culture solution was replaced with a medium containing different compound concentrations, and the culture was continued for 2 days, and the cytotoxicity was detected on the 3rd day. The compounds to be tested were prepared as solutions at different concentrations using DMSO. Three parallel wells were set up for each concentration, and a control group without compound treatment was set up for comparison.

[0047] S3. Test method.

[0048] MTT [3-(4,5-dimethylthiazole-...

Embodiment 3

[0054] Example 3: Osteoclast Differentiation Inhibition Experiment

[0055] S1. Cell culture.

[0056] RAW264.7 cells were cultured in vitro. DMEM high-glucose medium containing 10% fetal bovine serum was used for routine maintenance and passage at 37°C and 5% carbon dioxide concentration.

[0057] S2. Compound intervention.

[0058] Collect logarithmic phase cells and make the cell suspension concentration 2×10 4 cells / ml, added to 96-well cell culture plate. After culturing in a carbon dioxide incubator for 24 hours, the culture solution was replaced with a medium containing 100ng / ml RANKL and different compound concentrations, and the culture continued for 5 days, and the medium with the same RANKL concentration and compound concentration was replaced every 2 days. Osteoclasts were stained by TRAP staining method. Three parallel wells were set up for each concentration, and a control group without compound treatment was set up for comparison.

[0059] S3. Test method....

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Abstract

The invention relates to medicine application, and specifically discloses application of acrylophenone amide derivates to the preparation of anti-osteoporosis medicine. The structural formula of the acrylophenone amide derivates is shown as formula (I) or formula (II). The compound is different from a molecular skeleton of medicine for preventing and treating osteoporosis used clinically at present, does not belong to a phosphate compound, and is neither estrogen medicine. Cytology experiment researches indicate that the compound can inhibit osteoclast differentiation so as to be of an anti-osteoporosis effect; cytotoxicity tests indicate that the compound is little in toxicity, and can be used for preventing and treating related diseases, particularly osteoporosis, caused by osteoclast prosoplasia.

Description

technical field [0001] The present invention relates to the technical field of pharmaceutical use, in particular to the application of a class of phenyllactyl enylamide derivatives in the preparation of anti-osteoporosis drugs. Background technique [0002] Osteoporosis (Osteoporosis, referred to as OP) is a systemic and systemic bone disease characterized by decreased bone mass and destruction of bone tissue microstructure leading to increased bone fragility and fracture risk. The main clinical manifestations and signs are pain, followed by shortened body length, hunchback, fractures and respiratory system disorders. Epidemiological research shows that among people over 50 years old, about 50% of women and 20% of men are at risk of fracture (Rachner, Khosla et al. 2011). According to the data of the National Bureau of Statistics: by 2050, the population over 50 years old in my country will be nearly half (49%) of the national population, about 636 million. It is estimated ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/381A61K31/428A61P19/10
CPCA61K31/352A61K31/381A61K31/428
Inventor 顾琼徐峻黄丹娥
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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