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Application of isopentenyl dihydroflavonoids in the field of prevention and treatment of bone diseases

A technology of prenyl dihydroflavonoids and compounds, applied in the preparation of bone disease prevention and treatment drugs and health care products, in the field of prenyl dihydroflavonoids, can solve the problem of curative effect, unclear side effects, and difficult quality control , the mechanism of action is not clear, etc.

Active Publication Date: 2019-11-19
THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although there are many chemical studies on the monomer components in drynaria, such as separation and identification, the pharmacological research, especially the research on the mechanism of action, is not deep enough. Most of the active reports on drynaria mainly focus on the crude extraction of drynaria. thing
However, since the drynaria crude extract contains complex and diverse chemical components, its mechanism of action is mostly unclear. If the crude drynaria extract is used directly as a therapeutic drug, there may be risks such as unclear curative effect, side effects, and difficult quality control.

Method used

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  • Application of isopentenyl dihydroflavonoids in the field of prevention and treatment of bone diseases
  • Application of isopentenyl dihydroflavonoids in the field of prevention and treatment of bone diseases
  • Application of isopentenyl dihydroflavonoids in the field of prevention and treatment of bone diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation method of compound 1 and compound 2 comprises the following steps:

[0054] S11. Take 50 kg of rhizome of Quercus fern (DF), heat and reflux extraction with 8 times the amount of 60% ethanol for 2 hours, extract twice in total, evaporate the solvent to 37L under reduced pressure (take 100mL, evaporate to dryness under reduced pressure, weigh about 10.3 g, equivalent to the total extract (DF) 3.8kg, take out 2000mL, evaporate to dryness, freeze-dry, and keep it for animal experiments). Steam until the macroporous resin on the alcohol-free liquid extract (￠25×150cm);

[0055] S12. Use 0, 30% (v / v), 50% (v / v), 70% (v / v), 95% (v / v) ethanol water to elute sequentially (about 200L / gradient), The 95% ethanol elution fraction of the solvent was recovered under reduced pressure, and a total of 72 g was obtained (shown by activity screening that this fraction has anti-osteoporosis activity);

[0056] S13. Take 15 g of 95% ethanol eluting part and separate it wit...

Embodiment 2

[0075] Effects of compound 1 and compound 2 obtained in Example 1 on the catalytic activity of cathepsin K.

[0076] The Cathepsin K inhibitor screening kit was used for verification. Since Cathespin K can selectively cut off the linkage between its polypeptide substrate and AFC, a fluorescent AFC fragment product can be generated. By detecting the fluorescence intensity of its degradation product AFC, the test compound Inhibition of Cathepsin K protein activity for quantitative detection. Dissolve Cathepsin K (Human Recombinant) protein with reaction buffer, prepare Cathepsin K protein solution, mix and evenly add to black 96 microwell plate at the ratio of 1 μl Ctsk protein solution, 1 μl Ctsk reaction solution, and 48 μl reaction buffer per well . Then 10 μl of the positive drug compound FF-FMK at the concentration to be tested and different concentrations of compound 1 (expressed as SG) and compound 2 (expressed as KF) were added, mixed evenly with the protein mixture, an...

Embodiment 3

[0082] Effects of Compound 1 and Compound 2 on the Survival of Osteoclast Precursor Cells, Macrophage Cell Line RAW264.7

[0083] The effect of compound 1 and compound 2 isolated in Example 1 on the survival of osteoclast precursor cells was evaluated by the cell proliferation activity of osteoclast precursor cell macrophage cell line RAW264.7.

[0084] RAW264.7 cells were inoculated in 96-well plates (1×104 cells / well), cultured in DMEM medium containing 10% FBS (fetal bovine serum) and 1% antibiotics, and after 24 hours (37°C, humidity 95 %, 5% CO2).

[0085] One day later, different concentrations of compound 2 (5-50 μM), compound 1 (5-50 μM), negative control group (1% ethanol) were added and replaced with new culture medium, co-cultivated for four days, and replaced with a new medium every two days. culture medium and drugs.

[0086] After the fourth day, discard the original nutrient solution, and prepare 0.2mg / ml 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxybenzene...

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Abstract

Being applicable to the field of natural drugs, the invention provides application of a prenylflavanone compound with a structure shown as formula I in the specification in preparation of drugs and health care products for control of bone diseases. Specifically, the prenylflavanone compound comprises a compound 1 with R1 shown as the specification and R2 as H, and a compound 2 with R1 as H and R2 shown as the specification.

Description

technical field [0001] The invention belongs to the field of natural medicines, and relates to the application of prenyl dihydroflavonoids in the field of prevention and treatment of bone diseases, in particular to the application of prenyl dihydroflavonoids in the preparation of bone disease prevention and treatment drugs and health care products. Background technique [0002] Osteoporosis (OP) is a systemic metabolic skeletal disease characterized by decreased bone mass and destruction of bone microstructure, which is manifested by increased bone fragility and easily induced fractures. According to statistics, at present, about 200 million people in the world suffer from osteoporosis, and its incidence rate ranks seventh among common diseases and frequently-occurring diseases. The prevalence rate of osteoporosis is 8.8%, ranking the third in the prevalence rate of chronic diseases among Chinese residents. At present, about 69.44 million people over the age of 50 suffer fr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P19/02A61P19/10A61P19/08A61P35/00A61P35/04C07D311/32C07D311/40A23L33/10
CPCA23V2002/00A61K31/352C07D311/32C07D311/40A23V2200/306
Inventor 黄文秀姚新生邱佐成董晓莉戴毅
Owner THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST
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