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Pharmaceutical application of caffeic acid 3, 4-dihydroxyl phenethylester

A technology of hydroxyphenethyl ester and caffeic acid, which is applied to medical preparations containing active ingredients, pharmaceutical formulas, antineoplastic drugs, etc., can solve problems such as hyperparathyroidism, affect bone strength, and accelerate calcium deposition, and achieve Effects of promoting osteoblast differentiation, inhibiting resorption function, and promoting its function

Inactive Publication Date: 2013-02-20
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term use can lead to an increase in the incidence of breast cancer, or greatly increase the incidence of cardiovascular and cerebrovascular diseases
The second is selective estrogen receptor modulators, such as tamoxifen, which can selectively bind to estrogen receptors on bone cells, but long-term use can lead to endometrial hyperplasia and endometrial cancer
The third is calcitonin, which can inhibit the activity of osteoclasts, reduce the concentration of calcium ions in the blood, promote the formation and activity of osteoblasts, and accelerate calcium deposition. It has a good effect on osteoporotic bone pain, but The effect of this type of drug on inhibiting bone resorption cannot be exerted for a long time, and it can cause hypocalcemia and secondary hyperparathyroidism when used alone, so it needs to be used in combination with calcium agents
The fourth is bisphosphonate drugs, which inhibit bone resorption mediated by osteoclasts and increase bone density. Due to their strong inhibition of bone resorption and long half-life, long-term use will affect bone strength
[0005] Although there are some drugs targeting osteoclasts clinically, they all have problems such as relatively large side effects when used, and fewer drugs targeting both osteoclasts and osteoblasts
There is no report on the treatment of osteoporosis-related diseases by sarcomas

Method used

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  • Pharmaceutical application of caffeic acid 3, 4-dihydroxyl phenethylester
  • Pharmaceutical application of caffeic acid 3, 4-dihydroxyl phenethylester
  • Pharmaceutical application of caffeic acid 3, 4-dihydroxyl phenethylester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 : CADPE inhibits osteoclast precursor cell differentiation

[0030] Principle: Under the stimulation of cytokine M-CSF, bone marrow stem cells will differentiate into osteoclast precursor cells, and at the same time, under the continuous stimulation of cytokines (such as RANKL, M-CSF) Contact and fuse with each other to form multinucleated cells, and then continue to differentiate to form mature osteoclasts with a seal ring structure. The mouse osteoclast precursor cell line RAW264.7 can also differentiate into multinucleated osteoclasts under the action of RANKL cytokine. Mature osteoclasts can be adsorbed on the bone matrix and degrade the bone by analyzing protease, so as to achieve the purpose of metabolizing the bone. By detecting the formation ability of osteoclasts, the inhibitory effect of drugs on osteoclast differentiation and formation can be detected, so that the potential therapeutic effect of drugs on osteoporosis can be analyzed.

[0031] In...

Embodiment 2

[0038] Example 2 : Cytotoxicity test of CADPE on osteoclasts

[0039] Principle: Sulforhodamine B staining is a classic technique aimed at evaluating the toxicity of living cells by quantitatively measuring the total protein synthesis rate in cells by using a protein-binding red dye, ie, colorimetry. As one of the protein stains, sulforhodamine B (SRB), also known as acid red 52 (Acid Red 52), is an anionic dye that binds to protein electrostatics and absorbs at a wavelength of 540nm Peak: The absorbance value is linearly positively correlated with the cell mass.

[0040] The cytotoxicity test method of present embodiment CADPE to osteoclast is as follows:

[0041] BMMs in 96-well plate , after overnight cell attachment, containing M-CSF (20ng / ml) - MEM culture prepared CADPE with concentrations of 0, 0.5 μM, 1 μM, 5 μM, 10 μM, 25 μM to treat the cells for 3 days, and change the medium every other day. After the experiment, the cytotoxicity of CADPE was analyzed by the ...

Embodiment 3

[0043] Example 3 : CADPE inhibits actin filament loop formation

[0044] Principle: When osteoclasts perform the function of resorbing bone, they will form a closed acidic environment in the local area of ​​the surface in contact with the bone, and the formation of this environment depends on a special ring structure. The main component of this structure is Actin, so this structure is called actin ring (actin-ring). Actin ring formation is a prerequisite for bone resorption by osteoclasts. Therefore, the effect of drugs on osteoclast bone resorption can be evaluated by detecting the formation of actin ring structure.

[0045] In this embodiment, CADPE inhibits the formation of actin filament rings and the experimental method is as follows:

[0046] The precursor cells were differentiated into mature osteoclasts under the stimulation of M-CSF (20ng / ml) and RANKL (30ng / ml). Thereafter, the cells were fixed with 4% paraformaldehyde for 10 min and washed three times with PBS....

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Abstract

Belonging to the technical field of medicine application, the invention discloses pharmaceutical application of caffeic acid 3, 4-dihydroxyl phenethylester. A prevention and / or treatment medicine prepared from the caffeic acid 3, 4-dihydroxyl phenethylester (CADPE) can be used for inhibiting osteoclast differentiation, inhibiting an osteoclast bone erosion function, promoting osteoblast differentiation, and promoting an osteoblast bone formation function. The medicine can be used for preventing and / or treating osteoclast activity abnormality caused diseases, which include osteoporosis, rheumatoid arthritis, periodontitis, tooth loss, Paget's disease, rickets, osteoclastoma, myeloma bone disease and cancer bone metastasis caused bone destruction, etc.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical application, and relates to a pharmaceutical use of 3,4-dihydroxyphenethyl caffeic acid, which is used to prepare osteoclast differentiation and function inhibitors containing 3,4-dihydroxyphenethyl caffeic acid And osteoblast differentiation and function promoter drugs. Background technique [0002] Osteoporosis (osteoporosis) is a chronic systemic bone disease caused by multiple factors. It is characterized by a decrease in bone matrix and bone mass per unit volume, thinning of the cortical bone, and the size and number of trabecular bone. All decrease, the bone marrow cavity widens, and the mineral composition in the bone is unbalanced, resulting in increased bone fragility, prone to back pain, bone pain, spinal deformity, and eventually fractures. Osteoporosis is a common disease in women, the number of women is more than men, and it is common in postmenopausal women. With the aging p...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P19/10A61P19/02A61P19/08A61P1/02A61P35/00
Inventor 罗剑吴限汤杰仇文卫刘明耀
Owner EAST CHINA NORMAL UNIV
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