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Application of 2-bromopalmitate in preparation of drugs for prevention and treatment of bone loss related diseases

A bromopalmitic acid, bone loss technology, applied in the field of medicine, can solve the problems of kidney toxicity, mandibular osteonecrosis, transient "flu-like" symptoms, etc.

Inactive Publication Date: 2020-10-20
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of bisphosphonates has gastrointestinal adverse reactions, transient "flu-like" symptoms, renal toxicity, and the risk of osteonecrosis of the jaw and atypical femoral fractures
Antiosteoporotic drugs such as calcitonin, estrogen receptor modulators (raloxifene), menopausal hormone therapy, parathyroid hormone analogs (teriparatide), and RANKL monoclonal antibody (denosumab) are all There are different indications, usage, dosage, and side effects, and some drugs are too expensive to be widely used

Method used

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  • Application of 2-bromopalmitate in preparation of drugs for prevention and treatment of bone loss related diseases
  • Application of 2-bromopalmitate in preparation of drugs for prevention and treatment of bone loss related diseases
  • Application of 2-bromopalmitate in preparation of drugs for prevention and treatment of bone loss related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: 2--BP inhibits osteoclast differentiation without significant cytotoxicity

[0024] (1) Isolation and culture of primary bone marrow-derived monocyte-macrophage BMMs

[0025] Take a C57BL / 6 mouse aged 5 to 8 weeks, put it to death by pulling its neck, soak it in 75% medical alcohol for 3 minutes, dissect the lower limbs of the mouse in a clean workbench, separate the skin, fascia, and knee and hip joint capsules, The mouse femur and tibia were obtained and placed in a bacterial culture dish previously added with sterilized phosphate-buffered saline. Use sterile scissors to cut the upper end of the femur and the lower end of the tibia, separate the bone marrow by centrifugation at 10,000 rpm, add 2ml of red blood cell lysate to resuspend the bone marrow, and let stand for 5 minutes to lyse the red blood cells. Then centrifuge horizontally at room temperature (1000rpm, 5 minutes), discard the liquid, add 10ml of complete Alpha MEM culture solution containing 3...

Embodiment 2

[0034] Example 2: 2-BP inhibits the expression of related characteristic genes in the process of osteoclast differentiation

[0035] (1) Cell treatment and RNA collection and separation

[0036] A control group and 3 drug-treated groups were set up, with 3 replicate wells in each group, and mononuclear macrophages were planted in a 6-well plate (40×10 4 cells / well), the next day, the culture medium was replaced with complete Alpha MEM medium containing 50ng / ml RANKL and 30ng / ml M-CSF, and 6.25, 12.5, 25μM 2-BP were added to the drug treatment group, and the control group Add the same amount of dimethyl sulfoxide solvent as the 25 μM 2-BP group, change the medium every other day, culture for 6 days, and terminate when the control group has obviously mature and hypertrophic osteoclasts. Use the RNA extraction kit to extract the total RNA, after measuring the concentration, take 500ng RNA reaction system to synthesize cDNA. The reaction system includes reverse transcription buf...

Embodiment 3

[0039] Example 3: 2-BP inhibits the expression of important transcription factors NFATc1 and c-Fos downstream of the signaling pathway during osteoclast differentiation

[0040] (1)Protein sample processing and extraction

[0041] Mononuclear macrophages were seeded in 6-well plates (40 × 10 4 Cells / well, 30ng / ml M-CSF complete Alpha MEM culture medium), divided into control group and drug treatment group, after overnight, the medium was replaced with 50ng / ml RANKL, 30ng / ml M-CSF complete Alpha MEM culture solution, and 25 μM 2-BP was added to the drug treatment group, and the same amount of dimethyl sulfoxide solvent was added to the control group, the solution was changed every other day, and protein samples were collected on days 0, 1, 3, and 5, respectively.

[0042] Protein sample extraction and concentration determination: After culturing to the corresponding time point, quickly discard the supernatant, wash once with phosphate-buffered saline at 4°C, place the 6-well p...

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Abstract

The invention discloses application of 2-bromopalmitate (2-BP) in preparation of drugs for prevention and treatment of bone loss related diseases, and belongs to the technical field of medicine. The invention, for the first time, clearly defines that 2-BP can inhibit osteoclast differentiation process of BMMs stimulated by RANKL through various experimental techniques, including tartrate resistantacid phosphatase staining, phalloidin fluorescence staining, bone lamella bone resorption function evaluation, reverse transcription real-time fluorescence quantitative PCR, Western blot, etc. In addition, the invention clearly states that 2-BP also has effects in inhibiting osteoclast differentiation and activation in vivo, and 2-BP can significantly alleviate the pathological process of massivebone loss caused by estrogen deficiency through the establishment of a mouse model of ovariectomy-induced osteoporosis, thus providing experimental data basis in vivo for the role of 2-BP in the prevention and treatment of bone loss related diseases.

Description

technical field [0001] The invention relates to the application of 2-bromopalmitic acid in the preparation of medicines for preventing and treating diseases related to bone loss, and belongs to the technical field of medicine. Background technique [0002] As an important part of the motor system, bone provides structural support and protection for the body, and participates in physiological processes such as hematopoiesis, calcium metabolism, and endocrine regulation in the body. Bone remodeling occurs throughout a person's life, and most diseases related to bone metabolism affect the bone remodeling process. Bone remodeling in a normal body depends on the direct dynamic balance between bone resorption mediated by osteoclasts and bone formation mediated by osteoblasts, and an imbalance between the two will cause excessive bone formation and sclerosis-related diseases Or bone formation imperfection, excessive resorption-related diseases. Osteoporosis (Osteoporosis) is a sy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/20A61P19/08A61P19/10A61P19/02A61P29/00
CPCA61K31/20A61P19/08A61P19/10A61P19/02A61P29/00
Inventor 陈建权章礼炜杨惠林
Owner SUZHOU UNIV
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