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Aromatic compound as activator of neuroplexin-B2 and application of aromatic compound in preparation of medicine for treating osteoporosis

An aromatic compound, a technology for osteoporosis, which is applied in the application field of preparing a drug for treating osteoporosis, can solve problems such as unsatisfactory treatment effect, and achieves inhibition of osteoclast formation, promotion of osteoblast formation, and delay of osteoporosis. effect of development

Active Publication Date: 2022-04-08
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the unsatisfactory therapeutic effect of existing drugs for the treatment of osteoporosis, and provide an aromatic compound as an activator of plexin-B2 and in the preparation of osteoporosis treatment Application in Porosis Drugs

Method used

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  • Aromatic compound as activator of neuroplexin-B2 and application of aromatic compound in preparation of medicine for treating osteoporosis
  • Aromatic compound as activator of neuroplexin-B2 and application of aromatic compound in preparation of medicine for treating osteoporosis
  • Aromatic compound as activator of neuroplexin-B2 and application of aromatic compound in preparation of medicine for treating osteoporosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Through computer drug-aided design screening to obtain small molecular compounds that can bind to Plexin-B2, and to screen small molecular compounds that affect the expression level of the osteoclast gene CTSK;

[0041] 1. Prepare 10mg / ml storage solution: ①Small molecular compounds (as shown in Table 1) were obtained through computer drug-aided design screening, all purchased from Chemdiv Company, centrifuged at 1000r / min for 5mins; ②In an ultra-clean workbench, absorb 100ulDMSO Add it to 1mg of powder, and repeatedly pipette and mix; ③ Divide the mixed liquid and store it at -20°C.

[0042] 2. Prepare 10ug / ml working solution: ①Take the aliquoted storage solution and place it at room temperature for rewarming; ②Add 1ul of storage solution to every 1ml of culture medium to prepare a working solution for subsequent cell experiments.

[0043] 3. The mouse bone marrow mononuclear cells were mixed with 1×10^ 5 The density of cells / well was inoculated in the medium...

Embodiment 2K784-9621

[0048] Example 2 K784-9621 can significantly promote the expression of Plexin-B2, promote osteoblast formation and inhibit osteoclast formation

[0049] (1) The specific experimental steps for detecting Plexin-B2 protein and gene expression are as follows:

[0050] Mouse bone marrow mononuclear cells were treated with 1×10^ 5 Cells / well density were inoculated in α-MEM medium containing macrophage colony-stimulating factor (M-CSF, 30ng / ml), 10% fetal bovine serum, 1% double antibody, and divided into control group (Control ), K784-9621 treatment group (K784-9621). After 48 hours of K784-9621 intervention, cellular protein and RNA were extracted, and the expression levels of Plexin-B2 protein and gene were detected by WB and q-PCR, respectively. (References for specific experimental methods of WB: Chang-JunLi, et al. Long noncoding RNA Bmncr regulates mesenchymal stem cell fate during skeletal aging. J Clin Invest, 2018, 128(12): 5251-5266.).

[0051] For specific results, s...

Embodiment 3

[0074] Example 3 K784-9621 can increase bone mass in postmenopausal osteoporosis mice by promoting bone formation and inhibiting bone resorption

[0075] Postmenopausal osteoporosis (PMO) is a metabolic bone disease in which bone mass is significantly lost due to the decrease of estrogen. A slight increase eventually leads to a significant decrease in bone mass due to greater bone resorption than bone formation. Since we previously observed that K784-9621 can significantly inhibit osteoclastogenesis and promote osteoblastogenesis in vitro, we further speculate whether it can improve the bone loss of postmenopausal osteoporosis. After adaptive feeding for 1 week, C57BL / C mice were divided into sham operation+vehicle group (sham), ovariectomy+vehicle group (OVX) and ovariectomy+K784-9621 group (K784-9621), operation for 1 week Afterwards, vehicle or K784-9621 (70mg / kg, once a day) was injected intraperitoneally, and the weight of mice in each group was weighed after 7 weeks of ...

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Abstract

The invention discloses an aromatic compound serving as an activator of neuroplexin protein-B2 and application of the aromatic compound to preparation of a medicine for treating osteoporosis. The aromatic compound is preferably a compound as shown in a formula II, and the compound as shown in the formula II can obviously increase the expression level of Plexin-B2 protein and gene and activate downstream signal channels thereof, and also can obviously promote osteoblast generation and inhibit osteoclast generation, so that the bone mass is obviously increased, and the development of osteoporosis is delayed; the invention provides a research basis and a theoretical basis for developing medicines for treating OP, and can be applied to preparation of medicines for preventing and / or treating osteoporosis.

Description

technical field [0001] The invention belongs to the technical field of medicine and biochemistry, and specifically relates to the application of aromatic compounds as plexin-B2 (Plexin-B2) activators and in the preparation of medicines for treating osteoporosis. Background technique [0002] Osteoporosis (Osteoporosis, OP) is the most common bone metabolic disease, characterized by decreased bone mass, bone microarchitecture damage, increased bone fragility, and increased fracture risk. OP mainly includes senile osteoporosis and postmenopausal osteoporosis, and the high-risk groups are the elderly and postmenopausal women. In China, OP has jumped to the top of the list of common diseases and frequently-occurring diseases, and its incidence rate is increasing year by year. One, it significantly increases the risk of disability and all-cause death of the elderly, especially elderly women, and brings a heavy economic and medical burden to the society. [0003] At present, cli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4406A61K31/4709A61K31/519A61P19/10
CPCA61K31/4406A61K31/4709A61K31/519A61P19/10
Inventor 李长俊黄梅罗湘杭肖业
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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