53 results about "Osteoclast cell differentiation" patented technology

The invention provides an application of bifidobacterium animalis subsp. Lactis CP-9 in preparation of a product for promoting bone growth and development or improving bone health. Long-term research and a large number of experiments show that the bifidobacterium animalis subsp. Lactis CP-9 can improve the bone volume fraction, the bone trabecula thickness, the bone density and the bone volume of an organism, and can also effectively improve the growth hormone level and the insulin-like growth factor 1 level, so that bone growth and development are promoted. Meanwhile, the bifidobacterium animalis subsp. Lactis CP-9 can effectively improve the N-terminal propeptide level, osteocalcin level, bone morphogenetic protein level and osteoprotectin level of I-type procollagen in a body, and remarkably reduce the amino-terminal peptide level of the I-type collagen and the ligand level of nuclear factor kappa B receptor activating factor, so that osteoblast differentiation is promoted, osteoclast differentiation is inhibited, and osteoclast differentiation is inhibited. Furthermore, bone formation is promoted, bone resorption is inhibited, bone metabolism is improved, and finally the effect of improving bone health is achieved.

The invention provides a polyketone compound and application thereof in preparation of an osteoclast differentiation inhibitor, and relates to the technical field of marine natural products. The compound is obtained by separation and purification from a fermentation culture of a marine fungus talaromyces sp. GMIMD 02524 (the preservation number is GDMCC No. 66968), the compound is named as talaromyces furanone A, and the structure of the compound is as shown in the formula (I) in the specification. The compound can effectively inhibit RANKL-induced osteoclast differentiation by inhibiting an NF-kappa B signal channel in vitro, and has no obvious cytotoxicity at an effective concentration. Therefore, the compound talaromyfuranone A can be used for developing medicines for preventing and treating osteoclast-related osteolytic diseases such as osteoporosis and the like, and has a good application prospect.

The invention discloses application of a compound with a benzo-aza structure in preparation of a medicine for inhibiting osteoclast formation, the structure of the compound is shown as a formula (1), and R substituent is one of H, OCH3, Br, F and i-Pr. Cell experiments prove that the compound with the benzo-aza structure has a remarkable inhibiting effect on RANKL-induced osteoclast differentiation and marker gene expression, can be used as a candidate medicine which is novel in structure and is used for inhibiting osteoclast formation, and is used for targeting osteoclast to treat osteoporosis related diseases.

The present invention relates to a ginseng peptide and a preparation method and application thereof, belonging to the field of biotechnology. The present invention provides a ginseng peptide, wherein the ginseng peptide comprises a characteristic peptide having an amino acid sequence of at least one of LY, MM, LR, AP, LAR, RLDFR, SALAFR, LLLLGH and LLLLLHG. The present invention obtains ginseng peptides by treating fermented ginseng residue, and identifies the characteristic peptides containing the amino acid sequences of LY, MM, LR, AP, LAR, RLDFR, SALAFR, LLLLGH and LLLLLHG in the ginseng peptides by HPLC-MS / MS. The present invention confirms through experiments that ginseng peptides and fermented ginseng hydrolysates containing ginseng peptides have excellent efficacy in inhibiting the differentiation of bone marrow mononuclear cells into osteoclasts, can improve hormone-induced osteoporosis, and can be applied to products for improving osteoporosis and its related symptoms.

The present invention belongs to the field of medicine and relates to the use of benzothiazinone vinylidene indene compounds in the preparation of osteoclast differentiation inhibitors. The present invention uses tartrate-resistant acid phosphatase (TRAP) staining and reverse transcription real-time fluorescence quantitative polymerase chain reaction (RT-qPCR) technology to confirm for the first time that this series of compounds can significantly inhibit RANKL-induced osteoclast differentiation and the formation of multinucleated osteoclasts, and are non-cytotoxic at concentrations of 5μM and below. Based on these findings, the benzothiazinone vinylidene indene compounds provided by the present invention can be used as candidate drug molecules for novel osteoclast differentiation inhibitors, for the prevention and / or treatment of bone metabolic diseases caused by excessive activation of osteoclasts, such as osteoporosis, periprosthetic bone dissolution, tumor metastasis bone destruction, and rheumatoid arthritis.

The present application relates to the pharmaceutical use of 4-[9-(6-aminopurine)]-2(S)-hydroxybutyric acid methyl ester, in particular to its use in the preparation of a medicament for preventing and / or treating diseases associated with abnormal osteoclast activity. It has been found that 4-[9-(6-aminopurine)]-2(S)-hydroxybutyric acid methyl ester has a significant inhibitory effect on osteoclast differentiation, and intra-articular injection of 4-[9-(6-aminopurine)]-2(S)-hydroxybutyric acid methyl ester has a therapeutic effect on MIA-induced osteoarthritis. Therefore, 4-[9-(6-aminopurine)]-2(S)-hydroxybutyric acid methyl ester has the prospect of being developed into a therapeutic drug for diseases associated with abnormal osteoclast activity.

The present invention discloses a PP-BST 3‑x The invention relates to an implant and its preparation method and application, which belongs to the field of medical material technology. The invention constructs oxygen vacancies (BST) on the surface of strontium ion-doped barium titanate. 3‑x ), under ultrasonic conditions, the internal electron movement of the material is enhanced, making the electron-hole separation easier, thereby accelerating the reaction of electrons with surrounding substances and improving the efficiency of ROS generation. And the PP-BST prepared by the present invention 3‑x On the one hand, the implant can polarize macrophages through electrical potential and inhibit inflammation; on the other hand, it can regulate Sr release through ultrasound, thereby inhibiting osteoclast differentiation in an infected environment, achieving dual-pathway osteogenesis, and improving the high osteoclast environment brought about by the bacterial microenvironment while inhibiting bacteria, thereby promoting bone regeneration, accelerating bone healing ability, and reducing patient recovery time.

The invention belongs to the technical field of biological medicines, discloses application of an STK26 gene in preparation of medicines for treating or preventing osteoporosis, and particularly relates to application of STK26 protein or a coding gene thereof in preparation of medicines for treating osteoporosis. According to the present invention, osteoclast differentiation is inhibited by knocking out the STK26 gene so as to treat osteoporosis, osteoclast differentiation can be promoted by overexpressing the specific STK26 protein and the encoded gene thereof so as to aggravate osteoporosis, and osteoporosis can be alleviated by specifically knocking out the STK26 in an ovariectomized osteoporosis mouse model and an age-related osteoporosis mouse model; overexpression of the STK26 recombinant protein can aggravate osteoporosis, and the STK26 protein and the coding gene thereof can be used as targets of clinical drug treatment, and have good prospects in screening and preparation of drugs for treating osteoporosis.

To provide a novel Lactobacillus paracasei strain with bone regeneration effects, and pharmaceutical and food compositions containing the same. [Solution] The present invention relates to a novel Lactobacillus paracasei L-30 and its uses, and more particularly to Lactobacillus paracasei L-30 (KCTC16035BP) which has the ability to promote the differentiation or formation of osteoblasts, the ability to suppress the differentiation or formation of osteoclasts, and the ability to promote immune activity, and which can regenerate bone, and to a pharmaceutical composition for the treatment or prevention of bone diseases containing the same.

The invention provides a novel hydroxyl indanone compound and application thereof in preparation of an osteoclast differentiation inhibitor, and belongs to the field of marine natural products. The invention discloses a hydroxyl indanone compound which is named as (R)-3, 4-dihydroxy-2, 3-dihydro-1H-indan-1-one, the structural formula of the hydroxyl indanone compound is shown as a formula (I), the hydroxyl indanone compound has a remarkable inhibition effect on LPS (Lipopolysaccharide) induced NF-kappa B luciferase, can remarkably inhibit RANKL induced bone marrow macrophages from being differentiated into osteoclasts at the concentration of 20 mu M or below, and does not generate cytotoxicity at the concentration of 20 mu M or below. The hydroxyindanone compound can be used as an osteoclast differentiation inhibitor medicine and is used for preventing and treating osteolytic diseases such as osteoporosis. # imgabs0 #

The present application relates to the technical field of medicine, and more particularly to the application of beta-hydroxybutyric acid in the preparation of a drug for preventing and / or treating osteoporosis, including postmenopausal osteoporosis due to estrogen deficiency and diabetic osteoporosis, wherein the concentration of the beta-hydroxybutyric acid is 150 mM, the application of beta-hydroxybutyric acid in the preparation of a drug for inhibiting the differentiation of osteoclasts or inhibiting the formation of osteoclasts, wherein the beta-hydroxybutyric acid inhibits the differentiation of osteoclast precursor cells into osteoclasts, and the concentration of the beta-hydroxybutyric acid is 10 mM; the present application proves that beta-hydroxybutyric acid improves the bone microstructure of OVX mice and db / db mice, inhibits the differentiation of osteoclasts, and reduces bone resorption, thereby providing a new target for the prevention and treatment of osteoporosis.

The invention discloses an application of a branched ketonic acid dehydrogenase kinase (BCKDK) inhibitor in preparation of a medicine for preventing and treating osteoporosis. The invention finds that BCKDK can inhibit osteoblast differentiation and reduce the expression of endogenous BCKDK in osteogenic precursor cells so as to promote osteoblast differentiation; a small molecule compound inhibitor BT2 (3, 6-dichloro-2-benzothiophene carboxylic acid) of BCKDK promotes osteoblast differentiation of ovariectomized mice, inhibits osteoclast differentiation, reduces ovariectomized mouse bone loss and increases bone mass. According to the invention, the BCKDK inhibitor is proposed for the first time to be capable of promoting osteoblast differentiation, inhibiting osteoclast differentiation and increasing body bone mass by reducing BCKDK expression or inhibiting BCKDK protein biological functions, and has the effect of preventing and treating osteoporosis.

The present invention relates to a composition for the prevention, improvement, or treatment of bone diseases comprising a complex extract composed of deer antler, white soybean, Angelica gigas, and Cnidium officinale as an active ingredient. The complex extract has the effect of promoting the differentiation of bone-forming osteoblasts and bone formation, and promoting the differentiation of bone-resorbing osteoclasts and inhibiting bone resorption at an in vitro level. Furthermore, since it promotes fracture union in a fracture-induced animal model and exhibits a significant recovery effect on fractures, it can be usefully utilized as a health functional food or pharmaceutical related to bone diseases.

This invention relates to the application of 5-(tetradecoxy)-2-furoic acid (TOFA) in the preparation of drugs that inhibit osteoclast differentiation and function. Using a RANKL-induced mouse bone marrow macrophage osteoclast differentiation model, experiments demonstrated that TOFA can effectively inhibit osteoclast differentiation and function by inhibiting ROS and downregulating the expression of key osteoclast differentiation and function proteins such as Nfatc1, Src, and Ctsk. Furthermore, TOFA at concentrations of 40 μM and below showed no significant cytotoxicity, proving that TOFA can serve as a candidate compound for developing drugs that inhibit osteoclast differentiation and function, and for treating diseases caused by excessive activation of osteoclasts, thus possessing significant clinical application value. Additionally, by constructing a mouse ovariectomized osteoporosis model, the preventive and therapeutic effects of TOFA on estrogen-deficiency-induced osteoporosis were demonstrated.

The invention discloses application of a migration body in preparation of a medicine for inhibiting osteoclast differentiation or promoting osteogenesis. By optimizing cell culture conditions, the secretion amount of the migration body is remarkably increased, large-scale preparation can be realized, and the production cost is greatly reduced. According to the invention, active components in the migration body are enriched through pressure stimulation, so that the migration body has a more excellent effect of promoting bone defect repair. In addition, by utilizing the larger size and stable membrane structure of the migration body, the in-vivo residence time is prolonged, and the long-acting repair of single-time administration is realized, so that the problems of long-acting property and clinical transformation are solved. The migration body disclosed by the invention has a wide application prospect in the field of bone defect repair.

The present invention relates to a pharmaceutical composition containing Cbfβ (Core-binding factor subunit beta) expressing vascular smooth muscle cells or a culture fluid thereof as an active ingredient for the prevention or treatment of age-related diseases. It has been found that inhibition of Cbfβ expression in vascular smooth muscle cells promotes vascular calcification and osteoclast differentiation and that the culture fluid of Cbfβ-expressing vascular smooth muscle cells inhibits osteoclast differentiation. Thus, the composition can be advantageously utilized as a pharmaceutical composition for the prevention, treatment, alleviation, or diagnosis of age-related diseases.

The present invention provides an application of animal Bifidobacterium lactis subspecies CP-9 in the preparation of a product that promotes bone growth and development or improves bone health. After long-term research and a large number of experiments, the present invention found that animal Bifidobacterium lactis subspecies CP-9 can improve the body's bone volume fraction, trabecular thickness, bone density and bone mass, and can also effectively increase the level of growth hormone and insulin-like growth factor 1, thereby promoting bone growth and development. At the same time, animal Bifidobacterium lactis subspecies CP-9 can effectively increase the level of type I procollagen N-terminal propeptide, osteocalcin level, bone morphogenetic protein level, and osteoprotegerin level in the body, and significantly reduce the level of type I collagen amino-terminal peptide and nuclear factor κB receptor activator ligand level, thereby promoting osteoblast differentiation, inhibiting osteoclast differentiation, and then promoting bone formation, inhibiting bone resorption, improving bone metabolism, and ultimately achieving the effect of improving bone health.

The invention discloses a drug for combined treatment of breast cancer bone metastasis, the drug comprises two active components, namely a first active component and a second active component, the first active component is Bufalin and its pharmaceutically acceptable salt, prodrug and derivative, and the second active component is RANKL targeted drug; bufalin and a derivative thereof are combined with an RANKL targeted drug for use, the Bufalin and the derivative thereof are synergistically complementary, and the Bufalin is used for regulating and controlling a tumor microenvironment, reducing secretion of high bone metastatic breast cancer cells HMGB1 and inhibiting differentiation of mononuclear / macrophages in bone marrow to osteoclasts, so that occurrence and development of breast cancer bone metastasis are inhibited; the RANKL targeted drug can specifically block an OPG / RANK / RANKL signal channel, inhibit osteoclast activation, reduce bone destruction and block vicious circle of bone metastasis; when the two active ingredients are combined for use, the effect of inhibiting breast cancer bone metastasis is obviously better than that of single use of any active ingredient, the occurrence of breast cancer bone metastasis can be effectively prevented and delayed, the progress of bone metastasis focus is controlled, and the occurrence risk of bone related events is reduced.

The application discloses a furan coumarin compound and application thereof in preparation of a drug for treating osteoporosis, and belongs to the technical field of drug research and development. 50 The furan coumarin compound has an IC of 37.86 nM, has no obvious cytotoxicity and systemic toxicity, can inhibit a key path of RANKL-induced osteoclast differentiation, and can be used for preparing the drug for treating osteoporosis.

A Lactobacillus paracasei L-30 strain deposited under Accession Number KCTC16035BP has ability to promote osteoblast differentiation or formation, inhibiting osteoclast differentiation or formation, and enhancing immune activity, thereby enabling bone regeneration. A pharmaceutical composition including the Lactobacillus paracasei L-30 strain, a lysate thereof, a culture thereof, an extract thereof, and / or a fraction of the extract may be used for treating or preventing bone diseases.

The present invention relates to a group of anti-osteoporosis compounds and their applications. These compounds can upregulate OPG expression, inhibit inflammatory pathway activation, inhibit osteoclast differentiation or bone resorption, and promote osteoblast differentiation or bone formation; and have high oral bioavailability and anti-osteoporosis activity.

The invention provides a novel compound for inhibiting osteoclast differentiation and preparation and application thereof, and belongs to the technical field of chemical drugs. Cell in-vitro experiments prove that the compound provided by the invention has a significant inhibition effect on osteoclast differentiation induced by RANKL and inflammatory factor TNF-alpha stimulation, and does not have cytotoxicity, so that the compound can be used as a potential drug with a novel structure for inhibiting osteoclast-mediated bone resorption; the pharmaceutical composition is used for treating osteoporosis and inflammatory osteolytic diseases.

This invention discloses the application of OXR1 as a target in the preparation of drugs for treating osteoclast-related bone diseases. This invention reveals for the first time the crucial role of OXR1 in osteoclast differentiation: OXR1 directly binds to the KEAP1 protein, promoting the interaction between KEAP1 and p62, thereby mediating mitophagy, clearing excess reactive oxygen species generated during osteoclast differentiation, and maintaining mitochondrial homeostasis. Inhibiting OXR1 expression or function can effectively block osteoclast differentiation and reduce bone loss. Based on this, this invention provides two intervention strategies targeting OXR1: one is gene therapy using adeno-associated viruses carrying shRNA targeting OXR1; the other is screening and validating the novel use of the FDA-approved drug velpatasvir as an OXR1 inhibitor. In vitro and in vivo experiments confirmed that both significantly inhibit osteoclast activity and improve the osteoporotic phenotype in ovariectomized mice.

The invention relates to the technical field of osteoporosis prevention and treatment. The invention provides an application of a G alpha i gene as an osteoporosis treatment target. According to the invention, the expression of the G alphai in osteoporosis patients and osteoclast / osteoclast progenitor cells is researched, and the influence of the G alphai on osteoclast formation and bone metabolism is evaluated. By explaining the specific mechanism of the G alphai for regulating bone metabolism and related signal pathways, the G alphai is confirmed to be a key medium for RANKL signal transduction. In addition, it is proved that a specific functional domain of G alpha i plays a key role in osteoclast differentiation. It is worthy of noting that when it is found that G alpha i is lacked, the anti-osteoporosis effect of the dinomonoclonal antibody is damaged, and it is prompted that the treatment effect of G alpha i on the dinomonoclonal antibody is indispensable. The research result emphasizes that the G alphai is used as a potential target spot for diagnosing and treating osteoporosis, and paves a way for developing a novel treatment strategy.

The invention discloses application of aporphine alkaloid Tinopaine A in hemsleya amabilis ox gall in preparation of a medicine for treating bone destruction related diseases, and belongs to the technical field of biological medicine. Experiments prove that the Tinpaine A monomer has an inhibition effect on osteoclast differentiation formation in vivo and in vitro; by regulating and controlling key factors for osteoclast formation, the compound has an inhibiting effect on in-vitro osteoclast formation under the concentration of 1-10 mu M and on in-vivo osteoclast formation of mice under the dosage of 2-20 mg / kg, can effectively reduce the number of osteoclasts and protect bone trabecula structures, and has an excellent treatment effect on bone destruction related diseases. The invention relates to a medicine for inhibiting osteoclast differentiation in vivo and in vitro and treating diseases related to bone destruction, which takes Tinopaine A as an active ingredient and can relieve bone destruction by regulating and controlling bone metabolism balance so as to achieve the purpose of treating the diseases related to bone destruction.

The invention relates to an application of N-sulfinyl formylhydrazone derivatives in preparation of drugs for inhibiting osteoclast generation and bone resorption, the N-sulfinyl formylhydrazone derivatives HTM-13, HTM-17, HTM-18, HTM-25 and HTM-37 can directly and effectively inhibit bone marrow macrophages from differentiating to osteoclasts by inhibiting the expression of osteoclast differentiation marker genes, and can be used for preparing drugs for inhibiting osteoclast generation and bone resorption. The cell toxicity is not shown when the concentration is not higher than 5 mu M. The N-sulfinyl formylhydrazone derivative has the beneficial effects that the N-sulfinyl formylhydrazone derivative provided by the invention can be used as a candidate drug molecule of a novel osteoclast differentiation inhibitor, and is used for developing a novel anti-bone resorption drug and treating diseases caused by overexpression of osteoclasts. Therefore, the invention has important clinical significance and application prospect.

The invention discloses application of a diaryl-substituted alpha-carbonyl amide compound. The diaryl-substituted alpha-carbonyl amide compound can be used for preparing medicines for treating osteoporosis, tumor bone metastasis or inflammatory bone destruction. Cell experiments prove that the diaryl-substituted alpha-carbonyl amide compound Z1-Z4 provided by the invention has a remarkable inhibition effect on osteoclast differentiation and bone resorption induced by RANKL, has no obvious cytotoxicity, and can be used as a candidate drug with a novel structure for inhibiting osteoclast differentiation and bone resorption; the method is used for targeting osteoclast to treat bone mass loss related diseases.

This invention provides a concentration gradient cell culture system that solves the problem of large errors in manual drug addition and the difficulty in constructing a stable, continuous concentration gradient in studies on the control of osteoclast progenitor cell differentiation using propionic acid-GPR43. [Solution] The system comprises a housing assembly with an inner container, a first liquid storage cylinder 2, a second liquid storage cylinder 3, a tuned crossbeam 4, an adjustable screw rod 5, a flow-dividing branch pipe array frame, a spiral mixing unit, a porous diffusion plate, and a culture tray 9. The tuned crossbeam is driven by the adjustable screw rod to synchronously supply liquid from both liquid storage cylinders. After gradient distribution by the flow-dividing branch pipe array frame and mixing by the spiral mixing unit, the porous diffusion plate forms a continuous and stable propionic acid concentration gradient field on the culture tray. This avoids manual errors, provides accurate concentration gradients to RAW264.7 and BMMs cells in a single experiment, and supports the calculation of dose-effect curves and IC50, as well as the elucidation of the mechanism of osteoclast differentiation control by propionic acid-GPR43 signaling.