bone resorption

1-Methylimidazole is a metabolite of 1-methyl-2-thioimidazole (methimazole) which inhibits bone resorption.

Risedronic Acid (Risedronate), a pyridinyl biphosphonate, can inhibit osteoclast-mediated bone resorption.

Alendronate sodium hydrate (MK 217) is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

Minodronic acid monohydrate is an farnesyl diphosphate synthase inhibitor that acts as a bone resorption inhibitor.

Risedronate Sodium (NE 58095 Sodium) is an aminobisphosphonate derivative of etidronic acid and CALCIUM CHANNEL BLOCKER that inhibits BONE RESORPTION and is used for the treatment of OSTEOPOROSIS.

Flurbiprofen (dl-Flurbiprofen) is an anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

Pamidronate disodium pentahydrate is a bone resorption inhibitor, a compound capable of preventing osteoporosis.

Etidronic acid (HEDP) is a diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis. Studies indicate it can also slow the course of osteoarthritis of the knee. The drug is unusual in that it both increases deposition of new bone by osteoblasts and reduces the resorption of bone by osteoclasts. It is therefore promoted as a dual action bone agent (DABA) indicated for use in the treatment of severe osteoporosis.

Zoledronic acid monohydrate (CGP 42446) is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Ipriflavone (Osteofix) (Osteofix) is a feed additive and a catabolic agent. It is used to inhibit bone resorption.

Sodium etidronate (Didronel) is a synthetic therapeutic diphosphonate analog of endogenous pyrophosphate. As a member of the family of drugs known as bisphosphonates, Sodium etidronate differs from endogenous pyrophosphate in its resistance to enzymatic hydrolysis. This agent adsorbs to hydroxyapatite cells and reduces the number of osteoclasts, thereby inhibiting abnormal bone resorption. Etidronate may also directly stimulate bone formation by osteoblasts.

3,7,4'-Trihydroxyflavone(5-Deoxykampferol) is a DNA-breaking flavonoid isolated from rosewood heartwood. It inhibits osteoclast differentiation, actin ring formation, and bone resorption in RAW 264.7 cells and bone marrow macrophages induced by NF-κB ligand (RANKL) receptor activators.

DPC-AJ1951 acetate, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR). And characterized the activity of DPC-AJ1951 acetate in ex vivo and in vivo assays of bone resorption[1].

GRGDSPK acetate shows inhibitory activity against integrin-fibronectin binding and can be used in research on integrins in bone formation and resorption.

ONO-5334 is a selective, orally active and potent histone K inhibitor with anti-SAR-COV-2 and anti-bone resorption activity for the study of osteoporosis.

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

Cimicifugoside H1 shows the protective function to cerebral neuron during cerebral ischemia.

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

Icariside I (Lcariside I) is isolated from Epimedium herb. It can stimulate osteogenic differentiation of BMSCs and inhibit bone resorption activity of osteoclasts.

Clodronate disodium tetrahydrate (Clastoban) inhibits bone resorption and soft tissue calcification.

L-006235 is a potent and reversible inhibitor of cathepsin K with IC50 of 0.25 nM.

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

Blosozumab (LY2541546), an anti-sclerostin (SOST) antibody, promotes bone formation while decreasing bone resorption, with potential applications in osteoporosis research [1] [2].

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V, exhibiting high affinity with Ki values of 41 pM, 68 pM, and 53 pM, respectively. It effectively inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. In vitro studies confirm its inhibitory effect on bone resorption in human tissue, and in vivo studies on cynomolgus monkeys validate its efficacy in reducing bone resorption.

DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.

Galactosylhydroxylysine hydrochloride, a bone collagen component generated through hydroxylysine's post-translational glycosylation, is liberated during bone resorption. Its levels increase in cases of metabolic bone loss [1].

Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and 0.317 nM alone and with RAMP1, 2, or 3, respectively. It induces cAMP accumulation in COS-7 cells transfected with CTR2 (EC50 = 0.166 nM). Salmon calcitonin inhibits bone resorption by osteoclasts in a pit formation assay using rat bone slices (ID50 = 0.003 pg/mL) and lowers calcium level in vivo in a bioassay of hypocalcemia in rats (ED15 = 33.9 mg/kg). Formulations containing salmon calcitonin have been used to treat hypercalcemia, bone destruction by osteoporosis, and Paget's disease.

Concanamycin B is a macrolide antibiotic that selectively inhibits vacuolar type H+-ATPases (IC50 = 5 nM), thereby blocking vacuolar organelle acidification and early to late endosomal transport. It interferes with bone resorption, maturation of CD8 T lymphocytes, and prevents processing of major histocompatibility complex (MHC) class II precursors in human B cells, inhibiting MHC class II molecule expression on the cell surface.

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A .

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

C-telopeptide, a cross-linked peptide from type I collagen, is released during bone resorption and shows a correlation with bone mineral density (BMD).

Gossypetin, a hexahydroxylated flavonoid extractable from Rhodiola rosea Linn. is a potent MKK3 and MKK6 inhibitor that strongly attenuates the MKK3 6-p38 signaling pathway.Gossypetin exhibits antimutagenic, antiatherosclerotic, antioxidant, as well as cytoprotective and antimicrobial effects.It inhibits bone resorption by downregulating lysosomal caspase K activity and inducing autophagy-associated proteins in actin ring osteoclasts. Gossypetin has anti-mutagenic, anti-atherosclerotic, anti-oxidant, cytoprotective and antibacterial effects, and it inhibits bone resorption by down-regulating lysosomal caspase K activity and by inducing autophagy-associated protein in actin ring osteoblasts.

Cgp 47072 is a bisphosphonate, used in the treatment of bone diseases, particularly where there is uncontrolled bone resorption.

Aminobutane bisphosphonate is a powerful inhibitor of bone resorption. It can potentially be a useful measure for controlling hypercalcemia in patients with carcinoma.

Incadronate, also known as Cimadronate and YM-175, is a bone resorption inhibitor. Incadronate disodium inhibits macrophage migration to site of inflammation in vivo and proliferation and causes apoptosis in cancer cells in vitro. Incadronate disodium is a bone density conservation, antitumor and anti-inflammatory agent.

Calcitriol Impurities D (24-Homo Calcitriol) is a hormonal form of the vitamin that promotes the differentiation of HL-60 human promyelocytic leukemia cells into monocytes.Calcitriol Impurities D has bone resorption activity and inhibits the replication of human immunodeficiency virus in human cells.Calcitriol Impurities D has antiviral activity and can be used to treat AIDS and viral infections. 25-dihydroxyvitamin D3 has antiviral activity and can be used in the treatment of AIDS and viral infections.

Curculigoside B shows antioxidative and antiosteoporotic activities, it can decrease area of bone resorption pit, osteoclastic formation and TRAP activity.

Flurbiprofen sodium is an anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting carbonic anhydrase.

A-75943 is a bone resorption inhibitor from streptomyces.

DPC-AJ1951 TFA, a 14-amino acid peptide, functions as a potent agonist for the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR). It has been characterized for its activity through ex vivo and in vivo bone resorption assays [1].

Bavachalcone, a major bioactive compound isolated from *Psoralea corylifolia* L., may serve as a therapeutic drug for bone resorption-associated diseases. It protects endothelial function by increasing AMPK activity and MnSOD expression while reducing mitochondrial oxidative stress.

Rubiadin-1-methyl ether (Rubiadin 1-methyl ether) is a natural product.It inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.

1. Obtusifolin has antioxidant properties and improves chemically induced diabetes and its complications by modulation of oxidative stress. 2. Obtusifolin suppresses phthalate esters-mediated bone resorption, thus may be a novel anti-breast-cancer bone me

GRGDSPK TFA (EMD 56574 TFA) is a peptide containing the Arg-Gly-Asp (RGD) sequence, serving as a competitive and reversible inhibitor of integrin-fibronectin binding. This compound is utilized in research to elucidate integrins' involvement in bone formation and resorption [1] [2].