osteoclast

Velutin shows the strongest inhibitory effect in NF-κB activation and exhibits the greatest effects in blocking the degradation of inhibitor of NF-κB as well as in inhibiting mitogen-activated protein kinase p38 and JNK phosphorylation. Velutin has anti-inflammatory property. Velutin exhibits the greatest potency among all flavones which reduce TNF-α and IL-6 production.

Toddaculine may be beneficial for the prevention and treatment of osteoporosis, it can not only inhibit the differentiation of osteoclasts via activation of the NF-κB, ERK 1 2, and p38 MAPK signaling pathways, but can induce differentiation and mineralization of osteoblasts by regulating differentiation factors. Toddaculine also may serve as a pharmacological prototype for the development of novel anti-leukemic agents, it displays a dual effect as a cell differentiating agent and apoptosis inducer in U-937 cells.

Usnic Acid (Usniacin) is an antimicrobial, antitumor and enzyme inhibiting agent shown to uncouple oxidative phosphorylation in mouse-liver mitochondria. Usnic acid induces necrosis in certain cells.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.

Eupenicisirenin C (compound 1), a sirenin derivative, exhibits strong NF-κB inhibitory activities and suppresses the cGAS-STING pathway. Additionally, Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells [1].

Picrasidine I has antiosteoclastogenic effect by inhibiting inflammation induced activation of MAPKs, NF-κB and ROS generation followed by suppressing the gene expression of c-Fos and NFATc1 in osteoclast precursors.

Kahweol Acetate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Anti-osteoporosis agent-2 (Compound 10) inhibits RANKL-induced osteoclast differentiation [1].

Eudebeiolide B, isolated from Salvia plebeia R. Br., impedes osteoclastogenesis by modulating RANKL-induced NF-κB, c-Fos, and calcium signaling pathways, and is applicable in the study of osteoclast-related diseases [1].

Kahweol stearate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1-induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

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.

Tectorigenin (4',5,7-Trihydroxy-6-methoxyisoflavone) is an O-methylated isoflavone. Tectorigenin Promotes Osteoblast Differentiation and in vivo Bone Healing, but Suppresses Osteoclast Differentiation and in vivo Bone Resorption.

Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG

6''-O-acetylsaikosaponin A is an acetyl saikosaponin isolated from the roots of Bupleurum chinense. Itshows some osteoclast-inhibiting activities

Kahweol Eicosanate is a semi-syntetic derivative of kahweol. Kahweol Eicosanate exhibits a wide variety of biological activities, including inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, inhibiting RANKL-induced osteoclast

1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) exhibits vasodilator action through an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx via L-type voltage-operated Ca(2+) channels. A minor contribution to HM-1's effects may stem from inhibiting protein kinase C-mediated release of intracellular Ca(2+) stores. At 1 µg mL, HM-1 effectively inhibits osteoclast differentiation in co-cultures with mouse osteoblastic calvarial and bone marrow cells and protects mice from acute lung injury induced by lipopolysaccharide (LPS), likely by increasing IκB-α protein expression and suppressing inducible nitric oxide synthase and cyclooxygenase-Ⅱ protein expression.

Kahweol linoleate is a semi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

(-)-Epiafzelechin is a COX inhibitor with antioxidant and anti-inflammatory activity, osteoprotective effects in a mature ovariectomized mouse model, ability to stimulate osteoblast activity and inhibit osteoclast activity.

Sauristolactam inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation. Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus Chi

1. Geraniin has a protective effect against OVX-induced rat osteoporosis. 2. Geraniin has cytotoxic activity towards cancer cells in vitro and in vivo. 3. Geraniin exerts inhibitory effects on osteoclast differentiation in vitro and suppresses Ti particle

Ganoderic acid DM is an antiandrogenic osteoclastogenesis inhibitor, it especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1), this suppression leads to the inhibition of dendritic cell-specific transmembrane pr

Kahweol palmitate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1-induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Kahweol oleate is emi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.