bone-protective

Alfacalcidol (Etalpha) (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma.

Coelogin is an orally effective bone-protective agent that activates ER-Erk and Akt-dependent signaling pathways, thereby stimulating osteoblast differentiation. It is utilized in osteoporosis research.

BT-Amide is an orally active Pyk2 kinase (Pyk2kinase) inhibitor with an IC50 of 44.69 nM. It prevents glucocorticoid-induced bone loss and demonstrates bone-protective activity in C57BL 6 mice.

Tigogenin is one of steroidal sapogenins which is widely used for synthesizing steroid drugs. It might have protective effect on bone and be helpful in preventing the development of osteoporosis.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of myeloma xenografts in mice and enhanced the antitumor activity of relevant agents in combination studies. INCB16562 is a potent JAK1 2 inhibitor and that mitigation of JAK STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. ( source: Neoplasia. 2010 Jan;12(1):28-38. ).

Gigantol is a novel inhibitor of the Wnt/β-catenin pathway. It inhibits Wnt/β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K/Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K/Akt/NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

Kobophenol A has antimicrobial, and anti-inflammatory activities, it might be a candidate for treatment of inflammatory bone diseases relevant to osteoblast cell death. Kobophenol A inhibits AChE activity in a dose-dependent manner, and the IC50 value is