Zoledronic Acid

Zoledronic acid induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.(In Vitro):Zoledronic Acid (0.1-1 μM; 48 hours) increases receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells.Zoledronic Acid increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells.Zoledronic Acid enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells.Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways.Zoledronic Acid (10-100 μM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells.Zoledronic Acid (10-100 μM; 1-7 days) induces apoptosis in MC3T3-E1 cells.Zoledronic Acid (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis.Zoledronic Acid exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 μM.(In Vivo):Zoledronic Acid (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content.Zoledronic Acid (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) inhibits both osteoclast and osteoblasts function and bone remodeling in vivo interfering with bone mechanical properties.