Baicalin positively regulates osteoclast function by activating MAPK/Mitf signalling
AbstractActivation of osteoblasts in bone formation and osteoclasts in bone resorption is important during the bone fracture healing process. There has been a long interest in identifying and developing a natural therapy for bone fracture healing. In this study, we investigated the regulation of osteoclast differentiation by baicalin, which is a natural molecule extracted from Eucommiaulmoides (small tree native to China). It was determined that baicalin enhanced osteoclast maturation and bone resorption activity in a dose‐dependent manner. Moreover, this involves the activation of MAPK, increased Mitf nuclear translocation and up‐regulation of downstream osteoclast‐related target genes expression. The baicalin‐induced effect on osteoclast differentiation can be mimicked by specific inhibitors of p‐ERK (U0126) and the Mitf‐specific siRNA, respectively. Protein–ligand docking prediction identified that baicalin might bind to RANK, which is the upstream receptor of p‐ERK/Mitf signalling in osteoclasts. This indicated that RANK might be the binding target of baicalin. In sum, our findings revealed baicalin increased osteoclast maturation and function via p‐ERK/Mitf signalling. In addition, the results suggest that baicalin can potentially be used as a natural product for the treatment of bone fracture.
[…] The ligand–protein docking prediction was performed using the SwissDock system, which is a web provider dedicated service for the small molecules and target proteins docking prediction. To submit the docking task, we selected the RANK as target protein. Then, we searched the baicalin structure in the database and selected the proper structure for docking task. All docking calculations were completed on the web side. The docking results were demonstrated in the UCSF Chimera molecular viewer which can be used for result analysis . […]
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