Sweroside promotes osteoblastic differentiation and mineralization via interaction of membrane estrogen receptor-α and GPR30 mediated p38 signalling pathway on MC3T3-E1 cells.

摘要: Abstract Background Dipsaci Radix has been clinically used for thousands of years in China strengthening muscles and bones. Sweroside is the major active iridoid glycoside isolated from Radix. It reported that sweroside can promote alkaline phosphatase (ALP) activity both human osteosarcoma cell line MG-63 rat osteoblasts. However, underlying mechanism involved these osteoblastic processes poorly understood. Purpose This study aimed to characterize bone protective effects investigate signaling pathway its actions MC3T3-E1 cells. Methods Cell proliferation, differentiation mineralization were evaluated by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay, ALP test Alizarin Red S staining, respectively. The concentration intracellular extracellular fluids was determined ultra-performance liquid chromatography coupled triple quadrupole xevo-mass spectrometry (UPLC/TQ-XS-MS). Proteins associated with analysed western blot immunofluorescence methods. Results did not obviously affect proliferation but significantly promoted maximal absorption amount 0.465 ng/ml (1.3 × 10−9 M) extremely lower than tested 358.340 ng/ml (10−6 M), indicating an low rate Moreover, activity, protein expression ER-α G protein-coupled receptor 30 (GPR30) induced markedly blocked ER antagonist ICI 182780 GPR30 G15. In addition, also activated phosphorylation p38 kinase (p-p38), while together activities completely a antagonist, SB203580. Additionally, Conclusions present indicated sweroside, as potential agent treatment osteoporosis, might exert beneficial on cells interaction membrane estrogen receptor-α then activates pathway. first report specific