xy9902对MC3T3-E1细胞的增殖和分化作用

目的研究化合物xy9902对成骨细胞MC3T3-E1的增殖和分化的影响,并初步探讨其机制。方法采用MTT比色法测定化合物对成骨细胞MC3T3-E1的增殖作用;通过硝基苯磷酸盐法测定细胞内碱性磷酸酶(A lkaline phosphatase,ALP)活性的变化,观察化合物对细胞分化的影响;用放射性配体结合法考察化合物与雌激素受体(Estrogen ic recep-tor,ER)的亲和力。结果化合物xy9902对成骨细胞有促增殖和促分化作用,这一作用可被tamoxifen阻断;xy9902与ER有亲和力,对ERα和ERβ的IC50分别为8.45×10-6mol.L-1和1.66×10-6mol.L-1。结论化合物xy9902对成骨细胞有促增殖和促分化作用,其作用机制可能与ER激动有关。

Effects of xy9902 on the proliferation and differentiation of MC3T3-E1 cells

Aim To investigate the effects of xy9902 on the proliferation and differentiation in MC3T3-E1 cells and its mechanism.Methods Effects of xy9902 on the proliferation and differentiation of MC3T3-E1 cells was determined by MTT and ALP activity measurement.Competitive estrogen-receptor binding assay was used to investigate the affinity of xy9902 to ER.Results xy9902 induced cell proliferation and increased alkaline phosphatase(ALP) activity of MC3T3-E1 cells.Antiestrogen tamoxifen eliminated the stimulation of proliferation and ALP activity of MC3T3-E1 induced by xy9902.The relative binding affinity of xy9902 for ERα and ERβ showed an IC_(50)of 8.45×10~(-6) mol·L~(-1) and 1.66×10~(-6) mol·L~(-1) respectively.Conclusion xy9902 directly stimulates cell proliferation and differentiation of MC3T3-E1 cells through ligand-receptor binding,which indicated that xy9902 behaves as an estrogen agonist in MC3T3-E1 cells.