摘要
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。
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 meaurement. 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 stimu-lation of proliferation and ALP activity of Mc3rI3-E1 induced by xy9902. The relative binding affinity of xy9902 for ERot and ERI3 showed an IC50 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.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2006年第5期529-532,共4页
Chinese Pharmacological Bulletin
基金
国家高技术研究发展计划(863计划)资助项目(No2004AA2Z3480)
