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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2006, Vol. 11 ›› Issue (5): 565-568.

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Effects of xy9902 a centchroman derivative on proliferation of MCF-7 cells

HOU Jin1,2, XIONG Xiao-yun1, MI Man2, WANG Jie-pin1, LIU Li1, MEI Qi-bing1   

  1. 1Department of Pharmacology, the Fourth Military Medical University, Xi'an 710032, Shanxi, China;
    2Department of Pharmacology, Medical College, Xi'an 710068, Shanxi, China
  • Received:2005-12-29 Revised:2006-03-09 Online:2006-05-26 Published:2020-12-09

Abstract: AIM: To investigate the effects of xy9902 on the proliferation in MCF-7 cells and its mechanism. METHODS: Effects of xy9902 on the proliferation of MCF-7 cellswere determined by MTT measurement.Cell cycle was examined by flow cytometry.Competitive estro-gen-receptor binding assay was used to investigate the af-finity of xy9902 to ER.RESULTS: xy9902 induced cell proliferation of MCF-7 cells at a lower concentration with an increase of the number of cells in S phase.On the contrary, inhibited cell proliferation at higher concentra-tionswith a decrease of the number of cells in S phase. Tamoxifen could block the stimulation of proliferation ef-fect of MCF-7 induced by xy9902.The relative binding affinity of xy9906 for ERαand ERβ showed an IC50 of 8.45 ×10-6 and 1.66 ×10-6 mol·L-1 respectively. CONCLUSION: xy9902 directly stimulates cell prolifer-ation of MCF-7 cells through ligand-receptor binding at a low concentrations and inhibits cell proliferation at high concentrations.

Key words: benzaodihydropyran, derivative, xy9902, MCF-7 cells, estrogen receptor, proliferation

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