Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2015, Vol. 20 ›› Issue (6): 616-620.
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Abstract: 【Abstract】Objective To investigate the antitumor effect and potential mechanism of 6,8-ditrifluoromethy-5-hydroxyl-7-acetoy chrysin(dFMAChR) on human breast cancer MCF-7 cells. Methods Using MTT assay to assess the proliferative inhibitory effect of dFMAChR on MCF-7 cells; Hochest staining was used to observe the morphologic changes of apoptosis induced by dFMAChR in MCF-7 cells. DNA agarose electrophoresis was used to detect the fragment of DNA in MCF-7 cells. The protein level and activity of PPARγ、PTEN、p-Akt、Caspase-3 were tested by Western blot to explore the molecular mechanism of dFMAChR against breast cancer. Results dFMAChR inhibited proliferation of MCF-7 cells in a dose-dependent manner , the IC50 value of which was 8.51 μM; Hochest staining shown lots of apoptosis cells with nucleus condensation after treatment with dFMAChR(3.0, 10.0, 30.0 μM)for 48 h and DNA ladder bands could appear by DNA agarose gel electrophoresis after treatment with dFMAChR(10.0, 30.0 μM)for 48 h. It indicated that dFMAChR could significantly induce apoptosis of MCF-7 cells. The results of Western blot shown the expression of PPARγ、PTEN and Caspase-3 was enhanced while the expression of p-Akt was decreased in a concentration-dependent manner with treatment at various concentration dFMAChR for 48 h in MCF-7 cells. Conclusion dFMAChR had anti-breast cancer activity in vitro and its mechanism may be related to the activation of PPARγ/PTEN pathway and finally increased the expression of Caspase-3 and induced the apoptosis of MCF-7 cells .
WANG Juan, QIN Yong, TANG Yan-Yan, ZHANG Min, QIN Li, ZHANG Hai-Tao. The Antitumor Effect and Potential Mechanism of dFMAChR in Human breast cancer in vitro[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2015, 20(6): 616-620.
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