目的 研究desmosdumotin-C（Des-C）B环对位氟修饰衍生物TPP对人乳腺癌细胞MCF-7的增殖抑制作用，并探讨其作用机制。方法 MTT法检测质量浓度为1.0、2.5、5.0、10.0、20.0 μg/mL的TPP作用48 h后，对MCF-7细胞的增殖抑制率；流式细胞术检测20.0 μg/mL TPP作用0、24、48 h诱导MCF-7细胞的凋亡程度；流式细胞术检测20.0 μg/mL TPP作用0、24、48 h对MCF-7细胞中NF-κB P65阳性细胞表达率的影响。结果 作用48 h后，2.5、5.0、10.0、20.0 μg/mL的TPP对MCF-7细胞增殖均有显著抑制作用，且抑制率随着浓度的升高而增大；20 μg/mL TPP作用24、48 h均可诱导细胞凋亡；作用48 h后，20 μg/mL TPP可显著减少MCF-7中NF-κB P65阳性细胞率。结论 TPP显著抑制MCF-7细胞增殖，诱导MCF-7细胞凋亡，作用机制可能与下调NF-κB表达有关。

Objective To study the inhibitory effects of TPP, a desmosdumotin-C B ring para-fluoro modified derivative, on human breast cancer MCF-7 cell proliferation, and investigate the possible mechanisms.Methods MTT assay was used to measure the proliferation suppression of MCF-7 cells after treated with 1.0, 2.5, 5.0, 10.0, and 20.0 μg/mL TPP for 48 h, and then the cell apoptosis rate and expression rate of NF-κB P65 positive cells were tested by flow cytometry after 20.0 μg/mL TPP treatment for 0, 24, and 48 h.Results MTT assay showed that, after treatment for 48 h, 1.0, 2.5, 5.0, 10.0, and 20.0 μg/mL TPP all exhibited the inhibitory effects and showed a dose-dependent relationship. Flow cytometry results showed that 20.0 μg/mL TPP induced cell apoptosis after treatment for 24 and 48 h. TPP (20.0 μg/mL) significantly reduced the rate of NF-κB P65-positive cells in MCF-7 cells after treatment for 48 h.Conclusion TPP could inhibit the proliferation of MCF-7 cells, which may be induced by cell apoptosis. Down-regulation of NF-κB is possible to be related with apoptosis.

国家自然科学基金项目（81072546；81470156）