髓系白血病
细胞凋亡
癌症研究
雌激素受体
细胞因子
程序性细胞死亡
半胱氨酸蛋白酶
药理学
生物
白血病
化学
医学
免疫学
生物化学
内科学
癌症
乳腺癌
作者
Alessia Roma,Sarah G. Rota,Paul A. Spagnuolo
标识
DOI:10.1021/acs.molpharmaceut.7b01151
摘要
Acute myeloid leukemia is an aggressive disease with limited and nonselective therapeutic options. This study explored the bioactivity and cell death inducing mechanism of diosmetin, a novel compound identified in a nutraceutical screen to impart selective anti-AML activity. Diosmetin, a citrus flavone, induced apoptosis characterized by increases in caspases 8 and 3/7 and the death inducing cytokine TNFα. In fact, through protein and mRNA expression analysis, activity was shown to be dependent on expression of estrogen receptor (ER) β. Treatment with diosmetin also delayed tumor growth in AML mouse xenografts. In summary, these studies highlight diosmetin as a novel therapeutic that induces apoptosis through estrogen receptor β.
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