Diphenyl difluoroketone: a potent chemotherapy candidate for human hepatocellular carcinoma.
Diphenyl difluoroketone: a potent chemotherapy candidate for human hepatocellular carcinoma.
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二苯基二氟酮：人类肝细胞癌的有效化疗候选物。
DOI：
10.1371/journal.pone.0023908
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发表时间：
2011
期刊：
影响因子：
3.7
通讯作者：
Liu L
中科院分区：
文献类型：
--
作者：
Liang Y;Yin D;Hou L;Zheng T;Wang J;Meng X;Lu Z;Song X;Pan S;Jiang H;Liu L
二苯二氟酮（EF 24）是一种与姜黄素结构相似的分子，最近报道其显著抑制多种癌细胞的增殖。本研究旨在探讨EF 24对肝癌细胞的作用及其机制。发现2 μM EF 24抑制PLC/PRF/5、Hep 3B、HepG 2、SK-HEP-1和Huh 7细胞系的增殖。然而，即使8 μM EF 24处理也不影响正常肝LO 2细胞的增殖。因此，20 mg/kg/d EF 24显著抑制了肿瘤异种移植物的生长，而肝、脾或体重没有明显变化。流式细胞仪检测细胞凋亡及G2/M期阻滞。此外，还观察到半胱天冬酶和PARP激活以及典型的凋亡特征，包括核碎片和染色质浓缩。其作用机制可能与核因子κ B（NF-κB）通路及NF-κ B调控的基因产物Bcl-2、考克斯-2、Cyclin B1的表达减少有关。本研究为EF 24作为肝癌的治疗药物提供了策略。
Diphenyl difluoroketone (EF24), a molecule having structural similarity to curcumin, was recently reported to inhibit proliferation of various cancer cells significantly. Here we try to determine the effect and mechanism of EF24 on hepatocellular carcinoma. 2 µM EF24 was found to inhibit the proliferation of PLC/PRF/5, Hep3B, HepG2, SK-HEP-1 and Huh 7 cell lines. However, even 8 µM EF24 treatment did not affect the proliferation of normal liver LO2 cells. Accordingly, 20 mg/kg/d EF24 inhibited the growth of the tumor xenografts conspicuously while causing no apparent change in liver, spleen or body weight. In addition, significant apoptosis and G2/M phase cell cycle arrest were found using flow cytometry. Besides, caspases and PARP activation and features typical of apoptosis including fragmented nuclei with condensed chromatin were also observed. Furthermore, the mechanism was targeted at the reduction of nuclear factor kappa b (NF-κB) pathway and the NF-κB–regulated gene products Bcl-2, COX-2, Cyclin B1. Our study has offered a strategy that EF24 being a therapeutic agent for hepatocellular carcinoma.
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影响因子：
2.3
作者：
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