New and known symmetrical curcumin derivatives inhibit the formation of Fos-Jun-DNA complex
New and known symmetrical curcumin derivatives inhibit the formation of Fos-Jun-DNA complex
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DOI：
10.1016/s0304-3835(02)00170-2
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发表时间：
2002-10-08
期刊：
影响因子：
9.7
通讯作者：
Yang, CH
中科院分区：
文献类型：
--
作者：
Hahm, ER;Cheon, G;Yang, CH
我们以前报道，姜黄色素，姜黄的黄色色素，抑制Fos-Jun-DNA复合物的形成。因此，我们合成了12个对称的姜黄素类化合物。我们使用Pabon方法的略微修改版本来寻找比姜黄素更有效的抑制剂。在合成的姜黄素类化合物中，BJC 005、CHCO 11和CHC 007显示出非常高的抑制活性。它们的IC 50值分别为5.4 μ M、0.30 mM和0.38 mM。这些IC 50数据表明BJC 005的有效性比姜黄素高近90倍。BJC 005显示出比苦瓜素更强大的特性，苦瓜素到目前为止已被报道为有效的Fos-Jun抑制剂。此外，BJC 005和CHC 007以前也没有合成过。我们首次报道了新的BJC 005和CHC 007对转录活性表现出高度的抑制活性。(C)2002爱思唯尔科学爱尔兰有限公司保留所有权利。
We previously reported that curcumin, the yellow pigment of turmeric, inhibited the formation of the Fos-Jun-DNA complex. Thus, we have synthesized 12 symmetrical curcuminoids. We used a slightly modified version of Pabon's method to search for an inhibitor more potent than curcumin. Of the synthesized curcuminoids, BJC005, CHCO11, and CHC007 exhibited a remarkably high inhibitory activity. Their IC50 values are 5.4 muM, 0.30 mM, and 0.38 mM, respectively. These IC50 data indicated that BJC005 is nearly 90 times more effective than curcumin. The BJC005 has shown a more powerful profile than momordin, which, until now, has been reported as a potent Fos-Jun inhibitor. Also BJC005 and CHC007 have not been synthesized before. We report for the first time that the novel BJC005 and CHC007 exhibit highly inhibitory activity against transcription activity. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.