Laboratory of Chemical Biology and Genomics, Korea Research Institute of Bioscience and Biotechnology, 52 Uendong, Yoosung, Daejeon 305-806, Republic of Korea.
Bioorg Med Chem Lett. 2011 Jan 15;21(2):747-51. doi: 10.1016/j.bmcl.2010.11.114. Epub 2010 Nov 28.
2-Hydroxycinnamaldehyde (HCA) and curcumin have been reported to have antitumor effects against various human tumor cells in vitro and in vivo by generation of ROS. Aldehyde-free HCA analogs were synthesized based on the structure of curcumin, which we have called 2-hydroxycurcuminoids. The hydroxyl group of curcuminoids enhances the ability to generate ROS. 2-Hydroxycurcuminoid (HCC-7) strongly inhibited the growth of SW620 colon tumor cells with a GI(50) value of 7μM, while the parent compounds, HCA and curcumin, displayed GI(50) values of 12 and 30μM, respectively. HCC-7 was found to induce apoptosis through the reactive oxygen species-mitochondria pathway and cell cycle arrest at G2/M phase.
2-羟基肉桂醛（HCA）和姜黄素已被报道通过生成 ROS 具有体外和体内针对各种人类肿瘤细胞的抗肿瘤作用。根据姜黄素的结构合成了无醛 HCA 类似物，我们称之为 2-羟基姜黄素类化合物。姜黄素类化合物的羟基增强了生成 ROS 的能力。2-羟基姜黄素类化合物（HCC-7）强烈抑制 SW620 结肠肿瘤细胞的生长，GI（50）值为 7μM，而母体化合物 HCA 和姜黄素的 GI（50）值分别为 12 和 30μM。发现 HCC-7 通过活性氧-线粒体途径诱导细胞凋亡，并使细胞周期停滞在 G2/M 期。
