Oxepinamides: Novel Liver X Receptor Agonists from Aspergillus puniceus

作者:Lu Xin Hua; Shi Qing Wen*; Zheng Zhi Hui; Ke Ai Bing; Zhang Hua; Huo Chang Hong; Ma Ying; Ren Xiao; Li Ye Ying; Lin Jie; Jiang Qin; Gu Yu Cheng; Kiyota Hiromasa
来源:European Journal of Organic Chemistry, 2011, 2011(4): 802-807.
DOI:10.1002/ejoc.201000812

摘要

Four novel oxepin-containing pyrimidines, namely oxepinamides D-G (1-4), were isolated from cultures of Aspergillus puniceus F02Z-1744. The structures of 1-4 were elucidated by analyzing their spectroscopic data generated by 1D and 2D NMR and MS methods. The configurations of 1 and 2 were established based on single-crystal X-ray crystallographic analysis. All four compounds 1-4 showed transcriptional activation on Liver X Receptor alpha (LXR alpha) with EC(50) values of 10.6, 12.8, 13.6, and 12.1 mu M, respectively.