Ren Yulin, Acuña Ulyana Muñoz, Jiménez Francisco, García Ricardo, Mejía Melciades, Chai Heebyung, Gallucci Judith C, Farnsworth Norman R, Soejarto Djaja D, Carcache de Blanco Esperanza J, Kinghorn A Douglas
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Tetrahedron. 2012 Mar 25;68(12):2671-2678. doi: 10.1016/j.tet.2012.01.061. Epub 2012 Jan 26.
Six new (1-6) and eight known germacranolide-type sesquiterpene lactones, along with several known phenylpropanol coumarates and methylated flavonoids, were isolated from the leaves of Piptocoma rufescens, collected in the Dominican Republic. The new compounds were identified by analysis of their spectroscopic data, with the molecular structure of 3 being established by single-crystal X-ray diffraction. The absolute configurations of the sesquiterpene lactones isolated were determined from their CD and NOESY NMR spectra, together with the analysis of Mosher ester reactions. Bioassay screening results showed the majority of the sesquiterpene lactones isolated (1-13) to be highly cytotoxic toward the HT-29 human colon cancer cell line, with the most potent compound being 15-deoxygoyazensolide (10, IC(50), 0.26 µM). In addition, several of the sesquiterpene lactones exhibited NF-κB (p65) inhibitory activity.
从采集于多米尼加共和国的红皮樟树叶中分离出6种新的（1 - 6）和8种已知的吉马烷型倍半萜内酯，以及几种已知的苯丙醇香豆酸盐和甲基化黄酮类化合物。通过对其光谱数据的分析鉴定了新化合物，其中3的分子结构通过单晶X射线衍射确定。从分离得到的倍半萜内酯的圆二色光谱（CD）和核Overhauser效应光谱（NOESY NMR），以及对莫舍尔酯反应的分析确定了其绝对构型。生物活性筛选结果表明，大多数分离得到的倍半萜内酯（1 - 13）对HT - 29人结肠癌细胞系具有高度细胞毒性，其中最有效的化合物是15 - 脱氧戈亚泽醇内酯（10，IC(50)，0.26 μM）。此外，几种倍半萜内酯表现出NF - κB（p65）抑制活性。
