National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, and Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, University, Mississippi 38677, USA.
J Nat Prod. 2009 Dec;72(12):2091-7. doi: 10.1021/np900334k.
Nine new tetranorditerpenoid dilactones (2-10), together with two previously reported norditerpenoids dilactones (1, 11), and two known putative biosynthetic intermediates, oidiolactone-E (12) and 13, were isolated from an ethyl acetate extract of a culture medium of Sclerotinia homoeocarpa. Structures and absolute configurations of these compounds were determined by spectroscopic methods and confirmed by X-ray crystallographic analysis of representative compounds. Compounds were evaluated for herbicidal, antiplasmodial, and cytotoxic activities. Compounds 1, 2, 6, 7, and 11 were more active as growth inhibitors in a duckweed bioassay (I(50) values of 0.39-0.95 microM) than more than half of 26 commercial herbicides previously evaluated using the same bioassay. Some of these compounds exhibited strong antiplasmodial activities as well, but they also had cytotoxic activity, thus precluding them as potential antimalarial agents.
从核盘菌（Sclerotinia homoeocarpa）发酵培养基的乙酸乙酯提取物中分离得到了 9 个新的四环二萜内酯（2-10），以及 2 个先前报道的四环二萜内酯（1、11）和 2 个已知的假定生物合成中间体，奥地奥内酯-E（12）和 13。通过光谱方法确定了这些化合物的结构和绝对构型，并通过代表化合物的 X 射线晶体学分析得到了证实。对这些化合物进行了除草、抗疟原虫和细胞毒性活性评价。与以前使用相同生物测定法评估的 26 种商业除草剂中的一半以上相比，化合物 1、2、6、7 和 11 作为浮萍生物测定中的生长抑制剂更为有效（I(50) 值为 0.39-0.95 microM）。其中一些化合物还表现出很强的抗疟原虫活性，但也具有细胞毒性，因此不能作为潜在的抗疟药物。
