State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
J Nat Prod. 2013 Jun 28;76(6):1039-46. doi: 10.1021/np400029d. Epub 2013 May 21.
Twelve new minor diterpenoids, possessing 5/6/8 (1 and 2), 5/6/7/3 (3-9), and 5/6/6/4 (10-12) fused-ring skeletons, as determined by spectroscopic analysis, were isolated from an ethanol extract of the roots of Euphorbia micractina, together with 25 known compounds. The structures of the diterpene skeletons are rare and have been found only in compounds isolated from Euphorbia micractina and Euphorbia villosa. On the basis of the octant rule for cyclohexanones, the absolute configurations of 1-12, as well as of the known euphactins A-D and euphoractins A-D (13-15), could be assigned by circular dichroism spectroscopy. In addition, the co-occurring jolkinol B (16) was chemically transformed to euphoractin E (17), supporting the absolute configuration assignment and the biogenetic relationship between the different types of diterpenes. Compound 9 showed activity against HIV-1 replication in vitro, with an IC50 value of 8.8 ± 0.6 μM.
从细叶飞扬草(Euphorbia micractina)的乙醇提取物中分离得到了 12 个新的小二萜类化合物，它们具有 5/6/8(1 和 2)、5/6/7/3(3-9)和 5/6/6/4(10-12)的稠合环骨架，这是通过光谱分析确定的。此外，还分离得到了 25 个已知化合物。这些二萜骨架的结构很罕见，只在从细叶飞扬草和飞扬草(Euphorbia villosa)中分离得到的化合物中发现过。根据环己酮的八分位规则，通过圆二色光谱可以确定 1-12 的绝对构型，以及已知的 euphactins A-D 和 euphoractins A-D(13-15)的绝对构型。此外，同时存在的jolkinol B(16)被化学转化为 euphoractin E(17)，这支持了绝对构型的分配和不同类型二萜之间的生物发生关系。化合物 9 对 HIV-1 复制具有体外抑制活性，IC50 值为 8.8±0.6 μM。
