Jiao Wei, Dong Weiwei, Li Zhefeng, Deng Meicai, Lu Runhua
Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, China.
Bioorg Med Chem. 2009 Jul 1;17(13):4786-92. doi: 10.1016/j.bmc.2009.04.041. Epub 2009 Apr 24.
Two lathyrane diterpenes (1-2) together with previous ones (3-6) were isolated from Euphorbia lathyris. The structures of 1 and 2 were established on the basis of extensive spectroscopic methods, including two-dimensional NMR techniques. Stereo configuration and conformation of 1 and 2 were analyzed by X-ray diffraction for the first time. The configuration of the unique isolathyrol diterpene 2 from the seeds of E. Lathyris, was rectified from S * to R * at C-5. All compounds were examined as modulators of multidrug resistance on MCF-7/ADM cell lines in vitro. Their structure-activity relationship was discussed from aspect of different skeletons. A class of potential P-gp inhibitors with five different types (jokinol, isolathyrol, epoxylathyrol, 7-hydroxylathyrol, lathyrol) was discovered.
从续随子中分离出两种赖百当型二萜（1-2）以及之前的几种（3-6）。1和2的结构是基于广泛的光谱方法确定的，包括二维核磁共振技术。首次通过X射线衍射分析了1和2的立体构型和构象。续随子种子中独特的异千金二萜2在C-5位的构型从S校正为R。所有化合物均在体外作为MCF-7/ADM细胞系多药耐药性的调节剂进行了检测。从不同骨架的角度讨论了它们的构效关系。发现了一类具有五种不同类型（千金二萜醇、异千金二萜醇、环氧千金二萜醇、7-羟基千金二萜醇、千金二萜醇）的潜在P-糖蛋白抑制剂。
