Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.
School of Biomedical Sciences, The University of Western Australia, Perth, Western Australia 6009, Australia.
J Nat Prod. 2020 Apr 24;83(4):1005-1017. doi: 10.1021/acs.jnatprod.9b00929. Epub 2020 Apr 1.
Eighteen new jatrophane diterpenoids, euphoesulatins A-R (-), and three known diterpenoids (-) were isolated from Compounds -, , and represent a rare type of jatrophane-type diterpenoid containing a nicotinoyloxy group. The absolute configuration of was determined by X-ray crystallography. The compounds were assayed for their antiosteoporotic activity in a bone-marrow-derived macrophage cell line, and compounds , , and significantly inhibited the formation of osteoclasts, with IC values of 1.2, 3.5, and 2.3 μM, respectively. These three compounds also dose-dependently reduced the activity of nuclear factor activated T-cell cytoplasmic 1. This study reveals the antiosteoporotic effects of jatrophane diterpenoids for the first time.
十八种新的大戟烷二萜类化合物， euphoesulatins A-R（-），以及三种已知的二萜类化合物（-）从 中分离得到。化合物-、-和-代表了一种罕见的含烟酰氧基的大戟烷型二萜类化合物。通过 X 射线晶体学确定了 的绝对构型。对这些化合物在骨髓来源的巨噬细胞系中的抗骨质疏松活性进行了检测，化合物-、-和-显著抑制破骨细胞的形成，IC 值分别为 1.2、3.5 和 2.3 μM。这三种化合物还剂量依赖性地降低了核因子激活 T 细胞细胞质 1 的活性。这项研究首次揭示了大戟烷二萜类化合物的抗骨质疏松作用。
