Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.
Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.
Fitoterapia. 2020 Oct;146:104718. doi: 10.1016/j.fitote.2020.104718. Epub 2020 Aug 31.
Two new ingenane diterpenoids (1-2), four new jatrophane diterpenoids (3-6), and seven known analogues (7-13), were isolated from the 95% ethanol extract of Euphorbia esula. Their structures were determined by extensive spectroscopic methods and ECD data analysis. These compounds were assayed for their anti-osteoporotic activity in a bone marrow-derived macrophage (BMM) cell line, and compounds 2, 4, 7, 8, 9, and 11 significantly inhibited the formation of osteoclasts with IC values of 3.4, 4.3, 2.1, 0.5, 1.5, and 4.5 μM, respectively. These compounds also dose-dependently reduced the activity of nuclear factor activated T-cell cytoplasmic 1 (NFATc1). This study reveals the anti-osteoporotic effects of ingenane diterpenoids for the first time.
从Euphorbia esula 的 95%乙醇提取物中分离得到了两种新的 ingenane 二萜（1-2）、四种新的 jatrophane 二萜（3-6）和七种已知类似物（7-13）。通过广泛的光谱方法和 ECD 数据分析确定了它们的结构。这些化合物在骨髓来源的巨噬细胞（BMM）细胞系中进行了抗骨质疏松活性测试，化合物 2、4、7、8、9 和 11 分别以 3.4、4.3、2.1、0.5、1.5 和 4.5 μM 的 IC 值显著抑制破骨细胞的形成。这些化合物还剂量依赖性地降低了核因子活化 T 细胞胞浆 1（NFATc1）的活性。这项研究首次揭示了 ingenane 二萜的抗骨质疏松作用。
