College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, People's Republic of China.
Org Biomol Chem. 2018 Dec 19;17(1):195-202. doi: 10.1039/c8ob02519c.
Crotonols A and B (1 and 2), two tigliane diterpenoids featuring a rare C-7/C-14 cyclized and novel 5/7/7-fused carbon skeleton, along with the known tigliane wallichiioid A, were isolated from the leaves of Croton tiglium. Their structures were determined through spectroscopic methods, X-ray crystallography and ECD analysis. To the best of our knowledge, crotonol B (2) represents the first example of 13,14-seco-tigliane diterpenoids. Crotonols A and B displayed strong cytotoxic activities against the K562 cell line with IC50 values of 0.20 and 0.21 μM, respectively. Furthermore, crotonol A promoted the apoptosis of K562 cells through the cleavage of PARP and the accumulation of bax as well as the degradation of bcl-2.
克罗桐醇 A 和 B(1 和 2),两种具有罕见 C-7/C-14 环化和新颖的 5/7/7 稠合碳骨架的丁香烷二萜,以及已知的丁香烷壁衣酸 A,从巴豆叶中分离得到。通过光谱方法、X 射线晶体学和 ECD 分析确定了它们的结构。据我们所知,克罗桐醇 B(2)代表了第一个 13,14-去甲丁香烷二萜类化合物的例子。克罗桐醇 A 和 B 对 K562 细胞系表现出强烈的细胞毒性,IC50 值分别为 0.20 和 0.21 μM。此外,克罗桐醇 A 通过 PARP 的切割以及 bax 的积累和 bcl-2 的降解促进 K562 细胞的凋亡。