Department of Natural Products Chemistry, Key Laboratory of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University , No. 44 West Wenhua Road, Jinan 250012, People's Republic of China.
J Nat Prod. 2014 Jun 27;77(6):1336-44. doi: 10.1021/np5000507. Epub 2014 Jun 18.
Four new ent-labdane diterpenoids, heteroscyphins A-D (1-4), and four known diterpenoids (5-8) were isolated from the Chinese liverwort Heteroscyphus tener (Steph.) Schiffn. The absolute configuration of compound 1 was defined by single-crystal X-ray diffraction using Cu Kα radiation. Cytotoxicity tests revealed that compounds 3 and 5 exhibited modest activity against seven cancer cell lines. Compound 5 showed inhibitory effects on prostate cancer (PCa) cell proliferation but with less inhibition on non-neoplastic prostate epithelial cells. Compound 5 markedly caused cell growth arrest at the G0/G1 phase and induced cellular apoptosis through ROS-mediated DNA damage in PCa cells.
从中国的地钱属植物 Heteroscyphus tener (Steph.) Schiffn 中分离得到了四个新的 ent-labdane 二萜，分别为 heteroscyphins A-D（1-4），以及四个已知的二萜（5-8）。化合物 1 的绝对构型是通过单晶 X 射线衍射用 Cu Kα 辐射确定的。细胞毒性试验表明，化合物 3 和 5 对七种癌细胞系具有中等活性。化合物 5 对前列腺癌（PCa）细胞增殖具有抑制作用，但对非肿瘤前列腺上皮细胞的抑制作用较弱。化合物 5 通过 ROS 介导的 DNA 损伤，显著地将细胞生长阻滞在 G0/G1 期，并诱导 PCa 细胞发生细胞凋亡。
