College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea.
Bioorg Med Chem. 2011 Apr 15;19(8):2625-32. doi: 10.1016/j.bmc.2011.03.009. Epub 2011 Mar 12.
Four new cembranoids, namely laevigatol A-D (1-4), and six known metabolites (5-10), were isolated from the Vietnamese soft coral Lobophytum laevigatum. The structures of these compounds were elucidated by extensive spectroscopic analyses, and the absolute stereochemistry of 1 was determined using the modified Mosher's method. Compounds 5, and 7-10 exhibited cytotoxic activity against selected human cancer cell lines. Compounds 1, 2, 8, and 9 showed dose-dependent inhibitory effects on the TNFα-induced NF-κB transcriptional activity in Hep-G2 cells. Moreover, compounds 1, 2, 8, and 9 significantly inhibited the induction of COX-2 and iNOS mRNA dose-dependently, indicating that these compounds attenuated the synthesis of these transcripts at the transcriptional level.
从越南软珊瑚 Lobophytum laevigatum 中分离得到四个新的海鞘素类似物，即 laevigatol A-D（1-4），以及六个已知代谢物（5-10）。通过广泛的光谱分析阐明了这些化合物的结构，并使用改良的 Mosher 法确定了 1 的绝对立体化学。化合物 5、7-10 对选定的人癌细胞系表现出细胞毒性活性。化合物 1、2、8 和 9 对 Hep-G2 细胞中 TNFα 诱导的 NF-κB 转录活性具有剂量依赖性抑制作用。此外，化合物 1、2、8 和 9 显著抑制 COX-2 和 iNOS mRNA 的诱导，呈剂量依赖性，表明这些化合物在转录水平上减弱了这些转录物的合成。
