Nam Sang-Jip, Ko Hyunsil, Ju Moon Kyeong, Hwang Hoosang, Chin Jungwook, Ham Jungyeob, Lee Byoungchan, Lee Jaehwan, Won Dong Hwan, Choi Hyukjae, Ko Jaeyoung, Shin Kyoungjin, Oh Taekyung, Kim Seokho, Rho Jung-Rae, Kang Heonjoong
Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul, 151-747, Korea.
J Nat Prod. 2007 Nov;70(11):1691-5. doi: 10.1021/np070024k. Epub 2007 Nov 8.
Three new scalarane-based sesterterpenes, 1- 3, were isolated from a marine sponge of the genus Spongia, and their chemical structures were elucidated by analysis of HRMS and 2-D NMR spectra. The isolated compounds 1 and 3 showed inhibition against the farnesoid X-activated receptor (FXR) with IC50 values of 2.4 and 24 microM, respectively. In particular, compound 3 directly inhibited the interaction between FXR and a coactivator peptide (SRC-1) as determined by surface plasmon resonance (SPR) spectroscopy.
从海绵属的一种海洋海绵中分离出三种新的基于半日花烷的倍半萜烯（1 - 3），并通过高分辨质谱（HRMS）和二维核磁共振（2-D NMR）光谱分析阐明了它们的化学结构。分离出的化合物1和3对法尼醇X激活受体（FXR）具有抑制作用，IC50值分别为2.4和24微摩尔。特别地，通过表面等离子体共振（SPR）光谱测定，化合物3直接抑制FXR与共激活肽（SRC-1）之间的相互作用。
