来自海绵属海洋海绵的半日花烷倍半萜及其法尼醇X受体拮抗活性。

Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.

作者信息

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

机构信息

Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul, 151-747, Korea.

出版信息

J Nat Prod. 2007 Nov;70(11):1691-5. doi: 10.1021/np070024k. Epub 2007 Nov 8.

DOI:10.1021/np070024k

PMID:17988093

Abstract

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.

摘要

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。