Scalarane Sesterterpenes from a Marine Sponge of the Genus Spongia and Their FXR Antagonistic Activity

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• 作者：Sang-Jip Nam ; Hyunsil Ko ; Moon Kyeong Ju ; Hoosang Hwang ; Jungwook Chin ; Jungyeob Ham ; Byoungchan Lee ; Jaehwan Lee ; Dong Hwan Won ; Hyukjae Choi ; Jaeyoung Ko ; Kyoungjin Shin ; Taekyung Oh ; Seokho Kim ; Ju
• 刊名：Journal of Natural Products
• 出版年：2007
• 出版时间：November 2007
• 年：2007
• 卷：70
• 期：11
• 页码：1691 - 1695
• 全文大小：210K
• 年卷期：v.70,no.11(November 2007)
• ISSN：1520-6025

文摘

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 µM, 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.