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

Sang Jip Nam, Hyunsil Ko, Kyeong Ju Moon, Hoosang Hwang, Jungwook Chin, Jungyeob Ham, Byoungchan Lee, Jaehwan Lee, Hwan Won Dong, Hyukjae Choi, Jaeyoung Ko, Kyoungjin Shin, Taekyung Oh, Seokho Kim, Jung Rae Rho, Heonjoong Kang

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

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 IC 50 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.

Original languageEnglish
Pages (from-to)1691-1695
Number of pages5
JournalJournal of Natural Products
Volume70
Issue number11
DOIs
StatePublished - Nov 2007

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