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

doi:10.1021/np070024k

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

Department of Chemistry & Nanoscience

Research output: Contribution to journal › Article › peer-review

38 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 language	English
Pages (from-to)	1691-1695
Number of pages	5
Journal	Journal of Natural Products
Volume	70
Issue number	11
DOIs	https://doi.org/10.1021/np070024k
State	Published - Nov 2007

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title = "Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity",

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.",

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

year = "2007",

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doi = "10.1021/np070024k",

language = "English",

volume = "70",

pages = "1691--1695",

journal = "Journal of Natural Products",

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T1 - Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity

AU - Nam, Sang Jip

AU - Ko, Hyunsil

AU - Moon, Kyeong Ju

AU - Hwang, Hoosang

AU - Chin, Jungwook

AU - Ham, Jungyeob

AU - Lee, Byoungchan

AU - Lee, Jaehwan

AU - Dong, Hwan Won

AU - Choi, Hyukjae

AU - Ko, Jaeyoung

AU - Shin, Kyoungjin

AU - Oh, Taekyung

AU - Kim, Seokho

AU - Rho, Jung Rae

AU - Kang, Heonjoong

PY - 2007/11

Y1 - 2007/11

N2 - 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.

AB - 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.

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EP - 1695

JO - Journal of Natural Products

JF - Journal of Natural Products

IS - 11

ER -

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

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