Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.
Three novel (1-3) and two known (4-5) scalarane sesterterpenes were isolated from a marine sponge of the genus Spongia. The isolated compounds showed potent inhibition of transactivation for the nuclear hormone receptor, FXR (farnesoid X-activated receptor), which is a promising drug target to treat hypercholesterolemia in humans.
Nam
Sang-Jip
SJ
Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul, 151-747, Republic of Korea.
Ko
Hyunsil
H
Shin
Mihee
M
Ham
Jungyeob
J
Chin
Jungwook
J
Kim
Youngshin
Y
Kim
Heeyoung
H
Shin
Kyoungjin
K
Choi
Hyukjae
H
Kang
Heonjoong
H
D000818:Animals; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002522:Chlorocebus aethiops; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D009682:Magnetic Resonance Spectroscopy / Q000379:methods / Q000592:standards; D008968:Molecular Conformation; D011161:Porifera / Q000737:chemistry*; D018160:Receptors, Cytoplasmic and Nuclear / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D012015:Reference Standards; D054830:Sesterterpenes; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000737:chemistry / Q000494:pharmacology*; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D015533:Transcriptional Activation / Q000187:drug effects*; D014162:Transfection; D000099150:Receptor, Farnesoid X-Activated
D004268:DNA-Binding Proteins; D018160:Receptors, Cytoplasmic and Nuclear; D054830:Sesterterpenes; D013729:Terpenes; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated