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.

The isolation and structures of three novel scalarane sesterterpenes 1–3 and their inhibition of FXR transactivation are reported.Figure optionsDownload as PowerPoint slide