Planta Med 2015; 81 - PQ16
DOI: 10.1055/s-0035-1556350

Isolation of strongylophorines from the marine sponge Petrosia corticata, as proteasome inhibitors

S Tsukamoto 1, A Noda 1, E Sakai 1, H Kato 1
  • 1Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto 862 – 0973, Japan

The proteasome is a new oncology target after the approval of Velcade® and we have been searching for new inhibitors from natural sources. Recently, we isolated two new strongylophorines (1 and 2) along with six known congeners (3-8) from the marine sponge Petrosia corticata and measured their inhibitory activities against the chymotrypsin-like activity of the proteasome.

Fig. 1: Structure-activity relationship of strongylophorines with their IC50 values for the inhibition of the proteasome.