Avarol, a cytostatically active compound from the marine sponge dysidea avara

Abstract

1. A main metabolic product of the sponge Dysidea avara was isolated and purified and subsequently identified as avarol by applying a series of analytical techniques, e.g. [ 13C]NMR, [ 1H]NMR and i.r. spectroscopy. 2.This sesquiterpenoid hydroquinone was found to possess strong cytostatic activity. Using the L5178y mouse lymphoma cell system in vitro (roller tube assays) avarol reduced cell growth to 50% at a concentration of 0.9μM. Avarol treated cells did not show “unbalanced growth”. 3. Avarol interfered with mitotic processes, preventing telophase formation. 4. Incorporation studies with precursors for DNA, RNA, protein and glycoprotein syntheses revealed increased incorporation rates in response to avarol treatment. 5. From these results and further autoradiographical experiments it is suggested that inhibition of cell growth is due to changes of the intraeellular pools and/or alterations of the permeability properties of the cell membrane for the precursors. 6. Avarol diacetate caused the same cytostatic effect as avarol.