title: Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor.
abstract: Aaptamine (1), isoaaptamine (2), and demethylaaptamine (3) were isolated from the marine sponge Aaptossuberitoides collected in Indonesia as inhibitors of the proteasome. They inhibited the chymotrypsin-like and caspase-like activities of the proteasome with IC(50) values of 1.6-4.6 microg/mL, while they showed less inhibition of the trypsin-like activity of the proteasome. The three compounds showed cytotoxic activities against HeLa cells, but their cytotoxicity did not correlate with their potency as proteasome inhibitors, strongly suggesting that their proteasomal inhibitory activity is dispensable to their cytotoxicity.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan. sachiko@kumamoto-u.ac.jp
authors.forename: Sachiko
authors.initials: S
authors.lastname: Tsukamoto
authors.forename: Rumi
authors.initials: R
authors.lastname: Yamanokuchi
authors.forename: Makiko
authors.initials: M
authors.lastname: Yoshitomi
authors.forename: Kohei
authors.initials: K
authors.lastname: Sato
authors.forename: Tsuyoshi
authors.initials: T
authors.lastname: Ikeda
authors.forename: Henki
authors.initials: H
authors.lastname: Rotinsulu
authors.forename: Remy E P
authors.initials: RE
authors.lastname: Mangindaan
authors.forename: Nicole J
authors.initials: NJ
authors.lastname: de Voogd
authors.forename: Rob W M
authors.initials: RW
authors.lastname: van Soest
authors.forename: Hideyoshi
authors.initials: H
authors.lastname: Yokosawa
mesh_terms: D000818:Animals; D006367:HeLa Cells; D006801:Humans; D009287:Naphthyridines / Q000302:isolation & purification / Q000494:pharmacology*; D011161:Porifera / Q000737:chemistry*; D011480:Protease Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D061988:Proteasome Inhibitors
chemical_list: D009287:Naphthyridines; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; C043986:aaptamine