2. Academic Validation
  3. Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor

Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor

  • Bioorg Med Chem Lett. 2010 Jun 1;20(11):3341-3. doi: 10.1016/j.bmcl.2010.04.029.
Sachiko Tsukamoto 1,  Rumi Yamanokuchi,  Makiko Yoshitomi,  Kohei Sato,  Tsuyoshi Ikeda,  Henki Rotinsulu,  Remy E P Mangindaan,  Nicole J de Voogd,  Rob W M van Soest,  Hideyoshi Yokosawa
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan. sachiko@kumamoto-u.ac.jp
PMID: 20451377 DOI: 10.1016/j.bmcl.2010.04.029
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.

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