Aaptamine is a spongean alkaloid that can activate the p21 promoter in the absence of p53 and can function as a proteasome inhibitor. The compound is a competitive antagonist of AR (α-adrenoreceptors) in vascular smooth muscle. Aaptamine can be converted to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine, with some of the aaptamine derivatives, such as 9-demethylaaptamine, showing antimicrobial activities. Research suggests that aaptamine can inhibit cancer cell growth and that its cytotoxicity may be due to its ability to intercalate DNA. Aaptamine is an inhibitor of CTRL.
1. Ohizumi, Y., et al. 1984. J. Pharm. Pharmacol. 36: 785-786. PMID: 6150989
2. Pettit, G.R., et al. 2004. J. Org. Chem. 69: 2251-2256. PMID: 15049616
3. Aoki, S., et al. 2006. Biochem. Biophys. Res. Commun. 342: 101-106. PMID: 16480688
4. Bowling, J.J., et al. 2008. Chem Biol Drug Des. 71: 205-215. PMID: 18251774
5. Tsukamoto, S., et al. 2010. Bioorg. Med. Chem. Lett. 20: 3341-3343. PMID: 20451377