ECB-ART-48206
Bioorg Med Chem Lett
2010 Jul 01;2013:3848-50. doi: 10.1016/j.bmcl.2010.05.057.
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Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids.
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Five new naphthopyrones (1-5) along with the known compounds TMC-256A1, 5,8-dihydroxy-6-methoxy-2-propyl-4H-naphtho[2,3-b]pyran-4-one, TMC-256C1, comaparvin, 6-methoxycomaparvin, and 6-methoxycomaparvin 5-methyl ether (6-11) were isolated from crinoids of the family Comasteridae. All compounds were tested for their ability to inhibit the multidrug transporter ABCG2, which plays a role in drug resistance. Six of the seven angular naphthopyrones showed moderate activity with <60% inhibition of ABCG2-mediated transport as compared to the positive control fumitremorgin C. None of the linear naphthopyrones inhibited ABCG2-mediated efflux.
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Genes referenced: LOC578540
References [+] :
Folmer,
NF-kappaB-inhibiting naphthopyrones from the Fijian echinoderm Comanthus parvicirrus.
2008, Pubmed,
Echinobase