Abstract
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.
Published by Elsevier Ltd.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, N.I.H., Intramural
MeSH terms
-
ATP Binding Cassette Transporter, Subfamily G, Member 2
-
ATP-Binding Cassette Transporters / antagonists & inhibitors*
-
ATP-Binding Cassette Transporters / metabolism
-
Animals
-
Cell Line, Tumor
-
Dose-Response Relationship, Drug
-
Echinodermata / chemistry*
-
Humans
-
Molecular Conformation
-
Naphthalenes / chemistry
-
Naphthalenes / isolation & purification
-
Naphthalenes / pharmacology*
-
Neoplasm Proteins / antagonists & inhibitors*
-
Neoplasm Proteins / metabolism
-
Pyrones / chemistry
-
Pyrones / isolation & purification
-
Pyrones / pharmacology*
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
ABCG2 protein, human
-
ATP Binding Cassette Transporter, Subfamily G, Member 2
-
ATP-Binding Cassette Transporters
-
Naphthalenes
-
Neoplasm Proteins
-
Pyrones