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. 2010 Jul 1;20(13):3848-50.
doi: 10.1016/j.bmcl.2010.05.057. Epub 2010 May 21.

Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids

Heidi R Bokesch  1 , Laura K Cartner, Richard W Fuller, Jennifer A Wilson, Curtis J Henrich, James A Kelley, Kirk R Gustafson, James B McMahon, Tawnya C McKee
Affiliations

Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids

Heidi R Bokesch et al. Bioorg Med Chem Lett. .

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.

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References

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    1. Capillaster multiradiatus was collected in Palau (1993) by P. Collin of the Coral Reef Research Foundation. Comanthus parvicirrus and a taxonomically unidentified crinoid were collected in northern Australia (1991 and 1988, respectively) by P. Murphy of the Australian Institute of Marine Sciences. Voucher specimens (Capillaster - 0CDN1152, Comanthus – Q66C5685, unknown - Q66C1600) are maintained at the Smithsonian Institute.

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