Topoisomerase II-mediated DNA cleavage by adocia- and xestoquinones from the Philippine sponge Xestospongia sp

J Med Chem. 1995 Oct 27;38(22):4503-7. doi: 10.1021/jm00022a016.

G P Concepción ¹, T A Foderaro, G S Eldredge, E Lobkovsky, J Clardy, L R Barrows, C M Ireland

Affiliations

Affiliation

1 Marine Science Institute, University of the Philippines, Quezón City, Philippines.

PMID: 7473578 DOI: 10.1021/jm00022a016

Abstract

Investigation of an orange Xestospongia sp. Sponge collected at Cape Bolinao in northern Luzon, Philippines, yielded the known compounds adociaquinones A and B (1, 2) and six new metabolites, secoadociaquinones A and B (3, 4), 14-methoxyxestoquinone (5), 15-methoxyxestoquinone (6), 15-chloro-14-hydroxyxestoquinone (7), and 14-chloro-15-hydroxyxestoquinone (8). All compounds showed inhibition of Topoisomerase II in catalytic DNA unwinding and/or decatenation assays. Furthermore, adociaquinone B showed activity in a KSDS assay, suggesting it inhibits the enzyme by freezing the enzyme-DNA cleavable complex. Interestingly, adociaquinone B did not displace ethidium bromide from DNA or unwind supercoiled DNA, implying it does not intercalate DNA.

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