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.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Crystallography, X-Ray
  • DNA / drug effects*
  • DNA / metabolism
  • Drug Screening Assays, Antitumor
  • Humans
  • Intercalating Agents
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Philippines
  • Porifera / chemistry*
  • Quinones / chemistry
  • Quinones / isolation & purification
  • Quinones / pharmacology*
  • Topoisomerase II Inhibitors*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Intercalating Agents
  • Quinones
  • Topoisomerase II Inhibitors
  • DNA
  • xestoquinone