Planta Med 2014; 80 - PB8
DOI: 10.1055/s-0034-1382374

Characterization of membranolides B-H from Dendrilla membranosa and their activity against leishmaniasis

C Witowski 1, 2, A Maschek 1, B Vesely 3, D Kyle 3, J McClintock 4, C Amsler 4, B Baker 1, 2
  • 1Departments of Chemistry
  • 2Global Health
  • 3Center for Drug Discovery and Innovation, University of South Florida, Tampa, FL 33612
  • 4Department of Biology, University of Alabama at Birmingham, Birmingham, AL 35294

Leishmaniasis is a neglected tropical disease that affects nearly one million people per year and can be fatal if left untreated. In a screening program, the Antarctic sponge Dendrilla membranosa was found to produce diterpenoid secondary metabolites with activity against the leishmaniasis-causing parasite Leishmania donovani. Dichloromethane/methanol (1:1) extracts of the sponge yielded aplysulphurin, its tetrahydro- derivative, and a suite of membranolides, some of which displayed potent bioactivity. In an investigation of membranolides B-H, aplysulphurin was subjected to methanolic treatments and the newly formed compounds were isolated. Upon characterization, these compounds showed identical spectral characteristics to the methoxy-bearing membranolides. The IC50 values of these compounds were assessed in a structure activity relationship (SAR) study targeting anti-leishmanial efficacy.

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