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DOI: 10.1055/s-0034-1382374
Characterization of membranolides B-H from Dendrilla membranosa and their activity against leishmaniasis
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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