Antiplasmodial high-throughput screening of extracts derived from marine invertebrates collected from northern NSW, Australia, resulted in the methanol extract of the bryozoan Orthoscuticella ventricosa being identified as inhibitory toward the 3D7 strain of Plasmodium falciparum. Purification of this extract resulted in two new bis-β-carbolines that possess a cyclobutane moiety, orthoscuticellines A and B (1 and 2), three new β-carboline alkaloids, orthoscuticellines C−E (3−5), and six known compounds, 1-ethyl-4methylsulfone-β-carboline ( 6), 1-ethyl-β-carboline ( 7), 1-acetyl-β-carboline (8) 1-(1′-hydroxyethyl)-β-carboline ( 9), 1-methoxycarbonyl-β-carboline (10), and 1-vinyl-β-carboline (11). The structures of all compounds were determined from analysis of MS and 1D and 2D NMR data. The compounds showed modest antiplasmodial activity against P. falciparum in the range of 12−21 μM.
Diffusion-ordered NMR spectroscopy (DOSY) can be used to analyze mixtures of compounds since resonances deriving from different compounds are distinguished by their diffusion coefficients (D). Previously, DOSY has mostly been...
An extract from the bryozoan Amathia lamourouxi with antiplasmodial activity was identified through high-throughput screening of an Australian marine invertebrate extract library against Plasmodium falciparum. Chemical investigation of A. lamourouxi resulted in the isolation of six new brominated alkaloids, convolutamines K and L (1 and 2), volutamides F−H (3−5), and 2,5-dibromo-1-methyl-1H-indole-3-carbaldehyde (6). Three of the compounds (2−4) displayed moderate to potent antiplasmodial activity against both the chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) parasite strains of Plasmodium falciparum with an IC 50 range of 0.57−1.7 μM and a high selectivity index against a human cell line (HEK293).
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