1. Antiproliferative and Antiplasmodial Dimeric Phloroglucinols from Mallotus oppositifolius from the Madagascar Dry Forest1#
- Author
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Harinantenaina, Liva, Bowman, Jessica D., Brodie, Peggy J., Slebodnick, Carla, Callmander, Martin W., Rakotobe, Etienne, Randrianaivo, Richard, Rasamison, Vincent E., Gorka, Alexander, Roepe, Paul D., Cassera, Maria B., and Kingston, David G. I.
- Subjects
Molecular Structure ,Plasmodium falciparum ,Drug Resistance ,Chloroquine ,Phloroglucinol ,Antineoplastic Agents, Phytogenic ,Article ,Trees ,Plant Leaves ,Antimalarials ,Inhibitory Concentration 50 ,Mallotus Plant ,Madagascar ,Humans ,Female ,Drug Screening Assays, Antitumor - Abstract
Bioassay-guided fractionation of an ethanol extract of the leaves and inflorescence of Mallotus oppositifolius collected in Madagascar led to the isolation of the two new bioactive dimeric phloroglucinols mallotojaponins B (1) and C (2), together with the known mallotophenone (3). The structures of the new compounds were determined on the basis of spectroscopic evidence, including their 1D- and 2D-NMR spectra, mass spectrometry, and an X-ray crystal structure. Compounds 1 and 2 showed potent antimalarial activity against chloroquine-resistant Plasmodium falciparum, with IC50 values of 0.75 ± 0.30 and 0.14 ± 0.04 μM, while 3 was inactive in this assay. Compounds 1-3 also displayed strong antiproliferative activity against the A2780 human ovarian cancer cell line (IC50 1.10 ± 0.05, 1.3 ± 0.1 and 6.3 ± 0.4 μM, respectively).
- Published
- 2013