np300750q_si_003.cif (23.84 kB)
Antiproliferative and Antiplasmodial Dimeric Phloroglucinols from Mallotus oppositifolius from the Madagascar Dry Forest
dataset
posted on 2016-02-19, 16:25 authored by Liva Harinantenaina, Jessica D. Bowman, Peggy J. Brodie, Carla Slebodnick, Martin W. Callmander, Etienne Rakotobe, Richard Randrianaivo, Vincent E. Rasamison, Alexander Gorka, Paul D. Roepe, Maria B. Cassera, David G. I. KingstonBioassay-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).
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6.3falciparum1.10assayantimalarialcompoundantiproliferativeAntiplasmodial Dimeric PhloroglucinolsfractionationcrystalCompoundIC 50 valuesmallotophenonespectroscopicethanolinflorescencebioactive0.30Plasmodiumbasis0.04cancer cell linemallotojaponinphloroglucinolisolationdimericAntiproliferativespectrometryMadagascar1.30.10.4evidenceMallotus oppositifolius0.750.14spectra
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