Antiproliferative and antimalarial sesquiterpene lactones from Piptocoma antillana from Puerto Rico.

作者: Liu Yixi Liu Yixi , LH Rakotondraibe , PJ Brodie , JD Wiley , MB Cassera

DOI: 10.1177/1934578X1400901002

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摘要: Bioassay-directed fractionation of an antiproliferative ethanol extract the leaves and twigs Piptocoma antillana (Asteraceae) afforded two new goyazensolide-type sesquiterpene lactones named 5-O-methyl-5-epiisogoyazensolide (1) 15-O-methylgoyazensolide (2), together with known compounds 1-oxo-3,10-epoxy-8-(2-methylacr1 0-epoxy-8-(2-methylacryloxy)-l 5-acetoxygermacra-2,4, 11(1 3)-trien-6(12)-olide (3) 5-epiisogoyazensolide (4). The structure elucidation all was carried out based on NMR mass spectroscopic data analyses. relative absolute configurations isolated were determined from their CD NOESY spectra. Compounds 1-4 showed moderately potent activities against A2780 ovarian cancer cells, IC50 values 1.5 +0.5, 0.6 ± 0.3, 1.62 0.05, 1.56 0.04 μM, respectively. They also displayed antimalarial activity Plasmodiumfalciparum, 6.2 05 22 0.5, 2.2± 8.0 0.4, 9.0

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