期刊
MARINE DRUGS
卷 7, 期 4, 页码 640-653出版社
MDPI
DOI: 10.3390/md7040640
关键词
Pseudoceratina; Pfnek-1; homogentisic acid derivatives; Plasmodium falciparum
As part of our search for new antimalarial drugs in South Pacific marine sponges, we have looked for inhibitors of Pfnek-1, a specific protein kinase of Plasmodium falciparum. On the basis of promising activity in a preliminary screening, the ethanolic crude extract of a new species of Pseudoceratina collected in Vanuatu was selected for further investigation. A bioassay-guided fractionation led to the isolation of a derivative of homogentisic acid [methyl (2,4-dibromo-3,6-dihydroxyphenyl)acetate, 4a] which inhibited Pfnek-1 with an IC50 around 1.8 mu M. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC50 = 12 mu M). From the same sponge, we isolated three known compounds [11,19-dideoxyfistularin-3 (1), 11-deoxyfistularin-3 (2) and dibromo-verongiaquinol (3)] which were inactive against Pfnek-1. Synthesis and biological evaluation of some derivatives of 4a are reported.
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