Abstract
Nine bromotyrosine-derived compounds were isolated from the Caribbean marine sponge Verongula rigida. Two of them, aeroplysinin-1 (1) and dihydroxyaerothionin (2), are known compounds for this species, and the other seven are unknown compounds for this species, namely: 3,5-dibromo-N,N,N-trimethyltyraminium (3), 3,5-dibromo-N,N,N, O-tetramethyltyraminium (4), purealidin R (5), 19-deoxyfistularin 3 (6), purealidin B (7), 11-hydroxyaerothionin (8) and fistularin-3 (9). Structural determination of the isolated compounds was performed using one- and two-dimensional NMR, MS and other spectroscopy data. All isolated compounds were screened for their in vitro activity against three parasitic protozoa: Leishmania panamensis, Plasmodium falciparum and Trypanosoma cruzi. Compounds 7 and 8 showed selective antiparasitic activity at 10 and 5 μM against Leishmania and Plasmodium parasites, respectively. Cytotoxicity of these compounds on a human promonocytic cell line was also assessed.
Highlights
Tropical diseases caused by single-celled parasites, like malaria, leishmaniasis and Chagas disease, are of particular importance in tropical regions of the world
300,000 cells/well, which were treated with 1 μM of phorbol myristate acetate (PMA) for 48 h at 37 °C, after which they were infected with promastigotes of L. (V.) panamensis in stationary growth phase in modified NNN medium, at a 1:25 cell/parasite
Antiplasmodial activity was determined by DNA analysis using a fluorometric method with ethidium bromide dye (EtBr), and fluorescence was read at emission 510 nm and excitation 590 nm [41]
Summary
Tropical diseases caused by single-celled parasites, like malaria, leishmaniasis and Chagas disease, are of particular importance in tropical regions of the world. In the absence of a long-term protective vaccine, the control of these parasitic infections is based on a few chemotherapeutic agents Most of these agents are facing parasitic resistance, severe adverse effects and variable efficiency according to the phase of the disease. We have already investigated the antimicrobial, antiparasitic and antitumoral activity of the extracts of some sponges of this area, and Verongula rigida (Esper 1794, Verongida, Aplysinidae) appeared of high interest for its chemical composition [5,6,7]. This species, like other Verongida marine sponges, are of much biological and chemical interest. The selectivity indices were measured by dividing the antiparasitic activity of the compounds by their cytotoxicity against the promonocytic macrophage cell line U937
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