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Molecules 2014, 19(6), 7869-7880; doi:10.3390/molecules19067869

Secondary Metabolites from Vietnamese Marine Invertebrates with Activity against Trypanosoma brucei and T. cruzi

1
College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea
2
Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam
3
Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea
4
Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus, Corrensstrasse 48, Münster D-48149, Germany
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 4 April 2014 / Revised: 5 June 2014 / Accepted: 5 June 2014 / Published: 11 June 2014
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Abstract

Marine-derived natural products from invertebrates comprise an extremely diverse and promising source of the compounds from a wide variety of structural classes. This study describes the discovery of five marine natural products with activity against Trypanosoma species by natural product library screening using whole cell in vitro assays. We investigated the anti-trypanosomal activity of the extracts from the soft corals and echinoderms living in Vietnamese seas. Of the samples screened, the methanolic extracts of several marine organisms exhibited potent activities against cultures of Trypanosoma brucei and T. cruzi (EC50 < 5.0 μg/mL). Among the compounds isolated from these extracts, laevigatol B (1) from Lobophytum crassum and L. laevigatum, (24S)-ergost-4-ene-3-one (2) from Sinularia dissecta, astropectenol A (3) from Astropecten polyacanthus, and cholest-8-ene-3β,5α,6β,7α-tetraol (4) from Diadema savignyi showed inhibitory activity against T. brucei with EC50 values ranging from 1.57 ± 0.14 to 14.6 ± 1.36 μM, relative to the positive control, pentamidine (EC50 = 0.015 ± 0.003 μM). Laevigatol B (1) and 5α-cholest-8(14)-ene-3β,7α-diol (5) exhibited also significant inhibitory effects on T. cruzi. The cytotoxic activity of the pure compounds on mammalian cells was also assessed and found to be insignificant in all cases. This is the first report on the inhibitory effects of marine organisms collected in Vietnamese seas against Trypanosoma species responsible for neglected tropical diseases. View Full-Text
Keywords: soft coral; echinoderm; marine natural product; Trypanosoma brucei; Trypanosoma cruzi; neglected tropical diseases soft coral; echinoderm; marine natural product; Trypanosoma brucei; Trypanosoma cruzi; neglected tropical diseases
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MDPI and ACS Style

Thao, N.P.; No, J.H.; Luyen, B.T.T.; Yang, G.; Byun, S.Y.; Goo, J.; Kim, K.T.; Cuong, N.X.; Nam, N.H.; Van Minh, C.; Schmidt, T.J.; Kang, J.S.; Kim, Y.H. Secondary Metabolites from Vietnamese Marine Invertebrates with Activity against Trypanosoma brucei and T. cruzi. Molecules 2014, 19, 7869-7880.

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