Secondary metabolites from Vietnamese marine invertebrates with activity against Trypanosoma brucei and T. cruzi

• Published in: Molecules (Basel, Switzerland) Switzerland), 2014-06, Vol.19 (6), p.7869-7880
• Main Authors: Thao, Nguyen Phuong, No, Joo Hwan, Luyen, Bui Thi Thuy, Yang, Gyongseon, Byun, Soo Young, Goo, Junghyun, Kim, Kyung Tae, Cuong, Nguyen Xuan, Nam, Nguyen Hoai, Van Minh, Chau, Schmidt, Thomas J, Kang, Jong Seong, Kim, Young Ho
• Format: Article
• Language: English
• Subjects: Animals; Anthozoa - metabolism; Aquatic Organisms - metabolism; Astropecten polyacanthus; Biological Products - adverse effects; Biological Products - pharmacology; Cell Line; Cell Survival - drug effects; Chagas Disease - drug therapy; Cytotoxicity; Diadema savignyi; Drugs; echinoderm; Echinodermata - metabolism; HEK293 Cells; Hep G2 Cells; Humans; Infections; Invertebrata; Invertebrates; Investigations; Libraries; Lobophytum crassum; Marine; marine natural product; Metabolites; Natural products; Neglected Diseases - drug therapy; neglected tropical diseases; Pharmaceutical industry; Protozoa; R&D; Research & development; Secondary Metabolism; Sinularia dissecta; soft coral; Tropical diseases; Trypanocidal Agents - pharmacology; Trypanosoma brucei; Trypanosoma brucei brucei - drug effects; Trypanosoma cruzi; Trypanosoma cruzi - drug effects; Trypanosomiasis, African - drug therapy; Vietnam
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules19067869

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.