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

Molecules

Nguyen Phuong Thao³  Joo Hwan No¹  Bui Thi Thuy Luyen³  Gyongseon Yang¹  Soo Young Byun¹  Junghyun Goo¹  Kyung Tae Kim³  Nguyen Xuan Cuong²  Nguyen Hoai Nam²  Chau Van Minh²  Thomas J. Schmidt⁴  Jong Seong Kang³ 

[1] Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea; E-Mails:;Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam; E-Mails:;College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea; E-Mails:;Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus, Corrensstrasse 48, Münster D-48149, Germany; E-Mail:

关键词: soft coral;    echinoderm;    marine natural product;    Trypanosoma brucei;    Trypanosoma cruzi;    neglected tropical diseases;   

DOI  :  10.3390/molecules19067869

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.