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Molecules 2015, 20(7), 12459-12468; doi:10.3390/molecules200712459

Anti-Protozoal Activities of Cembrane-Type Diterpenes from Vietnamese Soft Corals

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
Swiss Tropical and Public Health Institute (Swiss TPH), Socinstrasse 57, Basel CH-4002, Switzerland
4
University of Basel, Petersplatz 1, Basel CH-4003, Switzerland
5
Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus, Corrensstrasse 48, Münster D-48149, Germany
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 29 May 2015 / Revised: 2 July 2015 / Accepted: 3 July 2015 / Published: 8 July 2015
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Abstract

Based on our previous finding that certain cembranoid diterpenes possess selective toxicity against protozoan pathogens of tropical diseases such as Trypanosoma and Plasmodium, we have subjected a series of 34 cembranes isolated from soft corals living in the Vietnamese sea to an in vitro screening for anti-protozoal activity against Trypanosoma brucei rhodesiense (Tbr), T. cruzi (Tc), Leishmania donovani (Ld), and Plasmodium falciparum (Pf). Twelve of the tested compounds displayed significant activity against at least one of the parasites. Specifically, 7S,8S-epoxy-1,3,11-cembratriene-16-oic methyl ester (1), (1R,4R,2E,7E,11E)-cembra-2,7,11-trien-4-ol (2), crassumol D (12), crassumol E (13), and (1S,2E,4S,6E,8S,11S)-2,6,12(20)-cembrantriene-4,8,11-triol (16) from Lobophytum crassum, L. laevigatum, and Sinularia maxima showed the highest level of inhibitory activity against T. b. rhodesiense, with IC50 values of about 1 µM or less. Lobocrasol A (6) and lobocrasol C (8) from L. crassum and L. laevigatum exhibited particularly significant inhibitory effects on L. donovani with IC50 values < 0.2 µM. The best antiplasmodial effect was exerted by laevigatol A (10), with an IC50 value of about 3.0 µM. The cytotoxicity of the active compounds on L6 rat skeletal myoblast cell was also assessed and found to be insignificant in all cases. This is the first report on anti-protozoal activity of these compounds, and points out the potential of the soft corals in discovery of new anti-protozoal lead compounds. View Full-Text
Keywords: soft coral; cembrane-type diterpenes; marine natural product; anti-protozoal activity; Trypanosoma brucei; Leishmania donovani; Plasmodium falciparum; neglected tropical diseases soft coral; cembrane-type diterpenes; marine natural product; anti-protozoal activity; Trypanosoma brucei; Leishmania donovani; Plasmodium falciparum; neglected tropical diseases
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Thao, N.P.; Luyen, B.T.T.; Brun, R.; Kaiser, M.; Van Kiem, P.; Van Minh, C.; Schmidt, T.J.; Kang, J.S.; Kim, Y.H. Anti-Protozoal Activities of Cembrane-Type Diterpenes from Vietnamese Soft Corals. Molecules 2015, 20, 12459-12468.

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