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

Molecules

Nguyen Phuong Thao⁴  Bui Thi Thuy Luyen⁴  Reto Brun²  Marcel Kaiser²  Phan Van Kiem³  Chau Van Minh³  Thomas J. Schmidt¹  Jong Seong Kang⁴  Young Ho Kim⁴ 

[1] Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus, Corrensstrasse 48, Münster D-48149, Germany;Swiss Tropical and Public Health Institute (Swiss TPH), Socinstrasse 57, Basel CH-4002, Switzerland; 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:

关键词: soft coral;    cembrane-type diterpenes;    marine natural product;    anti-protozoal activity;    Trypanosoma brucei;    Leishmania donovani;    Plasmodium falciparum;    neglected tropical diseases;   

DOI  :  10.3390/molecules200712459

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.