Cynaropicrin : the first natural product with in vivo activity against Trypanosoma bruce rhodesiense

Zimmermann, S. and Kaiser, M. and Brun, R. and Hamburger, M. and Adams, M.. (2012) Cynaropicrin : the first natural product with in vivo activity against Trypanosoma bruce rhodesiense. Planta medica, Vol. 78, H. 6. pp. 553-556.

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Official URL: http://edoc.unibas.ch/dok/A6043786

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A screen of 1800 plant and fungal extracts with subsequent HPLC-based activity profiling was done to identify new antiprotozoal leads from nature. This led to the identification of cynaropicrin (1) from the herb CENTAUREA SALMANTICA L. (Asteraceae) as a potent IN VITRO inhibitor of TRYPANOSOMA BRUCEI RHODESIENSE. It preferentially inhibited T. B. RHODESIENSE (IC (50) of 0.3 microM) and T. BRUCEI GAMBIENSE (IC (50) of 0.2 microM), compared to TRYPANOSOMA CRUZI (IC (50) of 4.4 microM) and PLASMODIUM FALCIPARUM (IC (50) of 3.0 microM). Testing against melarsoprol- and pentamidine-resistant strains (IC (50)s of 0.3 microM and 0.1 microM, respectively) showed no cross-resistance. Intraperitoneal administration of 2 x 10 mg/kg body weight/day in the T. B. RHODESIENSE STIB 900 acute mouse model led to a 92 % reduction of parasitemia compared to untreated controls on day seven post-infection. Removal of the 2-hydroxymethyl-2-propenoyl moiety of cynaropicrin led to a loss of toxicity towards T. B. RHODESIENSE. Cytotoxicities against rat myoblasts (L6 cells), human colon adenocarcinoma cells, and murine peritoneal macrophages were measured, and selectivity indices of 7.8, 62, and 9.5 were determined. This is the first report of a plant natural product with potent IN VIVO activity against TRYPANOSOMA BRUCEI
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Ehemalige Einheiten Pharmazie > Pharmazeutische Biologie (Hamburger)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Hamburger, Matthias and Zimmermann, Stefanie and Adams, Michael and Kaiser, Marcel and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:19 Jul 2013 07:37
Deposited On:04 Jan 2013 08:35

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