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Sci. Pharm. 2012, 80(1), 205-214; doi:10.3797/scipharm.1111-13

Screening and HPLC-Based Activity Profiling for New Antiprotozoal Leads from European Plants

1
Departement of Pharmaceutical Sciences, Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland
2
Parasite Chemotherapy, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland
*
Author to whom correspondence should be addressed.
Received: 14 November 2011 / Accepted: 23 December 2011 / Published: 23 December 2011
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Abstract

Based on a survey of remedies used in Renaissance Europe to treat malaria, we prepared and screened a library of 254 extracts from 61 plants for antiplasmodial activity in vitro. HPLC-based activity profiling was performed for targeted identification of active constituents in extracts. One of the most remarkable results was the identification of onopordopicrin, a germacranolide sesquiterpene lactone isolated from Arctium nemorosum as a potent inhibitor of P. falciparum with an IC50 of 6.9 μM. It was tested similarly against Trypanosoma brucei rhodesiense, the parasite which causes African sleeping sickness. With an IC50 of 0.37 μM, onopordopicrin was one of the most potent natural products reported so far. Cytotoxicity was determined against rat myoblast L6 cells (IC50: 3.06).
Keywords: European plants; Plasmodium falciparum; Trypanosoma brucei rhodesiense; Arctium nemorosum; Onopordopicrin European plants; Plasmodium falciparum; Trypanosoma brucei rhodesiense; Arctium nemorosum; Onopordopicrin
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

ZIMMERMANN, S.; THOMI, S.; KAISER, M.; HAMBURGER, M.; ADAMS, M. Screening and HPLC-Based Activity Profiling for New Antiprotozoal Leads from European Plants. Sci. Pharm. 2012, 80, 205-214.

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