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

Stefanie Zimmermann

doi:10.3797/scipharm.1111-13

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).

Highlights

Malaria is still the most deadly parasitic disease in the world, leading to one million deaths every year, mostly in Sub-Saharan Africa
More than 1200 plant species from 160 families have been described as traditional antimalarial remedies, and hundreds of extracts and purified compounds from such plants have shown antiplasmodial activities tested in the last decades [4]
Two hundred and fifty-four extracts were prepared from 61 plants and tested for antiplasmodial activity at two test concentrations (0.8 and 4.8 μg/ml) according to an established procedure

Summary

Introduction

Malaria is still the most deadly parasitic disease in the world, leading to one million deaths every year, mostly in Sub-Saharan Africa. More than 1200 plant species from 160 families have been described as traditional antimalarial remedies, and hundreds of extracts and purified compounds from such plants have shown antiplasmodial activities tested in the last decades [4]. We purchased or collected 61 European medicinal plants from various sources (see Table S1 in the Supporting Information), 34 of which had been described as antimalarials in the herbals [8].

Results

Conclusion