Antiprotozoal Screening of 60 South African plants, and the identification of the Antitrypanosomal Germacranolides Schkuhrin I and II

Abstract

Two hundred and seven extracts were prepared from sixty plants from South Africa and screened for in vitro activity against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. For the 21 extracts which inhibited the growth of one or more parasites with more than 95 % at 10 µg/mL, the IC(sub)50 values against all four protozoal parasites and cytotoxic IC(sub)50 values against L6 myoblasts were determined. Amongst the most notable results are the activities of Psoralea pinnata (IC(sub)50 of 0.15 µg/mL), Schkuhria pinnata (2.04 µg/mL), and Vernonia mespilifolia (1.01 µg/mL) against Trypansoma brucei rhodesiense. HPLC-based activity profiling was used to identify the active constituents in the extracts, and the germacranolide sesquiterpene lactones schkuhrin I and II from S. pinnata, and cynaropicrin from V. mespilifolia were identified, with IC(sub)50 values of 0.9, 1.5, and 0.23 µM, respectively.