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Title: Activity of selected phytochemicals against Plasmodium falciparum
Authors: Florian Astelbauer
Maria Gruber
Brigitte Brem
Harald Greger
Andreas Obwaller
Gunther Wernsdorfer
Kanungnit Congpuong
Walther H. Wernsdorfer
Julia Walochnik
Medizinische Universitat Wien
Universitat Wien
Orphanidis Pharma Research
Mahidol University
Thailand Ministry of Public Health
Keywords: Immunology and Microbiology;Medicine
Issue Date: 1-Aug-2012
Citation: Acta Tropica. Vol.123, No.2 (2012), 96-100
Abstract: According to the WHO, in 2008, there were 247 million reported cases of malaria and nearly one million deaths from the disease. Parasite resistance against first-line drugs, including artemisinin and mefloquine, is increasing. In this study the plant-derived compounds aglafolin, rocaglamid, kokusaginine, arborine, arborinine and tuberostemonine were investigated for their anti-plasmodial activity in vitro. Fresh Plasmodium falciparum isolates were taken from patients in the area of Mae Sot, north-western Thailand in 2008 and the inhibition of schizont maturation was determined for the respective compounds. With inhibitory concentrations effecting 50%, 90% and 99% inhibition (IC 50 , IC 90 and IC 99 ) of 60.95nM, 854.41nM and 7351.49nM, respectively, rocaglamid was the most active of the substances, closely followed by aglafoline with 53.49nM, 864.55nM and 8354.20nM. The activity was significantly below that of artemisinin, but moderately higher than that of quinine. Arborine, arborinine, tuberostemonine and kokusaginine showed only marginal activity against P. falciparum characterized by IC 50 and IC 99 values higher than 350nM and 180μM, respectively, and regressions with relatively shallow slopes S > 14.38. Analogues of rocaglamid and aglafoline merit further exploration of their anti-plasmodial activity. © 2012 Elsevier B.V.
ISSN: 18736254
Appears in Collections:Scopus 2011-2015

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