Activity of selected phytochemicals against Plasmodium falciparum

作者：Astelbauer Florian; Gruber Maria; Brem Brigitte; Greger Harald; Obwaller Andreas; Wernsdorfer Gunther; Congpuong Kanungnit; Wernsdorfer Walther H^*; Walochnik Julia

来源：Acta Tropica, 2012, 123(2): 96-100.

DOI：10.1016/j.actatropica.2012.04.002

• Plasmodium falciparum
• Phytochemicals
• Rocaglamid
• Aglafoline
• Antimalarial activity

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 (IC50, IC90 and IC99) of 60.95 nM, 854.41 nM and 7351.49 nM, respectively, rocaglamid was the most active of the substances, closely followed by aglafoline with 53.49 nM, 864.55 nM and 8354.20 nM. 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 IC50 and IC99 values higher than 350 nM and 180 mu M, respectively, and regressions with relatively shallow slopes S %26gt; 14.38. Analogues of rocaglamid and aglafoline merit further exploration of their anti-plasmodial activity.

• 出版日期2012-8