Artemisinin and its derivatives are used for the second line therapy of malaria infections with Plasmodium falciparum and Plasmodium vivax. Artemisinins also reveal profound antitumor activity in vitro and in vivo which rely at least in part on a strong anti-angiogenic acitivity of the drug (Dell’Eva et al, Biochem. Pharmacol. 2004:68, 2359). In the present investigation, we correlated the mRNA expression data of 90 angiogenesis-related genes obtained by microarray hybridization from the database of the U.S. National Cancer Institute with the inhibition concentration 50% (IC50) values for 8 artemisinins (artemisinin, arteether, arteether, artesunate, artemisetene, arteanuine B, dihydroartemisinylester stereoisomers 1 and 2). Messenger RNA expression of 30 of 90 angiogenesis related genes (two of which were represented with each two different clones) significantly correlated with IC50 values for ART and at least three further artemisinin derivatives. Hierarchical cluster analysis of the mRNA expression values of these 30 genes identifies clusters containing mainly ART resistant or ART sensitive cell lines, respectively. This pattern of distribution was statistically significant (p = 0.01, χ2 test) indicating that sensitivity or resistance of cell lines to ART extends to the baseline expression level of the present set of angiogenesis-related genes. Supported by grants from AIRC to AA and FIRB to UP

[Proc Amer Assoc Cancer Res, Volume 46, 2005]