Synthesis and antiangiogenic activity of thioacetal artemisinin derivatives

Microarray expression profiles of angiogenesis-related genes predict tumor cell response to artemisinins

“…We and others have described antiangiogenic effects of ARS in vitro and in vivo. [25][26][27][28][29][30][31][32] ART strongly reduced neovascularization of Matrigel plugs injected under the skin of mice when administered with the drinking water. No apoptotic effects on endothelial cells were observed.…”

“…27 ART and dihydroARS reduced the expression of the two major VEGF receptors, Flt-1 and Table 1 THBS1 TGFB2 PLAU AXL CYR61 FGF2 FGF2 EphA2 MPDZ IL6ST COL18A1 NID2 FN1 MMP9 BMP1 ANG PIN BMPR2 DVL3 MMP11 GJA4 COL4A2 HIF1A NOS2A ABCG1 COL1A2 VEGFC F3 TFPI2 NRCAM EFEMP1 EFEMP1 SNB- Angiogenesis-related genes predict cellular response to artemisinins L Anfosso et al induction of cellular apoptosis and inhibition of expression of VEGF receptors. 28,29,31 In addition to ARSs, other sesquiterpene lactones, such as costunolide also inhibit the VEGFR KDR/Flk-1 signaling pathway. 47 It merits further investigation to analyze, whether the correlations between gene expression and GI 50 values for ARSs found in the present investigation are events downstream of the inhibition of the VEGF ligand/receptor system or whether other angiogenic regulators are also causative affected by these drugs.…”

“…14 The observation that ART inhibits the growth of many transformed cell lines has led to the hypothesis that the drug can also be useful for the treatment of human neoplasia. [15][16][17][18][19][20][21][22][23][24] As shown by us and others, [25][26][27][28][29][30][31][32] ARSs reveal antiangiogenic features in vitro and in vivo. The molecular determinants of the antiangiogenic activity of ARSs are incompletely understood at present.…”

Therapeutic and Toxicological Inhibition of Vasculogenesis and Angiogenesis Mediated by Artesunate, a Compound with Both Antimalarial and Anticancer Efficacy

“…AS and DHA have been shown to reduce the expression of the two major VEGF receptors, Flt-1 and KDR/flk-1, as determined by immune histochemistry in the chicken chorioallantoic membrane neovascularization model, in HUVE cells , and in nude mice injected with the human ovarian cancer line HO-8910, respectively. The results of these authors and others suggest that the antiangiogenic effect induced by ARTs might occur by induction of cellular apoptosis and inhibition of expression of VEGF receptors (Chen et al, 2004a;Oh et al, 2004;Wartenberg et al, 2003).…”

“…The inhibitory effect of ART on HUVE cell proliferation was stronger than the effect of ART on HO-8910 cancer cells, NIH-3T3 fibroblast cells or human endometrial cells (Chen et al, 2004b). ART derivatives also inhibited HUVE cell tube formation and exhibited antiangiogenic effects (Oh et al, 2004). In addition to affecting expression of the VEGFs, ART and its derivatives have been shown to target the VEGF receptors.…”