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Plants and plant extracts play a crucial role in the research into novel antineoplastic agents. Four sesquiterpene lactones, artecanin ( 1 ), 3β-chloro-4α,10α-dihydroxy-1α,2α-epoxy-5α,7α H -guaia-11(13)- en -12,6α-olide ( 2 ),  iso - seco -tanapartholide 3- O -methyl ether ( 3 ) and 4β,15-dihydro-3-dehydrozaluzanin C ( 4 ), were isolated from two traditionally used Asteraceae species ( Onopordum acanthium  and  Artemisia asiatica ). When tested for antiproliferative action on HL-60 leukemia cells, these compounds exhibited reasonable IC 50  values in the range 3.6–13.5 μM. Treatment with the tested compounds resulted in a cell cycle disturbance characterized by increases in the G1 and G2/M populations, while there was a decrease in the S phase. Additionally,  1 – 3  elicited increases in the hypodiploid (subG1) population. The compounds elicited concentration-dependent chromatin condensation and disruption of the membrane integrity, as revealed by Hoechst 33258–propidium staining. Treatment for 24 h resulted in significant increases in activity of caspases-3 and -9, indicating that the tested sesquiterpenes induced the mitochondrial pathway of apoptosis. The proapoptotic properties of the sesquiterpene lactones were additionally demonstrated withannexin V staining. Compounds  1  and  2  increased the Bax/Bcl-2 expression and decreased the expressions of CDK1 and cyclin B2, as determined at the mRNA level by means of RT-PCR. These experimental results indicate that sesquiterpene lactones may be regarded as potential starting structures for the development of novel anticancer agents.

Investigation of the Antiproliferative Properties of Natural Sesquiterpenes from Artemisia asiatica and Onopordum acanthium on HL-60 Cells in Vitro