Cytotoxicity of the Sesquiterpene Lactone Spiciformin and Its Acetyl Derivative against the Human Leukemia Cell Lines U-937 and HL-60.
作者： Ester Saavedra , Francisco Estévez-Sarmiento , Mercedes Said , José Luis Eiroa , Sara Rubio
DOI: 10.3390/IJMS21082782
关键词:
摘要: Spiciformin (1) is a sesquiterpene lactone with germacrane skeleton that found in two Tanacetum species endemic to the Canary Islands. In this study, cytotoxicities of 1 and its acetyl derivative (2) were evaluated against human tumor cells. These lactones cytotoxic acute myeloid leukemia (U-937 HL-60) cells, even cells over-expressing pro-survival protein Bcl-2, but melanoma (SK-MEL-1) mononuclear isolated from blood healthy donors more resistant. Both compounds are apoptotic inducers U-937 Cell death was mediated by processing activation initiator effector caspases cleavage poly(ADP-ribose) polymerase, it blocked broad-spectrum caspase inhibitor (in case 2) selective caspase-3/7, -8, -9 inhibitors. addition, certainly compound 2, be associated decrease mitochondrial membrane potential, downregulation anti-apoptotic mitogen-activated kinases signaling pathway, generation reactive oxygen species. It will, therefore, relevant continue characterization class compounds.
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