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Title: Cytotoxicity of the Sesquiterpene Lactone Spiciformin and Its Acetyl Derivative against the Human Leukemia Cell Lines U-937 and HL-60
Authors: Saavedra Díaz, Ester Gloria 
Estévez Sarmiento, Francisco 
Said, Mercedes
Eiroa Martínez, José Luis 
Rubio Sánchez, Sara 
Quintana, José 
Estévez Rosas, Francisco Jesús 
UNESCO Clasification: 2302 Bioquímica
Keywords: Apoptosis
Poly(ADP-ribose) polymerase
Sesquiterpene lactone
Issue Date: 2020
Journal: International Journal of Molecular Sciences 
Abstract: Spiciformin (1) is a sesquiterpene lactone with a germacrane skeleton that is found in two Tanacetum species endemic to the Canary Islands. In this study, the cytotoxicities of 1 and its acetyl derivative (2) were evaluated against human tumor cells. These sesquiterpene lactones were cytotoxic against human acute myeloid leukemia (U-937 and HL-60) cells, even in cells over-expressing the pro-survival protein Bcl-2, but melanoma (SK-MEL-1) and human mononuclear cells isolated from blood of healthy donors were more resistant. Both compounds are apoptotic inducers in human leukemia U-937 cells. Cell death was mediated by the processing and activation of initiator and effector caspases and the cleavage of poly(ADP-ribose) polymerase, and it was blocked by a broad-spectrum caspase inhibitor and (in the case of sesquiterpene lactone 2) by the selective caspase-3/7, -8, and -9 inhibitors. In addition, certainly in the case of compound 2, this was found to be associated with a decrease in mitochondrial membrane potential, downregulation of the anti-apoptotic protein Bcl-2, activation of the mitogen-activated protein kinases signaling pathway, and generation of reactive oxygen species. It will, therefore, be relevant to continue characterization of this class of compounds.
ISSN: 1661-6596
DOI: 10.3390/ijms21082782
Source: International Journal of Molecular Sciences [ISSN 1661-6596], v. 21 (8), 2782
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