Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/74604
Title: Cytotoxicity of the Sesquiterpene Lactone Spiciformin and Its Acetyl Derivative against the Human Leukemia Cell Lines U-937 and HL-60
Authors: Saavedra Santana, 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
Cytotoxicity
Caspase
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.
URI: http://hdl.handle.net/10553/74604
ISSN: 1661-6596
DOI: 10.3390/ijms21082782
Source: International Journal of Molecular Sciences [ISSN 1661-6596], v. 21 (8), 2782
Appears in Collections:Artículos
Unknown (2,45 MB)
Show full item record

Page view(s)

56
checked on Jun 12, 2021

Download(s)

24
checked on Jun 12, 2021

Google ScholarTM

Check

Altmetric


Share



Export metadata



Items in accedaCRIS are protected by copyright, with all rights reserved, unless otherwise indicated.