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Title: Chlorinated Guaiane-Type Sesquiterpene Lactones as Cytotoxic Agents against Human Tumor Cells
Authors: Estévez Sarmiento, Francisco 
Saavedra Díaz, Ester Gloria 
Mercedes Ruiz-Estévez
Francisco León
José Quintana
Ignacio Brouard
Estévez Rosas, Francisco Jesús 
UNESCO Clasification: 32 Ciencias médicas
320713 Oncología
Keywords: Apoptosis
Poly(ADP-ribose) polymerase
Sesquiterpene lactone
Issue Date: 2020
Journal: International Journal of Molecular Sciences 
Abstract: Guaiane-type sesquiterpene lactones are naturally occurring compounds which have attracted attention due to their array of biological activities. In this study, chlorinated guaianolides 1–8, isolated from plants of the genus Centaurea, were evaluated against the human leukemia cell lines HL-60, U-937, a specific U-937 cell line that overexpresses the anti-apoptotic Bcl-2 protein and the human melanoma cell line SK-MEL-1. This established the relevant structure-growth inhibition relationships. Chlorohyssopifolins A (1), C (3) and D (4) and linichlorin A (6) were the most potent compounds in terms of inducing growth inhibition in the four cell lines. IC50 values were below 10 μM in all cases. Chlorohyssopifolins A (1) and D (4) and linichlorin A (6) were potent apoptotic inducers in human U-937 leukemia cells, as determined by fluorescent microscopy and flow cytometry, and their mechanism of action was associated with cytochrome c release, caspase activation and poly(ADP-ribose)polymerase cleavage. Overall this study shows that guaianolides induce cytotoxicity against human tumor cells and provides important insights into the cell death pathways that are involved.
ISSN: 1422-0067
DOI: 10.3390/ijms21249767
Source: International Journal of Molecular Sciences [EISSN 1422-0067], v. 21 (24), 9767 (Diciembre. 2020)
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