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Chlorinated Guaiane-Type Sesquiterpene Lactones as Cytotoxic Agents against Human Tumor Cells

AuthorsEstévez-Sarmiento, Francisco; Saavedra, Ester; Ruiz-Estévez, Mercedes; León, Francisco ; Quintana, José; Brouard, Ignacio ; Estévez, Francisco
Poly(ADP-ribose) polymerase
Sesquiterpene lactone
Issue Date21-Dec-2020
PublisherMultidisciplinary Digital Publishing Institute
CitationInternational Journal of Molecular Sciences 21(24): 9767 (2020)
AbstractGuaiane-type sesquiterpene lactones are naturally occurring compounds which have attracted attention due to their array of biological activities. In this study, chlorinated guaianolides <b>1</b>–<b>8</b>, isolated from plants of the genus <i>Centaurea</i>, 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 (<b>1</b>), C (<b>3</b>) and D (<b>4</b>) and linichlorin A (<b>6</b>) were the most potent compounds in terms of inducing growth inhibition in the four cell lines. IC<sub>50</sub> values were below 10 μM in all cases. Chlorohyssopifolins A (<b>1</b>) and D (<b>4</b>) and linichlorin A (<b>6</b>) 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 <i>c</i> 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.
DescriptionThis article belongs to the Section Bioactives and Nutraceuticals.
Publisher version (URL)http://doi.org/10.3390/ijms21249767
Identifiersdoi: 10.3390/ijms21249767
Appears in Collections:(IPNA) Artículos
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