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Advances in the Properties of Incomptine A: Cytotoxic Activity and Downregulation of Hexokinase II in Breast Cancer Cell Lines

dc.contributor.authorArietta García, Angel Giovanni
dc.contributor.authorCalzada, Fernando
dc.contributor.authorRamírez Sánchez, Israel
dc.contributor.authorBautista Redonda, Francisco Elihú
dc.contributor.authorGarcía Hernández, Normand
dc.contributor.authorOrdoñez Razo, Rosa María
dc.date.accessioned2024-05-30T21:28:28Z
dc.date.available2024-05-30T21:28:28Z
dc.date.issued2023
dc.identifier.citationArietta-García, A.G.; Calzada, F.; Ramírez-Sánchez, I.; Bautista, E.; García-Hernandez, N.; Ordoñez-Razo, R.M. Advances in the Properties of Incomptine A: Cytotoxic Activity and Downregulation of Hexokinase II in Breast Cancer Cell Lines. Int. J. Mol. Sci. 2023, 24, 12406. https://doi.org/10.3390/ijms241512406
dc.identifier.urihttp://hdl.handle.net/11627/6558
dc.description.abstractBreast cancer treatments are limited by the cancer subtype and its selectivity towards tumor cells, hence the importance of finding compounds that increase the survival of healthy cells and target any subtype. Incomptine A (IA) is a sesquiterpene lactone with demonstrated cytotoxic activity. In this study, through in vitro assays, it was observed that IA has similar cytotoxic activity between the subtypes triple negative, HER2+, and luminal A of the breast cancer cell lines. IA cytotoxic activity is higher in cancer than in nontumorigenic cells, and its selectivity index for cancer cells is more than that of the drug doxorubicin. Molecular docking and its in silico comparison with the 2-Deoxyglucose inhibitor suggest that IA could bind to Hexokinase II (HKII), decreasing its expression. Since we did not find changes in the expression of the glycolytic pathway, we suppose that IA could affect the antiapoptotic function of HKII in cancer cells. The IA-HKII union would activate the voltage-gated anion channel 1 (VDAC1), resuming apoptosis. Therefore, we suggest that IA could be used against almost any subtype and that its cytotoxic effect could be due to the reactivation of apoptosis in breast cancer cells
dc.publisherMDPI
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internacional
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectIncomptine A
dc.subjectBreast cancer cells
dc.subjectCytotoxic activity
dc.subjectHexokinase II
dc.subject.classificationBIOQUÍMICA
dc.titleAdvances in the Properties of Incomptine A: Cytotoxic Activity and Downregulation of Hexokinase II in Breast Cancer Cell Lines
dc.typearticle
dc.identifier.doihttps://doi.org/10.3390/ijms241512406
dc.rights.accessAcceso Abierto


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Attribution-NonCommercial-NoDerivatives 4.0 Internacional
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