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Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells

dc.contributor.authorCalzada, Fernando
dc.contributor.authorGarcía Hernández, Normand
dc.contributor.authorHidalgo Figueroa, Sergio Nemorio
dc.contributor.authorBautista Redonda, Francisco Elihú
dc.contributor.authorBarbosa Cabrera, Elizabeth
dc.contributor.authorVelázquez González, Claudia
dc.contributor.authorHernández Caballero, Marta Elena
dc.identifier.citationCalzada, F.; Garcia-Hernandez, N.; Hidalgo-Figueroa, S.; Bautista, E.; Barbosa, E.; Velázquez, C.; Hernández-Caballero, M.E. Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells. Molecules 2022, 27, 1687.
dc.description.abstract"Heliangolide-type sesquiterpene lactones (HTSLs) are phytocompounds with several pharmacological activities including cytotoxic and antitumor activity. Both bioactivities are related to an ?-methylene-?-lactone moiety and an ester group on carbon C-8 in the sesquiterpene lactone (SL) structure. Two HTSLs, incomptines A (AI) and B (IB) isolated from Decachaeta incompta, were evaluated for their cytotoxic activity on three leukemia cell lines: HL-60, K-562, and REH cells. Both compounds were subjected to a molecular docking study using target proteins associated with cancer such as topoisomerase II?, topoisomerase II?, dihydrofolate reductase, methylenetetrahydrofolate dehydrogenase, and Bcl-2-related protein A1. Results show that IA and IB exhibit cytotoxic activity against all cell lines used. The CC50 value of IA was 2–4-fold less than etoposide and methotrexate, two anticancer drugs used as positive controls. The cytotoxic activity of IB was close to that of etoposide and methotrexate. The molecular docking analysis showed that IA and IB have important interaction on all targets used. These findings suggest that IA and IB may serve as scaffolds for the development of new treatments for different types of leukemia."
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internacional
dc.subjectIncomptine A
dc.subjectIncomptine B
dc.subjectSesquiterpene lactones
dc.subjectCytotoxic activity
dc.subjectHuman cancer cell lines
dc.titleExpanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells
dc.rights.accessAcceso Abierto

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Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 Internacional