Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells
Fernando Calzada,
Normand Garcia-Hernandez,
Sergio Hidalgo-Figueroa,
Elihú Bautista,
Elizabeth Barbosa,
Claudia Velázquez,
Marta Elena Hernández-Caballero
Affiliations
Fernando Calzada
Unidad de Investigación Médica en Farmacología, Unidad Médica de Alta Especialidad, Hospital de Especialidades-2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Ciudad de México 06725, Mexico
Normand Garcia-Hernandez
Unidad de Investigación Médica en Genética Humana, Unidad Médica de Alta Especialidad, Hospital de Pediatría, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Ciudad de México 06725, Mexico
Sergio Hidalgo-Figueroa
CONACyT-Instituto Potosino de Investigación Científica y Tecnológica A. C., Camino a la Presa San José 2055, Lomas 4ª Sección, San Luis Potosí 78216, Mexico
Elihú Bautista
CONACyT-Instituto Potosino de Investigación Científica y Tecnológica A. C., Camino a la Presa San José 2055, Lomas 4ª Sección, San Luis Potosí 78216, Mexico
Elizabeth Barbosa
Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Salvador Díaz Mirón esq. Plan de San Luis S/N, Miguel Hidalgo, Casco de Santo Tomas, Ciudad de México 11340, Mexico
Claudia Velázquez
Área Académica de Farmacia, Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Km 4.5, Carretera Pachuca-Tulancingo, Unidad Universitaria, Pachuca 42076, Mexico
Marta Elena Hernández-Caballero
Facultad de Medicina, Biomedicina, Benemérita Universidad Autónoma de Puebla, Puebla 72410, Mexico
Heliangolide-type sesquiterpene lactones (HTSLs) are phytocompounds with several pharmacological activities including cytotoxic and antitumor activity. Both bioactivities are related to an α-methylene-γ-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 IIα, topoisomerase IIβ, 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.
