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Lupane triterpene derivatives improve antiproliferative effect on leukemia cells through apoptosis induction
Lía S Valencia Chan
NEPTIS ABIGAIL ESTRADA ALFARO
Jimmy Josué Ceballos Cruz
Luis Wiliunfo Torres Tapia
SERGIO RUBEN PERAZA SANCHEZ
ROSA MOO_PUC
Acceso Abierto
Atribución-NoComercial-SinDerivadas
https://doi.org/10.3390/molecules27175616
LEUKEMIA
LUPINE-TYPE TRITERPENE
APOPTOSIS
MOLECULAR DOCKING
Leukemia is one of the most frequent types of cancer. No effective treatment currently exists, driving a search for new compounds. Simple structural modifications were made to novel triterpenes isolated from Phoradendron wattii. Of the three resulting derivatives, 3α-methoxy-24-hydroxylup-20(29)-en-28-oic acid (T1m) caused a decrease in the median inhibitory concentration (IC50) on the K562 cell line. Its mode of action was apparently apoptosis, ROS generation, and loss of mitochondrial membrane potential (MMP). Molecular docking analysis showed T1m to produce lower binding energies than its precursor for the Bcl-2 and EGFR proteins. Small, simple, and viable modifications to triterpenes can improve their activity against leukemia cell lines. T1m is a potentially promising element for future research. Clarifying the targets in its mode of action will improve its applicability. © 2022 by the authors.
2022
Artículo
Molecules, 27(23), 8263, 2022.
Español
Valencia-Chan, L.S.; Estrada-Alfaro, N.; Ceballos-Cruz, J.J.; Torres-Tapia, L.W.; Peraza-Sánchez, S.R.; Moo-Puc, R.E. Lupane Triterpene Derivatives Improve Antiproliferative Effect on Leukemia Cells through Apoptosis Induction. Molecules 2022, 27, 8263.https://doi.org/ 10.3390/molecules27238263
FARMACOLOGÍA MOLECULAR
Versión publicada
publishedVersion - Versión publicada
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