Lupane Triterpene Derivatives Improve Antiproliferative Effect on Leukemia Cells through Apoptosis Induction

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 . Of the three resulting derivatives, 3α-methoxy-24-hydroxylup-20(29)-en-28-oic acid ( ) cau...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2022-11, Vol.27 (23), p.8263
Main Authors: Valencia-Chan, Lía S, Estrada-Alfaro, Neptis, Ceballos-Cruz, Jimmy Josué, Torres-Tapia, Luis W, Peraza-Sánchez, Sergio R, Moo-Puc, Rosa E
Format: Article
Language:English
Subjects:
Acids
Apoptosis
Bcl-2 protein
Bioavailability
Cancer therapies
Cell cycle
Cell growth
Cell Line, Tumor
Drug delivery systems
Flow cytometry
Force and energy
Hematopoietic stem cells
Humans
Kinases
Leukemia
Leukemia - drug therapy
Lupanes
lupine-type triterpene
Membrane potential
Mitochondria
Mode of action
Molecular docking
Molecular Docking Simulation
Natural products
Proteins
Saponins
Terpenes
Transplantation
Triterpenes
Triterpenes - chemistry
Tumor cell lines
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Summary: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 . Of the three resulting derivatives, 3α-methoxy-24-hydroxylup-20(29)-en-28-oic acid ( ) caused a decrease in the median inhibitory concentration (IC ) 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 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. is a potentially promising element for future research. Clarifying the targets in its mode of action will improve its applicability.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules27238263