Apoptotic and Cell Cycle Effects of Triterpenes Isolated from <i>Phoradendron wattii</i> on Leukemia Cell Lines

Current antineoplastic agents present multiple disadvantages, driving an ongoing search for new and better compounds. Four lupane-type triterpenes, 3α,24-dihydroxylup-20(29)-en-28-oic acid (<b>1</b>), 3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid (<b>2</b>), 3α,23-<i>...

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Bibliographic Details
Main Authors: Lía S. Valencia-Chan, Dafné Moreno-Lorenzana, Jimmy Josué Ceballos-Cruz, Sergio R. Peraza-Sánchez, Antonieta Chávez-González, Rosa E. Moo-Puc
Format: Article
Language:English
Published: MDPI AG 2022-08-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/27/17/5616
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Summary:Current antineoplastic agents present multiple disadvantages, driving an ongoing search for new and better compounds. Four lupane-type triterpenes, 3α,24-dihydroxylup-20(29)-en-28-oic acid (<b>1</b>), 3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid (<b>2</b>), 3α,23-<i>O</i>-isopropylidenyl-3α,23-dihydroxylup-20(29)-en-28-oic acid (<b>3</b>), and 3α,23-dihydroxylup-20(29)-en-28-oic acid (<b>4</b>), previously isolated from <i>Phoradendron wattii</i>, were evaluated on two cell lines of chronic (K562) and acute (HL60) myeloid leukemia. Compounds <b>1</b>, <b>2</b>, and <b>4</b> decreased cell viability and inhibit proliferation, mainly in K562, and exhibited an apoptotic effect from 24 h of treatment. Of particular interest is compound <b>2</b>, which caused arrest in active phases (G2/M) of the cell cycle, as shown by in silico study of the CDK1/Cyclin B/Csk2 complex by molecular docking. This compound [3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid] s a promising candidate for incorporation into cancer treatments and deserves further study.
ISSN:1420-3049