Apoptotic and Cell Cycle Effects of Triterpenes Isolated from Phoradendron wattii on Leukemia Cell Lines

MOLECULES(2022)

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摘要
Current antineoplastic agents present multiple disadvantages, driving an ongoing search for new and better compounds. Four lupane-type triterpenes, 3 alpha,24-dihydroxylup-20(29)-en-28-oic acid (1), 3 alpha,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid (2), 3 alpha,23-O-isopropylidenyl-3 alpha,23-dihydroxylup-20(29)-en-28-oic acid (3), and 3 alpha,23-dihydroxylup-20(29)-en-28-oic acid (4), previously isolated from Phoradendron wattii, were evaluated on two cell lines of chronic (K562) and acute (HL60) myeloid leukemia. Compounds 1, 2, and 4 decreased cell viability and inhibit proliferation, mainly in K562, and exhibited an apoptotic effect from 24 h of treatment. Of particular interest is compound 2, 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 [3 alpha,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid] s a promising candidate for incorporation into cancer treatments and deserves further study.
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关键词
leukemia, lupane-type triterpene, apoptosis, cell cycle, molecular docking
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