1. Synthetic menthyl α/β-(1→6)-diglucopyranosides-induced cell death in human leukemia cells is dependent on caspases.
- Author
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Marrero MT, Tejera S, Estévez S, Quintana J, Mayato C, Dorta RL, Vázquez JT, and Estévez F
- Subjects
- Amino Acid Chloromethyl Ketones pharmacology, Cell Line, Tumor, Cytochromes c metabolism, Disaccharides chemical synthesis, Disaccharides pharmacology, HL-60 Cells, Humans, Leukemia enzymology, Leukemia pathology, Reactive Oxygen Species metabolism, bcl-2-Associated X Protein metabolism, Apoptosis drug effects, Caspases metabolism, Disaccharides chemistry
- Abstract
A series of alkyl α/β-(1→6)-diglucopyranosides 1-12 were synthesized and assessed for cytotoxicity against HL-60, U937, Molt-3 and MCF-7 cancer cell lines. The menthyl derivatives displayed strong cytotoxic properties showing IC(50) values between 6 and 16 μM. Furthermore, we demonstrated that the selected synthetic (+)-menthyl β-(1→6)-diglucopyranoside 5 induces apoptotic cell death in human leukemia cells through a mechanism that involves activation of multiple caspases. Cell death was completely prevented by the non-specific caspase inhibitor z-VAD-fmk and found to be associated with the release of cytochrome c, an increase in the expression of Bax levels and a decrease in the generation of reactive oxygen species., (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Published
- 2012
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