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Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer

2017; American Chemical Society; Volume: 65; Issue: 28 Linguagem: Inglês

10.1021/acs.jafc.7b01668

1520-5118

Carlotta Granchi, Serena Fortunato, Serena Meini, Flavio Rizzolio, Isabella Caligiuri, Tiziano Tuccinardi, Hyang Yeon Lee, Paul J. Hergenrother, Filippo Minutolo,

Flavonoids in Medical Research

Inhibition of lactate dehydrogenase (LDH) represents an innovative approach to tackle cancer because this peculiar glycolytic metabolism is characteristic of most invasive tumor cells. An investigation into the biological properties of saffron extracts led to the discover of their LDH-inhibition properties. In particular, the most important saffron components, crocetin, was found to inhibit LDH (IC50 = 54.9 ± 4.7 μM). This carotenoid was independently produced by chemical synthesis, and its LDH-inhibition properties manifested via its antiproliferative activity against two glycolytic cancer cell lines (A549 and HeLa, IC50 = 114.0 ± 8.0 and 113.0 ± 11.1 μM, respectively). The results described in this article suggest that saffron may be a helpful alimentary component in the prevention of cancer that potentially contributes to the efficacy of approved cancer therapies.