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

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

doi:10.1021/acs.jafc.7b01668

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

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

Research output: Contribution to journal › Article › peer-review

Abstract

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.

Original language	English (US)
Pages (from-to)	5639-5649
Number of pages	11
Journal	Journal of Agricultural and Food Chemistry
Volume	65
Issue number	28
DOIs	https://doi.org/10.1021/acs.jafc.7b01668
State	Published - Jul 19 2017

Keywords

cancer
crocetin
glycolysis
lactate dehydrogenase
saffron

ASJC Scopus subject areas

General Chemistry
General Agricultural and Biological Sciences

Online availability

10.1021/acs.jafc.7b01668

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Granchi, C., Fortunato, S., Meini, S., Rizzolio, F., Caligiuri, I., Tuccinardi, T., Lee, H. Y., Hergenrother, P. J., & Minutolo, F. (2017). Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer. Journal of Agricultural and Food Chemistry, 65(28), 5639-5649. https://doi.org/10.1021/acs.jafc.7b01668

Granchi, C, Fortunato, S, Meini, S, Rizzolio, F, Caligiuri, I, Tuccinardi, T, Lee, HY, Hergenrother, PJ & Minutolo, F 2017, 'Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer', Journal of Agricultural and Food Chemistry, vol. 65, no. 28, pp. 5639-5649. https://doi.org/10.1021/acs.jafc.7b01668

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abstract = "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.",

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author = "Carlotta Granchi and Serena Fortunato and Serena Meini and Flavio Rizzolio and Isabella Caligiuri and Tiziano Tuccinardi and Lee, {Hyang Yeon} and Hergenrother, {Paul J.} and Filippo Minutolo",

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AU - Granchi, Carlotta

AU - Fortunato, Serena

AU - Meini, Serena

AU - Rizzolio, Flavio

AU - Caligiuri, Isabella

AU - Tuccinardi, Tiziano

AU - Lee, Hyang Yeon

AU - Hergenrother, Paul J.

AU - Minutolo, Filippo

PY - 2017/7/19

Y1 - 2017/7/19

N2 - 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.

AB - 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.

KW - cancer

KW - crocetin

KW - glycolysis

KW - lactate dehydrogenase

KW - saffron

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

Abstract

Keywords

ASJC Scopus subject areas

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