A novel heteroleptic Cu(II)-phenanthroline-UDCA complex as lipoxygenase inhibitor and ER-stress inducer in cancer cell lines

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Authors

MASURI Sebastiano MORÁŇ Lukáš VESSELÁ Tereza CADONI Enzo CABIDDU Maria Grazia PEČINKA Lukáš GABRIELOVÁ Viktorie MELONI Francesca HAVEL Josef VAŇHARA Petr PIVETTA Tiziana

Year of publication 2023
Type Article in Periodical
Magazine / Source Journal of Inorganic Biochemistry
MU Faculty or unit

Faculty of Medicine

Citation
Web https://doi.org/10.1016/j.jinorgbio.2023.112301
Doi http://dx.doi.org/10.1016/j.jinorgbio.2023.112301
Keywords Copper complex; Solution equilibria; Mass spectrometry; Lipoxygenase; Molecular docking; ER stress
Description A new heteroleptic copper(II) compound named C0-UDCA was prepared by reaction of [Cu(phen)2(OH2)](ClO4)2 (C0) with the bile ursodeoxycholic acid (UDCA). The resulting compound is able to inhibit the lipoxygenase enzyme showing more efficacy than the precursors C0 and UDCA. Molecular docking simulations clarified the interactions with the enzyme as due to allosteric modulation. The new complex shows antitumoral effect on ovarian (SKOV-3) and pancreatic (PANC-1) cancer cells at the Endoplasmic Reticulum (ER) level by activating the Unfolded Protein Response. In particular, the chaperone BiP, the pro-apoptotic protein CHOP and the transcription factor ATF6 are upregulated in the presence of C0-UDCA. The combination of Intact Cell MALDI-MS and statistical analysis have allowed us to discriminate between untreated and treated cells based on their mass spectrometry fingerprints.
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