Amalia Di Petrillo
A novel heteroleptic Cu(II)-phenanthroline-UDCA complex as lipoxygenase inhibitor and ER-stress inducer in cancer cell lines
Sebastiano Masuri;Enzo Cadoni;Maria Grazia Cabiddu;Francesca Meloni;Tiziana Pivetta
2023-01-01
Abstract
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.File | Size | Format | |
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C0UDCA_manuscript_Pivetta_PREPRINT.pdf open access
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Type: versione pre-print
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1-s2.0-S0162013423001836-main.pdf Solo gestori archivio
Type: versione editoriale
Size 6.2 MB
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6.2 MB | Adobe PDF | & nbsp; View / Open Request a copy |
1-s2.0-S0162013423001836-main.pdf open access
Type: versione editoriale
Size 6.21 MB
Format Adobe PDF
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6.21 MB | Adobe PDF | View/Open |
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