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Your search keyword '"Salerno, Loredana"' showing total 15 results
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15 results on '"Salerno, Loredana"'

6. Discovery of SI 1/20 and SI 1/22 as Mutual Prodrugs of 5‐Fluorouracil and Imidazole‐Based Heme Oxygenase 1 Inhibitor with Improved Cytotoxicity in DU145 Prostate Cancer Cells

Author

Salerno, Loredana, primary, Sorrenti, Valeria, additional, Pittalà, Valeria, additional, Consoli, Valeria, additional, Modica, Maria N., additional, Romeo, Giuseppe, additional, Marrazzo, Agostino, additional, Giuliano, Michela, additional, Zajdel, Paweł, additional, Vanella, Luca, additional, and Intagliata, Sebastiano, additional

Published
2023
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8. Heme Oxygenase Modulation Drives Ferroptosis in TNBC Cells

Author

Consoli, Valeria, primary, Sorrenti, Valeria, additional, Pittalà, Valeria, additional, Greish, Khaled, additional, D’Amico, Agata Grazia, additional, Romeo, Giuseppe, additional, Intagliata, Sebastiano, additional, Salerno, Loredana, additional, and Vanella, Luca, additional

Published
2022
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9. Novel Tyrosine Kinase Inhibitors to Target Chronic Myeloid Leukemia

Author

Ciaffaglione, Valeria, primary, Consoli, Valeria, additional, Intagliata, Sebastiano, additional, Marrazzo, Agostino, additional, Romeo, Giuseppe, additional, Pittalà, Valeria, additional, Greish, Khaled, additional, Vanella, Luca, additional, Floresta, Giuseppe, additional, Rescifina, Antonio, additional, Salerno, Loredana, additional, and Sorrenti, Valeria, additional

Published
2022
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10. CAPE and its synthetic derivative VP961 restore BACH1/NRF2 axis in Down Syndrome

Author

Pagnotta, Sara, primary, Tramutola, Antonella, additional, Barone, Eugenio, additional, Di Domenico, Fabio, additional, Pittalà, Valeria, additional, Salerno, Loredana, additional, Folgiero, Valentina, additional, Caforio, Matteo, additional, Locatelli, Franco, additional, Petrini, Stefania, additional, Butterfield, D. Allan, additional, and Perluigi, Marzia, additional

Published
2022
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11. Potential Health Benefits of a Pomegranate Extract, Rich in Phenolic Compounds, in Intestinal Inflammation

Author

Raffaele, Marco, primary, Greish, Khaled, additional, Vanella, Luca, additional, Carota, Giuseppe, additional, Bahman, Fatemah, additional, Bindayna, Khalid M., additional, Ezzat, Hicham, additional, Salerno, Loredana, additional, Pittalà, Valeria, additional, Ballistreri, Gabriele, additional, Amenta, Margherita, additional, and Sorrenti, Valeria, additional

Published
2021
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13. Discovery of Novel Acetamide-Based Heme Oxygenase-1 Inhibitors with Potent In Vitro Antiproliferative Activity

Author

Fallica, Antonino N., primary, Sorrenti, Valeria, additional, D’Amico, Agata G., additional, Salerno, Loredana, additional, Romeo, Giuseppe, additional, Intagliata, Sebastiano, additional, Consoli, Valeria, additional, Floresta, Giuseppe, additional, Rescifina, Antonio, additional, D’Agata, Velia, additional, Vanella, Luca, additional, and Pittalà, Valeria, additional

Published
2021
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14. Novel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation.

Author

Salerno, Loredana, Vanella, Luca, Sorrenti, Valeria, Consoli, Valeria, Ciaffaglione, Valeria, Fallica, Antonino N., Canale, Vittorio, Zajdel, Paweł, Pignatello, Rosario, and Intagliata, Sebastiano

Subjects
*FLUOROURACIL, *HEME, *ANTINEOPLASTIC agents, *EPITHELIAL cells, *PRODRUGS, *ANTIBODY-dependent cell cytotoxicity, *CELL survival
Abstract

In this work, the first mutual prodrug of 5-fluorouracil and heme oxygenase1 inhibitor (5-FU/HO-1 hybrid) has been designed, synthesised, and evaluated for its in vitro chemical and enzymatic hydrolysis stability. Predicted in silico physicochemical properties of the newly synthesised hybrid (3) demonstrated a drug-like profile with suitable Absorption, Distribution, Metabolism, and Excretion (ADME) properties and low toxic liabilities. Preliminary cytotoxicity evaluation towards human prostate (DU145) and lung (A549) cancer cell lines demonstrated that 3 exerted a similar effect on cell viability to that produced by the reference drug 5-FU. Among the two tested cancer cell lines, the A549 cells were more susceptible for 3. Of note, hybrid 3 also had a significantly lower cytotoxic effect on healthy human lung epithelial cells (BEAS-2B) than 5-FU. Altogether our results served as an initial proof-of-concept to develop 5-FU/HO-1 mutual prodrugs as potential novel anticancer agents. [ABSTRACT FROM AUTHOR]

Published
2021
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15. Discovery of SI 1/20 and SI 1/22 as Mutual Prodrugs of 5-Fluorouracil and Imidazole-Based Heme Oxygenase 1 Inhibitor with Improved Cytotoxicity in DU145 Prostate Cancer Cells

Author

Loredana Salerno, Valeria Sorrenti, Valeria Pittalà, Valeria Consoli, Maria N. Modica, Giuseppe Romeo, Agostino Marrazzo, Michela Giuliano, Paweł Zajdel, Luca Vanella, Sebastiano Intagliata, Salerno, Loredana, Sorrenti, Valeria, Pittalà, Valeria, Consoli, Valeria, Modica, Maria N, Romeo, Giuseppe, Marrazzo, Agostino, Giuliano, Michela, Zajdel, Paweł, Vanella, Luca, and Intagliata, Sebastiano

Subjects
Pharmacology, Organic Chemistry, Drug Discovery, Molecular Medicine, cancer, 5-fluorouracil, Prodrugs, General Pharmacology, Toxicology and Pharmaceutics, DU145 prostate cancer cells, Biochemistry, heme oxygenase 1
Abstract

In this work, we extend the concept of 5-fluorouracil/heme oxygenase 1 (5-FU/HO-1) inhibitor hybrid as an effective strategy for enhancing 5-FU-based anticancer therapies. For this purpose, we designed and synthesized new mutual prodrugs, named SI 1/20 and SI 1/22, in which the two active parent drugs (i. e., 5-FU and an imidazole-based HO-1 inhibitor) were connected through an easily cleavable succinic linker. Experimental hydrolysis rate, and in silico ADMET predictions were indicative of good drug-likeness and pharmacokinetic properties. Novel hybrids significantly reduced the viability of prostate DU145 cancer cells compared to the parent compounds 5-FU and HO-1 inhibitor administered alone or in combination. Interestingly, both compounds showed statistically significant lower toxicity, than 5-FU at the same dose, against non-tumorigenic human benign prostatic hyperplasia (BPH-1) cell line. Moreover, the newly synthesized mutual prodrugs inhibited the HO-1 activity both in a cell-free model and in vitro, as well as downregulated the HO-1 expression and increased the reactive oxygen species (ROS) levels.

Published
2023

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