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5 results on '"Antonella Fioravanti"'

2. In Vitro Effects of VA441, a New Selective Cyclooxygenase-2 Inhibitor, on Human Osteoarthritic Chondrocytes exposed to IL-1β

Author

Antonella Fioravanti, Laura Tinti, Nicola Antonio Pascarelli, Angela Di Capua, Antonello Lamboglia, Andrea Cappelli, Mariangela Biava, Antonio Giordani, Silvia Niccolini, Mauro Galeazzi, and Maurizio Anzini

Subjects
Therapeutics. Pharmacology, RM1-950
Abstract

The aim of this in vitro study was to examine the possible effect of [2-methyl-5-(4-methylsulphonyl)phenyl-1-phenyl-3-(2-n-propyloxyethyl)]-1H-pyrrole (VA441), a new selective cyclooxygenase (COX)-2 inhibitor, on human osteoarthritic (OA) chondrocyte cultivated in the presence or absence of interleukin-1β (IL-1β). In particular, we assessed the effects of 1 and 10 μM of VA441, celecoxib, and indomethacin on cell viability, COX-2 and inducible nitric oxide synthase (iNOS) gene expression, prostaglandin E2 (PGE2) production, and nitric oxide (NO) and metalloproteinase-3 (MMP-3) release. Furthermore, we carried out morphological assessment by transmission electron microscopy (TEM). The presence of IL-1β led to a significant increase in PGE2, MMP-3, and NO production, as well as a significant increase in gene expression of COX-2 and iNOS. All the drugs tested had a statistically significant inhibitory effect on PGE2 production and gene expression of COX-2 stimulated by IL-1β. VA441 and celecoxib significantly suppressed IL-1β-stimulated MMP-3 and NO and iNOS gene expression in a dose-dependent manner, while indomethacin did not show any significant effect on MMP-3 and NO production or on iNOS gene expression. TEM demonstrated that IL-1β severely alters the structure of chondrocytes; after coincubation with VA441 or celecoxib, the cells recovered their ultrastructure. Our data suggest that VA441 and celecoxib may have a beneficial effect on chondrocyte metabolism. Keywords:: VA441, celecoxib, indomethacin, cyclooxygenase-2 inhibitor, chondrocyte

Published
2012
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4. List of Contributors

Author

Arnon Afek, Antonella Afeltra, Gabriele Gallo Afflitto, Cristiano Alessandri, Stefano Alivernini, Alessia Alunno, Howard Amital, Laura Andreoli, Alessandro Antonelli, Mariachiara Arisi, Carolina Artusi, Fabiola Atzeni, Eleonora Ballanti, Cristiana Barbati, Giuseppe Barilaro, Elena Bartoloni, Dana Ben-Ami, Andreia Bettencourt, Nicola Bizzaro, Miri Blank, Dimitrios P. Bogdanos, Daniela Boleixa, Vânia Vieira Borba, Paola Borgiani, Nicola Luigi Bragazzi, Iwona Brzosko, Marek Brzosko, Piergiacomo Calzavara-Pinton, Irene Campi, Luca Cantarini, Rosa A. Carranza-Muleiro, Cláudia Carvalho, Francesco Caso, Fulvia Ceccarelli, Ricard Cervera, Joab Chapman, Xian Chen, Maria Sole Chimenti, Cinzia Ciccacci, Enrica Cipriano, Jan Willem Cohen Tervaert, Tania Colasanti, Paola Conigliaro, Fabrizio Conti, Louis Coplan, Luisa Costa, Stefania Croci, María del Pilar Cruz-Domínguez, Maurizio Cutolo, Shani Dahan, Jan Damoiseaux, Caterina De Carolis, Antonio Del Puente, Vinicius Domingues, David H. Dreyfus, Tali Drori, Michael Ehrenfeld, Gerard Espinosa, Antonella Farina, Giuseppina Alessandra Farina, Gianfranco Ferraccioli, Annacarla Finucci, Antonella Fioravanti, Katarzyna Fischer, Giulia Lavinia Fonti, Barone Francesca, Franco Franceschini, Jozélio Freire de Carvalho, Keishi Fujio, Grettel García-Collinot, Elena Generali, Maria Chiara Gerardi, Roberto Gerli, Smadar Gertel, Eitan Giat, Elisabetta Greco, Elisa Gremese, Eyal Grunebaum, Roberta Gualtierotti, Maria Domenica Guarino, Hanan Guzner-Gur, Shu-Gui He, Cristina Iannuccelli, Luis J. Jara, Pierre-Yves Jeandel, Dr Shaye Kivity, Przemyslaw J. Kotyla, Alec Krosser, Andrea Latini, Matilde Leon-Ponte, Aaron Lerner, Roger Abramino Levy, Benjamin Lichtbroun, Ramona Lucchetti, Qianjin Lu, Domenico P.E. Margiotta, António Marinho, Michel A. Martínez-Bencomo, Torsten Matthias, Gabriela Medina, Pier Luigi Meroni, Michael Lichtbroun, Gustavo Guimarães Moreira Balbi, Francesco Muratore, Luca Navarini, Giuseppe Novelli, Viviana Antonella Pacucci, Rosario Peluso, Monica Pendolino, Dolores Pérez, Carlo Perricone, Roberto Perricone, Luca Persani, Luca Petricca, Nicolò Pipitone, Guilherme Ramires de Jesús, Gustavo Resende, Chen Rizenbah, Ignasi Rodríguez-Pintó, Noel R. Rose, Eric Rosenthal, Mariateresa Rossi, Lazaros I. Sakkas, Carlo Salvarani, Piercarlo Sarzi-Puttini, Raffaele Scarpa, Yahel Segal, Michael J. Segel, Carlo Selmi, Dr Lior Seluk, Colafrancesco Serena, Amir Sharabi, Kassem Sharif, Netta Shoenfeld, Yehuda Shoenfeld, Flavio Signorelli, Ana Martins Silva, Berta Martins Silva, Sharon Slomovich, Raz Somech, Alessandra Soriano, Zoltán Szekanecz, Yoshiya Tanaka, Sara Tenti, Angela Tincani, Barbara Tolusso, Jiram Torres-Ruiz, Elias Toubi, Renato Tozzoli, Paola Triggianese, Amelia Chiara Trombetta, George C. Tsokos, Yumi Tsuchida, Zahava Vadasz, Guido Valesini, Joyce van Beers, Pieter van Paassen, Guia Maria Vannucchi, Carlos Vasconcelos, Marina Venturini, Olga Vera-Lastra, Mathilde Versini, Marta Vomero, Abdulla Watad, Haijing Wu, and Yong Zeng

Published
2019

5. In vitro comprehensive analysis of VA692 a new chemical entity for the treatment of osteoarthritis

Author

Mercedes Fernández-Moreno, Antonella Fioravanti, Francisco J. Blanco, Sara Cheleschi, Maurizio Anzini, Valentina Calamia, Mariangela Biava, and Antonio Giordani

Subjects
0301 basic medicine, Proteomics, Immunology, Interleukin-1beta, Apoptosis, Pharmacology, Chondrocyte cultures, 03 medical and health sciences, 0302 clinical medicine, Chondrocytes, Superoxide Dismutase-1, VA692, Osteoarthritis, medicine, Immunology and Allergy, Humans, Cells, Cultured, 030203 arthritis & rheumatology, Proteomic Profile, biology, Cyclooxygenase 2 Inhibitors, Chemistry, Anti-Inflammatory Agents, Non-Steroidal, Hsp90, In vitro, 030104 developmental biology, Cell culture, Celecoxib, Proteome, biology.protein, Intracellular proteome, Selective cyclooxigenase 2 inhibitors, Intracellular, medicine.drug
Abstract

[Abstract] Selective cyclooxigenase (COX)-2 inhibitors were developed to prevent traditional non-steroidal anti-inflammatory drugs (tNSAIDs) gastro-intestinal adverse effects. VA692, a recently disclosed selective COX-2 inhibitor, structurally related to well-known marketed coxibs, showed anti-inflammatory, and anti-nociceptive properties. The aim of this study was to analyze the anti-inflammatory effect of VA692, in comparison with celecoxib. At this purpose we evaluated the pro-inflammatory cytokines and anti-oxidant enzymes gene expression, apoptosis and ROS production, and PGE2 release in chondrocytes (both primary cultures and immortalized T/C-28a2 cell line) treated with the two drugs. Furthermore, a proteomic analysis has been performed in T/C-28a2 cell line to evaluate modifications in their proteomic profile following drug treatment in presence of IL-1β. Our results demonstrated the anti-inflammatory effect of the novel synthesized VA692, and confirmed those of celecoxib, in counteracting the stimulus of IL-1β in both osteoarthritic (OA) chondrocytes and T/C-28a2 cell line. Furthermore, the data underlined the possible anti-apoptotic and anti-oxidant role of VA692, implying its regulation in superoxide anion production as indicated by the modulation of anti-oxidant enzymes. The proteomic analysis provides new information about the effect of VA692 on human T/C-28a2 intracellular proteome, demonstrating the usefulness of this approach in the identification and quantifications of several proteins. Modulation of some proteins such as Hsp90 and SOD by VA692 could explain its role in the therapeutic approach of OA. Based on our results, we can affirm that VA692 has more beneficial effect compared with celecoxib particularly regarding the modulation of oxidant/anti-oxidant system and proteome profile of human articular chondrocytes.

Published
2018

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