Gallorini, Marialucia and Rapino, Monica and Schweikl, Helmut and Cataldi, Amelia and Amoroso, Rosa and Maccallini, Cristina (2021) Selective Inhibitors of the Inducible Nitric Oxide Synthase as Modulators of Cell Responses in LPS-Stimulated Human Monocytes. MOLECULES, 26 (15): 4419. ISSN , 1420-3049
Full text not available from this repository. (Request a copy)Abstract
Inducible nitric oxide synthase (iNOS) is a crucial enzyme involved in monocyte cell response towards inflammation, and it is responsible for the production of sustained amounts of nitric oxide. This free radical molecule is involved in the defense against pathogens; nevertheless, its continuous and dysregulated production contributes to the development of several pathological conditions, including inflammatory and autoimmune diseases. In the present study, we investigated the effects of two new iNOS inhibitors, i.e., 4-(ethanimidoylamino)-N-(4-fluorophenyl)benzamide hydrobromide (FAB1020) and N-{3-[(ethanimidoylamino)methyl]benzyl}-l-prolinamidedihydrochloride (CM554), on human LPS-stimulated monocytes, using the 1400 W compound as a comparison. Our results show that CM544 and FAB1020 are selective and decrease cytotoxicity, IL-6 secretion and LPS-stimulated monocyte migration. Furthermore, the modulation of iNOS, nitrotyrosine and Nrf2 were analyzed at the protein level. Based on the collected preliminary results, the promising therapeutic value of the investigated compounds emerges, as they appear able to modulate the pro-inflammatory LPS-stimulated response in the low micromolar range in human monocytes.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CYTOKINE PRODUCTION; INOS; DIFFERENTIATION; INFLAMMATION; MACROPHAGES; immunomodulation; inflammation; inhibitors; monocytes; nitric oxide |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Medicine > Lehrstuhl für Zahnerhaltung und Parodontologie > Prof. Dr. rer. nat. Helmut Schweikl |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 13 Sep 2022 08:56 |
| Last Modified: | 13 Sep 2022 08:56 |
| URI: | https://pred.uni-regensburg.de/id/eprint/47296 |
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