Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages
(1) Background: Neosaxitoxin (NeoSTX) has been used as a local anesthetic, but its anti-inflammatory effects have not been well defined. In the present study, we investigate the effects of NeoSTX on lipopolysaccharide (LPS)-activated macrophages. (2) Methods: Raw 264.7 and equine PBMC cells were inc...
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MDPI AG
2020-05-01
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| Series: | Marine Drugs |
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| Online Access: | https://www.mdpi.com/1660-3397/18/6/283 |
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| author | M. Cecilia Montero Miguel del Campo M. Bono M. Valeska Simon Julia Guerrero Néstor Lagos |
| author_facet | M. Cecilia Montero Miguel del Campo M. Bono M. Valeska Simon Julia Guerrero Néstor Lagos |
| author_sort | M. Cecilia Montero |
| collection | DOAJ |
| description | (1) Background: Neosaxitoxin (NeoSTX) has been used as a local anesthetic, but its anti-inflammatory effects have not been well defined. In the present study, we investigate the effects of NeoSTX on lipopolysaccharide (LPS)-activated macrophages. (2) Methods: Raw 264.7 and equine PBMC cells were incubated with or without 100 ng/mL LPS in the presence or absence of NeoSTX (1µM). The expression of inflammatory mediators was assessed: nitric oxide (NO) content using the Griess assay, TNF-α content using the ELISA assay, and mRNA of inducible nitric oxide synthase (iNOS), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α) using a real-time polymerase chain reaction. (3) Results: NeoSTX (1 μM) significantly inhibited the release of NO, TNF-α, and expression of iNOS, IL-1β, and TNF-α in LPS-activated macrophages of both species studied. Furthermore, our study shows that the LPS-induced release of inflammatory mediators was suppressed by NeoSTX. Additionally, NeoSTX deactivated polarized macrophages to M1 by LPS without compromising its polarization towards M2. (4) Conclusions: NeoSTX inhibits LPS-induced release of inflammatory mediators from macrophages, and these effects may be mediated by the blockade of voltage-gated sodium channels (VGSC). |
| first_indexed | 2024-03-10T19:35:03Z |
| format | Article |
| id | doaj.art-c49530e0b4b94fefbca86772ef97b205 |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-03-10T19:35:03Z |
| publishDate | 2020-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-c49530e0b4b94fefbca86772ef97b2052023-11-20T01:51:30ZengMDPI AGMarine Drugs1660-33972020-05-0118628310.3390/md18060283Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in MacrophagesM. Cecilia Montero0Miguel del Campo1M. Bono2M. Valeska Simon3Julia Guerrero4Néstor Lagos5Membrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, ChileMembrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, ChileLaboratory of Immunology, Faculty of Sciences, University of Chile, Santiago 7810000, ChileLaboratory of Immunology, Faculty of Sciences, University of Chile, Santiago 7810000, ChileProgram of Physiology, Faculty of Medicine and Department of Internal Medicine Hospital Clínico, University of Chile, Santiago 8380453, ChileMembrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, Chile(1) Background: Neosaxitoxin (NeoSTX) has been used as a local anesthetic, but its anti-inflammatory effects have not been well defined. In the present study, we investigate the effects of NeoSTX on lipopolysaccharide (LPS)-activated macrophages. (2) Methods: Raw 264.7 and equine PBMC cells were incubated with or without 100 ng/mL LPS in the presence or absence of NeoSTX (1µM). The expression of inflammatory mediators was assessed: nitric oxide (NO) content using the Griess assay, TNF-α content using the ELISA assay, and mRNA of inducible nitric oxide synthase (iNOS), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α) using a real-time polymerase chain reaction. (3) Results: NeoSTX (1 μM) significantly inhibited the release of NO, TNF-α, and expression of iNOS, IL-1β, and TNF-α in LPS-activated macrophages of both species studied. Furthermore, our study shows that the LPS-induced release of inflammatory mediators was suppressed by NeoSTX. Additionally, NeoSTX deactivated polarized macrophages to M1 by LPS without compromising its polarization towards M2. (4) Conclusions: NeoSTX inhibits LPS-induced release of inflammatory mediators from macrophages, and these effects may be mediated by the blockade of voltage-gated sodium channels (VGSC).https://www.mdpi.com/1660-3397/18/6/283neosaxitoxininflammationNav channelsmacrophages |
| spellingShingle | M. Cecilia Montero Miguel del Campo M. Bono M. Valeska Simon Julia Guerrero Néstor Lagos Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages Marine Drugs neosaxitoxin inflammation Nav channels macrophages |
| title | Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages |
| title_full | Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages |
| title_fullStr | Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages |
| title_full_unstemmed | Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages |
| title_short | Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages |
| title_sort | neosaxitoxin inhibits the expression of inflammation markers of the m1 phenotype in macrophages |
| topic | neosaxitoxin inflammation Nav channels macrophages |
| url | https://www.mdpi.com/1660-3397/18/6/283 |
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