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Open AccessArticle

Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages

1
Membrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, Chile
2
Laboratory of Immunology, Faculty of Sciences, University of Chile, Santiago 7810000, Chile
3
Program of Physiology, Faculty of Medicine and Department of Internal Medicine Hospital Clínico, University of Chile, Santiago 8380453, Chile
*
Author to whom correspondence should be addressed.
Mar. Drugs 2020, 18(6), 283; https://doi.org/10.3390/md18060283
Received: 8 May 2020 / Revised: 19 May 2020 / Accepted: 22 May 2020 / Published: 27 May 2020
(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). View Full-Text
Keywords: neosaxitoxin; inflammation; Nav channels; macrophages neosaxitoxin; inflammation; Nav channels; macrophages
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Montero, M.C.; del Campo, M.; Bono, M.; Simon, M.V.; Guerrero, J.; Lagos, N. Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages. Mar. Drugs 2020, 18, 283.

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