{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T04:55:01Z","timestamp":1787028901599,"version":"build-2736575974"},"reference-count":61,"publisher":"MDPI AG","issue":"6","license":[{"start":{"date-parts":[[2020,5,27]],"date-time":"2020-05-27T00:00:00Z","timestamp":1590537600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Marine Drugs"],"abstract":"<jats:p>(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 (1\u00b5M). The expression of inflammatory mediators was assessed: nitric oxide (NO) content using the Griess assay, TNF-\u03b1 content using the ELISA assay, and mRNA of inducible nitric oxide synthase (iNOS), interleukin-1\u03b2 (IL-1\u03b2), and tumor necrosis factor-\u03b1 (TNF-\u03b1) using a real-time polymerase chain reaction. (3) Results: NeoSTX (1 \u03bcM) significantly inhibited the release of NO, TNF-\u03b1, and expression of iNOS, IL-1\u03b2, and TNF-\u03b1 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).<\/jats:p>","DOI":"10.3390\/md18060283","type":"journal-article","created":{"date-parts":[[2020,5,27]],"date-time":"2020-05-27T05:35:52Z","timestamp":1590557752000},"page":"283","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Neosaxitoxin Inhibits the Expression of Inflammation Markers of the M1 Phenotype in Macrophages"],"prefix":"10.3390","volume":"18","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0097-7669","authenticated-orcid":false,"given":"M. Cecilia","family":"Montero","sequence":"first","affiliation":[{"name":"Membrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Miguel","family":"del Campo","sequence":"additional","affiliation":[{"name":"Membrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M.","family":"Bono","sequence":"additional","affiliation":[{"name":"Laboratory of Immunology, Faculty of Sciences, University of Chile, Santiago 7810000, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M. Valeska","family":"Simon","sequence":"additional","affiliation":[{"name":"Laboratory of Immunology, Faculty of Sciences, University of Chile, Santiago 7810000, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Julia","family":"Guerrero","sequence":"additional","affiliation":[{"name":"Program of Physiology, Faculty of Medicine and Department of Internal Medicine Hospital Cl\u00ednico, University of Chile, Santiago 8380453, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"N\u00e9stor","family":"Lagos","sequence":"additional","affiliation":[{"name":"Membrane Biochemistry Laboratory, Faculty of Medicine, University of Chile, Santiago 8380453, Chile"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,5,27]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"953","DOI":"10.1038\/nri1733","article-title":"Monocyte and Macrophage Heterogeneity","volume":"5","author":"Gordon","year":"2005","journal-title":"Nat. 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