Characterization of βN-Octadecanoyl-5-hydroxytryptamide Anti-Inflammatory Effect.

Thais Biondino Sardella Giorno,Ana Laura Macedo Brand,Fernanda Alves Lima,Camila Martins de Oliveira,Patricia Dias Fernandes,Claudia Moraes Rezende

doi:10.3390/molecules26123709

Thais Biondino Sardella Giorno, Ana Laura Macedo Brand + Show 4 more

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https://doi.org/10.3390/molecules26123709

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Abstract

Background: N-octadecanoyl-5-hydroxytryptamide (C18-5HT) is an amide that can be obtained by the coupling of serotonin and octadecanoic acid. This study aims to characterize the in vivo and in vitro anti-inflammatory activity of C18-5HT. Methods: A subcutaneous air pouch model (SAP) was used. The exudates were collected from SAP after carrageenan injection to assess cell migration and inflammatory mediators production. RAW 264.7 cells were used for in vitro assays. Results: C18-5HT significantly inhibited leukocyte migration into the SAP as well as nitric oxide (NO) and cytokines production and protein extravasation. We also observed an reduction in some cytokines and an increase in IL-10 production. Assays conducted with RAW 264.7 cells indicated that C18-5HT inhibited NO and cytokine produced. Conclusions: Taken together, our data suggest that C18-5HT presents a significant effect in different cell types (leukocytes collected from exudate, mainly polumorphonuclear leukocytes and cell culture macrophages) and is a promising compound for further studies for the development of a new anti-inflammatory drug.

Highlights

Inflammation is a dynamic response to tissue injury and pathogen invasion.Macrophages are the first cells to recognize the potential threat, followed by mast cells, leukocytes, and neutrophils
We demonstrated that the serotonin amide presented affects the second phase of the formalin-induced licking response, which is a well-established model for the screening of possible antinociceptive and anti-inflammatory compounds
Neutrophils are attracted to sites of inflammation by various stimuli, such as microorganism products (LPS) and chemotactic factors released by resident cells, such as cytokines, chemokines, and eicosanoids [19,20,21]

Summary

Introduction

Macrophages are the first cells to recognize the potential threat, followed by mast cells, leukocytes, and neutrophils. These cells release inflammatory mediators that amplify the immune response, such as cytokines, nitric oxide (NO), chemokines, vasoactive amines, leukotrienes, and prostaglandins (PGs), and they promote fever, redness, edema, and pain [1]. The chemokines produced by resident cells recruit, through their receptors, circulating neutrophils [2]. These neutrophils transmigrate through the endothelium, reach the inflamed tissue, degranulate, generate reactive oxygen species (ROS), and produce other mediators such as NO and PGs, amplifying the inflammatory response [2]

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