Issue 38, 2020, Issue in Progress

Flaxseed orbitides, linusorbs, inhibit LPS-induced THP-1 macrophage inflammation

Abstract

Linusorbs (flaxseed orbitides) are a family of naturally-occurring cyclic peptides. Previously, we reported that their anticancer effects were associated with their structures. In this study, we investigated the anti-inflammatory activities of 2 different linusorbs ([1–9-NαC]-linusorb B2 and [1–9-NαC]-linusorb B3) in lipopolysaccharide (LPS)-induced THP-1 macrophage activation as well as the underlying mechanism of this inflammatory response. Both molecules suppressed pro-inflammatory mediators (TNF-α, IL-1β, IL-6, NO and COX-2) and were involved in downregulating the NF-κB signaling pathway. The suppressive effects on pro-inflammatory mediators were comparable and the concentration range of action was similar (1–4 μM). However, the concentration of compound that induced downregulation of the NF-κB pathway was different for each compound. While [1–9-NαC]-linusorb B3 could inhibit the activation of the NF-κB pathway at concentrations of 1 and 2 μM, [1–9-NαC]-linusorb B2 induced a comparable inhibitory effect at a concentration of 4 μM.

Graphical abstract: Flaxseed orbitides, linusorbs, inhibit LPS-induced THP-1 macrophage inflammation

Article information

Article type
Paper
Submitted
02 Nov 2019
Accepted
10 May 2020
First published
15 Jun 2020
This article is Open Access
Creative Commons BY license

RSC Adv., 2020,10, 22622-22630

Flaxseed orbitides, linusorbs, inhibit LPS-induced THP-1 macrophage inflammation

X. Zou, Y. Y. Shim, J. Y. Cho, D. Jeong, J. Yang, Z. Deng and M. J. T. Reaney, RSC Adv., 2020, 10, 22622 DOI: 10.1039/C9RA09058D

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