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

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Flaxseed orbitides, linusorbs, inhibit LPS-induced THP-1 macrophage inflammation
RSC Advances ( IF 3.9 ) Pub Date : 2020-6-15 , DOI: 10.1039/c9ra09058d
Xian-Guo Zou _{1,

2,

3} , Youn Young Shim _{3,

4,

5,

6} , Jae Youl Cho ₆ , Deok Jeong ₆ , Jian Yang ₇ , Ze-Yuan Deng ₂ , Martin J T Reaney _{3,

4,

5}

Affiliation

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.

中文翻译：

亚麻籽轨道化合物、linusorbs 可抑制 LPS 诱导的 THP-1 巨噬细胞炎症

Linusorbs（亚麻籽轨道化合物）是一类天然存在的环肽。之前，我们报道过它们的抗癌作用与其结构有关。在本研究中，我们研究了 2 种不同的 linusorb（[1–9-NαC]-linusorb B2 和 [1–9-NαC]-linusorb B3）在脂多糖 (LPS) 诱导的 THP-1 巨噬细胞活化中的抗炎活性以及这种炎症反应的潜在机制。这两种分子均抑制促炎介质（TNF-α、IL-1β、IL-6、NO 和 COX-2），并参与下调 NF-κB 信号通路。对促炎介质的抑制作用相当，作用浓度范围相似（1-4 μM）。然而，每种化合物诱导 NF-κB 通路下调的化合物浓度不同。 [1–9-NαC]-linusorb B3 在 1 和 2 μM 浓度下可抑制 NF-κB 通路的激活，而 [1–9-NαC]-linusorb B2 在 4 μM 浓度下可诱导类似的抑制作用。

更新日期：2020-06-15

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