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Title 

DPIE [2-(1,2-diphenyl-1H-indol-3-yl)ethanamine] augments pro-inflammatory cytokine production in IL-1β-stimulated primary human oral cells

Authors 

S H AhnJ K LeeN D KimSeok Ho KimS LeeS JungK O ChayT H Lee

Publisher 

MDPI AG

Issue Date 

2018

Citation 

International Journal of Molecular Sciences

Keywords 

IL-1R1IL-1βOral fibroblastsPro-inflammatory cytokinesSPR

Abstract 

Interleukin-1β (IL-1β) is a prominent pro-inflammatory cytokine that is implicated in a variety of autoimmune diseases and plays an important role in host defense against infections. IL-1β activity increases with its increasing binding capacity to IL-1 receptors (IL-1Rs). Thus, numerous studies have targeted the discovery of molecules modulating the interactions between IL-1β and IL-1R1. We have conducted an IL-1R1 structure-based virtual screening to identify small molecules that could alter IL-1β activity, using in silico computational analysis. Sixty compounds from commercial libraries were predicted to bind to IL-1R1, and their influence on cytokine production in IL-1β-stimulated gingival fibroblasts (GFs) was determined. Of these, only (2-(1,2-diphenyl-1H-indol-3-yl)ethanamine (DPIE) showed a synergistic increase in inflammatory molecules and cytokine production (IL-6, IL-8, and COX-2) at both mRNA and protein levels in IL-1β-stimulated GFs. The enhancing activity of DPIE in IL-1β-induced cytokine production increased in a dose-dependent manner without cytotoxicity. This pattern was also observed in IL-1β-stimulated primary human periodontal ligament cells (PDLs). Furthermore, we measured the impact of DPIE on the IL-1β?IL-1R1 system using surface plasmon resonance and demonstrated that DPIE increased the binding affinity of IL-1β to IL-1R1. These data indicate that DPIE boosts IL-1β signaling by enhancing the binding of IL-1β to IL-1R1 in oral primary cells

ISSN 

1422-0067

Link 

http://dx.doi.org/10.3390/ijms19071835

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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