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Molecules 2016, 21(6), 809; doi:10.3390/molecules21060809

Syk and IRAK1 Contribute to Immunopharmacological Activities of Anthraquinone-2-carboxlic Acid

1
Department of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Korea
2
Department of Pharmacy, Sunchon National University, Suncheon 57922, Korea
3
School of Systems Biomedical Science, Soongsil University, Seoul 06978, Korea
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 21 May 2016 / Revised: 16 June 2016 / Accepted: 18 June 2016 / Published: 22 June 2016
(This article belongs to the Section Molecular Diversity)
View Full-Text   |   Download PDF [4164 KB, uploaded 22 June 2016]   |  

Abstract

Anthraquinone-2-carboxlic acid (9,10-dihydro-9,10-dioxo-2-anthracenecarboxylic acid, AQCA) was identified as one of the major anthraquinones in Brazilian taheebo. Since there was no report explaining its immunopharmacological actions, in this study, we aimed to investigate the molecular mechanism of AQCA-mediated anti-inflammatory activity using reporter gene assays, kinase assays, immunoblot analyses, and overexpression strategies with lipopolysaccharide (LPS)-treated macrophages. AQCA was found to suppress the release of nitric oxide (NO) and prostaglandin (PG) E2 from LPS-treated peritoneal macrophages without displaying any toxic side effects. Molecular analysis revealed that AQCA was able to inhibit the activation of the nuclear factor (NF)-κB and activator protein (AP)-1 pathways by direct suppression of upstream signaling enzymes including interleukin-1 receptor-associated kinase 1 (IRAK1) and spleen tyrosine kinase (Syk). Therefore, our data strongly suggest that AQCA-mediated suppression of inflammatory responses could be managed by a direct interference of signaling cascades including IRAK and Syk, linked to the activation of NF-κB and AP-1. View Full-Text
Keywords: anthraquinones; anthraquinone-2-carboxylic acid; inflammatory response; IRAK1 anthraquinones; anthraquinone-2-carboxylic acid; inflammatory response; IRAK1
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MDPI and ACS Style

Park, J.G.; Son, Y.-J.; Kim, M.-Y.; Cho, J.Y. Syk and IRAK1 Contribute to Immunopharmacological Activities of Anthraquinone-2-carboxlic Acid. Molecules 2016, 21, 809.

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