Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid

Jae Gwang Park, Seung Cheol Kim, Yun Hwan Kim, Woo Seok Yang, Yong Kim, Sungyoul Hong, Kyung Hee Kim, Byong Chul Yoo, Shi Hyung Kim, Jong Hoon Kim, Jae Youl Cho

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36 Scopus citations


Anthraquinone compounds are one of the abundant polyphenols found in fruits, vegetables, and herbs. However, the in vivo anti-inflammatory activity and molecular mechanisms of anthraquinones have not been fully elucidated. We investigated the activity of anthraquinones using acute inflammatory and nociceptive experimental conditions. Anthraquinone-2-carboxylic acid (9,10-dihydro-9,10-dioxo-2-anthracenecarboxylic acid, AQCA), one of the major anthraquinones identified from Brazilian taheebo, ameliorated various inflammatory and algesic symptoms in EtOH/HCl-and acetylsalicylic acid-(ASA-) induced gastritis, arachidonic acid-induced edema, and acetic acid-induced abdominal writhing without displaying toxic profiles in body and organ weight, gastric irritation, or serum parameters. In addition, AQCA suppressed the expression of inflammatory genes such as cyclooxygenase-(COX-) 2 in stomach tissues and lipopolysaccharide-(LPS-) treated RAW264.7 cells. According to reporter gene assay and immunoblotting analyses, AQCA inhibited activation of the nuclear factor-(NF-) B and activator protein-(AP-) 1 pathways by suppression of upstream signaling involving interleukin-1 receptor-associated kinase 4 (IRAK1), p38, Src, and spleen tyrosine kinase (Syk). Our data strongly suggest that anthraquinones such as AQCA act as potent anti-inflammatory and antinociceptive components in vivo, thus contributing to the immune regulatory role of fruits and herbs.

Original languageEnglish
Article number1903849
JournalMediators of Inflammation
StatePublished - 2016

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© 2016 Jae Gwang Park et al.


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