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

Abstract

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-) κB 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.

• Authors: 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
• Journal: Mediators of inflammation (Mediators Inflamm) Vol. 2016 Pg. 1903849 ( 2016) ISSN: 1466-1861 [Electronic] United States
• PMID: 27057092 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics
• Anthraquinones
• Anti-Inflammatory Agents
• Lipopolysaccharides
• NF-kappa B
• Plant Extracts
• Taheebo
• anthraquinone-2-carboxylic acid
• Arachidonic Acid
• Ranitidine
• Cyclooxygenase 2
• Acetic Acid

Topics

• Acetic Acid (pharmacology)
• Analgesics (administration & dosage, therapeutic use)
• Animals
• Anthraquinones (administration & dosage, therapeutic use)
• Anti-Inflammatory Agents (administration & dosage, therapeutic use)
• Arachidonic Acid (pharmacology)
• Cyclooxygenase 2 (metabolism)
• Edema (chemically induced, drug therapy)
• Lipopolysaccharides (pharmacology)
• Male
• Mice
• Mice, Inbred ICR
• NF-kappa B (metabolism)
• Plant Extracts (chemistry)
• RAW 264.7 Cells
• Ranitidine (administration & dosage, therapeutic use)
• Signal Transduction (drug effects)