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

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 n...

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Main 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
Format: Article
Language:English
Published: Wiley 2016-01-01
Series:Mediators of Inflammation
Online Access:http://dx.doi.org/10.1155/2016/1903849
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author 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
author_facet 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
author_sort Jae Gwang Park
collection DOAJ
description 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.
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spelling doaj-art-9c2ea2c6dc0a430f9fa7863ad5a749bd2025-08-20T02:20:16ZengWileyMediators of Inflammation0962-93511466-18612016-01-01201610.1155/2016/19038491903849Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic AcidJae Gwang Park0Seung Cheol Kim1Yun Hwan Kim2Woo Seok Yang3Yong Kim4Sungyoul Hong5Kyung-Hee Kim6Byong Chul Yoo7Shi Hyung Kim8Jong-Hoon Kim9Jae Youl Cho10Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaDivision of Gynecologic Oncology, Department of Obstetrics and Gynecology, Ewha Womans University Mokdong Hospital College of Medicine, Ewha Womans University, Seoul 158-710, Republic of KoreaDivision of Gynecologic Oncology, Department of Obstetrics and Gynecology, Ewha Womans University Mokdong Hospital College of Medicine, Ewha Womans University, Seoul 158-710, Republic of KoreaDepartment of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaDepartment of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaDepartment of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaColorectal Cancer Branch, Research Institute, National Cancer Center, Goyang 410-769, Republic of KoreaColorectal Cancer Branch, Research Institute, National Cancer Center, Goyang 410-769, Republic of KoreaDepartment of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaDepartment of Veterinary Physiology, College of Veterinary Medicine, Biosafety Research Institute, Chonbuk National University, Iksan 54596, Republic of KoreaDepartment of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of KoreaAnthraquinone 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.http://dx.doi.org/10.1155/2016/1903849
spellingShingle 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
Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
Mediators of Inflammation
title Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
title_full Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
title_fullStr Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
title_full_unstemmed Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
title_short Anti-Inflammatory and Antinociceptive Activities of Anthraquinone-2-Carboxylic Acid
title_sort anti inflammatory and antinociceptive activities of anthraquinone 2 carboxylic acid
url http://dx.doi.org/10.1155/2016/1903849
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