Gentiopicroside prevents interleukin-1 beta induced inflammation response in rat articular chondrocyte.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE:

In traditional Chinese medicine, Gentiana macrophylla Pall have been prescribed for the treatment of pain and inflammatory conditions. In addition, it is a common Tibetan medicinal herb used for the treatment of tonsillitis, urticaria, and rheumatoid arthritis (RA), while the flowers of G. macrophylla Pall have been traditionally treated as an anti-inflammatory agent to clear heat in Mongolian medicine. The secoiridoid glycosides and their derivatives are the primary active components of G. macrophylla and have been demonstrated to be effective as anti-inflammatory agents.

MATERIALS AND METHODS:

Solvent extraction and D101 macroporous resin columns were employed to concentratethe gentiopicroside. Gentiopicroside cytotoxicity was assessed by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay; the toxicity of gentiopicroside in chondrocytes was reconfirmed using Hoechst staining. Western blotting, reverse transcriptase-polymerase chain reaction (RT-PCR) and immunohistochemistry were utilized to explore the protective effects and mechanisms of gentiopicroside prevents interleukin-1 beta induced inflammation response in rat articular chondrocyte.

RESULTS:

The MTT assay demonstrated that 50, 500, and 1,500 μg/mL of gentiopicroside exhibited no significant toxicity to chondrocytes (P>0.05) after 24h. Using immunohistochemistry, ELISA, RT-PCR, Western blot method to explore the protective effect and mechanism of gentiopicroside on chondrocytes induced by IL-1β. The results showed some pathways of IL-1β signal transduction were inhibited by gentiopicroside in rat chondrocytes: p38, ERK and JNK. Meanwhile, gentiopicroside showed inhibition in the IL-1β-induced release of MMPs while increasing Collagen type II expression.

CONCLUSIONS:

The current study demonstrated that gentiopicroside exhibited a potent protective effect on IL-1β induced inflammation response in rat articular chondrocyte. Thus, gentiopicroside could be a potential therapeutic strategy for treatment of OA.

• Authors: Lei Zhao, Juan Ye, Guo-Tai Wu, Xue-Jing Peng, Peng-Fei Xia, Yuan Ren
• Journal: Journal of ethnopharmacology (J Ethnopharmacol) Vol. 172 Pg. 100-7 (Aug 22 2015) ISSN: 1872-7573 [Electronic] Ireland
• PMID: 26116164 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

Chemical References

• Anti-Inflammatory Agents
• Collagen Type II
• Interleukin-1beta
• Iridoid Glucosides
• gentiopicroside
• Cyclooxygenase 2
• Mitogen-Activated Protein Kinases
• Collagenases
• Dinoprostone

Topics

• Animals
• Anti-Inflammatory Agents (isolation & purification, pharmacology, therapeutic use)
• Cell Survival (drug effects)
• Cells, Cultured
• Chondrocytes (drug effects, metabolism)
• Collagen Type II (metabolism)
• Collagenases (biosynthesis)
• Cyclooxygenase 2 (biosynthesis)
• Dinoprostone (metabolism)
• Gene Expression (drug effects)
• Inflammation (drug therapy, immunology, prevention & control)
• Interleukin-1beta (antagonists & inhibitors, immunology)
• Iridoid Glucosides (isolation & purification, pharmacology, therapeutic use)
• Mitogen-Activated Protein Kinases (metabolism)
• Rats
• Signal Transduction (drug effects)