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Suppressing mPGES-1 expression by sinomenine ameliorates inflammation and arthritis.

Abstract
Recently, microsomal prostaglandin E synthase 1 (mPGES-1) has attracted much attention from pharmacologists as a promising strategy and an attractive target for treating various types of diseases including rheumatoid arthritis (RA), which could preserve the anti-inflammatory effect while reducing the adverse effects often occur during administration of non-steroidal anti-inflammatory drugs (NSAIDs). Here, we report that sinomenine (SIN) decreased prostaglandin (PG)E2 levels without affecting prostacyclin (PG)I2 and thromboxane (TX)A2 synthesis via selective inhibiting mPGES-1 expression, a possible reason of low risk of cardiovascular event compared with NSAIDs. In addition, mPGES-1 protein expression was down-regulated by SIN treatment in the inflamed paw tissues both in carrageenan-induced edema model in rats and the collagen-II induced arthritis (CIA) model in DBA mice. More interestingly, SIN suppressed the last step of mPGES-1 gene expression by decreasing the DNA binding ability of NF-κB, paving a new way for drug discovery.
AuthorsHua Zhou, Jian-Xin Liu, Jin-Fang Luo, Chun-Song Cheng, Elaine Lai-Han Leung, Ying Li, Xiao-Hui Su, Zhong-Qiu Liu, Ting-Bo Chen, Fu-Gang Duan, Yan Dong, Yi-Han Zuo, Chong Li, Chon Kit Lio, Ting Li, Pei Luo, Ying Xie, Xiao-Jun Yao, Pei-Xun Wang, Liang Liu
JournalBiochemical pharmacology (Biochem Pharmacol) Vol. 142 Pg. 133-144 (10 15 2017) ISSN: 1873-2968 [Electronic] England
PMID28711625 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2017 Elsevier Inc. All rights reserved.
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Morphinans
  • sinomenine
  • Prostaglandin-E Synthases
  • Ptges protein, mouse
  • Ptges protein, rat
Topics
  • A549 Cells
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (adverse effects, isolation & purification, pharmacology, therapeutic use)
  • Arthritis, Experimental (drug therapy, immunology)
  • Cell Culture Techniques
  • Cell Survival (drug effects)
  • Edema (drug therapy, immunology)
  • Female
  • Gene Expression (drug effects)
  • Macrophages, Peritoneal (drug effects)
  • Male
  • Mice, Inbred DBA
  • Morphinans (adverse effects, isolation & purification, pharmacology, therapeutic use)
  • Prostaglandin-E Synthases (genetics)
  • Rats, Sprague-Dawley
  • Transfection

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