scholarly journals Designing Anti-inflammatory Drugs from Parasitic Worms: A Synthetic Small Molecule Analogue of the Acanthocheilonema viteae Product ES-62 Prevents Development of Collagen-Induced Arthritis

2013 ◽  
Vol 56 (24) ◽  
pp. 9982-10002 ◽  
Author(s):  
Lamyaa Al-Riyami ◽  
Miguel A. Pineda ◽  
Justyna Rzepecka ◽  
Judith K. Huggan ◽  
Abedawn I. Khalaf ◽  
...  
Keyword(s):  
Small Molecule ◽  
Collagen Induced Arthritis ◽  
Acanthocheilonema Viteae ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Parasitic Worms ◽  
Synthetic Small Molecule

scholarly journals Identification of small molecule inhibitors of RANKL and TNF signalling as anti-inflammatory and antiresorptive agents in mice

2013 ◽  
Vol 74 (1) ◽  
pp. 220-226 ◽  
Author(s):  
Emmanuel Coste ◽  
Iain R Greig ◽  
Patrick Mollat ◽  
Lorraine Rose ◽  
Mohini Gray ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Bone Loss ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Joint Destruction ◽  
Luciferase Reporter ◽  
Collagen Induced Arthritis ◽  
Arthritis Model ◽  
Anti Inflammatory ◽  
Systemic Bone Loss

IntroductionInflammatory joint diseases such as rheumatoid arthritis are associated with local bone erosions and systemic bone loss, mediated by increased osteoclastic activity. The receptor activator of nuclear factor (NF) κB ligand (RANKL) plays a key role in mediating inflammation-induced bone loss, whereas tumour necrosis factor (TNF) plays a central role in the inflammatory process. Here we tested whether a recently identified class of small molecule inhibitors of RANKL signalling (ABD compounds) also affect TNF signalling and whether these compounds inhibit inflammation in an animal model of rheumatoid arthritis.MethodsThe inhibitory effects of the ABD compounds on TNF-induced signalling were tested in mouse macrophage cultures by western blotting and in an NFκB luciferase-reporter cell line. The anti-inflammatory effects of the compounds were tested in the mouse collagen-induced arthritis model of rheumatoid arthritis.ResultsThe ABD compounds ABD328 and ABD345 both inhibited TNF-induced activation of the NFκB pathway and the extracellular signal-regulated kinase (ERK) and Jun kinase (JNK) mitogen activated protein kinases (MAPKs). When tested in the mouse collagen-induced arthritis model of rheumatoid arthritis, the compounds suppressed inflammatory arthritis, inhibited joint destruction and prevented systemic bone loss. Furthermore, one of the compounds (ABD328) showed oral activity.ConclusionsHere we describe a novel class of small molecule compounds that inhibit both RANKL- and TNF-induced NFκB and MAPK signalling in osteoclasts and macrophages, and inflammation and bone destruction in a mouse model of rheumatoid arthritis. These novel compounds therefore represent a promising new class of treatments for inflammatory diseases, such as rheumatoid arthritis.

scholarly journals Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Progress in Small Molecule Drug Development

2010 ◽  
Vol 3 (5) ◽  
pp. 1530-1549 ◽  
Author(s):  
Praveen P. N. Rao ◽  
Saad N. Kabir ◽  
Tarek Mohamed
Keyword(s):  
Drug Development ◽  
Small Molecule ◽  
Small Molecule Drug ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

New small molecule analgesics

2021 ◽  
Vol 28 ◽  
Author(s):  
Sergey S. Laev ◽  
Nariman F. Salakhutdinov
Keyword(s):  
Pain Management ◽  
Small Molecule ◽  
Opioid Analgesics ◽  
Analgesic Drugs ◽  
Analgesic Effects ◽  
Design And Synthesis ◽  
Analgesic Agents ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Perspective

: Pain is a symptom of ninety percent of human diseases, and pain management is a very important medicinal problem. Various modulators of the pain response have been detected and analgesic effects are obtained by increasing inhibition or decreasing excitation in the nervous system. Various known analgesic drugs are commonly used to relieve the pain; however, this problem is still not fully resolved by currently available treatments. Available analgesic drugs (non-steroidal anti-inflammatory drugs, opioids, and analgesic adjuvants) are not too effective and are severely limited by adverse effects, for example, opioid addiction. Therefore, developing effective pain management is a difficult but necessary task. Thus, there is an urgent need for further development of the design and synthesis of new analgesic agents. The aim of this review is to present recent progress in search of new small molecule analgesics. The structures and effects of new perspective analgesic agents (anti-inflammatory agents, opioid analgesics, adjuvant agents for pain management and natural compounds) are presented and discussed. The review covers the literature published in 2015-2020 years and includes 173 references.

Polyphenols from Cymbopogon citratus inhibit iNOS expression and NO production – a promising source of new anti-inflammatory drugs

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
V Francisco ◽  
A Figueirinha ◽  
B Neves ◽  
C Garcia-Rodriguez ◽  
M Lopes ◽  
...  
Keyword(s):  
Inos Expression ◽  
No Production ◽  
Cymbopogon Citratus ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Promising Source

Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page
Keyword(s):  
Inflammatory Diseases ◽  
Therapeutic Applications ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

Sign in / Sign up

Export Citation Format

Share Document