alexa Synthesis and anti-inflammatory effect of chalcones and related compounds.


Modern Chemistry & Applications

Author(s): Hsieh HK, Lee TH, Wang JP, Wang JJ, Lin CN

Abstract Share this page

Abstract PURPOSE: Mast cell and neutrophil degranulations are the important players in inflammatory disorders. Combined with potent inhibition of chemical mediators released from mast cells and neutrophil degranulations, it could be a promising anti-inflammatory agent. 2',5'-Dihydroxychalcone has been reported as a potent chemical mediator and cyclooxygenase inhibitor. In an effort to continually develop potent anti-inflammatory agents, a novel series of chalcone, 2'- and 3'-hydroxychalcones, 2',5'-dihydroxychalcones and flavanones were continually synthesized to evaluate their inhibitory effects on the activation of mast cells and neutrophils and the inhibitory effect on phlogist-induced hind-paw edema in mice. METHODS: A series of chalcones and related compounds were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehyde and the anti-inflammatory activities of these synthetic compounds were studied on inhibitory effects on the activation of mast cells and neutrophils. RESULTS: Some chalcones showed strong inhibitory effects on the release of beta-glucuronidase and histamine from rat peritoneal mast cells stimulated with compound 48/80. Almost all chalcones and 4'-hydroxyflavanone exhibited potent inhibitory effects on the release of beta-glucuronidase and lysozyme from rat neutrophils stimulated with formyl-Met-Leu-Phe (fMLP). Some chalcones showed potent inhibitory effects on superoxide formation of rat neutrophils stimulated with fMLP/cytochalasin B (CB) or phorbol myristate acetate (PMA). 2',3-Dihydroxy-, 2',5'-dihydroxy-4-chloro-, and 2',5'-dihydroxychalcone showed remarkable inhibitory effects on hind-paw edema induced by polymyxin B in normal as well as in adrenalectomized mice. CONCLUSIONS: These results indicated that the anti-inflammatory effects of these compounds were mediated, at least partly, through the suppression of chemical mediators released from mast cells and neutrophils.
This article was published in Pharm Res and referenced in Modern Chemistry & Applications

Relevant Expert PPTs

Relevant Speaker PPTs

  • Yanina H Arana P
    Role of co-inhibitory pathways during experimental infection by Trypanosoma cruzi Tulahuen strain
    PPT Version | PDF Version
  • Eugene Stephane Mananga
    On Fer and Floquet-Magnus expansions: Application in solid-state nuclear magnetic resonance and physics
    PDF Version
  • Diego Gallego García
    Complex ungulate and predator effects on foraging behaviour and acorn dispersal by Algerian mice: an experimental approach
    PPT Version | PDF Version
  • Jahid Zeghiche
    Jahid-Zeghiche-Univesity-of-Al-Baha- Saudi-Arabia- Compressive- Strength-of-Concerete-filled-Thin- Steel-Stubs-Theoretical-and-Experimental-Study
    PPT Version | PDF Version
  • Merve Sagiroglu
    Merve-Sagıroglu- Erzurum-Technical-University-Turkey- Experimental-Investigation-of-Moment-Rotation-Curves-of-End-Plate-Connection-using-Sinusoidal-Beam
    PPT Version | PDF Version
  • Omnia AbouEl-Hamd
    Omnia-AbouEl-Hamd-United-Arab-Emirates-University-UAE- Experimental-Investigation-of-the-Fastening-Parameters-Influencing-the-Interfacial-Behavior-of-Composite-Steel-Anchored-Lap-Connections
    PPT Version | PDF Version
  • Yosef Yarden
    Classically, the 3’untranslated region (3’UTR) is that region in eukaryotic protein-coding genes from the translation termination codon to the polyA signal. It is transcribed as an integral part of the mRNA encoded by the gene. However, there exists another kind of RNA, which consists of the 3’UTR alone, without all other elements in mRNA such as 5’UTR and coding region. The importance of independent 3’UTR RNA (referred as I3’UTR) was prompted by results of artificially introducing such RNA species into malignant mammalian cells. Since 1991, we found that the middle part of the 3’UTR of the human nuclear factor for interleukin-6 (NF-IL6) or C/EBP gene exerted tumor suppression effect in vivo. Our subsequent studies showed that transfection of C/EBP 3’UTR led to down-regulation of several genes favorable for malignancy and to up-regulation of some genes favorable for phenotypic reversion. Also, it was shown that the sequences near the termini of the C/EBP 3’UTR were important for its tumor suppression activity. Then, the C/EBP 3’UTR was found to directly inhibit the phosphorylation activity of protein kinase CPKC in SMMC-7721, a hepatocarcinoma cell line. Recently, an AU-rich region in the C/EBP 3’UTR was found also to be responsible for its tumor suppression. Recently we have also found evidence that the independent C/EBP 3’UTR RNA is actually exists in human tissues, such as fetal liver and heart, pregnant uterus, senescent fibroblasts etc. Through 1990’s to 2000’s, world scientists found several 3’UTR RNAs that functioned as artificial independent RNAs in cancer cells and resulted in tumor suppression. Interestingly, majority of genes for these RNAs have promoter-like structures in their 3’UTR regions, although the existence of their transcribed products as independent 3’UTR RNAs is still to be confirmed. Our studies indicate that the independent 3’UTR RNA is a novel non-coding RNA species whose function should be the regulation not of the expression of their original mRNA, but of some essential life activities of the cell as a whole.
    PPT Version | PDF Version
  • Daniel Smith
    The editor as auteur: The modern role of editors and preditors
    PPT Version | PDF Version
  • Junio Cota Silva
    Enzymes and biotechnology: Can we overcome modern challenges?
    PPT Version | PDF Version
  • Hayam I Gad
    Effects of Pravastatin or 12/15 lipoxygenase pathway inhibitors on indices of Diabetic nephropathy in an experimental model of diabetic renal disease
    PPT Version | PDF Version
  • Donald Min
    USP Monograph Modernization – Procedure Review and Development
    PPT Version | PDF Version
  • Cheryl Atherley Todd
    Modern trends in the treatment of dementia
    PPT Version | PDF Version
  • Khadiga G Adham
    Impact of metal-loaded industrial dust on the physiology of a model experimental animal
    PPT Version | PDF Version
  • John Pixley
    In utero transplantation (IUT) an experimental window into immune self Basic and applied implications
    PPT Version | PDF Version
  • Klara Kubelkova
    The cellular basis of protective immunity against experimental infection caused by Francisella tularensis
    PPT Version | PDF Version

Recommended Conferences

Relevant Topics

Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version