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Therapeutic effect of (Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile (DMMA) against Staphylococcus aureus infection in a murine model.

Abstract
Sortase enzymes belong to a family of transpeptidases found in Gram-positive bacteria. Sortase is responsible for the reaction that anchors surface protein virulence factors to the peptidoglycan cell wall of the bacteria. The compound (Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile (DMMA) has previously been reported as a novel sortase inhibitor in vitro, but the in vivo effects of DMMA have not been studied. Here, we evaluated the in vivo effects of DMMA against infection by wild-type and sortase A- and/or sortase B-deficient Staphylococcus aureus in Balb/c mice. With DMMA treatment, survival rates increased and kidney and joint infection rates decreased (p<0.01) in a dose-dependent manner. The rate of kidney infection was significantly reduced in the mice treated with sortase A knock-out S. aureus (p<0.01). These results indicate that by acting as a potent inhibitor of sortase A and moderate inhibitor of sortase B, DMMA can decrease kidney and joint infection rates and reduce mortality in mice infected with S. aureus. These findings suggest that DMMA is a promising therapeutic compound against Gram-positive bacteria.
AuthorsKi-Bong Oh, Kung-Woo Nam, Hyunjin Ahn, Jongheon Shin, Sanghee Kim, Woongchon Mar
JournalBiochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 396 Issue 2 Pg. 440-4 (May 28 2010) ISSN: 1090-2104 [Electronic] United States
PMID20433810 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright (c) 2010 Elsevier Inc. All rights reserved.
Chemical References
  • 3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Enzyme Inhibitors
  • Stilbenes
  • sortase B
  • Aminoacyltransferases
  • sortase A
  • Cysteine Endopeptidases
  • Acrylonitrile
Topics
  • Acrylonitrile (analogs & derivatives, therapeutic use)
  • Aminoacyltransferases (antagonists & inhibitors, genetics)
  • Animals
  • Anti-Bacterial Agents (therapeutic use)
  • Bacterial Proteins (antagonists & inhibitors, genetics)
  • Cysteine Endopeptidases (genetics)
  • Disease Models, Animal
  • Enzyme Inhibitors (therapeutic use)
  • Female
  • Joints (microbiology)
  • Kidney (microbiology)
  • Mice
  • Mice, Inbred BALB C
  • Staphylococcal Infections (drug therapy)
  • Staphylococcus aureus (enzymology, genetics)
  • Stilbenes (therapeutic use)

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