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Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide...
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Upon diagnosis, managing Inflammatory Bowel Disease (IBD) involves addressing several crucial aspects. The primary goals include resting the bowel, correcting malnutrition, and providing symptomatic relief. Resting the bowel may consist of medications to reduce inflammation and promote healing. Correcting malnutrition is essential, often requiring dietary adjustments and nutritional supplements. Symptomatic relief aims to ease pain, diarrhea, and other discomforts in IBD.
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Tumor Necrosis Factor (TNF), a proinflammatory cytokine, contributes significantly to the inflammation seen in Crohn's disease. It exists as soluble TNF and membrane-bound TNF, with actions mediated through TNF receptors (TNFR). TNFR activation leads to the release of proinflammatory cytokines, T-cell activation, collagen production, and leukocyte migration, all contributing to inflammation in Crohn's disease. Anti-TNF monoclonal antibodies, namely infliximab (Remicade), adalimumab...
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Aspirin-Conjugated Cholic Acid Derivative Combats Polymicrobial Infections and Inflammation.

Sayed M Safwan1, Devashish Mehta1, Varsha Saini1

  • 1Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 3rd Milestone, Faridabad-Gurgaon Expressway, NCR Biotech Cluster, Faridabad, Haryana, 121001, India.

Chemmedchem
|September 14, 2025
PubMed
Summary

A novel cholic acid-derived amphiphile effectively combats Gram-positive and Gram-negative bacterial infections and inflammation by disrupting bacterial membranes and degrading biofilms. This promising therapeutic agent shows efficacy in animal models for polymicrobial infections.

Keywords:
biofilmscholic acidinflammationpolymicrobial infections

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Area of Science:

  • Biochemistry
  • Materials Science
  • Infectious Diseases

Background:

  • Antibiotic resistance poses a significant challenge in treating Gram-positive and Gram-negative bacterial wound infections.
  • Conventional antibiotics exhibit limited efficacy against complex polymicrobial infections and associated inflammation.

Purpose of the Study:

  • To design and synthesize a novel aspirin-derived amphiphile based on cholic acid (amphiphile 1).
  • To investigate the therapeutic potential of amphiphile 1 against bacterial infections and inflammation.

Main Methods:

  • Synthesis of a facile amphiphile (amphiphile 1) utilizing cholic acid and aspirin.
  • Evaluation of amphiphile 1's mechanism of action, including bacterial membrane interaction and biofilm degradation.
  • In vivo assessment of hydrogel-based amphiphile 1 delivery in animal models of bacterial infection and inflammation.

Main Results:

  • Amphiphile 1 effectively disrupts bacterial membranes by interacting with lipoteichoic acid and lipopolysaccharide.
  • Amphiphile 1 demonstrates degradation of both monomicrobial and polymicrobial biofilms.
  • Hydrogel-based delivery of amphiphile 1 successfully mitigated bacterial infections and resolved inflammation in animal studies.

Conclusions:

  • Amphiphile 1 exhibits potent antimicrobial and anti-inflammatory properties.
  • The novel amphiphile shows promise as a therapeutic agent for challenging polymicrobial infections.
  • Cholic acid derivatives offer a viable platform for developing new anti-infective strategies.