2. Academic Validation
  3. Synthesis and biological evaluation of diarylheptanoids as potential antioxidant and anti-inflammatory agents

Synthesis and biological evaluation of diarylheptanoids as potential antioxidant and anti-inflammatory agents

  • Eur J Med Chem. 2018 Jan 20:144:289-299. doi: 10.1016/j.ejmech.2017.12.033.
Kelly Maurent 1,  Corinne Vanucci-Bacqué 1,  Michel Baltas 1,  Anne Nègre-Salvayre 2,  Nathalie Augé 2,  Florence Bedos-Belval 3
Affiliations

Affiliations

  • 1 Université Paul Sabatier Toulouse III, UMR 5068, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France; CNRS, UMR 5068, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France.
  • 2 INSERM, UMR1048, I2MC, BP 84225, 31432 Toulouse Cedex 4, France.
  • 3 Université Paul Sabatier Toulouse III, UMR 5068, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France; CNRS, UMR 5068, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France. Electronic address: bedos@chimie.ups-tlse.fr.
PMID: 29275229 DOI: 10.1016/j.ejmech.2017.12.033
Abstract

Reactive Oxygen Species (ROS) are key signaling molecules and their overproduction plays an important role in the inflammation process, the secretion of inflammatory cytokines such as IL-1β and IL-6 and the progression of inflammatory disorders. Decreasing oxidative stress represents a promising challenge in the design of antioxidant and anti-inflammatory agents. In the present study, a series of new diarylheptanoids containing allylic alcohol, amide, hydantoin or triazole fragments were synthesized and fully characterized. We evaluated the ability of these agents to block the production of intracellular ROS and the subsequent inflammatory events exerted by lipopolysaccharide (LPS) on murine macrophage RAW 264.7. Five diarylheptanoids were found to exhibit the dual required properties.

Keywords

Anti-inflammatory activity; Antioxidant; Diarylheptanoid; Macrocycle.

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