title: Comparative evaluation of two structurally related flavonoids, isoliquiritigenin and liquiritigenin, for their oral infection therapeutic potential.
abstract: Isoliquiritigenin (1) and liquiritigenin (2) are structurally related flavonoids found in a variety of plants. The purpose of this study was to perform a comparative analysis of biological properties of these compounds in regard to their therapeutic potential for oral infections. Compound 1 demonstrated significant antibacterial activity against three major periodontopathogens, Porphyromonas gingivalis, Fusobacterium nucleatum, and Prevotella intermedia. In contrast, 2 exerted less pronounced effects on the above bacterial species. Neither compound was effective against cariogenic bacteria (Streptococcus mutans and Streptococcus sobrinus). Furthermore, 1 exhibited a stronger inhibitory activity than 2 toward P. gingivalis collagenase and human matrix metalloproteinase 9. Finally, the capacity of 1 to attenuate the inflammatory response of macrophages induced by Aggregatibacter actinomycetemcomitans lipopolysaccharide (LPS) was much higher when compared to 2. The activation of transcriptional factors nuclear factor-κB (NF-κB) p65 and activator protein-1 (AP-1) associated with the LPS-induced inflammatory response in macrophages was inhibited strongly by 1, but less affected by 2.
authors.affiliation: Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, 2420 Rue de la Terrasse, Québec City, QC, Canada, G1V 0A6.
authors.forename: Mark
authors.initials: M
authors.lastname: Feldman
authors.forename: Juliana
authors.initials: J
authors.lastname: Santos
authors.forename: Daniel
authors.initials: D
authors.lastname: Grenier
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D047188:Chalcones; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D044950:Flavanones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D016967:Fusobacterium nucleatum / Q000187:drug effects; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D016328:NF-kappa B / Q000187:drug effects; D019906:Nuclear Magnetic Resonance, Biomolecular; D016966:Porphyromonas gingivalis / Q000187:drug effects; D018808:Transcription Factor AP-1 / Q000187:drug effects; D051996:Transcription Factor RelA
chemical_list: D000900:Anti-Bacterial Agents; D047188:Chalcones; D004365:Drugs, Chinese Herbal; D044950:Flavanones; D008070:Lipopolysaccharides; D061965:Matrix Metalloproteinase Inhibitors; D016328:NF-kappa B; D018808:Transcription Factor AP-1; D051996:Transcription Factor RelA; C040920:isoliquiritigenin; C083152:liquiritigenin