title: Flavan-3-ols and proanthocyanidins from Limonium brasiliense inhibit the adhesion of Porphyromonas gingivalis to epithelial host cells by interaction with gingipains.
abstract: Porphyromonas gingivalis is a pathogen strongly involved in chronic and aggressive forms of periodontitis. Natural products, mainly polyphenols, have been described for advanced treatment of periodontitis by inhibition of the bacterial adhesion of P. gingivalis to the epithelial host cells. An acetone:water extract (LBE) from the rhizomes of Limonium brasiliense (Boiss.) Kuntze was tested under in vitro conditions for potential antiadhesive effects against P. gingivalis to human KB cells and for inhibition of the proteolytic activity of gingipains, the main virulence factor of P. gingivalis. LBE≤100μg/mL had no cytotoxicity against the bacteria and did not influence the cell physiology of human epithelial KB cells. At 100μg/mL LBE reduced the adhesion of P. gingivalis to KB cells significantly by about 80%. LBE at 20μg/mL reduced the proteolytic activity of the arginin-specific Rgp gingipain by about 75%. Chemical profiling of LBE indicated the presence of gallic acid, epigallocatechin-3-O-gallate and samarangenins A and B as lead compounds. UHPLC by using MS and UV detection displays a suitable method for quality control of the extract for identification and quantification of the lead compounds.
authors.affiliation: State University of Maringá, Postgraduate Program in Biological Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, BR-87020-900, Maringá, Brazil.
authors.forename: Angelo
authors.initials: A
authors.lastname: de Oliveira Caleare
authors.affiliation: University of Münster, Institute of Pharmaceutical Biology and Phytochemistry, Corrensstraße 48, D-48149 Münster, Germany. Electronic address: ahensel@uni-muenster.de.
authors.forename: Andreas
authors.initials: A
authors.lastname: Hensel
authors.affiliation: State University of Maringá, Postgraduate Program in Pharmaceutical Sciences, Pharmaceutical Biology Laboratory, Palafito, BR-87020-900, Maringá, Brazil.
authors.forename: João Carlos Palazzo
authors.initials: JC
authors.lastname: Mello
authors.affiliation: State University of Maringá, Postgraduate Program in Pharmaceutical Sciences, Pharmaceutical Biology Laboratory, Palafito, BR-87020-900, Maringá, Brazil.
authors.forename: Andressa Blainski
authors.initials: AB
authors.lastname: Pinha
authors.affiliation: State University of Maringá, Postgraduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, BR-87020-900, Maringá, Brazil.
authors.forename: Gean Pier
authors.initials: GP
authors.lastname: Panizzon
authors.affiliation: University of Münster, Institute of Pharmaceutical Biology and Phytochemistry, Corrensstraße 48, D-48149 Münster, Germany.
authors.forename: Matthias
authors.initials: M
authors.lastname: Lechtenberg
authors.affiliation: University of Münster, Institute of Pharmaceutical Biology and Phytochemistry, Corrensstraße 48, D-48149 Münster, Germany.
authors.forename: Frank
authors.initials: F
authors.lastname: Petereit
authors.affiliation: State University of Maringá, Postgraduate Program in Biological Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, BR-87020-900, Maringá, Brazil.
authors.forename: Celso Vataru
authors.initials: CV
authors.lastname: Nakamura
mesh_terms: D018829:Adhesins, Bacterial / Q000737:chemistry; D001422:Bacterial Adhesion / Q000187:drug effects*; D001578:Benzopyrans / Q000737:chemistry / Q000302:isolation & purification; D002392:Catechin / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification; D003546:Cysteine Endopeptidases / Q000737:chemistry; D004847:Epithelial Cells / Q000382:microbiology; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification; D005707:Gallic Acid / Q000737:chemistry / Q000302:isolation & purification; D000080867:Gingipain Cysteine Endopeptidases; D006801:Humans; D007624:KB Cells; D010936:Plant Extracts / Q000737:chemistry; D029606:Plumbaginaceae / Q000737:chemistry*; D016966:Porphyromonas gingivalis / Q000187:drug effects*; D044945:Proanthocyanidins / Q000737:chemistry* / Q000302:isolation & purification; D027343:Rhizome / Q000737:chemistry
chemical_list: D018829:Adhesins, Bacterial; D001578:Benzopyrans; D005419:Flavonoids; D000080867:Gingipain Cysteine Endopeptidases; D010936:Plant Extracts; D044945:Proanthocyanidins; C471026:samarangenin B; C404987:flavan-3-ol; D005707:Gallic Acid; D002392:Catechin; C045651:epigallocatechin gallate; D003546:Cysteine Endopeptidases
keywords: Adhesion; Cysteine proteases; Gingipains; Limonium brasiliense; Periodontitis; Porphyromonas gingivalis