title: Neuraminidase inhibition of Dietary chlorogenic acids and derivatives - potential antivirals from dietary sources.
abstract: Plants rich in chlorogenic acids (CGAs), caffeic acids and their derivatives have been found to exert antiviral effects against influenza virus neuroaminidase. In this study several dietary naturally occurring chlorogenic acids, phenolic acids and derivatives were screened for their inhibitory activity against neuroaminidases (NAs) from C. perfringens, H5N1 and recombinant H5N1 (N-His)-Tag using a fluorometric assay. There was no significant difference in inhibition between the different NA enzymes. The enzyme inhibition results indicated that chlorogenic acids and selected derivatives, exhibited high activities against NAs. It seems that the catechol group from caffeic acid was important for the activity. Dietary CGA therefore show promise as potential antiviral agents. However, caffeoyl quinic acids show low bioavailibility and are intensly metabolized by the gut micro flora, only low nM concentrations are observed in plasma and urine, therefore a systemic antiviral effect of these compounds is unlikely. Nevertheless, gut floral metabolites with a catechol moiety or structurally related dietary phenolics with a catechol moiety might serve as interesting compounds for future investigations.
authors.affiliation: Department of Life Sciences and Chemistry, Jacobs University Bremen, 28759 Bremen, Germany. n.kuhnert@jacobs-university.de.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Gamaleldin Elsadig Karar
authors.affiliation: Department of Life Sciences and Chemistry, Jacobs University Bremen, 28759 Bremen, Germany. n.kuhnert@jacobs-university.de.
authors.forename: Marius-Febi
authors.initials: MF
authors.lastname: Matei
authors.affiliation: Department of Life Sciences and Chemistry, Jacobs University Bremen, 28759 Bremen, Germany. n.kuhnert@jacobs-university.de.
authors.forename: Rakesh
authors.initials: R
authors.lastname: Jaiswal
authors.affiliation: Department of Life Sciences and Chemistry, Jacobs University Bremen, 28759 Bremen, Germany. n.kuhnert@jacobs-university.de.
authors.forename: Susanne
authors.initials: S
authors.lastname: Illenberger
authors.affiliation: Department of Life Sciences and Chemistry, Jacobs University Bremen, 28759 Bremen, Germany. n.kuhnert@jacobs-university.de.
authors.forename: Nikolai
authors.initials: N
authors.lastname: Kuhnert
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry* / Q000302:isolation & purification; D019659:Asteraceae / Q000737:chemistry*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D002726:Chlorogenic Acid / Q000494:pharmacology*; D003016:Clostridium perfringens / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D053124:Influenza A Virus, H5N1 Subtype / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry* / Q000302:isolation & purification; D014764:Viral Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism
chemical_list: D000998:Antiviral Agents; D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D014764:Viral Proteins; D002726:Chlorogenic Acid; D009439:Neuraminidase