Neuraminidase inhibition of Dietary chlorogenic acids and derivatives potential antivirals from dietary sources

• Published in: Food & function 2016-04, Vol.7 (4), p.252-259
• Main Authors: Gamaleldin Elsadig Karar, Mohamed, Matei, Marius-Febi, Jaiswal, Rakesh, Illenberger, Susanne, Kuhnert, Nikolai
• Format: Article
• Language: English
• Subjects: Antiviral Agents - chemistry; Antiviral Agents - isolation & purification; Asteraceae - chemistry; Bacterial Proteins - antagonists & inhibitors; Bacterial Proteins - chemistry; Bacterial Proteins - metabolism; Chlorogenic Acid - pharmacology; Clostridium perfringens; Clostridium perfringens - enzymology; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - isolation & purification; Influenza A Virus, H5N1 Subtype - drug effects; Influenza A Virus, H5N1 Subtype - enzymology; Influenza virus; Molecular Structure; Neuraminidase - antagonists & inhibitors; Neuraminidase - chemistry; Neuraminidase - metabolism; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Viral Proteins - antagonists & inhibitors; Viral Proteins - chemistry; Viral Proteins - metabolism
• ISSN: 2042-6496; 2042-650X
• DOI: 10.1039/c5fo01412c

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. Plants rich in chlorogenic acids (CGAs), caffeic acids and their derivatives have been found to exert antiviral effects against influenza virus neuroaminidase.