title: Natural Compounds as Inhibitors of Tyrosyl-tRNA Synthetase.
abstract: Tyrosyl-tRNA synthetases (TyrRSs) as essential enzymes for all living organisms are good candidates for therapeutic target in the prevention and therapy of microbial infection. We examined the effect of various polyphenols, alkaloids, and terpenes-secondary metabolites produced by higher plants showing many beneficial properties for the human organism, on bacterial aminoacylation reaction. The most potent inhibitors of Escherichia coli TyrRS are epigallocatechin gallate, acacetin, kaempferide, and chrysin, whereas the enzymes from Staphylococcus aureus and Pseudomonas aeruginosa are inhibited mainly by acacetin and chrysin. Most of them act as competitive inhibitors. Structure-activity relationship showed that the most potent flavonoid inhibitors contain hydroxyl group at position 5 and 7 of A ring and OCH3group at position 4' of B ring.
authors.affiliation: 1 Institute of Bioorganic Chemistry , Polish Academy of Sciences, Noskowskiego, Poznan, Poland .
authors.forename: Mirosława
authors.initials: M
authors.lastname: Skupińska
authors.affiliation: 2 BioInfoBank Institute , Św. Marcin, Poznan, Poland .
authors.forename: Piotr
authors.initials: P
authors.lastname: Stępniak
authors.affiliation: 3 Center of Microbiology and Infectious Diseases, National Institute of Public Health , Chelmska, Warsaw, Poland .
authors.forename: Iwona
authors.initials: I
authors.lastname: Łętowska
authors.affiliation: 2 BioInfoBank Institute , Św. Marcin, Poznan, Poland .
authors.forename: Leszek
authors.initials: L
authors.lastname: Rychlewski
authors.affiliation: 1 Institute of Bioorganic Chemistry , Polish Academy of Sciences, Noskowskiego, Poznan, Poland .
authors.forename: Mirosława
authors.initials: M
authors.lastname: Barciszewska
authors.affiliation: 1 Institute of Bioorganic Chemistry , Polish Academy of Sciences, Noskowskiego, Poznan, Poland .
authors.forename: Jan
authors.initials: J
authors.lastname: Barciszewski
authors.affiliation: 1 Institute of Bioorganic Chemistry , Polish Academy of Sciences, Noskowskiego, Poznan, Poland .
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Giel-Pietraszuk
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001688:Biological Products / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects / Q000378:metabolism; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000378:metabolism; D013211:Staphylococcus aureus / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D014448:Tyrosine-tRNA Ligase / Q000037:antagonists & inhibitors*
chemical_list: D000900:Anti-Bacterial Agents; D001688:Biological Products; D014448:Tyrosine-tRNA Ligase
keywords: aminoacyl-tRNA synthetase; flavonoids; inhibitor