Skupińska Mirosława, Stępniak Piotr, Łętowska Iwona, Rychlewski Leszek, Barciszewska Mirosława, Barciszewski Jan, Giel-Pietraszuk Małgorzata
1 Institute of Bioorganic Chemistry , Polish Academy of Sciences, Noskowskiego, Poznan, Poland .
2 BioInfoBank Institute , Św. Marcin, Poznan, Poland .
Microb Drug Resist. 2017 Apr;23(3):308-320. doi: 10.1089/mdr.2015.0272. Epub 2016 Aug 3.
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 OCH group at position 4' of B ring.
酪氨酰 - tRNA合成酶（TyrRSs）作为所有生物的必需酶，是预防和治疗微生物感染的治疗靶点的良好候选者。我们研究了高等植物产生的各种多酚、生物碱和萜类等对人体具有多种有益特性的次生代谢物对细菌氨基酰化反应的影响。大肠杆菌TyrRS的最有效抑制剂是表没食子儿茶素没食子酸酯、刺槐素、山柰酚和白杨素，而金黄色葡萄球菌和铜绿假单胞菌的酶主要被刺槐素和白杨素抑制。它们大多作为竞争性抑制剂起作用。构效关系表明，最有效的黄酮类抑制剂在A环的5位和7位含有羟基，在B环的4'位含有甲氧基。
