γ-Glutamyltransferase (γ-GT) is an essential biological enzyme for bacteria proliferation and infection, which is regarded as a virulence factor of pathogenic bacteria. On the basis of hydrolysis function of γ-GT, an enzyme-activated NIR fluorescent probe (DDAG) was designed and developed for sensing γ-GT activity. Herein, the endogenous bacterial γ-GT was detected in real time, and further various bacteria were imaged in vitro. Furthermore, a high-throughput screening system based on DDAG was established for effectively screening γ-GT potent inhibitors from natural compounds and herbal medicines library. Finally, baicalein, myricetin and amaronol A from herbal medicines were solidly confirmed as the novel inhibitors of bacterial γ-GT for the first time.

γ -Glutamyltransferase（γ -GT）是用于细菌的增殖和感染，这被认为是致病性细菌的毒力因子的重要生物酶。基于γ - GT的水解功能，设计并开发了一种酶激活的NIR荧光探针（DDAG），用于检测γ - GT的活性。在此，实时检测内源细菌γ- GT，并在体外对各种细菌成像。此外，建立了基于DDAG的高通量筛选系统以有效地筛选γ-GT来自天然化合物和草药库的有效抑制剂。最后，首次从草药中确定了黄ical素，杨梅素和Amaronol A作为细菌γ- GT的新型抑制剂。