细菌糖转移是抗生素药物开发中的一个有趣的目标。开发了一种体外转糖基化测定，并用于寻找金黄色葡萄球菌青霉素结合蛋白2介导的转糖基化的可能抑制剂。由于基板，脂质II，没有紫外线发色团，该测定依赖于与MS偶联的LC来分析孵育混合物。胸腺sipyleus的提取物，丹参，测试了丹参和乌龙茶，以及表没食子儿茶素没食子酸酯和熊果酸，它们是来自植物的化合物。基质效应阻碍了用非常高浓度的提取物处理的样品中的脂质II定量。这些提取物或分离的化合物似乎都没有对青霉素结合蛋白2的转糖基功能具有抑制活性。
Bacterial transglycosylation is an interesting target in antibiotic drug development. An in vitro transglycosylation assay was developed and used to search for possible inhibitors of Staphylococcus aureus Penicillin Binding Protein 2-mediated transglycosylation. Since the substrate, Lipid II, has no UV-chromophore, the assay relies on LC coupled to MS for analysis of the incubation mixtures. Extracts from Thymus sipyleus, Salvia verticillata, Salvia virgata and Oolong tea were tested, as well as epigallocatechin gallate and ursolic acid, which are chemical compounds derived from plants. Matrix effects hampered Lipid II quantification in samples treated with very high concentrations of extracts. None of these extracts or isolated compounds appeared to have inhibitory activities towards the transglycosylation function of Penicillin Binding Protein 2.
