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Journal of Pharmaceutical and Biomedical Analysis 2016-Aug

Bioanalytical LC/MS study of potential bacterial transglycosylation inhibitors.

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Bart Blanchaert
Ismail Murat Palabiyik
Alper Gökbulut
Ming-Juan Wang
Zhong Dai
Feng Wei
Shuang-Cheng Ma
Erwin Adams
Ann Van Schepdael

Ključne riječi

Sažetak

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.

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