title: Bioanalytical LC/MS study of potential bacterial transglycosylation inhibitors.
abstract: 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.
authors.affiliation: KU Leuven-University of Leuven, Department of Pharmaceutical and Pharmacological Sciences, Pharmaceutical Analysis, B-3000 Leuven, Belgium.
authors.forename: Bart
authors.initials: B
authors.lastname: Blanchaert
authors.affiliation: University of Ankara, Faculty of Pharmacy, Department of Analytical Chemistry, 06100 Tandogan, Ankara, Turkey.
authors.forename: Ismail Murat
authors.initials: IM
authors.lastname: Palabiyik
authors.affiliation: University of Ankara, Faculty of Pharmacy, Department of Pharmacognosy, 06100 Tandogan, Ankara, Turkey.
authors.forename: Alper
authors.initials: A
authors.lastname: Gökbulut
authors.affiliation: Institute for Control of Chinese Traditional Medicine and Ethnic Medicine, National Institutes for Food and Drug Control, Beijing 100050, China.
authors.forename: Ming-Juan
authors.initials: MJ
authors.lastname: Wang
authors.affiliation: Institute for Control of Chinese Traditional Medicine and Ethnic Medicine, National Institutes for Food and Drug Control, Beijing 100050, China.
authors.forename: Zhong
authors.initials: Z
authors.lastname: Dai
authors.affiliation: Institute for Control of Chinese Traditional Medicine and Ethnic Medicine, National Institutes for Food and Drug Control, Beijing 100050, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Wei
authors.affiliation: Institute for Control of Chinese Traditional Medicine and Ethnic Medicine, National Institutes for Food and Drug Control, Beijing 100050, China.
authors.forename: Shuang-Cheng
authors.initials: SC
authors.lastname: Ma
authors.affiliation: KU Leuven-University of Leuven, Department of Pharmaceutical and Pharmacological Sciences, Pharmaceutical Analysis, B-3000 Leuven, Belgium.
authors.forename: Erwin
authors.initials: E
authors.lastname: Adams
authors.affiliation: KU Leuven-University of Leuven, Department of Pharmaceutical and Pharmacological Sciences, Pharmaceutical Analysis, B-3000 Leuven, Belgium. Electronic address: Ann.vanschepdael@pharm.kuleuven.be.
authors.forename: Ann
authors.initials: A
authors.lastname: Van Schepdael
mesh_terms: D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000494:pharmacology*; D028241:Camellia sinensis / Q000737:chemistry; D002392:Catechin / Q000031:analogs & derivatives / Q000494:pharmacology; D002853:Chromatography, Liquid / Q000379:methods; D055808:Drug Discovery / Q000295:instrumentation / Q000379:methods*; D013058:Mass Spectrometry / Q000379:methods; D046915:Penicillin-Binding Proteins / Q000037:antagonists & inhibitors*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D027544:Salvia / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D046930:Thymus Plant / Q000737:chemistry; D014315:Triterpenes / Q000494:pharmacology; D014538:Uridine Diphosphate N-Acetylmuramic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D000097245:Ursolic Acid
chemical_list: D000900:Anti-Bacterial Agents; D002392:Catechin; D046915:Penicillin-Binding Proteins; D010936:Plant Extracts; D014315:Triterpenes; D014538:Uridine Diphosphate N-Acetylmuramic Acid; D000097245:Ursolic Acid; C069249:muramyl-NAc-(pentapeptide)pyrophosphoryl-undecaprenol; C045651:epigallocatechin gallate
keywords: Bacterial transglycosylation; LC/MS assay; Lipid II; Natural products; PBP2