Bioanalytical LC/MS study of potential bacterial transglycosylation inhibitors

Blanchaert B., PALABIYIK İ. M., GÖKBULUT A., Wang M., Dai Z., Wei F., ...Daha Fazla

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, cilt.127, ss.123-128, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 127
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1016/j.jpba.2015.12.050
  • Dergi Adı: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.123-128
  • Anahtar Kelimeler: Bacterial transglycosylation, LC/MS assay, Lipid II, PBP2, Natural products, THYMUS-SIPYLEUS, LIPID-II, ASSAY, ANTIBACTERIAL, ANTIOXIDANT, EXTRACTS, ACID
  • Ankara Üniversitesi Adresli: Evet

Özet

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. (C) 2016 Elsevier B.V. All rights reserved.