Labradorins with antibacterial activity produced by Pseudomonas sp.

Sammanfattning

The urgent need for new antibacterial drugs has led to renewed interest in microorganisms, which historically have been the main source of previously discovered antibiotics. The present study describes the discovery of two new antibacterial oxazolylindole type alkaloids, labradorins 5 (1) and 6 (2), which were isolated and characterized from two isolates of Pseudomonas sp., along with four previously known tryptophane derived alkaloids. The structures of 1 and 2 were determined by NMR spectroscopy and MS, and confirmed by synthesis. During bioassay-guided isolation using several human bacterial pathogens, 1 and 2 displayed activity towards Staphylococcus aureus and Acinetobacter baumannii. The minimal inhibitory concentrations (MIC) of compounds 1 and 2 against S. aureus were 12 mu g.mL(-1) and 50 mu g.mL(-1), respectively, whereas the MICs against A. baumannii were > 50 mu g.mL(-1). The CC50 values of compound 1 towards a liver cell line (HEP-G2) and a T-cell line (MT4) were 30 mu g.mL(-1) and 20 mu g.mL(-1), respectively, and for compound 2 were > 100 mu g.mL(-1) and 20 mu g.mL(-1), respectively. Due to the limited potency of compounds 1 and 2, along with their toxicity, the compounds do not warrant further development towards new antibiotics.

Nyckelord

antibiotics; secondary metabolites; labradorin; oxazolylindole; antibiotic resistant bacteria; Pseudomonas; Staphylococcus aureus; Acinetobacter baumannii

Publicerad i

Molecules
2017, volym: 22, nummer: 7, artikelnummer: 1072

SLU författare

• Broberg, Anders

  • Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
    

• Bjerketorp, Joakim

  • Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
    

• Andersson, Pierre

  • Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
    

• Levenfors, Jolanta

  • Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
    

Associerade SLU-program

AMR: Bakterier

Globala målen (SDG)

SDG3 God hälsa och välbefinnande

UKÄ forskningsämne

Mikrobiologi
Läkemedelskemi
Organisk kemi

Publikationens identifierare

• DOI: https://doi.org/10.3390/molecules22071072

Permanent länk till denna sida (URI)

https://res.slu.se/id/publ/83306