The antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug resistance that is caused by overexpression of genes encoding drug efflux proteins. The mechanism of antifungal action of HONV dipeptides involved uptake by the oligopeptide transport system, subsequent intracellular cleavage by cytosolic peptidases, and inhibition of homoserine dehydrogenase by the released HONV. The relative transport rates determined the anticandidal activity of HONV dipeptides.
Authors
- dr inż. Andrzej Stanisław Skwarecki link open in new tab ,
- mgr inż. Marta Schielmann link open in new tab ,
- Dorota Martynow link open in new tab ,
- mgr Marcin Kawczyński link open in new tab ,
- mgr Aleksandra Wiśniewska link open in new tab ,
- prof. dr hab. inż. Maria Jolanta Milewska link open in new tab ,
- prof. dr hab. inż. Sławomir Milewski link open in new tab
Additional information
- DOI
- Digital Object Identifier link open in new tab 10.1002/psc.3060
- Category
- Publikacja w czasopiśmie
- Type
- artykuł w czasopiśmie wyróżnionym w JCR
- Language
- angielski
- Publication year
- 2018