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Abstract

The chemo-enzymatic production of new glycosylated aminoglycoside (AG) derivatives was carried out. Acid hydrolysis of commercially available 2-deoxystrepatamine-containing AGs, which are already used in the clinics, provides pseudo-disaccharides as the substrates for in vitro enzymatic reaction catalyzed by a recombinant KanM2 glycosyltransferase. Five new glycosylated AGs biosynthesized were tested for antibacterial activity, cytotoxicity, and nonsense read-through inducing (NRI) activity by comparison with gentamicin and amikacin. These new AG derivatives appear to be valuable for the treatment of some human genetic disorders based on their lower antibacterial activity, decreased toxicity in human cell lines, as well as enhanced NRI activity compared to the existing antibiotics. This study provides an insight into the development of new improved AGAs using chemo-enzymatic synthetic approach and their therapeutic.