Apramycin is a unique aminoglycoside with a dissociation of antibacterial activity and ototoxicity. We assessed the antibacterial efficacy of apramycin in two murine models of infection, Mycobacterium tuberculosis aerosol infection and Staphylococcus aureus septicemia. In both infection models, the efficacy of apramycin was comparable to that of amikacin. These results suggest that apramycin ha...

Targeted delivery of anticancer therapeutics can potentially overcome the limitations associated with current chemotherapeutic regimens. Folate receptors are overexpressed in several cancers, including ovarian, triple-negative breast and bladder cancers, making them attractive for targeted delivery of nucleic acid therapeutics to these tumors. This work describes the synthesis, characterization...

The effect of gentamicin against 130 clinical isolates of Pseudomonas aeruginosa was compared with that of two investigational aminoglycoside antibiotics, tobramycin and amikacin. Minimal inhibitory concentration data indicated that, on a weight basis, tobramycin was two to four times as active as gentamicin against most isolates. However, 14 of 18 organisms highly resistant to gentamicin (>/=8...

Previous studies have reported that modification of histones alters aminoglycoside-induced hair cell death and hearing loss. In this study, we investigated three FDA-approved histone deacetylase (HDAC) inhibitors (vorinostat/SAHA, belinostat, and panobinostat) as protectants against aminoglycoside-induced ototoxicity in murine cochlear explants and in vivo in both guinea pigs and CBA/J mice. In...

Aminoglycosides are potent antibiotics deployed worldwide despite their known side-effect of sensorineural hearing loss. The main etiology of this sensory deficit is death of inner ear sensory hair cells selectively triggered by aminoglycosides. For decades, research has sought to unravel the molecular events mediating sensory cell demise, emphasizing the roles of reactive oxygen species and th...

A novel aminoglycoside antibiotic, boholmycin, was produced by Streptomyces hygroscopicus H617-25 isolated from a soil sample collected in Bohol Island, the Philippines. It has a pseudotetrasaccharide structure composed of a heptose, two aminosugars and dicarbamoyl-scyllo-inositol. Intrinsic antibacterial activity of boholmycin is weak but it exhibits broad spectrum activity against Gram-positi...

Clinical isolates of Providencia and Proteus with relative aminoglycoside resistance were tested for susceptibility to combinations of gentamicin or tobramycin with cephalothin or cefazolin. The minimal bactericidal concentration of aminoglycoside for one-third of the strains was reduced by fourfold or more in the presence of one-fourth of the minimal bactericidal concentration of either cephal...

Sir: As reported previously,1-5) aminoglycoside 6'-N-acetyltransferases [AAC(6')] in R factorcarrying Escherichia coli and Pseudomonas aeruginosa are involved in the mechanism of resistance to several aminoglycoside antibiotics such as kanamycin, kanamycin B, 3',4'dideoxykanamycin B (DKB) and ribostamycin. Gentamicin C1a and sisomicin are acetylated by these enzymes6,7). In this paper, we repor...

Introduction: Enterococci represent the third most common cause of infective endocarditis, after streptococcus and Staphylococcus aureus, and are responsible for 5–20% of all cases of endocarditis. We present a rare case of native valve Enterococcus faecalis (E. faecalis) endocarditis of mitral valve in a breast cancer patient. Case Report: A 56­year­old breast cancer patient presented with com...

The emergence of multidrug-resistant and extensively drug-resistant (XDR) tuberculosis (TB) is a serious global threat. Aminoglycoside antibiotics are used as a last resort to treat XDR-TB. Resistance to the aminoglycoside kanamycin is a hallmark of XDR-TB. Here, we reveal the function and structure of the mycobacterial protein Eis responsible for resistance to kanamycin in a significant fracti...