A New Broad-Spectrum Aminoglycoside Antibiotic Complex, Sporaricin

Deushi, Takeo; Iwasaki, Akio; Kamiya, Kazuhiro; Kunieda, Takafumi; Mizoguchi, Toshimi; Nakayama, Masahito; Itoh, Hisakatsu; Mori, Toshihito; Oda, Takeshi

doi:10.7164/antibiotics.32.173

Cited by 30 publications

(5 citation statements)

References 19 publications

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“…Its increased activity against P. aeruginosa compared with that of fortimicin A also seems superior to those recently described for sannamycin A, sporaricin A, and istamycin B (3,4,11). A49759 was very active against the Enterobacteriaceae, other pseudomonads, acinetobacters, and the staphylococci.…”

Section: Discussionmentioning

confidence: 73%

“…Only the AAC(3)-I enzyme (3-N-acetylation) routinely inactivates this series of drugs, as well as gentamicin, netilmicin, and sisomicin. Only amikacin and tobramycin among the currently available aminoglycosides were active against these isolates in vitro (3,5,12). Conversely, the AAC(6') enzymes (6'-N-acetylation) will not inactivate A49759 or fortimicin A, but they confer resistance against most other aminoglycosides, including amikacin and netilmicin.…”

Section: Discussionmentioning

confidence: 99%

“…The pseudodisaccharide aminocycitols are generally resistant to most bacteria-mediated (3,4,11,(13)(14)(15). Only the AAC(3)-I enzyme (3-N-acetylation) routinely inactivates this series of drugs, as well as gentamicin, netilmicin, and sisomicin.…”

Section: Discussionmentioning

confidence: 99%

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Compound A49759, the 3-O-demethyl derivative of fortimicin A: in vitro comparison with six other aminoglycoside antibiotics

Jones¹,

Thornsberry²,

Barry³

et al. 1980

Antimicrob Agents Chemother

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O-Demethylfortimicin A (compound A49759) was tested against 445 bacteria, and the results were compared with thooe obtained with fortimicin A, amikacin, gentamicin, netilmicin, sisomicin, and tobramycin. A49759 was found to be active and bactericidal against the Enterobacteriaceae, nonfermentative gram-negative bacilli, and Staphylococcus aureus. A49759 was two-to fourfold more active than fortimicin A against most species tested, but generally fourfold less active than amikacin against this population of Pseudomonas aeruginosa (85% inhibited at -16 ug of amikacin per ml and 85% inhibited at c64 ,ug of A49759 per ml). Only amikacin and A49759 were resistant to most aminoglycoside-inactivating enzymes and also had significant antipseudomonal activity. Amikacin was inactivated by aminoglycoside 6'-acetyltransferase, and A49759 was inactivated by aminoglycoside 3-acetyltransferase. The minimal inhibitory concentrations of all tested aminoglycosides were increased by augmenting the inoculum size. Several recent reports have described the in vitro antimicrobial activity of the pseudodisaccharide aminoglycoside antibiotics (4-8, 10, 11, 13, 14). Among these new compounds, the fortimicin group has been most extensively tested against recent clinical isolates (7). Numerous chemical and natural modifications of fortimicin have been presented (6,8,10,14,15). Fortimicin aminoglycosides are generally resistant to inactivating enzymes (6, 10, 13), but lack significant inhibitory activity against pseudomonads (6, 7). In recently presented abstracts no ototoxicity and very low renal toxicity for fortimicin A in the animal models were described (C. L

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Section: Discussionmentioning

confidence: 73%

Section: Discussionmentioning

confidence: 99%

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Compound A49759, the 3-O-demethyl derivative of fortimicin A: in vitro comparison with six other aminoglycoside antibiotics

Jones¹,

Thornsberry²,

Barry³

et al. 1980

Antimicrob Agents Chemother

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“…Sporaricin A, an aminoglycoside containing a unique aminocyclitol and epi-purpurosamine B, is active against a broad spectrum of gram-positive and gram-negative bacteria, including Providencia species and Serratia marcescens (1,6). Because of its refractoriness to most aminoglycosideinactivating enzymes, 3-acetyltransferase I excepted, sporaricin A is active against many aminoglycoside-resistant strains.…”

mentioning

confidence: 99%

In vitro and in vivo antibacterial activities of K-4619, a new semisynthetic aminoglycoside

Saino¹,

Hattori²,

Koshi³

et al. 1984

Antimicrob Agents Chemother

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The antibacterial activities of K-4619 (3-de-O-methylsporaricin A sulfate) were compared with those of sporaricin A, amikacin, dibekacin, and gentamicin. K-4619 exhibited a high order of activity against gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa. Its activity against Providencia species and Serratia marcescens was the highest of all drugs tested. K-4619 was highly effective against bacteria that produce various aminoglycoside-inactivating enzymes, except for 3-acetyltransferase I. The bactericidal activity of K-4619 was somewhat greater than that of amikacin. The activity of K-4619 against gram-negative bacteria increased at alkaline pH and was hardly affected by inoculum size, addition of horse serum, and composition of the medium. The in vivo protective effect of K-4619 against infections with Klebsiella pneumoniae, S. marcescens, and P. aeruginosa in mice was greater than that of sporaricin A. K-4619 was also active in mice infected with gentamicin- or amikacin-resistant strains bearing some of the aminoglycoside-inactivating enzymes.

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“…2 ) In recent sdudies, some new families such as fortimicins 3 ) or sporaricins 4 ) containing novel type of aminocyclitols have been found by Nara et al 5 ) or Deushi et al, 6) respectively. In the immediately preceding paper,!)…”

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confidence: 99%