Synthesis in vitro of Artemia salina proteins in an homologous cell-free system.
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Biomedical subjects
Publications and source records attributed to M Kondo.
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Maridomycin, a new macrolide antibiotic, and tetrahydromaridomycin were acylated into their mono, di, and tri acyl derivatives. These derivatives were compared with the parent antibiotic, maridomycin, for their (i) in vitro antimicrobial activities, (ii) protective effect in mice infected with Staphylococcus aureus (oral administration), (iii) blood levels attained in rats, and (iv) acute toxicity in mice (intraperitoneal administration). All the derivatives showed either the same or less activity in vitro, but 9-acyl, 9, 2'-diacylmaridomycin and 9, 13, 2'-triacetyltetrahydromaridomycin demonstrated improved therapeutic effects together with higher blood levels and low toxicity. 9-Propionylmaridomycin showed the most favorable biological properties.
9-Propionylmaridomycin shows in vitro antibacterial activity against gram-positive bacteria and has some action on Neisseria gonorrhoeae and Vibrio cholerae, but is generally inactive against many gram-negative rods. This antibiotic exhibits strong activity against clinical isolates of Staphylococcus aureus which are highly resistant to erythromycin or oleandomycin, or both, but which are sensitive to josamycin and kitasamycin. Strains resistant to josamycin and kitasamycin were also found to be resistant to this antibiotic. A significant feature of 9-propionylmaridomycin is a lack in its ability to induce resistance induction in resistance-inducible strains of staphylococci to erythromycin. Several antibacterial features of 9-propionylmaridomycin such as the influence of medium pH, inoculum size, effect of addition of horse serum, development of resistance, cross resistance, and bacteriostatic activity were shown to be almost identical to those of josamycin and kitasamycin. The antibacterial activity of 9-propionylmaridomycin was stable in solutions at pH levels of 4, 7, and 9.
The in vivo protecting activity of 9-propionylmaridomycin, a derivative of the new macrolide antibiotic, maridomycin, was compared with that of other macrolide antibiotics in mice infected with Staphylococcus aureus, Streptococcus pyogenes, and Diplococcus pneumoniae. The protective effect was almost similar to that afforded by several known macrolide antibiotics in mice infected intraperitoneally with certain strains of the gram-positive species described above. The skin lesion caused by intradermal challenge of S. aureus in mice also responded very effectively to treatment with 9-propionylmaridomycin.
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