Biological activity of (5R,6S,8R)-6-alpha-hydroxyethyl-2-acetoxymethyl-2-penem-3-carboxylate.
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Biomedical subjects
Publications and source records attributed to C Della Bruna.
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The biological properties of spiro-piperidyl-rifamycins, a new class of rifamycin antibiotics, are described. In these derivatives the positions 3 and 4 have been incorporated into an imidazolyl ring bearing a spiro-piperidyl group N substituted with linear and branched aliphatic chains. The in vitro antibacterial activity against Staphylococcus aureus and Mycobacterium tuberculosis increases with the number of the carbon atoms in the linera side chain, whereas the inhibitory effect on Escherichia coli is lowered. The antibacterial activity is only marginally affected by branching of the side chain. In vivo (experimental infections of mice) the optimal therapeutic activity against M. tuberculosis is shown by compounds bearing 3 approximately 5 carbon atoms as a linear or branched side chain; in comparison with rifampicin, the potency of these derivatives is 2 approximately 3 times higher. The finding is in a good agreement with the exceptional tissue tropism, which seems to be a favourable property of this group of derivatives.
The immune responsiveness of mice infected with 90 cercariae of Schistosoma mansoni has been investigated. Post-infection kinetics of antibody responses, delayed hypersensitivity and mitogen responsiveness show that there are profound disturbances of these immunological parameters starting 2 weeks after the infection. Although the final outcome is immunodepression the S. mansoni infection can produce immunostimulation. We have observed differences in the kinetics of the depression of humoral antibody responses in two strains of mice. It seems that the worms and not the eggs are of major importance in determining the observed alterations of immune responsiveness.
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A new type of hydrolyzable ester of penicillin G, benzamidomethyl benzylpenicillinate (FI 7303), was studied for the antibacterial activity and kinetics of absorption in comparison with DBED-penicillin G. FI 7303 resulted to be a good repository form of penicillin G, slowly eliminated in mouse, dog and man. It exerted a remarkable therapeutic activity in mice infected with Staphylococcus aureus even when administered 26 h before infection. The protective effect in mice was more prolonged than that of DBED-penicillin G, in agreement with the longer persistence of significant blood levels.
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The authors describe a simple method for collection and culture of chicken peritoneal macrophages. The macrophages are collected from peritoneum with polystirol disks on the surface of which they are subsequently cultured in vitro.
Axenomycins are a new group of macrolide antibiotics isolated from the fermentation broth of Streptomyces lisandri n.sp. They exhibit anthelmintic activity against tapeworms (Cestoda). Three different fractions, A, B, and D, have been obtained, the most active fraction being axenomycin D. The activities of the axenomycin complex and axenomycin D against Hymenolepis nana in mice, Taenia pisiformis, Dipylidium caninum, and Diphyllobothrium sp. in dogs, and Moniezia expansa, M. benedeni, and Avitellina centripunctata in lambs were studied in experimentally and naturally infected animals. Axenomycins were effective and well tolerated by the oral route. Worm reduction rates after a single oral dose were 90 to 100% with 5 to 10 mg of axenomycin D/kg and 50 to 100% with 20 mg of axenomycin complex/kg.
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