In Vitro and Clinical Effects of Cephaloridine

Gonnella, J. S.; Olexy, Vera M.; Jackson, George Gee

doi:10.1097/00000441-196707000-00009

“…It has been reported that cephalosporins, like penicillins, are inhibitors of cell-wall synthesis (1)(2)(3)(4)(5)16). The accumulation of N-acetylaminosugar in the cells of S. aureus treated with SCE-129 was observed at the concentration of 10 ,ug/ml, which did not affect the synthesis of DNA, RNA, and protein.…”

Section: C Until Usementioning

confidence: 99%

SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities

Tsuchiya

¹

,

Kondo

²

,

Nagatomo

³

1978

Antimicrob Agents Chemother

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SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7,8-(D-a-sulfophenylacetamido)-ceph-3-em-4-carboxylate monosodium salt], a new semisynthetic cephalosporin, shows potent in vitro antibacterial activities against Pseudomonas aeruginosa and some gram-positive bacteria, whereas it shows lower activity against many gram-negative rods. Against clinical isolates of P. aeruginosa this cephalosporin exhibited higher activity than did carbenicillin, and against the strains of Staphylococcus aureus, SCE-129 had similar activity to carbenicillin. Variations in pH, addition of horse serum, and type of growth medium had no significant effects on the activity of the cephalosporin; however, the inoculum size had some effect on the activity. SCE-129 is an effective bactericidal agent against P. aeruginosa and S. aureus. The protective effects of SCE-129 in mice infected with P. aeruginosa and S. aureus were more potent than those of carbenicillin. The protective effects of SCE-129 on Pseudomonas infection in mice varied according to the dosage schedule and the challenge dose. In a multiple dose schedule, a smaller amount of SCE-129 was necessary than that in a single dose schedule. The effects of SCE-129 after subcutaneous or intraperitoneal administration were more potent than were those by intravenous administration. No protective effect was observed by oral administration.

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“…The other cephalosporins tested induced spheroplasts in E. coli and had no effect on protoplasts.THE CEPHALOSPORINS are derivatives of 7-aminocephalosporanic acid, individual members differing in substituents R, and R, a t positions 7 and 3, respectively ( Table 1). Cephalosporins are generally considered to kill bacteria by a mechanism similar to, or identical with, that of the penicillins (Bond, Brimblecombe 6 Codner, 1962; Chang & Weinstein, 1964 a, b ; Gonnella, Olexy & Jackson, 1967;Russell, 1969), i.e. by inhibiting a transpeptidation reaction in cell wall synthesis (Park, 1968).…”

mentioning

confidence: 99%

Studies on the Mode of Action of Some Cephalosporin Derivatives

Fountain

¹

,

Russell

²

1969

Journal of Applied Bacteriology

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7.(s-benzylthioacetamido)-cephem-3-ylmethyl~~~dimeth~ldithiocarbamate~4carboxylic acid (cephalosporin 7/30) prevented benzylpenicillin from inducing spheroplasts in Escherichia coli, and inhibited growth of preformed spheroplasts. These effecrs were also noted with dimethyldithiocarbamate (DMDT), the side-chain at position 3 in 7/30. Cephalosporin 7/30 inhibited growth of protoplasts of Bacillus megaterium and &.repto-COGCUB faeculis. At high concentrations, 7-[(2-thienyl)acetamido]-cephem-3-ylmethyl-Ndimethyldithiocarbamate-4-carboxylic acid (cephalosporin 87/30), with the same sidechain at 7 as cephaloridine but with DMDT at position 3, prevented spheroplast formation in E. coli, and inhibited the growth of preformed spheroplasts. However, a t lower concentrations, 87/30 induced spherical forms in E . coli. The other cephalosporins tested induced spheroplasts in E. coli and had no effect on protoplasts.THE CEPHALOSPORINS are derivatives of 7-aminocephalosporanic acid, individual members differing in substituents R, and R, a t positions 7 and 3, respectively ( Table 1). Cephalosporins are generally considered to kill bacteria by a mechanism similar to, or identical with, that of the penicillins (Bond, Brimblecombe 6 Codner, 1962; Chang & Weinstein, 1964 a, b ; Gonnella, Olexy & Jackson, 1967;Russell, 1969), i.e. by inhibiting a transpeptidation reaction in cell wall synthesis (Park, 1968).However, a cephalosporin known as 7/30 (Table 1) has been found (P. W. Muggleton and C . H. O'Callaghan, pers. comm.) to inhibit, at as low a concentration as 2 pg/ml, the growth of Mycoplasmu pneumoniae and 41. gallisepticum, which suggests that this antibiotic has an effect additional to, or other than, an inhibition of cell wall synthesis. Thus, a comparison of the effects of 7/30 with other cephalosporins and with benzylpenicillin on Escherichia coli and on protoplasts of Bacillus megaterium and Streptococcusfuecalis has been made in an attempt to elucidate (a) its exact mechanism of action and (b) the reasons for the apparent difference in the mechanism of activity between 7/30 and the other cephalosporins. Materials and MethodsOrganisms and mpthods of culture The organisms used were E. coli NCTC 9001, Strep. faecalis ATCC 9790 and B. rnegaterium NCTC 6005. Escherichia coli was grown for 18 h at 37" in 50 ml of Nutrient Broth No. 2 (Oxoid), the culture centrifuged and the pellet washed twice with sterile water and finally resuspended in sterile water to give c. 2 x lo8 viable cells/ml. Streptococcus faecalis was grown for 18 h at 37" on the surface of double strength Brain Heart Infusion Agar (Difco) (BHI), the growth washed off with sterile water, [314

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“…Several cephalosporins showed bacteriolytic action against E. coli. Cephalosporin 7/30 [7-(S-benzylthioacetamido)-cephen-3-ylmethyl-N-dimethyldithiocarbamate-4-carboxylic acid)] inhibited the growth of E. coli, but did not reveal the bacteriolytic action (5). It is also reported that cephalosporin 7/30 inhibited the protein synthesis of E. coli (4).…”

Section: 'mentioning

confidence: 99%

SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities

1978

Antimicrob Agents Chemother

0

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SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7,8-(D-a-sulfophenylacetamido)-ceph-3-em-4-carboxylate monosodium salt], a new semisynthetic cephalosporin, shows potent in vitro antibacterial activities against Pseudomonas aeruginosa and some gram-positive bacteria, whereas it shows lower activity against many gram-negative rods. Against clinical isolates of P. aeruginosa this cephalosporin exhibited higher activity than did carbenicillin, and against the strains of Staphylococcus aureus, SCE-129 had similar activity to carbenicillin. Variations in pH, addition of horse serum, and type of growth medium had no significant effects on the activity of the cephalosporin; however, the inoculum size had some effect on the activity. SCE-129 is an effective bactericidal agent against P. aeruginosa and S. aureus. The protective effects of SCE-129 in mice infected with P. aeruginosa and S. aureus were more potent than those of carbenicillin. The protective effects of SCE-129 on Pseudomonas infection in mice varied according to the dosage schedule and the challenge dose. In a multiple dose schedule, a smaller amount of SCE-129 was necessary than that in a single dose schedule. The effects of SCE-129 after subcutaneous or intraperitoneal administration were more potent than were those by intravenous administration. No protective effect was observed by oral administration.

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In Vitro and Clinical Effects of Cephaloridine

Cited by 13 publications

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SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities

SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities

Studies on the Mode of Action of Some Cephalosporin Derivatives

SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities

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