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PubMed1964

ANTIBACTERIAL ACTIVITY OF SOME DERIVATIVES OF 7-AMINOCEPHALOSPORANIC ACID AGAINST STAPHYLOCOCCUS AUREUS AND SYNERGISM BETWEEN THESE AND OTHER ANTIBIOTICS.

The N-phenylacetyl derivative of 7-aminocephalosporanic acid (cephaloram) had roughly the same activity as benzylpenicillin against a number of Gram-positive organisms and about one-eighth of the activity of benzylpenicillin against penicillinsensitive strains of Staphylococcus aureus. This derivative and the N-alpha-phenoxypropionyl derivative of 7-aminocephalosporanic acid were 4 to 8 and 4 to 16 times as active as methicillin against penicillinase- and nonpenicillinase-producing staphylococcal strains, respectively. Neither the presence of horse serum nor changes in inoculum size appreciably affected the activities of any of the derivatives of 7-aminocephalosporanic acid which were tested. After forty-eight subcultures in the presence of antibiotic the increase in minimum inhibitory concentration against the staphylococcus was about four-times as great for cephaloram as for cephalosporin C. The resistant penicillinase-producing strains remained stable after six subcultures in antibiotic-free medium, and all the strains retained coagulase activity. Some degree of cross-resistance was found between the derivatives of 7-aminocephalosporanic acid and those of 6-aminopenicillanic acid. Synergism was observed in vitro between certain derivatives of 7-aminocephalosporanic acid and 6-aminopenicillanic acid when they were tested together or with fusidic acid or cephalosporin P(1) against a weak penicillinase-producing strain of Staphylococcus aureus. Cephalosporin C and cephalosporin C (pyridine), each in combination with benzylpenicillin, showed a significant degree of synergism in protection experiments in mice infected with a strong penicillinase-producing strain of Staphylococcus aureus.

Animals↗
PubMed1984

In vitro antibiotic susceptibility of Legionellaceae: search for alternative antimicrobial drugs.

Reference strains of Legionella pneumophila (serotypes 1-4, and 6), Legionella micdadei , and Legionella bozemanii proved susceptible (agar dilution test, buffered charcoal yeast extract agar) to erythromycin, rifampin, augmentin (amoxycillin plus clavulanic acid), cefotaxime, cefoxitin, enoxacin , fusidic acid, and norfloxacin; cefamandole was less active. The strains varied in susceptibility to fosfomycin.

Anti-Bacterial Agents↗
PubMed2001

Oral Acanthosis nigricans as a marker of internal malignancy. A case report.

BACKGROUND: Acanthosis nigricans (AN) is a rare mucocutaneous condition that can involve the oral tissues. There are 2 clinical forms of AN: benign and malignant. Benign AN is related to systemic diseases such as diabetes and obesity or can be induced by drugs such as systemic corticosteroids, nicotinic acid, estrogens, insulin, and fusidic acid. Malignant AN appears in association with tumors such as lung, ovarian, breast, and gastric carcinoma. METHODS: A rare case of malignant AN that initially manifested in the oral cavity of a 73-year-old patient is reported. RESULTS: A bladder and lung carcinoma were detected following the diagnosis of AN. CONCLUSIONS: The diagnostic importance of oral AN is emphasized because, in our patient, its recognition led to the detection of 2 occult malignant tumors.

Acanthosis Nigricans↗
PubMed1986

Probable chromosomal mutation to resistance to all aminoglycosides in Staphylococcus aureus selected by the therapeutic use of gentamicin: a preliminary report.

A patient suffering from burns was treated with gentamicin: subsequently, a 'methicillin-resistant' strain of Staphylococcus aureus (B27), was isolated which was highly resistant to this antibiotic and all other aminoglycosides. In all other respects this isolate resembled the gentamicin-sensitive 'methicillin-resistant' S. aureus prevalent on the Yorkshire Regional Burns Unit. Subsequently, fusidic acid treatment was substituted for gentamicin therapy, and a fusidic acid-resistant variant was isolated from the same patient. This article reports a preliminary characterization of these isolates.

Adult↗
PubMed1973

Protein initiation in eukaryotes: formation and function of a ternary complex composed of a partially purified ribosomal factor, methionyl transfer RNA, and guanosine triphosphate.

A protein factor contained in a 1 M KCl extract of L-cell ribosomes and partially purified by chromatography on DEAE-cellulose forms a specific ternary complex with rat-liver Met-tRNA(f) and GTP. The complex is measured by its quantitative retention on nitrocellulose membranes. Complex assembly is optimal at 100 mM KCl and 0.2 mM MgCl(2), and is independent of mRNA and of ribosomes. The GTP requirement can be replaced over 65% by its methylene analogue GDPCH(2)P, indicating that GTP hydrolysis is not involved. Complex formation is inhibited by 10 muM aurintricarboxylic acid, but is unaffected by 100 muM pactamycin, 100 muM fusidic acid, or by excess uncharged methionine tRNA(f). The ternary complex is relatively stable and appears at the void volume during filtration on Sephadex G-100. At 1-3 mM MgCl(2) and in the presence of other factors, the ternary complex is implicated in protein initiation by (i) its capacity to bind to the 40S ribosomal subunit to form a 48S complex; and (ii) the subsequent association of the 48S complex with a 60S subunit to form a functional "80S complex."

Adenosine Triphosphate↗
PubMed1975

Effects of taurodihydrofusidate, a bile salt analogue, on bile formation and biliary lipid secretion in the rhesus monkey.

Bile salts play a major role in bile formation and biliary lipid secretion. Sodium taurodihydrofusidate (TDHF), a derivative of the antibiotic fusidic acid, closely resembles bile salts in terms of structure, micellar characteristics, and capacity ot solubilize otherwise insolbule lipids. We have therefore studied the biliary secretion of this bile salt analogue and its influence on bile formation and biliary lipid secretion in primates. Alert, unanesthetized female rhesus monkeys prepared with a total biliary fistula were allowed to reach a steady bile salt secretion rate before each study. In three animals (group I),[14C]TDHF was infused intravenously. Most of the compound was secreted rapidly in bile chemically unchanged. The biliary secretion of this drug produced a twofold increase in bile flow; however, the bile salt output was markedly reduced during the infusion. In spite of this reduction, the phospholipid output remained essentially unchanged whereas the cholesterol output increased almost twofold. In five other animals (group II), the effect of TDHF on the bile salt secretion was further investigated by an intravenous infusion of [14C]taurocholate followed by a combined infusion of [14C]taurocholate and TDHF. When TDHF was added to the infusate, a reduction in the [14C]taurocholate output and a progressive rise in the plasma [14C]taurocholate concentration were observed in each animal. An analysis of the data in both groups indicates that (a) the most likely explanation to account for the decreased bile salt output is that the bile salt analogue, TDHF, interfered with bile salt secretion into the biliary canaliculi; (b) TDHF induces a greater secretion of biliary water than was observed with bile salts, an effect consistent with a stimulation of the bile salt-independent canalicular flow; (c) at similar 3alpha-hydroxysteroid secretion rates TDHF caused a significant increase in cholesterol secretion compared to that induced by bile salt. This finding suggests that TDHF affects cholesterol metabolism or secretion in a way distinct from bile salts. Thus, the solubilization of biliary lipids in mixed micelles, although essential, is only one of the factors which determine their secretion into bile.

Animals↗
PubMed1981

[Folliculitis decalvans].

A 58 year-old-male with folliculitis decalvans, a circumscribed chronic purulent folliculitis with subsequent hair loss and follicular atrophia is described. Staphylococcus aureus haemolyticus could be detected in the lesions. Local and systemic treatment with fusidic acid was effective.

Alopecia↗
PubMed2001

The Neurospora crassa colonial temperature-sensitive 3 (cot-3) gene encodes protein elongation factor 2.

At elevated temperatures, the Neurospora crassa mutant colonial, temperature-sensitive 3 (cot-3) forms compact, highly branched colonies. Growth of the cot-3 strain under these conditions also results in the loss of the lower molecular weight (LMW) isoform of the Ser/Thr protein kinase encoded by the unlinked cot-1 gene, whose function is also involved in hyphal elongation. The unique cot-3 gene has been cloned by complementation and shown to encode translation elongation factor 2 (EF-2). As expected for a gene with a general role in protein synthesis, cot-3 mRNA is abundantly expressed throughout all asexual phases of the N. crassa life cycle. The molecular basis of the cot-3 mutation was determined to be an ATT to AAT transversion, which causes an Ile to Asn substitution at residue 278. Treatment with fusidic acid (a specific inhibitor of EF-2) inhibits hyphal elongation and induces hyperbranching in a manner which mimics the cot-3 phenotype, and also leads to a decrease in the abundance of the LMW isoform of COT1. This supports our conclusion that the mutation in cot-3 which results in abnormal hyphal elongation/branching impairs EF-2 function and confirms that the abundance of a LMW isoform of COT1 kinase is dependent on the function of this general translation factor.

Amino Acid Sequence↗
PubMed1975

Studies on the in vitro synthesis of ppGpp and pppGpp.

The effect of a number of inhibitors of protein synthesis on ppGpp and pppGpp synthesis in vitro has been examined. As expected from in vivo results, chloramphenicol is without effect on this reaction. Aurintricarboxylic acid and chlortetracycline, on the other hand rapidly and specifically inhibit ppGpp synthesis. Fusidic acid in the presence of saturating amounts of EF G also inhibits the reaction completely, suggesting that an empty ribosomal acceptor site is necessary for this reaction. On the other hand, the 50-S subunit proteins L7 and L12 are not required for stringent factor activity. Ribosomes from Pseudomonas fluorescens can replace those from Escherichia coli in the complete system, while ribosomes from Ehrlich ascites cannot. A small but reproducible synthesis of ppGpp is observed when the ribosomal wash from E. coli is complemented with ribosomes from wheat germ cytoplasm.

Animals↗
PubMed2000

Functional expression, purification, and characterization of 3alpha-hydroxysteroid dehydrogenase/carbonyl reductase from Comamonas testosteroni.

3alpha-Hydroxysteroid dehydrogenase (3alpha-HSD) catalyzes the oxidoreduction at carbon 3 of steroid hormones and is postulated to initiate the complete mineralization of the steroid nucleus to CO(2) and H(2)O in Comamonas testosteroni. By this activity, 3alpha-HSD provides the basis for C. testosteroni to grow on steroids as sole carbon and energy source. 3alpha-HSD was cloned and overexpressed in E. coli and purified to homogeneity by an affinity chromatography system as His-tagged protein. The recombinant enzyme was found to be functional as oxidoreductase toward a variety of steroid substrates, including androstanedione, 5alpha-dihydrotestosterone, androsterone, cholic acid, and the steroid antibiotic fusidic acid. The enzyme also catalyzes the carbonyl reduction of nonsteroidal aldehydes and ketones such as metyrapone, p-nitrobenzaldehyde and a novel insecticide (NKI 42255), and, based on this pluripotent substrate specificity, was named 3alpha-hydroxysteroid dehydrogenase/carbonyl reductase (3alpha-HSD/CR). It is suggested that 3alpha-HSD/CR contributes to important defense strategies of C. testosteroni against natural and synthetic toxicants. Antibodies were generated in rabbits against the entire 3alpha-HSD/CR protein, and may now be used for evaluating the pattern of steroid induction in C. testosteroni on the protein level. Upon gel permeation chromatography the purified enzyme elutes as a 49.4 kDa protein revealing for the first time the dimeric nature of 3alpha-HSD/CR of C. testosteroni.

3-Hydroxysteroid Dehydrogenases↗
PubMed1976

The effects of pure and micellar solutions of different bile salts on mucosal morphology in rat jejunum in vivo.

The effects of pure and micellar solutions of different bile salts on mucosal morphology have been investigated in rat jejunum using a closed-loop technique; the effects of an anionic dihydroxy steroid antibiotic, fusidic acid, have also been studied. Mucosal changes were assessed by light-microscopical appearances and quantified by determining surface to volume ratios (c/1h). The unconjugated dihydroxy bile salts, chenodeoxycholate and deoxycholate (DC), produced similar and gross structural changes at concentrations of 2-5 to 5 mM, as judged by mucosal appearances, but not at 1 mM; the unconjugated trihydroxy bile salt cholate and a variety of di- and trihydroxy conjugated salts produced no changes at concentrations of 5 to 20 mM. Fusidate (5 mM) produced similar changes to 5 mM DC. Compared with control values DC (1,2-5 and 5 mM) and fusidate (5 mM) produced highly significant (P less than 0-001) reductions in c/1h ratios. DC-induced damage was completely abolished by mixed micellar solutions, whereas pure micellar solutions provided no protection. These results indicate, (i) a molecular specificity for bile salt-induced mucosal damage, and (ii) that the effects of the unconjugated dihydroxy species on mucosal structure depends not only on their intraluminal concentrations, but also on the relative concentrations of conjugated bile salts and lipids present in the lumen.

Animals↗
PubMed1996

Sensitivity of ribosomes from Agrobacterium tumefaciens to the ribosome-inactivating protein crotin 2 depending on the translocational state.

The GTP analog guanylylmethylene diphosphonate (GppCH2p) strongly inhibited polyuridylic acid-directed polypeptide synthesis in a cell-free translation system prepared from Agrobacterium tumefaciens. Fusidic acid increased even further the inhibitory action. The pre-translocational ribosomal complexes formed with the GppCH2p and the elongation factor G protected the ribosome against the depurinating action of crotin 2 assayed as the acid-dependent release of the RNA fragment whose terminal sequence is 5'-GAGGACCGGGAUGGAC-3'. The results allowed to conclude that the interaction of both crotin 2 and the elongation factor G with the A. tumefaciens ribosomes in the pre-translocational state must take place at overlapping, either sterically or allosterically, ribosomal sites which are equally accessible to the RIP.

Agrobacterium tumefaciens↗
PubMed1977

Characterization of the nucleoside triphosphate phosphohydrolase (ATPase) activity of RNA synthesi termination factor p. I. Enzymatic properties and effects of inhibitors.

The purification of p protein to homogeneity from Escherichia coli has shown that its RNA-dependent ATPase activity is physically inseparable from its termination activity. The biochemical properties of pATPase have been studied using poly(C) as the activating RNA. This reaction is stimulated by Mg2+ ions and Mn2+ ions and is prevented by excess EDTA; it is not stimulated by Ca2+ ions. The reaction is not affected by a Zn2+ ion chelator and is inhibited by 1 mM Zn2+. With Mg2+ present, the activity is essentially constant from pH 7 to pH 9.7. pATPase is sensitive to p-hydroxymercuribenzoate and to N-ethylmaleimide. All four ribonucleoside triphosphates are hydrolyzed by p action. ATP has the lowest Km (0.009 mM), while CTP has the highest Vmax. In a mixture containing all four nucleoside triphosphates at a concentration of 0.4 mM, p shows no strong preference for any one of the substrates. The response of p ATPase to a variety of inhibitors of other ATPases and GTPases and of transcription has been studied. Of the compounds tested, aurintricarboxylic acid, an inhibitor of protein-nucleic acid interactions, was found to be a potent inhibitor of p ATPase, while rifampicin and heparin had no effect. pATPase showed partial sensitivity to thiostrepton, fusidic acid, Dio 9, and sodium azide.

Adenosine Triphosphatases↗
PubMed1991

The outer membrane permeability-increasing action of linear analogues of polymyxin B nonapeptide.

Polymyxin nonapeptides such as polymyxin B nonapeptide (PMBN) are polymyxin-derived deacylated nonapeptides which contain a heptapeptide ring and are known as effective permeabilizers of the outer membrane (OM) of Gram-negative bacteria. In order to assess the role of the cyclic moiety of PMBN in the permeabilization of the OM, the author compared the OM permeabilizing activity of two synthetic linear PMBN analogues with the well-characterized activity of PMBN. While a low concentration (1-3 micrograms/ml) of PMBN was sufficient to sensitize both Escherichia coli and Pseudomonas aeruginosa to hydrophobic probe antibiotics (rifampin, fusidic acid) by a factor of 100, even a high concentration (100 micrograms/ml) of linear arginyl polymyxin B decapeptide sensitized E. coli only by a factor of 3 and did not sensitize P. aeruginosa at all. In identical assays, linear lysyl polymyxin B nonapeptide completely lacked any sensitizing activity. These findings indicate that the cyclic peptide ring is crucial for the OM-permeabilizing activity of polymyxin nonapeptides.

Amino Acid Sequence↗
PubMed2006

Management of infections of osteoarticular prosthesis.

Prosthetic joint infections are an uncommon complication of joint replacement surgery, but are associated with significant morbidity and costs when they do occur. Gram-positive cocci, in particular Staphylococcus aureus and Staphylococcus epidermidis, are the most commonly recovered microorganisms (>or=50% of all isolates). About 60% of prosthetic joint infections probably occur by direct contamination during the operative procedure. Certain systemic conditions in the patients, as well as foreign material, have been identified as risk factors for prosthetic joint infection. The clinical diagnosis is only certain when there are sinus tracts that reach the prosthesis or purulent secretion is obtained from joint aspiration or during open surgery. The treatment of an infected joint prosthesis must be individualised, but it generally involves both systemic antibiotics and surgical intervention. Exchange arthroplasty in one or two stages continues to be the standard approach to management. Prosthesis retention, in conjunction with debridement and prolonged (for at least 3 months) oral antibiotic therapy, can be an alternative for early postoperative or late acute haematogenous infections, when the duration of symptoms is less than 1 month, the implant is stable, and the pathogen is relatively avirulent and sensitive to an orally well absorbed antibiotic. Good results have been achieved under these conditions in staphylococcal infections with rifampin associated with quinolones and other antibiotics, e.g., cotrimoxazole, fusidic acid, and linezolid.

Acetamides↗
PubMed1975

[Postoperative synergistic progressive gangrene].

A case of synergistic postoperative progressive gangrene is presented. After a bibliographic review and a description of the main clinical chacteristics of the condition, the authors emphasize the fact that tests for cell mediated immunity showed slight impairment. Howeves the immediate type sensitivity tests and the leucocyte function were normal. The patient was treated successfully with fusidic acid after other antibiotics had proved ineffective.

Adult↗
PubMed1979

Inhibition of 3H-demethylphalloin uptake in isolated rat hepatocytes under various experimental conditions.

3H-Demethylphalloin (3H-DMP) a cyclopeptide very similar to phalloidin is taken up by isolated hepatocytes in vitro. Hepatocytes prepared from newborn animals are less sensitive to phalloidin. Their uptake of 3H-DMP is about one tenth of that of cells from adult animals. Ascites hepatoma cells, known to be insensitive to phalloidin took up negligible amounts of 3H-DMP. Cells prepared from regenerating livers took up insignificantly lower amounts of the toxin than in hepatocytes from adult animals. Treatment of hepatocytes with low concentrations of trypsin was found to switch off the phalloidin sensitivity in a reversible manner. This inhibition is due to a reduced uptake of 3H-DMP. Pretreatment of animals with CCl4, known to reduce the sensitivity to phalloidin, also decreases the uptake of 3H-DMP in isolated hepatocytes. Various agents, drugs and reagents were found to inhibit the response of isolated hepatocytes to phalloidin. All these compounds (bile acids, rifampicin, silybin, DIDS, glutardialdehyde, bromosulphophthalein, fusidic acid, antamanide, novobiocin) inhibit also the uptake of 3H-DMP in isolated hepatocytes. The results confirm our working hypothesis, presented in several previous papers, that decreased sensitivity to phalloidin is probably due to a reduced or blocked uptake of the toxin.

Alkaloids↗