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PubMed1978

[Pharmacological and toxicological studies of novoolean].

A toxicologic study and some pharmacologic investigations were carried out with the novobiocin salt of oleandomycin, formulated as novoolean. The LD50 of the of the preparation for i/m application to mice proved equal to 1500, and to rats--1800 mg per kg of body weight. For oral introduction the average lethal dose for mice amounts to 3250 mg/kg. At such route of application on deaths were observed in rats after the administration of 5 000 mg/kg. A 30-day treatment via i/m application to rats of 180 mg/kg (which is equal to one tenth part of LD50) did not lead to changes in the growth, blood picture, and a number of clinical and biochemical indices of the blood and urine; there were no changes in the development and the structure of the viscera as well as the reproductive capacity of the test animals. Electron-microscope studies with rats treated in the same period with 360 mg/kg (one fifth of the LD50 value) revealed certain injuries of the liver kidneys. With cats the venous infusion of the preparation at rates of up to 15 mg/kg showed no changes in the blood pressure and the rhythm and pulse rate, and the addition of novoolean to the nutrient solution in concentrations of up to 100 mg/cu. cm did not influence the tonus and the motor function of isolated (after Magnus) sectioned portions of the small intestine of rabbits and guinea pigs.

Animals↗
PubMed1980

Sensitivity to macrolide antibiotics and lincomycin in Francisella tularensis holarctica.

Among the 345 F. tularensis holarctica strains isolated in Europe, Asia and North America, two variants were found: one sensitive and the other resistant to erythromycin, oleandomycin and lincomycin. These characteristics were not associated with virulence, antigenicity, biochemical activity or source of isolation and displayed high stability in passages in laboratory animals or multiple passages in culture media. The two variants are proposed to be designated as biotype (biovar) I, erythromycin sensitive (erys), and biotype (biovar)II, erythromycin resistant (eryR). A predominance of biotype I was observed for western Europe, eastern Siberia and the Far East, as well as North America, whereas biotype II prevailed in central Europe, the European part of USSR, especially the south, and western Siberia. The distribution of biotype II largely coincided with the habitat area of Arvicola terrestris, from which it was isolated with the highest frequency. Within the areas of biotype II prevalence, erythromycin and other macrolide antibiotics, as well as lincomycin should not be used for tularemia therapy.

Animals↗
PubMed1980

[Pharmacokinetics of a new antibiotic preparation, novoolean].

We studied the resorption, the distribution, the duration of retention, as well as the routes of elimination by the organism of the complex antibiotic medicine (novobiocin salt of the oleandomycin). It was proved that after a single muscular injection of doses 20 and 50 mg/kg t the medicine, unlike its constituting components, possesses a retained action and keeps up bacteriostatic concentrations of blood in sheep, rabbits and chickens for a period of 12, respectively 24 hours. No substantial differences were observed between the blood levels created of the different species after the use of equal doses. No resorption was observed (or practically an insignificant one) in the digestive tract of rabbits. After its resorption from the place of its application the 'novoolean' penetrates into all organs studied, tissues and liquids of the organisms of guinea pigs, except for the brain. The longest period of retention is that in the lungs and in the kidneys. It is eliminated by the organism mainly through the urine and the bile secretion, and in the case of the lactating mammals-through the milk. The organism of the treated animals is practically free from 'novoolean' after the fourth day and as to the milk--after the second day of the last intramuscular injection.

Administration, Oral↗
PubMedDate not supplied

Effect of various feed additives on immune response of turkeys vaccinated with live Pasteurella multocida in drinking water.

Various feed additives were included in diets of young turkeys being administered live Pasteurella multocida, Clemson University (CU) strain, in drinking water. Erythromycin, Neomycin, and Oleandomycin reduced immune response the most. Most medications that are not effective against P. multocida can be included in turkey feed during CU vaccination.

Animal Feed↗
PubMed1976

A new semisynthetic macrolide antibiotic 3-O-oleandrosyl-5-O-desosaminylerythronolide A oxime.

A new antibiotic, 3-O-oleandrosyl-5-O-desosaminylerythronolide A oxime (3) was produced from erythronolide A oxime (1) by the oleandomycin-producing culture, Streptomyces antibioticus ATCC 11891. The structure of 3 was determined by degradative studies and confirmed by X-ray analysis. Compound 3 was found to be less active, but more stable to acid, then erythromycin A oxime.

Anti-Bacterial Agents↗
PubMed1994

Application of nuclear magnetic resonance spectrometry to measure the activity of bacterial macrolide esterase.

A new method of measuring the activity of macrolide antibiotic esterase in whole bacteria and in crude enzyme extracts was determined through the application of nuclear magnetic resonance spectrometry. The structure of the enzymatically esterolytic cleavage compound of oleandomycin was clearly shown to be the cyclic hemiacetal between the C-9 keto and the hydroxy group of C-13 in the open macrolide nucleus by physicochemical techniques.

Anti-Bacterial Agents↗
PubMedDate not supplied

[Electrocoagulation treatment of sewage in antibiotic production].

The data on the study of the electrocoagulation treatment of highly concentrated sewage in antibiotic production are presented. Aluminium plates were used as the electrodes. The influence of the anode current density, pH and temperature on the process of the electrocoagulation treatment of the sewage was investigated. The electrocoagulation treatment of the sewage in production of tetracycline, oleandomycin and benzyl-penicillin was shown to be efficient.

Aluminum↗
PubMed1976

Inactivation of HL-A antigens in vitro by action of antibiotics.

The effect of antibiotics on lymphocyte HL-A antigens in vitro is of variable character. All antibiotics under examination suppressed the absorption capacity of HL-A antigens after 2 hr of lymphocyte treatment at 37 degrees C. Ceporin and Kanamytrex inhibited even the cytotoxic reactivity of Hl-A antigens after 15-30 min of lymphocyte treatment. Chloramphenicol, aureomycin, streptomycin and oleandomycin, on the contrary, increased the specific cytotoxic reactivity of HL-A antigens after 15-30 min, after 1 hr they were ineffective for HL-A antigens, and after two or more hours they produced polyreactivity. Penicillin and erythromycin produced polyreactivity after only 15-30 min. The results show that for the follow-up of the drug effect on HL-A antigens the absorption test rather than the cytotoxicity test is of importance. The suppressed absorption capacity of HL-A antigens caused by the action of antibiotics proves their inactivation effect on the lymphocytes. The possibility of an analogous effect of antibiotics on lymphocyte HL-A antigens, even after administration to patients, is discussed.

Anti-Bacterial Agents↗
PubMed1999

Structural elucidation studies of erythromycins by electrospray tandem mass spectrometry II.

Erythromycin A (EryA), sec-butyl erythromycin B (SEryB), oleandomycin (Olean) and a synthetic derivative, roxithromycin (Rox), were used to investigate the fragmentation of polyketide macrolide antibiotics by collision induced dissociation (CID) tandem mass spectrometry (MS/MS). Analyses were performed with two commercially available mass spectrometers: a Q-TOF hybrid quadrupole time-of-flight instrument and a BioApex II (4.7 Tesla) Fourier transform ion cyclotron resonance (FTICR) instrument both equipped with electrospray ionisation (ESI) sources. One of the first fragmentation processes is the loss of an H(2)O molecule from the [M+H](+) ion. EryA has three hydroxyl groups on the polyketide ring and loses three H(2)O molecules during CID. This study indicates that these facts are not necessarily related. Deuterium exchange experiments were carried out in order to isotopically label free hydroxyl groups. (18)O-exchange experiments were also carried out in order to label the carbonyl group at the 9-position. In EryA and its analogue the first H(2)O loss shifts in mass from loss of 18 Da to loss of 20 Da in deuterated solvents. For both molecules the loss also shifts in mass from loss of 18 Da to loss of 20 Da during the (18)O-exchange experiments. This suggests that the first loss of H(2)O is from the 9-position carbonyl group, indicating that this, and not the nitrogen of the amino sugar, is the site of protonation of the activated MH(+) ions. For Rox the initial loss of H(2)O is replaced by loss of the 9-position oxime group, the rest of the fragmentation sequence being the same as for EryA. For Olean, there is no H(2)O loss from the parent ion. The results have allowed the proposal of a mechanism for the first loss of H(2)O in the EryA MS/MS fragmentation.

Anti-Bacterial Agents↗
PubMed2006

High-throughput screening for multi-class veterinary drug residues in animal muscle using liquid chromatography/tandem mass spectrometry with on-line solid-phase extraction.

A rapid qualitative method using on-line column-switching liquid chromatography/tandem mass spectrometry (LC/MS/MS) was developed and validated for screening 13 target veterinary drugs: four macrolides - erythromycin A, josamycin (leucomycin A3), kitasamycin (leucomycin A5), and tylosin A; six (fluoro)quinolones - ciprofloxacin, danofloxacin, enrofloxacin, flumequine, oxolinic acid, and sarafloxacin; and lincomycin, virginiamycin M1, and trimethoprim in different animal muscles. Clindamycin, norfloxacin, nalidixic acid, oleandomycin, ormetoprim, and roxithromycin were used as the internal standards. After simple deproteination and analyte extraction of muscle samples using acetonitrile, the supernatant was subjected to on-line cleanup and direct analysis by LC/MS/MS. On-line cleanup with an extraction cartridge packed with hydrophilic-hydrophobic polymer sorbent followed by fast LC using a short C18 column resulted in a total analysis cycle of 6 min for 19 drugs. This screening method considerably reduced the time and the cost for the quantitative and confirmatory analyses. The application of a control point approach was also introduced and explained.

Animals↗
PubMed2001

An experimental comparison of electrospray ion-trap and matrix-assisted laser desorption/ionization post-source decay mass spectra for the characterization of small drug molecules.

An experimental comparison of product ion spectra produced by matrix-assisted laser desorption/ionization (MALDI) and electrospray ion-trap MS( n) for a group of small drug molecules is presented in this paper. The goal of the study was to demonstrate the usefulness of MALDI-MS with post-source decay (PSD) and collision-induced dissociation (CID) for the structural analysis of small drug molecules in the drug discovery process, where traditionally electrospray LC/MS methods are used. PSD and PSD/CID gave diverse product ions that were highly indicative of the structure of the drugs investigated (a group of 4-quinolone antibiotics and oleandomycin). In addition, the number of different product ions generated with MALDI-MS was always higher than with electrospray ion-trap MS( n) (with n < or =4) for the drug molecules studied. This investigation also showed that the choice of a suitable MALDI matrix for the analysis of low molecular weight compounds is quite important. It was found that of the three matrices examined, alpha-cyano-4-hydroxycinnamic acid (alpha-CHCA) produced the most intense fragmentation levels while TiO2, with its advantage of virtually no low mass background signals, did not generate quite the same amount of information.

Indicators and Reagents↗
PubMed1986

Drug interactions with macrolide antibiotics: specificity of pseudo-suicide inhibition and induction of cytochrome P-450.

Macrolide antibiotics like Erythromycin and Tri-acetyl oleandomycin (TAO) are metabolized to nitrosoderivatives which cause inactivation of Cytochrome P-450 by forming stable complex with the Iron of the hemoporphyrin. Several derivatives of erythromycin having lost their cladinose moiety are stronger inducer of liver cytochrome P-450 itself. The major form of cytochrome P-450 induced by all these macrolides in rat liver electrophoretically and immunologically indistinguishable from the major form induced by pregnenolone 16 alpha carbonitrile (PCN). This form is particularly able to metabolize macrolide and to lead to the corresponding 456 nm absorbing cytochrome P-450 complexes in vivo and in vitro.

Animals↗
PubMed1995

Erythromycin inhibits the assembly of the large ribosomal subunit in growing Escherichia coli cells.

Erythromycin and other macrolide antibiotics have been examined for their effects on ribosome assembly in growing Escherichia coli cells. Formation of the 50S ribosomal subunit was specifically inhibited by erythromycin and azithromycin. Other related compounds tested, including oleandomycin, clarithromycin, spiramycin, and virginiamycin M1, did not influence assembly. Erythromycin did not promote the breakdown of ribosomes formed in the absence of the drug. Two erythromycin-resistant mutants with alterations in ribosomal proteins L4 and L22 were also examined for an effect on assembly. Subunit assembly was affected in the mutant containing the L22 alteration only at erythromycin concentrations fourfold greater than those needed to stop assembly in wild-type cells. Ribosomal subunit assembly was only marginally affected at the highest drug concentration tested in the cells that contained the altered L4 protein. These novel results indicate that erythromycin has two effects on translation, preventing elongation of the polypeptide chain and also inhibiting the formation of the large ribosomal subunit.

Anti-Bacterial Agents↗
PubMed1984

Effects of antibiotics on adhesion of enterotoxigenic Escherichia coli strains.

Subinhibitory concentrations of 28 antibiotics were tested for their effects on MRHA patterns of four enterotoxigenic Escherichia coli strains possessing colonization factor antigens CFA/I, CFA/II or CFA/III. Only penicillin G, oleandomycin, doxycycline and minocycline inhibited the haemagglutination pattern of three Escherichia coli strains with CFA/I and CFA/II when added to the medium culture at concentrations ranging from 1/2 to 1/50 of the MIC. At the same concentrations they also decreased the adhesion index of the four strains to human intestinal cells. However, neither the specific agglutination of bacterial cells with CFA antisera nor the production of CFAs was affected.

Adhesiveness↗
PubMed1996

An ABC transporter is essential for resistance to the antitumor agent mithramycin in the producer Streptomyces argillaceus.

Mithramycin is an antitumor antibiotic synthesized by Streptomyces argillaceus. This producer strain is highly resistant in vivo to mithramycin (MIC 100 micrograms/ml) but sensitive to the related drugs chromomycin and olivomycin (MIC 10 micrograms/ml). From a genomic library of S. argillaceus DNA two cosmid clones were isolated which confer a high level of resistance to mithramycin on S. albus. The resistance genes were mapped by subcloning to a 3.9-kb PstI-PvuII fragment. DNA sequence analysis of this fragment revealed one incomplete and three complete open reading frames. Subcloning experiments demonstrated that resistance to mithramycin is mediated by the genes mtrA and mtrB. The mtrA gene can potentially encode an ATP-binding protein of the ABC transporter superfamily, containing one nucleotide-binding domain and showing similarity with other ABC transporters involved in resistance to daunorubicin, oleandomycin and tetronasin in their respective producer strains. The mtrB gene codes for an integral membrane protein with six putative transmembrane helices. A mithramycin-sensitive mutant was generated in a gene replacement experiment by disrupting the mtrA gene, thus demonstrating that the system encoded by the mtrAB genes is essential for conferring resistance to mithramycin in S. argillaceus.

ATP-Binding Cassette Transporters↗
PubMedDate not supplied

A further interaction study of quinine with clinically important drugs by human liver microsomes: determinations of inhibition constant (Ki) and type of inhibition.

Our previous study showed that several drugs inhibited quinine 3-hydroxylation, a cytochrome P450 (CYP) 3A4-mediated reaction, in vitro. In this extended study, 13 drugs were selected and tested by human liver microsomes in order to further determine their respective inhibition constant (Ki) and type of inhibition. According to the apparent Ki values, the inhibitory rank order of these tested drugs was as follows: ketoconazole > doxycycline > omeprazole > tetracycline > troleandomycin (with pre-incubation) > primaquine > troleandomycin (without pre-incubation) > nifedipine > erythromycin > verapamil > oleandomycin > diltiazem > cimetidine > hydralazine. Among these drugs, doxycycline, tetracycline, ketoconazole, nifedipine and hydralazine were judged as mixed inhibitors; whereas, the remaining other drugs tested were judged as competitive inhibitors. When the plasma/serum concentrations possibly attained after their usual therapeutic doses were taken into account, tetracycline, doxycycline, omeprazole, ketoconazole, nifedipine, troleandomycin and erythromycin are likely to be inhibitors of quinine metabolism in patients when these drugs are co-administrated with quinine.

Calcium Channel Blockers↗
PubMedDate not supplied

Rapidly distinguishing reversible and irreversible CYP450 inhibitors by using fluorometric kinetic analyses.

In this study we have evaluated the reliability of a fluorescence-based method used for rapid identification of irreversible CYP inhibitors (mechanism-based inhibitors). This was accomplished by comparing the time-dependence pattern of IC50 values from fluorometric kinetic measurements. For irreversible CYP inhibitors, IC50 values decreased as incubation proceeded. This was due to progressive inactivation of corresponding enzymes by reactive metabolites generated during the incubation. This change pattern was confirmed using a number of known irreversible CYP inhibitors, including furafylline, midazolam, erythromycin, clarithromycin, oleandomycin, 17alpha-ethynylestradiol and verapamil. The pattern was different in reversible inhibition, depending upon the compounds tested in the fluorometric kinetic assay. For some compounds, such as clotrimazole, IC50 values remained relatively stable, whereas other compounds, such as miconazole, terfenadine and ketoconazole showed a significant increase with incubation time. Monitoring tested compounds by LC-MS/MS during the incubation confirmed that increases of IC50 were probably caused by the loss of inhibitors, resulting from either metabolic degradation, or non-specific binding to microsomal proteins.

Chromatography, Liquid↗
PubMed2003

Determination of antibiotics such as macrolides, ionophores and tiamulin in liquid manure by HPLC-MS/MS.

A method for the analysis of several macrolide and ionophore antibiotics as well as tiamulin in liquid manure was developed. Reversed-phase liquid chromatography and atmospheric pressure chemical ionisation (APCI) tandem mass spectrometry was used for detection.High-performance liquid chromatographic (HPLC) separation of the antibiotics was achieved in 35 min. The analytes were extracted with ethyl acetate and the extracts were cleaned up by solid-phase extraction on a diol SPE cartridge. Recovery experiments with spiked liquid manure concentrations varying from 6 to 2,000 microg kg(-1) gave constant recovery rates. The recovery rates for the macrolides erythromycin, roxithromycin and oleandomycin were 75-94%, that for the ionophore salinomycin was 119%, while that for the pleuromutilin tiamulin was 123%, when using a macrolide internal standard. The relative standard deviation was found to be 15-36% and the limits of detection were 0.4-11.0 micro g kg(-1). The maximum concentrations found in manure samples were 43 micro g kg(-1) for tiamulin and 11 micro g kg(-1) for salinomycin.

Animals↗