Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Tetracyclines”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 37 records · Page 2Linked to original sources
PubMed1992

Tissue concentration and localization of tetracycline following site-specific tetracycline fiber therapy.

The primary objective of this study was to evaluate the concentration and location of tetracycline hydrochloride in tissue adjacent to periodontal pockets treated with a tetracycline impregnated fiber. A secondary objective was to determine if the presurgical placement of fibers had any adverse effects on healing following periodontal surgery. The study population consisted of 10 patients with at least 2 pockets in both maxillary quadrants of > or = 5 mm in depth and exhibiting bleeding on probing. After an initial scaling and root planing, placebo or tetracycline fibers were randomly assigned by quadrant to 2 non-adjacent pockets. Fibers were removed at the time of surgery; i.e., day 8, and periodontal surgery was performed utilizing a flap incision that allowed biopsy of 1 interdental papilla from each of the 2 test sites in each quadrant. One biopsy was analyzed for tetracycline concentrations by high performance liquid chromatography (HPLC). The second biopsy was examined by both light and ultraviolet fluorescence microscopy to determine the location of residual tetracycline and the intensity of inflammatory cell infiltrates. Results showed that the tissue concentration of the antibiotic in tetracycline treated sites was 64.4 +/- 7.01 ng/mg (ng of tetracycline/mg tissue weight) which corresponds to 43 micrograms of tetracycline and was below levels of accurate measurement in placebo treated sites. Tetracycline tissue concentrations corresponded to the ultraviolet fluorescence microscopy with a Pearson correlation coefficient of r = 0.92. Tetracycline fluorescence was noted in the soft tissue wall ranging from 1 to 20 microns.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2001

Synthesis and analysis of ethylated tetracycline, an antibiotic derivative that inhibits the growth of tetracycline-resistant XL1-Blue bacteria.

Bacterial resistance to antibiotics is a significant problem in medical care facilities, causing increased fatalities due to infection. The present study demonstrates that antibiotic structures can be selectively altered in a manner that revives their ability to inhibit bacterial growth. The antibiotic tetracycline was ethylated at the position of the phenolic hydroxy group with the use of diazoethane, forming an ethyl ether functional group. This derivative was dissolved in Luria-Bertani (LB) agar medium, then placed in tissue culture for screening against a tetracycline-resistant bacterial strain. The growth of this bacterial strain, designated XL1-Blue, was inhibited by the ethylated form of tetracycline. The procedure for synthesizing ethylated tetracycline utilizes diazoethane and is presented with the molecular structures and IR spectra. The ethylated form of tetracycline was stable at -20 degrees C for many weeks, and was soluble in LB agar plate medium. Ethylated tetracycline induced growth inhibition of XL1-Blue bacteria within the first 24 h of incubation. The level of bacterial growth inhibition was greater than 30%. Calculation of the partition coefficient, log P, was accomplished and indicates that ethylated tetracycline has an increased lipophilic tendency relative to unmodified tetracycline, and therefore has greater solubility in lipid bilayers.

Acetates↗
PubMed1982

Tetracycline resistance determinants from groups A to D vary in their ability to confer decreased accumulation of tetracycline derivatives by Escherichia coli.

The ability of four genetically distinct plasmid-located tetracycline resistance determinants (TetA, B, C and D) to confer decreased accumulation of tetracycline and some of its analogues by Escherichia coli K12 was examined. Accumulation of oxytetracycline, tetracycline, demethylchlorotetracycline, 6-demethyl-6-deoxy-5-hydroxy-6-methylene-tetracycline, chlorotetracycline, doxycycline and 6-demethyl-6-deoxytetracycline was examined by fluorescence spectroscopy. The determinants varied in their ability to promote decreased accumulation of tetracyclines, defined as an R+/R- fluorescence ratio of less than 0.85. Plasmid pIP7 (TetA) caused reduced accumulation of only oxytetracycline, tetracycline and chlorotetracycline, but plasmid pDU301 (TetB) promoted reduced accumulation of all the compounds tested except 6-demethyl-6-deoxytetracycline. The TetC determinant of pBR322 caused decreased uptake of five derivatives, but not doxycycline or 6-demethyl-6-deoxytetracycline. Plasmid RA1 (TetD) encoded reduced accumulation of oxytetracycline, tetracycline, 6-demethyl-6-deoxy-5-hydroxy-6-methylenetetracycline and chlorotetracycline. In general, the resistance determinants were more efficient in promoting decreased accumulation of hydrophilic tetracyclines. These accumulation studies provide a satisfactory method for the phenotypic identification of Tet resistance determinants.

Drug Resistance, Microbial↗
PubMed2004

Effect of tetracycline on transfer and establishment of the tetracycline-inducible conjugative transposon Tn916 in the guts of gnotobiotic rats.

We have investigated the transfer of Tn916 among strains of Enterococcus faecalis OG1 colonizing in the intestines of gnotobiotic rats. This animal model allows a low limit of detection and efficient colonization of the chosen bacteria. The animals continuously received tetracycline in drinking water. A tetracycline-sensitive recipient strain was allowed to colonize the animals before the resistant donor was introduced. The numbers of donors, recipients, and transconjugants in fecal samples and intestinal segments were estimated. The bioavailable amounts of tetracycline in fecal samples and intestinal segments were monitored by using bacterial biosensors carrying a transcriptional fusion of a tetracycline-regulated promoter and a lacZ reporter gene. Chromosomal locations of Tn916 in transconjugants isolated either from the same animal or from different animals were compared by Southern blot analysis. Our results indicated that selection for the resistant phenotype was the major factor causing higher numbers of transconjugants in the presence of tetracycline. Tetracycline-sensitive E. faecalis cells colonized the intestine even when the concentrations of tetracycline in feces and intestinal luminal contents exceeded growth-inhibitory concentrations. This suggests the existence of tetracycline-depleted microhabitats in the intestinal environment.

Animals↗
PubMed1982

[Comparative analysis of tetracycline, doxycycline and minocycline on chromosomal and plasmid tetracycline-resistant and -sensitive strains of Staphylococcus aureus using MIC, microcalorimetric effect and ultrastructural alterations].

A staphylococcus aureus strain of a patient with plasmidical tetracyclinresistance has first been cured from the plasmid and after that selected in nutritive broth by increasing the concentrations of tetracyclin. By this way we found three variants of the same strain: a tetracyclin-sensitive and two tetracyclin-resistant: an R-plasmid-mediated and the other as a result of mutation. These three variants have been tested against tetracyclin, minocyclin and doxycyclin on an agarmedium. Under influence of these three substances a microcalorimetrical investigation of the strains has taken place. We then tested the strains with the electronic microscope for alterations in the ultra-structure by the three substances. Following results have been obtained: 1. The sensitive strains were inhibited in the same extent by all of the three substances. Plasmidical resistant strains were only resistant against tetracyclin but not against minocyclin and even less against doxycyclin. 2. The microcalorimetrical tests confirmed the conclusions from the cultural test. 3. Alterations in ultra-structure were only found under tetracyclin-influence by strains in division. Comparing the three tetracyclines we did not find any significant difference in quality. 4. With all of the three investigation-methods we proved that R-plasmid-mediated tetracyclin-resistance of staphylococci is not effective for minocyclin and even less for doxycyclin.

Calorimetry↗
PubMed1994

[A new look at the mechanism of action of antibiotics of the tetracycline series. Tetracyclines as components of radical-generating systems].

Tetracyclines were shown to be able to form radical-generating systems and to affect biological structures at the account of the radical form generation. The radical-generating systems were found to be based on the phenomenon revealed in this study that the tetracyclines catalyzed oxidation of ferrous oxide by oxygen after its binding by these compounds. In the presence of ascorbate the radical formation with the involvement of oxygen could be continuous and accompanied by reduction of ferrous oxide by ascorbate in complex with tetracyclines and its subsequent oxidation as well induced by them. Ca2+ and Mg2+ forming complexes with tetracyclines had no impact on the radical formation. In complex with tetracyclines the ions did not interfere with the tetracycline ability to catalyze oxidation of ferrous oxide after its binding by these compounds. A notion of two functional centres characteristic of tetracyclines was formulated. One of them (chelating) provided the tetracycline binding to Mg2+ and Ca2+ e.g. in ribosomes and the other (toxic) affected the surrounding biological structures by the radical formation.

Ascorbic Acid↗
PubMed2025

C10-Benzoate Esters of Anhydrotetracycline Inhibit Tetracycline Destructases and Recover Tetracycline Antibacterial Activity.

Tetracyclines (TCs) are an important class of antibiotics threatened by enzymatic inactivation. These tetracycline-inactivating enzymes, also known as tetracycline destructases (TDases), are a subfamily of class A flavin monooxygenases (FMOs) that catalyze hydroxyl group transfer and oxygen insertion (Baeyer-Villiger type) reactions on TC substrate scaffolds. Semisynthetic modification of TCs (e.g., tigecycline, omadacycline, eravacycline, and sarecycline) has proven effective in evading certain resistance mechanisms, such as ribosomal protection and efflux, but does not protect against TDase-mediated resistance. Here, we report the design, synthesis, and evaluation of a new series of 22 semisynthetic TDase inhibitors that explore D-ring substitution of anhydrotetracycline (aTC) including 14 C10-benzoate ester and eight C9-benzamides. Overall, the C10-benzoate esters displayed enhanced bioactivity and water solubility compared to the corresponding C9-benzamides featuring the same heterocyclic aryl side chains. The C10-benzoate ester derivatives of aTC were prepared in a high-yield one-step synthesis without the need for protecting groups. The C10-esters are water-soluble, stable toward hydrolysis, and display dose-dependent rescue of tetracycline antibiotic activity in E. coli expressing two types of tetracycline destructases, represented by TetX7 (Type 1) and Tet50 (Type 2). The best inhibitors recovered tetracycline antibiotic activity at concentrations as low as 2 &#x3bc;M, producing synergistic scores <0.5 in the fractional inhibitory concentration index (FICI) against TDase-expressing strains of E. coli and clinical P. aeruginosa. The C10-benzoate ester derivatives of aTC reported here are promising new leads for the development of tetracycline drug combination therapies to overcome TDase-mediated antibiotic resistance.

Anti-Bacterial Agents↗
PubMed1973

Uptake of minocycline and tetracycline by tetracycline-susceptible and -resistant bacteria.

Minocycline (7-dimethylamino-6-demethyl-6-deoxytetracycline) is a new semisynthetic tetracycline with potent activity against tetracycline-susceptible bacterial pathogens and unique activity against tetracycline-resistant staphylococci. Studies to determine the basis for this unique activity showed that, whereas tetracycline-resistant staphylococci took up less (3)H-tetracycline than the susceptible cells, both the tetracycline-resistant and -susceptible cells accumulated equivalent amounts of (14)C-minocycline. In contrast, tetracycline-resistant Escherichia coli cells were relatively resistant to minocycline and accumulated less of both drugs than did the susceptible organisms. It is proposed that minocycline is effective against tetracycline-resistant staphylococci because of its ability to penetrate the cells sufficiently to reach inhibiting concentrations at sensitive reaction sites.

Drug Resistance, Microbial↗
PubMed1982

Tetracycline-inducible transfer of tetracycline resistance in Bacteroides fragilis in the absence of detectable plasmid DNA.

Tetracycline resistance of three Bacteroides fragilis strains was shown to be inducible by subinhibitory concentrations of tetracycline. Tetracycline resistance markers could be transferred to another B. fragilis strain by filter mating. The transferability was inducible by subinhibitory concentrations of tetracycline and did not take place in the absence of tetracycline. The optimum concentration of tetracycline for induction of transfer was about 2 microgram/ml. The transfer was shown to be a conjugation-like process requiring cell-to-cell contact between donor and recipient. Screening of parental donor strains for the presence of plasmid DNA did not demonstrate any detectable plasmids in two of the strains. A 3.0-megadalton plasmid, designated pBY5, was present in the third donor strain. Mobilization of pBY5 by another plasmid (pBF4) showed that pBY5 did not carry the genes responsible for tetracycline resistance. It appears that the genes responsible for resistance to tetracycline as well as those responsible for conjugal transfer may be carried on the chromosome in all three donor strains.

Bacteroides fragilis↗
PubMed1982

Reversed-phase ion-pair chromatography of tetracycline, tetracycline analogs, and their potential impurities.

Methods are presented for the separation of tetracycline, tetracycline analogs, and their potential impurities by reversed-phase ion-pair chromatography. The mobile phase consisted of a phosphate buffer with tripropylamine or N,N-dimethyloctylamine as counterions and acetonitrile as the organic modifier. The chromatographic properties of the tetracyclines were significantly improved by addition of the tertiary amines. The best result was obtained with N,N-dimethyloctylamine as the counterion, which gave good separation efficiency and peak symmetry for most of the substances studies. Addition of the tertiary amines to the mobile phase also significantly affected the capacity factors of the tetracyclines. Stability studies of the tetracyclines showed a fast degradation of chlortetracycline to isochlortetracycline and of lymecycline to tetracycline in phosphate buffer solutions of different pH. The purity of pharmaceutical preparations of tetracyclines was also investigated.U

Acetonitriles↗