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 19 recordsLinked 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↗
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↗
PubMed1975

Effectiveness of achievable urinary concentrations of tetracyclines against "tetracycline-resistant" pathogenic bacteria.

Hospitalized patients with urinary tract infections caused by Pseudomonas aeruginosa or other bacterial pathogens are frequently treated with parenteral antibiotics such as gentamicin. Many of these organisms are shown by Kirby-Bauer disk sensitivity testing to be resistant to tetracycline. One hundred seventy-one such tetracycline-resistant bacterial isolates were studied; 84% were found to be sensitive to achievable urinary concentrations of tetracycline. Two patients with long-standing chronic urinary tract infection with Pseudomonas were treated with tetracycline for a year and a half with excellent results. In a pilot clinical trial, eight of 12 hospitalized patients with urinary tract infection were treated successfully with tetracycline without regard to disk sensitivity data. Institution of tetracycline as soon as the microscopic diagnosis of urinary tract infection is made might be an acceptable empiric approach to the treatment of urinary infection in hospitalized patients who do not show evidence of sepsis.

Bacteriuria↗
PubMed1977

Penetration of ocular compartments by tetracyclines. I. An experimental study with tetracycline.

Total antibiotic concentration of tetracycline hydrochloride was determined in the ocular structures of rabbits by radioactive tracer method. Concentration of tetracycline of 0.1 to 5 microgram/g, adequate to inhibit the growth of bacteria of high or medium susceptibility, was measured from all ocular structures with the exception of the lens. Tetracycline concentration in the aqueous humor was inferior to that in the vascularized ocular tissues and to that in the cornea. Vitreous body tetracycline level, about 0.3 microgram/g, was about half of the concentration in the aqueous humor. The disruption of the blood-aqueous barrier following paracentesis led to an immediate increase of tetracycline concentration in the anterior structures of the eye.

Animals↗
PubMed1976

Topical use of tetracycline in the treatment of acne: a double-blind study comparing topical and oral tetracycline therapy and placebo.

A group of 75 subjects with moderate or severe acne was divided by random selection into three treatment groups. One group was treated with a topically applied placebo liquid and with 500 mg of orally administered tetracycline hydrochloride daily; one group received orally administered lactose capsules and topically applied placebo liquid each day; and one group was treated with orally administered lactose capsules and with a topical preparation containing tetracycline hydrochloride and n-decylmethyl sulfoxide, an agent intended to enhance antibiotic penetration. At the conclusion of the 13-week study and at several points during the study, the conditions of the subjects receiving topically or orally administered tetracycline hydrochloride were significantly (P less than .05) more improved than the conditions of the subjects receiving lactose capsules and the topically applied placebo liquid. However, there was no significant difference between the effects of topically and orally administered tetracycline hydrochloride.

Acne Vulgaris↗
PubMed1979

Differential pulse polarography of tetracycline: determination of complexing tendencies of tetracycline analogs in the presence of cations.

The complexation tendencies, stoichiometries, and stability constants for tetracycline, minocycline, and demeclocycline with the metallic ions calcium(II), magnesium (II), zinc(II), aluminum(III), iron(II), and iron (III) were evaluated using a polarographic technique. Changes in pulse peak heights for each tetracycline deravative were measured as a function of cation concentration. The method provides an in vitro method of evaluating the selectivity of particular metal ions for different tetracycline analogs.

Aluminum↗
PubMed1976

R factor-mediated tetracycline resistance in Escherichia coli K12. Dominance of some tetracycline sensitive mutants and relief of dominance by deletion.

Strains of Escherichia coli K12 heterozygous for the R100-1 tetracycline resistance region were constructed. They carried the wild-type Tetr genes in the chromosome and single site Tets mutations on plasmids. Some heterozygotes could not express tetracycline resistance fully after induction. The mutant tet allele was thus partially dominant. When heterozygotes carrying the dominant tet mutant were plated on agar containing 20 mg/ml tetracycline, mutants which grew normally occurred at a frequency of 1-4 X 10(-4). Analysis of these dominance relief mutants showed that in 53/56 isolates the dominant tet allele was lost forming either Tra+ or Tra- deletion mutants of the plasmid. The mutation frequency was not affected either by the host chromosomal recA mutation or by the temperature of growth of the culture.

Chromosome Deletion↗
PubMed1977

[Comparative study of the physicochemical properties of the surface of Escherichia, their sensitivity to ampicillin and tetracycline and their capacity to absorb tetracycline].

Development of resistance to ampicillin and tetracycline in Escherichia resulted in an increase in the electrokinetic potential and a decrease in the level of hydration and isoelectric values of pH. The changes in the hydration level mainly depended on the accompanying dissociation. Studies on 3H-tetracycline binding revealed a low accumulation capacity of the resistant mutants. The rate of 3H-tetracycline binding did not depend on the changes in the physico-chemical parameters of the cell surface due to resistance and dissociation.

Absorption↗
PubMed1977

[Effect of tetracycline base crystallization on the conditions properties of the powders and drug forms obtained. The development of directed crystallization procedures for tetracycline base].

The study of the process of tetracycline base crystallization showed that with an increase in the rate of pH, temperature and mixed rotation changes, the specific surface of the crystalline precipitate increased with a simultaneous decrease in the bulk weight, looseness and volume density of the powder. The residual content of tetracycline in the mother solution decreased. The level of the effect of various parameters on the final results was different.

Chemistry, Pharmaceutical↗
PubMed1979

Distribution of pyrrolidinomethyl-tetracycline (rolitetracycline) and tetracycline in blood and various organs of mice measured by high pressure liquid chromatography.

By means of a newly developed high-pressure liquid chromatographic method the organ distribution of tetracycline (TC) and pyrrolidinomethyl-tetracycline (PMT) has been studied. When mice were treated with 50 mg/kg i.v. TC or PMT these antibiotics could be detected in all organs investigated (liver, kidney, heart, lung, muscle, spleen). Especially high concentrations were found in liver and kidneys, where TC and PMT could be detected up to 6 h. In animals treated with PMT part of the PMT applied decomposed slowly yielding TC, which was found together with PMT in blood and all organs.

Animals↗
PubMed1977

New compounds: organoboron derivatives of tetracyclines I: synthesis of carboxamido derivative of tetracycline with perhydro-2-phenyl-1,3,6,2-dioxazaborocine.

An organoboron carboxamido derivative of tetracycline, designed for use in the 105B-thermal neutron-capture treatment of cancer, was synthesized under the conditions of the Mannich reaction using perhydro-2-phenyl-1,3,6,2-dioxazaborocine as the amine component. Spectral data (UV, IR, and NMR) for the compound and its hydrolytic stability are discussed.

Boron Compounds↗
PubMed1975

Plasmid-determined tetracycline resistance in Streptococcus faecalis: evidence for gene amplification during growth in presence of tetracycline.

The tetracycline (TG)-resistant Streptococcus faecalis strain DS-5Cl harbors two plasmids designated alpha and gamma with molecular masses of approximately 6 and 35 million daltons, respectively. TC-sensitive variants were derived by storing cells at 45 degrees for 2-3 weeks. Analysis of covalently closed circular DNA from five such variants (derived independently) revealed that in each variant the alpha-plasmid, which normally sediments at 28 S (supercoiled) in a sucrose density gradient, was replaced by a 22S substance. Growth of DS-5Cl in the presence of 150 mug/ml of TC (minimum inhibitory concentration is 250 mug/ml in liquid broth) for a prolonged period of time (50-60 generations) resulted in the disappearance of 28S DNA and the appearance of a heterogeneous covalently-closed circular DNA sedimenting at about 40-48 S. This phenomenon was accompanied by an increase in the level of bacterial TC-resistance, whereby tells were subsequently grown in the absence of TC for 70-80 generations, the heterogeneous DNA disappeared and a typical 28S alpha-plasmid reappeared. The cells also became less resistant to TC, i.e., the minimum inhibitory concentration returned to 250 mug/ml. These data suggest that bacterial growth in the presence of TC results in a reversible gene amplification with respect to a TC-resistant determinant residing on the alpha-plasmid.

Cell Division↗
PubMed1992

A Bacteroides tetracycline resistance gene represents a new class of ribosome protection tetracycline resistance.

The ribosome protection type of tetracycline resistance (Tcr) has been found in a variety of bacterial species, but the only two classes described previously, Tet(M) and Tet(O), shared a high degree of amino acid sequence identity (greater than 75%). Thus, it appeared that this type of resistance emerged recently in evolution and spread among different species of bacteria by horizontal transmission. We obtained the DNA sequence of a Tcr gene from Bacteroides, a genus of gram-negative, obligately anaerobic bacteria that is phylogenetically distant from the diverse species in which tet(M) and tet(O) have been found. The Bacteroides Tcr gene defines a new class of ribosome protection resistance genes, Tet(Q), and has a deduced amino acid sequence that was only 40% identical to Tet(M) or Tet(O). Like tet(M) and tet(O), tet(Q) appears to have spread by horizontal transmission, but only within the Bacteroides group.

Amino Acid Sequence↗
PubMed1992

Mechanism of tetracycline-hydrochloride-induced pleurodesis. Tetracycline-hydrochloride-stimulated mesothelial cells produce a growth-factor-like activity for fibroblasts.

Intrapleural instillation of tetracycline hydrochloride (TCN) is an effective means of achieving pleural fibrosis. However, its mechanism of action remains unknown. To evaluate the hypothesis that TCN stimulates pleural mesothelial cells to release growth-factor-like activity for fibroblasts we performed the following experiments. Rat visceral pleural mesothelial cells were incubated with TCN at doses ranging from 0.01 microgram/ml to 100 mg/ml. The conditioned media (CM) were collected after incubation for 2 to 48 h. CM caused fibroblasts to increase incorporation of thymidine when compared with CM that was unexposed to TCN (p less than 0.05). This growth-factor-like activity continued to be produced by mesothelial cells for 48 h after removal of TCN from the medium. There was a dose-response relationship since increasing doses of TCN to as much as 1 mg/ml caused increasing production of growth-factor-like activity without mesothelial cell injury as measured by trypan blue exclusion. The growth factor activity was a competence-type activity. It coeluted with human PDGF at a molecular weight of 31,000. It was heat-stable (100 degrees C for 10 min) and sensitive to trypsin and papain but not to heat-inactivated trypsin. Addition of cycloheximide or actinomycin D inhibited its production. TCN did not have any direct effect on fibroblasts. Bleomycin CM did not contain growth-factor-like activity for fibroblasts. These data demonstrate that TCN stimulates mesothelial cells to release a growth-factor-like activity for fibroblasts. This phenomenon may play an important role in TCN-induced pleural fibrosis.

Animals↗
PubMed1992

Serum levels of tetracycline during treatment with tetracycline-containing fibers.

Four adult patients with at least 8 teeth that had attachment loss of 5 to 10 mm which bled on probing were included in this study. Polymeric tetracycline (TCN) containing fibers were placed and left in the pockets for a period of 10 days. Plasma samples were collected at baseline, 1 hour, 3 hours, 3 days, and 10 days after fiber placement. The mean length of fiber used averaged 187 cm with a range of 160 to 222 cm. The maximum TCN dose per patient averaged 105 mg with a range of 91 to 126 mg producing no detectable serum level greater than 0.1 micrograms/ml. This level was found in 3 of the 4 subjects at 3 hours after fiber placement and in 1 subject at 3 days after fiber placement. Transient and insignificant levels of TCN became available systemically shortly after the placement of multiple fibers. The dose of TCN in each patient was well tolerated and was not associated with any serious adverse effects.

Adult↗
PubMed1977

[Effect of the crystallization conditions of tetracycline base on the properties of the powders and drug forms obtained. The dependence of the degree of dispersion of tetracycline base on the crystallization conditions].

Characteristics of the powder dispersity of tetracycline base samples prepared by directed crystallization with variation of the process conditions were determined by the sedimentation method. It was found that the speed of the solution agitation had the maximum effect on the level and nature of the dispersity. The rate of the solution temperature and pH changing during the crystallization process had also a significant effect at low agitation speed.

Chemistry, Pharmaceutical↗
PubMed1976

Selective pressure of tetracyclines on the faecal flora. A comparison between tetracycline and doxycycline.

The aerobic faecal flora was studied in two groups of healthy adult persons, each group consisting of 18 individuals, before a course of either doxycycline or tetracycline HCI, at the cessation of therapy and 5 weeks afterwards. The main object of this study was to evaluate the effect of antibacterial treatment on the occurrence of mutagenic resistant and plasmid carried resistant strains in the faecal flora, and in particular development of resistant E. coli. The frequency of resistant strains increased after treatment with both of the drugs without significant differences.

Adult↗