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At least 109 records · Page 6Linked to original sources

Effect of erythromycin and tumour necrosis factor on the drug resistance of multidrug-resistant cells: reversal of drug resistance by erythromycin.

WEHI 164 murine fibrosarcoma cells were rendered multidrug-resistant (MDR) by culture in the presence of actinomycin D. In addition to resistance to actinomycin D, the cells acquired resistance to doxorubicin, mitomycin, vincristine and cycloheximide. The fact that development of resistance to one type of lipophilic chemotherapeutic drug also results in resistance to other structurally unrelated lipophilic drugs suggests that non-toxic lipophilic agents may interfere with drug resistance by saturating the pathway by which MDR-cells inhibit drug cytotoxicity. We show that the antibiotic erythromycin significantly reverses the resistance of MDR WEHI 164 cells to doxorubicin and actinomycin D. In addition to cross-resistance to chemotherapeutic drugs, 3 out of 4 actinomycin D-resistant WEHI 164 cell lines also showed higher resistance to tumour necrosis factor (TNF) than the parental WEHI 164 cells. However, whereas verapamil, a calcium antagonist known to reverse multidrug-resistance, rendered resistant cells more sensitive to chemotherapeutic drugs, it protected the cells from killing by TNF, suggesting that drug resistance and TNF resistance may not be directly connected. A synergistic cytotoxic effect of TNF and actinomycin D was obtained on both the parental and the MDR cells. However, higher concentrations of TNF and actinomycin D were required to obtain a cytotoxic effect in the MDR cells, reflecting actinomycin D and TNF resistance in these cells.

Animals↗

Erythromycin VI: kinetics of acid-catalyzed hydrolysis of erythromycin oxime and erythromycylamine.

Kinetic data were obtained, by qualitative and quantitative analysis, of the hydrolytic degradation of erythromycin oxime and erythromycylamine separated by TLC. The pseudo-first-order rate constants were determined at three temperatures (17,26, and 36 degrees), and the temperature dependency of the reaction was studied. The activation energy for the hydrolysis and methanolysis of the compounds was calculated. The factors contributing to the differences in the reaction rate are discussed.

Amines↗

An erythromycin-resistance gene from an erythromycin-producing strain of Arthrobacter sp.

A gene (ermA) coding for a presumed erythromycin-resistance (ErR) determinant from an Er-producing Arthrobacter sp. strain (NRRLB3381) was isolated from a gene bank in phage vector lambda 2001 by probing with a Streptomyces ErR gene. Strongly hybridizing fragments were subcloned and the appropriate segments sequenced. The ermA gene is 76 mol% G + C in content and specifies a protein of 340 aa with an Mr of 37454. S1 nuclease mapping and primer extension identified the putative promoter, which resembles the consensus sequence of Escherichia coli promoters particularly in the -10 region. A potential ribosome-binding site (RBS) (AGGAG) was also located. Unexpectedly, the majority of in vivo ermA transcripts detected were only 245 nt long, suggesting that expression of ErR may be regulated post-transcriptionally. Substantial homology is observed between the predicted aa sequences of the ermA-coded protein and the products of three other ErR determinants, from organisms that do not produce Er.

Arthrobacter↗

Introduction of a mini-gene encoding a five-amino acid peptide confers erythromycin resistance on Bacillus subtilis and provides temporary erythromycin protection in Proteus mirabilis.

A 15-bp mini-gene was introduced into Bacillus subtilis and into stable protoplast-like L-forms of Proteus mirabilis. This mini-gene encoded the peptide MVLFV and modeled a fragment of Escherichia coli 23S rRNA responsible for E. coli erythromycin (Ery) resistance. Expression of the introduced mini-gene conferred permanent Ery resistance on B. subtilis. In L-forms of P. mirabilis, the Ery-protective effect was maintained in the course of several generations. Herewith, the mechanism of Ery resistance mediated by expression of specific short peptides was shown to exist in evolutionary distant bacteria. Three new plasmids were constructed containing the gene under study transcriptionally fused with the genes encoding glutamylendopeptidase of Bacillus licheniformis or delta-endotoxin of Bacillus thuringiensis. The Ery resistance pentapeptide (E-peptide) mini-gene served as an efficient direct transcriptional reporter and allowed to select bacillar glutamylendopeptidase with improved productivity. The mini-genes encoding E-peptides may be applied as selective markers to transform both Gram-positive and Gram-negative bacteria. The small size of the E-peptide mini-genes makes them attractive selective markers for vector construction.

Amino Acid Sequence↗

[Mechanism of efficacy of erythromycin on diffuse panbronchiolitis--effect of erythromycin on cytokine mRNA expression in human whole blood model].

Recently, "low-dose and long-term" erythromycin (EM) has been reported to be effective in treatment of diffuse panbronchiolitis (DPB), but its mechanism is still obscure. We studied the effect of EM on cytokine mRNA expression by using LPS-stimulated human whole blood as an experimental vivo model. IL-8 mRNA was expressed in biphasic fashion with peak expression at 6 hours and 20 hours from the start of LPS stimulation. When whole blood was pretreated with EM (2 micrograms/ml) for 1 hours. IL-8 mRNA expression was depressed at 20 hours (p < 0.025) from the start of LPS (1 microgram/ml) stimulation. However, when pretreated for 12 hours, it was not depressed. EM (2 micrograms/ml) also depressed IL-1 beta (p < 0.025) and TNF alpha (p < 0.05) mRNA expressions at 6 hours from the start of LPS stimulation. From the above results, it was suggested that the direct inhibition of IL-1 beta and TNF alpha production by EM resulted in subsequent depression of production of IL-8 that is a potent chemotactic factor for neutrophil, and consequently, EM acts to protect the bronchiole tissues of DPB patients from destruction by proteolytic enzymes released from neutrophils. This assumption seems to be supported by our previous observation that when patients with DPB were treated with EM a marked decrease in number of neutrophil in bronchoalveolar lavage fluid (BALF) was accompanied by clinical and radiographic improvement.

Adult↗

A placebo-controlled clinical trial to compare a gel containing a combination of isotretinoin (0.05%) and erythromycin (2%) with gels containing isotretinoin (0.05%) or erythromycin (2%) alone in the topical treatment of acne vulgaris.

PURPOSE: To compare the clinical benefit of isotretinoin (0.05%) and erythromycin (2%) gels alone and in combination (Isotrexintrade mark) in acne patients. PROCEDURE: The study was a randomised placebo-controlled trial in acne patients who should benefit from topical therapy. RESULTS: All treatment groups except placebo produced a time-related reduction in lesion counts, with the combined therapy producing the largest mean decrease. Between-group comparisons showed several significant differences. CONCLUSION: Isotrexin was significantly better than placebo at all time points for inflamed and total lesions, and was better than isotretinoin at week 4. Side-effects were minimal.

Acne Vulgaris↗

Polyacrylic bone cement containing erythromycin and colistin. I. In vitro bacteriological activity and diffusion properties of erythromycin, colistin and erythromycin/colistin comibination.

Erythromycin and colistin demonstrate a non-antagonistic ability to inhibit the growth of a wide variety of aerobic and anaerobic bacterial isolates. When incorporated in Surgical Simplex P Radiopaque Bone Cement, fabricated cement pellets were effective in inhibiting 98% of all anaerobic and aerobic test isolates. Separate experiments indicate that each antibiotic can diffuse from polymerized cement, and that the concentration of each antibiotic is consistently above the minimum inhibitory concentration of 96% of the isolates. We conclude that erythromycin/colistin Surgical Simplex P radiopaque Bone Cement is a worthy candidate for clinical investigation.

Bone Cements↗

[A new salt of erythromycin (A-137 or erythromycin lauryl sulfate) in the topical treatment of acne].

Thirty six patients affected of acne vulgaris, preferently inflammatory, graded from I to IV according to Plewig & Kligman scale, were included in a double blind trial of erythromycin laurilsulfate (A-137) alcoholic solution versus only the vehicle, both for topical. The solutions were assigned after randomisation and both groups were found to be statistically comparable in what concerned to age, sex and length of the disease and initial number of the different lesions. The treatment has been carried over 8 weeks, the solution was applied 3 times daily and controls were made fortnightly. It was assessed: a) Individual count of lesions existing in one side of the face; b) Grade of severity (I to IV); c) Frontal and lateral colour pictures; d) Overall opinion of patient. The statistical analysis of results shows significant differences between both groups in behalf of A-137 in the following parameters: number of closed comedones in the 2nd week (P less than 0,05), in closed comedones (P less than 0,05) and pustules (P less than 0,005) during the 4th week, in the number of pustules (P less than 0,025) during the 6th week and in closed comedones (P less than 0,05), papules (P less than 0,05) and pustules (P less than 0,0,25) at the end of the 8 weeks treatment. The severity grade was equally lower (P less than 0,025) in the A-137 group on the 8th week. There were no intolerance phenomena reported nor any kind of unwanted side effects during the study.

Acne Vulgaris↗