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PubMedDate not supplied

[Radiosensitizing activity and metabolism of nitrofuran derivatives. Preparation M-106].

It was shown that the preparation of a nitrofuran M-106 series exerts a radiosensitizing effect on tumors with contact application. The observed effect is practically absent after noncontact administration of the preparation. On the basis of the data obtained from studies of M-106 metabolism in microsomes of liver and Ehrlich ascites tumor cells of mice it is concluded that the intact form of the preparation is responsible for the radiosensitizing effect, and that the absence of this effect with the noncontact administration is due to its low concentration in the tumor because of the active metabolic transformation of M-106 in the animal liver.

Animals↗
PubMed1979

[Characteristics of the antibiotic sensitivity of nitrofuran--resistant Gram-negative bacteria of clinical origin].

494 persons with various purulent inflammatory diseases were examined. Gram-negative nitrofuran resistant organisms isolated from the clinical material were found in 22.9 per cent of the cases. Representatives of Enterobacteriaceae, Klebsiella-Enterobacter-Serratia (26.8 per cent), Proteus-Providencia (16.8 per cent) and E. coli-Arizona-Citrobacter (16.1 per cent) predominated. Pseudomonas (32.1 per cent) and Acinetobacter (5.3 per cent) predominated among the aerobic gram-negative bacteria. Sensitivity of 131 strains to 10 chemotherapeutic drugs was determined. 60.4 per cent of the aerobic and 44.2 per cent of the Coli bacteria had multiple drug resistance (to 5 and more drugs). The organisms isolated from the urine and wound excretion were most resistant. Representatives of Pseudomonas and Klebsiella-Enterobacter predominated among the polyresistant cultures. High sensitivity of the isolates to gentamicin, carbenicillin and nalidixic acid was noted.

Anti-Bacterial Agents↗
PubMed1978

In vitro effect of alpha, beta-unsaturated sulphones of the 5-nitrofuran series on the incorporation of C-labelled precursors into Ehrlich's ascites carcinoma cells.

The effect of new 5-nitrofuran (5NF) derivatives on the incorporation of 14C precursors of nucleic acids and protein synthesis into Ehrlich's ascites carcinoma (EAC) cells in vitro has been studied. Of the 32 substances that were tested, 22 markedly inhibited the incorporation of adenine, L-valine, uridine and thymidine. The 5NF derivatives influenced the synthesis of nucleic acids in vitro and the proliferation of EAC cells. The effect of the derivatives depends on the nature and position of the substituents as well as on the spatial arrangement of the whole molecule. Some of the evaluated derivatives showed a weak virostatic effect and induced lysogenicity in E. coli C 600. As most of the tested 5NF inhibited E. coli(rec-) mutants, it can be concluded that the (rec-) gene evidently takes part in the repair of their damage.

Adenine↗
PubMedDate not supplied

[The effect of nitrofurans on the membrane apparatus of coccal bacteria].

Secondary membrane effects on the membrane apparatus of coccus bacteria were being studied. Cultivation of Micrococcus lysodeikticus and Staphylococcus aureus cells on subbacteriostatic concentrations of nitrofurans results in a lower biosynthesis of many membrane proteins, as well as in inhibiting the activity of respiratory enzymes, i. e. the specific concentration of cytochromes and specific activity of NADH-, malate-, lactate oxidases and some reductases drop. Some cytological changes were revealed, when cells were grown on solafur, furazolidone, and furacriline.

Bacterial Proteins↗
PubMed1984

[Use of antibiotics and nitrofurans in treating acute and chronic cholecystitis].

Sixty-two patients with acute cholecystitis and 108 patients with chronic calculous cholecystitis were examined. High levels of contamination of the bile, gallbladder mucosa and gallstones were shown. E. coli, Staphylococcus and Streptococcus were most frequent among 20 species of aerobic and anaerobic bacteria. Preoperative sanation of the hepatoduodenal area with antibiotics did not result in complete elimination of the bacteria in the bile, gallbladder mucosa and gallstones. The use of nitrofurans and especially furazolidone and furagin in the preoperative period prevented the microbial growth in the specimens collected during the operations. The data of the study allow recommending the use of furazolidone and furagin for preoperative sanation of the biliferous tract.

Anti-Bacterial Agents↗
PubMed1982

[Inhibition of the diffusion of plasmids by a nitrofuran derivative].

Antibiotic resistance plasmids PR4, R6K, and RGN238 can transfer between Escherichia coli cells by conjugation (transfer frequency: 3 to 3.5 x 10(-4)). Nifurzide, a nitrofuran derivative, greatly depresses plasmid transfer at concentrations (59 microM) which do not affect cell viability.

Anti-Bacterial Agents↗
PubMed1982

Mutagenic effects of two nitrofuran food preservatives.

Two structurally related food additives, 3-(5-nitro-2-furyl)acrylic acid (5-NFAA) and 2-(2-furyl)-3-(5-nitro-2-furyl)acrylamide (AF-2) showed a marked mutagenic effect on Salmonella typhimurium strains TA100 and TA98 and Escherichia coli WP2 uvrA+ and WP2 uvrA. On the molar basis 5-NFAA was about two orders of magnitude less effective than AF-2. In Salmonella typhimurium TA100 anaerobic conditions stimulated the mutagenic effect of 5-NFAA which was more pronounced in nitrofuran-reductase deficient strain of Salmonella typhimurium TA100 FR50. 5-NFAA increased the number of isoleucine revertants and induced mitotic recombination at tryptophan, threonine and adenine loci of the diploid strains Saccharomyces cerevisiae a/b and Saccharomyces cerevisiae SBTD. Activity of 5-NFAA was lower than that of AF-2. The test on sex-linked recessive lethal mutations in Drosophila melanogaster indicated that only 5-NFAA is mutagenic, increasing the mutation frequency about 10-fold above the control. Results with AF-2 fell within the control range.

Acrylates↗
PubMed1982

Induction of unscheduled DNA synthesis in primary culture of dog, rat, and mouse urothelial cells by arylamine and nitrofuran derivatives.

The induction of unscheduled DNA synthesis in primary cultures of urothelial cells from rats, mice, and dogs by nitrofurans and arylamines and their derivatives was examined. Electron microscopy of the culture from rat cells showed the characteristics of epithelial cells. The cultured cells were exposed to the test chemicals in a serum-free medium containing 10 mM hydroxyurea and [3H]thymidine for 24 hr, and unscheduled DNA synthesis was determined by autoradiography. N-Hydroxy-2-aminofluorene, N-hydroxy-2-acetylaminofluorene, N-hydroxy-4-amino-biphenyl, and N-hydroxy-4-acetylaminobiphenyl were active in inducing unscheduled DNA synthesis in the urothelial cells of rats, mice, and dogs. 2-Aminofluorene, N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide, and 2-amino-4-(5-nitro-2-furyl)thiazole were active only in dog cells. 2-Acetylaminofluorene and 4-aminobiphenyl were not active. These results demonstrate that urothelial cells contain enzymes that can selectively activate bladder carcinogens and their metabolites.

Amines↗
PubMedDate not supplied

Liquid chromatographic determination of nitrofuran residues in bovine muscle tissues.

A liquid chromatographic (LC) method was developed and statistically validated for simultaneous determination of nitrofurazone, nitrofurantoin, furazolidone, and furaltadone residues in bovine muscle tissues. These antimicrobial residues in samples stabilized at pH 6.0 were extracted with acetonitrile and purified by liquid-liquid partition between dichloromethane-ethyl acetate and hexane saturated with acetonitrile. The acetonitrile-ethyl acetate extract was concentrated, and drug residues were dissolved in LC mobile phase, filtered, and determined by LC. A C18 reversed-phase (ODS Hypersil) column at 35 degrees C, a mobile phase of 0.01M sodium acetate buffer (pH 4.5)-acetonitrile (70 + 30), and a UV/visible diode array detector at 365 nm were used. The retention times and UV spectra of peaks in spiked samples were compared with those of known nitrofurans. Limits of detection (LD) and quantitation (LQ) were 1 and 2 micrograms/kg, respectively. Average recoveries were 76% (range, 60-110%). Relative standard deviations ranged from 6 to 18% at 5 fortification levels from 1.5 to 20 micrograms/kg). (Fortification levels for furaltadone were 3 to 40 micrograms/kg). The method was used to analyze 350 samples per year from 1993 to 1995.

Animals↗
PubMed1975

Effect of activated nitrofurans on DNA.

Enzymically activated nitrofurazone reacts with co-valently closed circular DNA (derived from Escherichia coli minicells carrying lambdadv) to give at least two kinds of damage: breaks which are detected on neutral sucrose gradients and alkali-labile lesions in DNA which are converted to breaks when the DNA is subsequently Treated with alkali. DNA, isolated from nimicells exposed to the drug, also contains lesions which are converted to breaks upon treatment with endonuclease preparations obtained from Micrococcus luteus. Minicells repaired both breaks and nuclease-susceptible lesions within 2 h but did not repair alkali labile lesions within that time. Experiments with three other nitrofurans show that there are considerable differences in the degree to which DNA is damaged by activated metabolites of various derivatives and that the potency of the compounds as mutagens and carcinogens is correlated with the amount of damage caused to minicell DNA.

Binding Sites↗
PubMed1990

Studies on the effect of ascorbic acid and selenium on the genotoxicity of nitrofurans: nitrofurazone and furazolidone.

The genotoxic properties of nitrofurazone and furazolidone were studied using the Ames test and SOS-chromotest. Both compounds were found to act as strong mutagens on the TA97 and TA102 strains of S. typhimurium and to induce the SOS-repair system in the PQ37 strain of E. coli. A good concordance was found between the mutagenic activity and the ability to induce the SOS system. Ascorbic acid and sodium selenite only very slightly lowered the genotoxic effect of the 2 nitrofurans studied both in the Ames test and in the SOS-chromotest.

Antioxidants↗
PubMed1983

Nitrofuran reductase activity in nitrofurantoin-resistant strains of Escherichia coli K12: some with chromosomally determined resistance and others carrying R-plasmids.

The nitrofuran reductase activity of Escherichia coli K12 strains was separated into two components by passage through Sepharose 4B-200. The components differed in their sensitivity to 2 M urea and their reactivity with NADH and NADPH. Some nitrofurantoin-resistant mutants had lost one component (alpha) while retaining the other (beta). Other mutants, resistant to higher levels of nitrofurantoin, had lost most of the beta component as well. Transconjugants which had received plasmids conferring nitrofurantoin resistance were found to have only the alpha component and it was markedly less active when NADH rather than NADPH was supplied as co-enzyme.

Bacterial Proteins↗
PubMed1981

Studies on oxygen-insensitive nitrofuran reductase in Escherichia coli B/r.

Oxygen-insensitive nitrofuran reductase in Escherichia coli B/r was clearly resolved by DEAE-cellulose column chromatography into two components, one NADPH-linked, and the other both NADPH- and NADH-linked. It is known that the strain requires resistance to nitrofurazone in two mutational steps. It is known that the the first step mutants had no NADPH-linked component and the second step ones had neither this component nor the NAD(P)-H-linked one. The NADPH- and NADH-linked activities of the latter component were similarly inactivated by heat or urea treatment. In addition, it was found that these activities were significantly inhibited by dicoumarol, an NAD(P)H dehydrogenase inhibitor, to similar extents. These results suggest that the activities of the NAD(P)H-linked component originate from a single enzyme. On the other hand, the NADPH-linked component was less sensitive to heat, urea and dicoumarol.

Cell-Free System↗
PubMed1974

New antimicrobial nitrofuran, trans-5-amino-3-[2-(5-nitro-2-furyl)vinyl]-delta2-1,2,4-oxadiazole: antimicrobial efficacy in mice, rats, and guinea pigs.

A new antimicrobial nitrofuran designated SQ 18,506 showed some therapeutic activity when administered orally to mice infected with Escherichia coli, Salmonella schottmuelleri, Shigella flexneri, or Klebsiella pneumoniae. Animals infected parenterally with Streptococcus pyogenes, Proteus mirabilis, Mycobacterium tuberculosis, and Candida albicans, or topically with Trichophyton mentagrophytes, did not respond to therapy with the drug at the dosage levels used. The compound was as effective as metronidazole in the topical treatment of experimental trichomonal infections in mice and in guinea pigs and as effective as nystatin, candicidin, or a sulfanilamide-aminacrine hydrochloride cream in the treatment of a candidal vaginal infection in rats. The chemotherapeutic efficacy of SQ 18,506 in experimental vaginitis caused by Escherichia coli in the rat surpassed that shown by four commercial products available for the treatment of bacterial vaginitis.

5-Amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazol↗
PubMed1982

Oxygen--insensitive nitrofuran reductases in Salmonella typhimurium TA100.

The present study demonstrated by DEAE-cellulose column chromatography that oxygen-insensitive nitrofuran reductases in Salmonella typhimurium TA100 consisted of at least two reductases, NADPH- and NAD(P)H-linked enzymes. The NADPH- and NADH-linked activities of the latter enzyme seemed to originate from a single enzyme, because both activities were similarly inactivated by heat and urea treatments, and also inhibited by dicumarol. On the other hand, the NADPH-linked enzyme was less sensitive to heat, urea and dicumarol. Furthermore, the study showed that the NAD(P)H-linked enzyme was a flavoenzyme which could be inactivated by dialysis against 1 M potassium bromide and reactivated by FMN.

Apoenzymes↗
PubMed2004

Photocytotoxicity of a 5-nitrofuran-ethenyl-quinoline antiseptic (Quinifuryl) to P388 mouse leukemia cells.

Quinifuryl (MW 449.52), 2-(5'-nitro-2'-furanyl)ethenyl-4-[N-[4'-(N,N-diethylamino)-1'-methylbutyl]carbamoyl] quinoline, is a water soluble representative of a family of 5-nitrofuran-ethenyl-quinoline drugs which has been shown to be highly toxic to various lines of transformed cells in the dark. In the present study, the toxicity of Quinifuryl to P388 mouse leukemia cells was compared in the dark and under illumination with visible light (390-500 nm). Illumination of water solutions of Quinifuryl (at concentrations ranging from 0.09 to 9.0 microg/ml) in the presence of P388 cells resulted in its photodecomposition and was accompanied by elevated cytotoxicity. A significant capacity to kill P388 cells was detected at a drug concentration as low as 0.09 microg/ml. The toxic effect detected at this drug concentration under illumination exceeded the effect observed in the dark by more than three times. Moreover, the general toxic effect of Quinifuryl, which included cell proliferation arrest, was nearly 100%. Both dose- and time-dependent toxic effects were measured under illumination. The LC50 value of Quinifuryl during incubation with P388 cells was approximately 0.45 microg/ml under illumination for 60 min and >12 microg/ml in the dark. We have demonstrated that the final products of the Quinifuryl photolysis are not toxic, which means that the short-lived intermediates of Quinifuryl photodecomposition are responsible for the phototoxicity of this compound. The data obtained in the present study are the first to indicate photocytotoxicity of a nitroheterocyclic compound and demonstrate the possibility of its application as a photosensitizer drug for photochemotherapy.

Animals↗
PubMedDate not supplied

[Photosensitizing properties and antioxidant activity of furagin--an antimicrobial drug that is a derivative of nitrofuran].

Photosensitizing effect of antimicrobial drug nitrofuran derivative--furagin N-(5-nitro-2-furil)-allylidencamino-hydantoin) under irradiation with light longer than 280 nm was found. The method of investigation is based on photochemiluminescence of Gly-Trp peptide in aqueous solution. Maximum photosensitizing efficiency was observed at the furagin concentration 0.08 mM when chemiluminescence yield was 33 times greater than photochemiluminescence of Gly-Trp peptide in absence of drug. It was shown that photochemiluminescence sensitized by furagin occurred via free radical way. Life time of the triplet state of furagin determined by flash photolysis was 40 microseconds. A comparison of experimental data with kinetic calculation allowed us to estimate the rate constant of triplet quenching by oxygen ((2.2 +/- 0.3)10(8) M-1.s-1) and the total rate constants of physical quenching and chemical reaction with Gly-Trp peptide ((2.0 +/- 0.4)10(8) M-1.s-1). It was also found in experiments with photochemiluminescence of Gly-Trp peptide sensitized by riboflavin (irradiation with monochromatic light 436 nm) that furagin possesses antioxidant properties twice reducing the intensity of chemiluminescence at the drug concentration 0.029 mM.

Antioxidants↗