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International Journal of Environmental... Dec 2022Sulfonamides (SAs) and tetracyclines (TCs) are two classes of widely used antibiotics. There is a lack of easy models for estimating the parameters of antibiotic...
Sulfonamides (SAs) and tetracyclines (TCs) are two classes of widely used antibiotics. There is a lack of easy models for estimating the parameters of antibiotic sorption in soils. In this work, a dataset of affinity coefficients ( and ) of seven SA/TC antibiotics (i.e., sulfachlorpyridazine, sulfamethazine, sulfadiazine, sulfamethoxazole, oxytetracycline, tetracycline, and chlortetracycline) and associated soil properties was generated. Correlation analysis of these data showed that the affinity coefficients of the SAs were predominantly affected by soil organic matter and cation exchange capacity, while those of the TCs were largely affected by soil organic matter and pH. Pedotransfer functions for estimating and were built by multiple linear regression analysis and were satisfactorily validated. Their performances would be better for soils having higher organic matter content and lower pH. These pedotransfer functions can be used to aid environmental risk assessment, prioritization of antibiotics and identification of vulnerable soils.
Topics: Soil; Soil Pollutants; Adsorption; Anti-Bacterial Agents; Sulfanilamide; Sulfonamides; Tetracyclines
PubMed: 36554653
DOI: 10.3390/ijerph192416771 -
Antibiotics (Basel, Switzerland) Mar 2017Lyme disease is a most common vector-borne disease in the US. Although the majority of Lyme patients can be cured with the standard two- to four-week antibiotic...
Lyme disease is a most common vector-borne disease in the US. Although the majority of Lyme patients can be cured with the standard two- to four-week antibiotic treatment, at least 10%-20% of patients continue to suffer from prolonged post-treatment Lyme disease syndrome (PTLDS). While the cause for this is unclear, one possibility is that persisting organisms are not killed by current Lyme antibiotics. In our previous studies, we screened an FDA drug library and an NCI compound library on and found some drug hits including sulfa drugs as having good activity against stationary phase cells. In this study, we evaluated the relative activity of three commonly used sulfa drugs, sulfamethoxazole (Smx), dapsone (Dps), sulfachlorpyridazine (Scp), and also trimethoprim (Tmp), and assessed their combinations with the commonly prescribed Lyme antibiotics for activities against stationary phase cells. Using the same molarity concentration, dapsone, sulfachlorpyridazine and trimethoprim showed very similar activity against stationary phase enriched in persisters; however, sulfamethoxazole was the least active drug among the three sulfa drugs tested. Interestingly, contrary to other bacterial systems, Tmp did not show synergy in drug combinations with the three sulfa drugs at their clinically relevant serum concentrations against . We found that sulfa drugs combined with other antibiotics were more active than their respective single drugs and that four-drug combinations were more active than three-drug combinations. Four-drug combinations dapsone + minocycline + cefuroxime + azithromycin and dapsone + minocycline + cefuroxime + rifampin showed the best activity against stationary phase in these sulfa drug combinations. However, these four-sulfa-drug-containing combinations still had considerably less activity against stationary phase cells than the Daptomycin + cefuroxime + doxycycline used as a positive control which completely eradicated stationary phase cells. Future studies are needed to evaluate and optimize the sulfa drug combinations in vitro and also in animal models.
PubMed: 28327498
DOI: 10.3390/antibiotics6010010 -
Antimicrobial Agents and Chemotherapy Aug 1995Forty-four sulfa drugs were screened against crude preparations of recombinant Pneumocystis carinii dihydropteroate synthetase. The apparent Michaelis-Menten constants... (Comparative Study)
Comparative Study
Forty-four sulfa drugs were screened against crude preparations of recombinant Pneumocystis carinii dihydropteroate synthetase. The apparent Michaelis-Menten constants (Km) for p-aminobenzoic acid and 7,8-dihydro-6-hydroxymethylpterin pyrophosphate were 0.34 +/- 0.02 and 2.50 +/- 0.71 microM, respectively. Several sulfa drugs, including sulfathiazole, sulfachlorpyridazine, sulfamethoxypyridazine, and sulfathiourea, inhibited dihydropteroate synthetase approximately as well as sulfamethoxazole, as determined by the concentrations which cause 50% inhibition and/or by Ki. For all sulfones and sulfonamides tested, unsubstituted p-amino groups were necessary for activity, and sulfonamides containing an N1-heterocyclic substituent were found to be the most effective inhibitors. Folate biosynthesis in isolated intact P. carinii was approximately equally sensitive to inhibition by sulfamethoxazole, sulfachlorpyridazine, sulfamethoxypyridazine, sulfisoxazole, and sulfathiazole. Two of these drugs, sulfamethoxypyridazine and sulfisoxazole, are known to be less toxic than sulfamethoxazole and should be further evaluated for the treatment of P. carinii pneumonia.
Topics: Animals; Anti-Infective Agents; Dihydropteroate Synthase; Folic Acid; Kinetics; Lung; Male; Pneumocystis; Pneumocystis Infections; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Structure-Activity Relationship; Sulfonamides
PubMed: 7486915
DOI: 10.1128/AAC.39.8.1756 -
Environmental Research Apr 2021This work focuses on studying the efficacy of three different by-products to adsorb three antibiotics (sulfadiazine, SDZ; sulfamethazine, SMT; sulfachloropyridazine,...
This work focuses on studying the efficacy of three different by-products to adsorb three antibiotics (sulfadiazine, SDZ; sulfamethazine, SMT; sulfachloropyridazine, SCP). These antibiotics can be considered pollutants of the environment when they reach water, as well as in cases where they are spread on soils through irrigation or contained in sewage sludge or livestock manure. In this study, batch-type adsorption/desorption experiments were performed for each of the three sulfonamides, adding 7 different concentrations of the antibiotics, going from 1 to 50 μmol L, and with contact time of 24 h. The results indicate that pine bark is the most efficient bioadsorbent among those studied, as it adsorbs up to 95% of the antibiotics added, while desorption is always less than 11%. However, for "oak ash" and mussel shell the adsorption is always lower than 45 and 15%, respectively, and desorption is high, reaching up to 49% from "oak ash" and up to 81% from mussel shell. Adsorption data showed good fitting to the Linear and Freundlich models, with R values between 0.98 and 1.00 in both cases. K and K adsorption parameters showed similar values for the same sorbent materials but were much higher for pine bark than for the other two bioadsorbents. The Freundlich's n parameter showed values in the range 0.81-1.28. The highest K values (and therefore the highest adsorption capacities) were obtained for the antibiotic SCP in pine bark. Pine bark showed the highest capacity to adsorb each of the antibiotics, increasing as a function of the concentration added. When the concentration of sulfonamide added was 50 μM, the amounts adsorbed were 780 μmol kg for SDZ, 890 μmol kg for SMT, and 870 μmol kg for SCP. "Oak ash" and mussel shell have low adsorption capacity for all three sulfonamides, showing values always lower than 150 μmol kg (oak ash) and 20 μmol kg (mussel shell) when a concentration of 50 μmol L of antibiotic is added. The results of this study could aid to make an appropriate management of the by-products studied, in order to facilitate their valorization and recycling in the treatment of environmental compartments polluted with sulfonamide antibiotics.
Topics: Adsorption; Animals; Bivalvia; Plant Bark; Porosity; Quercus; Soil; Soil Pollutants; Sulfachlorpyridazine; Sulfadiazine; Sulfamethazine
PubMed: 33524329
DOI: 10.1016/j.envres.2021.110814 -
Antimicrobial Agents and Chemotherapy Apr 1996A remarkably high rate of adverse events is associated with the use of trimethoprim-sulfamethoxazole in patients with human immunodeficiency virus type 1 infection. We... (Comparative Study)
Comparative Study
A remarkably high rate of adverse events is associated with the use of trimethoprim-sulfamethoxazole in patients with human immunodeficiency virus type 1 infection. We examined the efficacies of sulfonamides alone in the prevention of Pneumocystis carinii pneumonitis, with the assumption that at least some of the adverse events with the drug combination might be due to trimethoprim. With the immunosuppressed rat model, eight sulfonamides were studied at 100, 10, and 1.0 mg/kg/day (10 rats per dosage and drug). P. carinii infection was prevented in all animals (100%) receiving dosages of as little as 1.0 mg of sulfamethoxazole, sulfamethoxypyridazine, and sulfadimethoxine per kg per day, as little as 10 mg of sulfameter, sulfachlorpyridazine, and sulfaquinoxaline per kg per day; and 100 mg of sulfaguanidine and sulfanilamide per kg per day. These studies suggest that a sulfonamide, such as sulfamethoxazole, might provide effective prophylaxis for P. carinii pneumonitis without trimethoprim.
Topics: Animals; Anti-Infective Agents; Dose-Response Relationship, Drug; Male; Pneumonia, Pneumocystis; Rats; Rats, Sprague-Dawley; Sulfadimethoxine; Sulfamethoxazole; Sulfamethoxypyridazine
PubMed: 8849260
DOI: 10.1128/AAC.40.4.962 -
Frontiers in Microbiology 2016Although currently recommended antibiotics for Lyme disease such as doxycycline or amoxicillin cure the majority of the patients, about 10-20% of patients treated for...
Although currently recommended antibiotics for Lyme disease such as doxycycline or amoxicillin cure the majority of the patients, about 10-20% of patients treated for Lyme disease may experience lingering symptoms including fatigue, pain, or joint and muscle aches. Under experimental stress conditions such as starvation or antibiotic exposure, Borrelia burgdorferi can develop round body forms, which are a type of persister bacteria that appear resistant in vitro to customary first-line antibiotics for Lyme disease. To identify more effective drugs with activity against the round body form of B. burgdorferi, we established a round body persister model induced by exposure to amoxicillin (50 μg/ml) and then screened the Food and Drug Administration drug library consisting of 1581 drug compounds and also 22 drug combinations using the SYBR Green I/propidium iodide viability assay. We identified 23 drug candidates that have higher activity against the round bodies of B. burgdorferi than either amoxicillin or doxycycline. Eleven individual drugs scored better than metronidazole and tinidazole which have been previously described to be active against round bodies. In this amoxicillin-induced round body model, some drug candidates such as daptomycin and clofazimine also displayed enhanced activity which was similar to a previous screen against stationary phase B. burgdorferi persisters not exposure to amoxicillin. Additional candidate drugs active against round bodies identified include artemisinin, ciprofloxacin, nifuroxime, fosfomycin, chlortetracycline, sulfacetamide, sulfamethoxypyridazine and sulfathiozole. Two triple drug combinations had the highest activity against amoxicillin-induced round bodies and stationary phase B. burgdorferi persisters: artemisinin/cefoperazone/doxycycline and sulfachlorpyridazine/daptomycin/doxycycline. These findings confirm and extend previous findings that certain drug combinations have superior activity against B. burgdorferi persisters in vitro, even when pre-treated with amoxicillin. These findings may have implications for improved treatment of Lyme disease.
PubMed: 27242757
DOI: 10.3389/fmicb.2016.00743 -
PloS One 2018Several antimicrobials are routinely used by the poultry farming industry on their daily operations, however, researchers have found for some antimicrobials that their...
Determination of sulfachloropyridazine residue levels in feathers from broiler chickens after oral administration using liquid chromatography coupled to tandem mass spectrometry.
Several antimicrobials are routinely used by the poultry farming industry on their daily operations, however, researchers have found for some antimicrobials that their residues persist for longer periods in feathers than they do in edible tissues, and at higher concentrations, as well. But this information is not known for other classes of antimicrobials, such as the sulfonamides. Therefore, this work presents an accurate and reliable analytical method for the detection of sulfachloropyridazine (SCP) in feathers and edible tissues from broiler chickens. This method was also validated in-house and then used to study the depletion of sulfachloropyridazine in those matrices. The experimental group comprised 54 broiler chickens, who were raised under controlled conditions and then treated with a commercial formulation of 10% sulfachloropyridazine for 5 days. Samples were analyzed via LC-MS/MS, using 13C6-sulfamethazine (SMZ-13C6) as an internal standard. Aromatic sulfonic acid solid phase extraction (SPE) cartridges were used to clean up the samples. The Limit of Detection (LOD) for this method was set at 10 μg kg-1 on feathers and liver; and at 5 μg kg-1 on muscle. Within the range of 10-100 μg kg-1, the calibration curves for all matrices presented a determination coefficient greater than 0.96. Our results show, with a 95% confidence level, that sulfachloropyridazine persisted in feathers for up to 55 days after ceasing treatment, and its concentrations were higher than in edible tissues. In consequence, to avoid re-entry of antimicrobial residues into the food-chain, we recommend monitoring and inspecting animal diets that contain feather derivatives, such as feathers meals, because they could be sourced from birds that might have been medicated with sulfachloropyridazine.
Topics: Administration, Oral; Animals; Anti-Bacterial Agents; Anti-Infective Agents; Chickens; Chromatography, Liquid; Drug Residues; Feathers; Limit of Detection; Muscles; Solid Phase Extraction; Sulfachlorpyridazine; Sulfonamides; Tandem Mass Spectrometry
PubMed: 29975750
DOI: 10.1371/journal.pone.0200206 -
Canadian Journal of Comparative... Jul 1976Among 300 isolates of bovine Escherichia coli, 56 which had been found enterotoxigenic in calf gut loops were characterized on the basis of O and K antigens, colonial...
Among 300 isolates of bovine Escherichia coli, 56 which had been found enterotoxigenic in calf gut loops were characterized on the basis of O and K antigens, colonial morphology and resistance to seven antimicrobial drugs. The 56 isolates enterotoxigenic in the calf were compared with the nonenterotoxigenic ones. Of the 56 enterotoxigenic E. coli the majority possessed the A type of K antigen and had OK groups, O9:K(PS274) or O101:K(RVC118). Fourteen of these isolates had the K99 antigen. None of 27 isolates found enterotoxigenic in the piglet but not in the calf possessed the K99 antigen or belonged to OK groups O9:K(PS274) or O101:K(RVC118). Comparison of the patterns of resistance to seven antimicrobial drugs showed that all enterotoxigenic and nonenterotoxigenic isolates were susceptible to nitrofurantoin and sulphachlorphyridiazine and that there was no significant difference in the patterns between the two groups. The majority of enterotoxigenic isolates were mucoid, whereas most of the nonenterotoxigenic isolates were nonmucoid.
Topics: Animals; Antigens, Bacterial; Cattle; Enterotoxins; Escherichia coli; Nitrofurantoin; Sulfachlorpyridazine; Swine
PubMed: 793694
DOI: No ID Found -
Journal of Agricultural and Food... Jul 2009Effects of oxytetracycline (OTC) and sulfachloropyridazine (SCP), two of the widely used antibiotics in livestock production, on beneficial environmental microorganisms...
Effects of oxytetracycline (OTC) and sulfachloropyridazine (SCP), two of the widely used antibiotics in livestock production, on beneficial environmental microorganisms were studied. Shewanella decolorationis S12 was selected as the target bacteria for the role in reduction of Fe(III) and dye under anaerobic conditions. The results showed that the antibiotics significantly inhibited Fe(III) reduction and dye decoloration in the reduction system. The rates of Fe(II) formed (-r) were 3.6 and 0.2 mg/L/day for the OTC concentrations of 0-1 mg/L and 1-50 mg/L, respectively, with 1 mg/L as the turning point of the inhibition effect. The turning point of inhibition effect was much higher for SCP treatments, at 4 mg/L. The results also showed higher production values for adsorbed Fe(II) than soluble Fe(II) in OTC treatments, but the reverse occurred in the SCP treatments. The difference between the treatments could be due to higher sorption coefficients of OTC as compared to SCP. Transmission electron micrographs showed changes in cell structures of S. decolorationis S12 grown in medium with OTC. Detached cell walls and large vacuoles in internal cell contents were found in OTC-treated cells. The results of the present study indicated that the inhibition of antibiotic on the reduction activity of S. decolorationis S12 may be due to a decrease in live S. decolorationis S12 population and/or damages of their cell structure in this reduction system.
Topics: Anti-Bacterial Agents; Coloring Agents; Ferrous Compounds; Microscopy, Electron, Transmission; Oxidation-Reduction; Oxytetracycline; Shewanella; Soil Microbiology; Sulfachlorpyridazine
PubMed: 19527026
DOI: 10.1021/jf900641e -
Memorias Do Instituto Oswaldo Cruz 1974
Comparative Study
Topics: Anti-Bacterial Agents; Brazil; Child; Drug Resistance, Microbial; Enterobacteriaceae; Enterobacteriaceae Infections; Humans; Sulfachlorpyridazine; Sulfanilamides
PubMed: 4465637
DOI: 10.1590/s0074-02761974000100006