Parent Antibiotic Research Articles

Application of antibiotic-derived fluorescent probes to bacterial studies.

Fluorescent probes are extensively applied as useful tools for imaging and determining dynamic processes in bacterial cells. In particular, antibiotic-derived fluorescent probes which can visualize the presence or the localization of antibiotics within bacteria through the monitoring of changes in fluorescence signal, are particularly useful. They form an emerging set of tools for studying the mode of action of their parent antibiotics and examining bacterial resistance and persistence, with the long-term goal of developing fresh approaches to the treatment of drug-resistant bacterial infections. In this chapter, we discuss the applications of antibiotic-based fluorescent probes to visualize bacteria, focusing on the techniques we have utilized to study their localization, penetration and efflux. We describe detailed protocols for analysis of bacteria using microscopy, flow cytometry, and plate reader-based methods based on these probes.

Fate of Phytometabolites of Antibiotics during In Vitro Digestion and Implications for Human Health.

Antibiotics are released into the environment as their global consumption increases. Uptake, accumulation, and metabolism of antibiotics by food crops is an emerging health concern as the associated risks of consuming food crops containing antibiotics are still largely unknown. This study investigated the fate of sulfamethazine, sulfamethoxazole, and their phytometabolites during in vitro digestion of the model plantArabidopsis thaliana. The amounts of parent antibiotics released during in vitro digestion were 4-5 times higher than those quantified in plant tissues prior to digestion, which was attributed to back transformation of the phytometabolites into the parent aglycones. These findings demonstrated that overlooking the proportions of phytometabolites in recent health risk assessment studies would considerably underestimate the realistic human exposure through consumption of contaminated food crops. New risk assessment frameworks are necessary to include these critical factors for comprehensively addressing human exposure to emerging contaminants through food chains.

Simultaneous Determination of Seven Antibiotics and Five of Their Metabolites in Municipal Wastewater and Evaluation of Their Stability under Laboratory Conditions.

The selection and spread of antibiotic resistance poses risks to public health by reducing the therapeutic potential of antibiotics against human pathogens. Wastewater-based epidemiology (WBE) is potentially the most reliable approach to estimate antibiotics use. Previous WBE studies used parent antibiotics as biomarkers, which may lead to overestimation since parent antibiotics may be directly disposed of. Using metabolites as biomarkers can avoid this drawback. This study developed a simultaneous solid-phase extraction coupled with ultra-high-performance liquid chromatography tandem mass spectrometry method for analyzing 12 antibiotics and human metabolites in wastewater to help assess health risk. Optimum conditions were achieved using a PEP cartridge at pH 3.0. The extraction efficiencies were 73.3~95.4% in influent and 72.0~102.7% in effluent for most of the target analytes. Method detection limit ranged from 0.1 to 1.5 ng/L for influent wastewater and 0.03 to 0.7 ng/L for effluent wastewater. A stability experiment showed that sulfonamide parents and their metabolites were stable at 4 °C, −20 °C and −80 °C, while macrolides metabolites were more stable than their corresponding parents at 4 °C and −20 °C. Finally, the method was applied to measure these analytes in wastewater samples collected from three Beijing WWTPs and to derive apparent removal rates. All metabolites were detected in wastewater samples with concentrations ranging from 1.2 to 772.2 ng/L in influent, from <MDL to 235.6 ng/L in effluent. The apparent removal rates of five metabolites were above 72.6%. These results set a solid foundation for applying WBE to evaluate antibiotics use and its public health effects.

High efficiency of osmotically stable laccase for biotransformation and micro-detoxification of levofloxacin in the urea-containing solution: Catalytic performance and mechanism

Laccase-catalyzed oxidation was applied in the biotransformation of levofloxacin (a potentially environmental antibiotic contamination); however, the enzyme may denature in urea-containing wastewater and lead to the formation of an inactive form followed by decreasing the yield of the bio-removal. In this study, the osmolytes-stabilized laccase was used to eliminate levofloxacin in the urea-containing solution. Sorbitol and proline 100 mM appeared to be the two most efficient laccase protectants against the urea-induced denaturation. In a 1-M urea solution, the maximum velocity (Vmax) of laccase was estimated to be 39.1 μmol min–1 mg–1. This value was improved to 101.7 and 51.8 μmol min–1 mg–1 in the presence of sorbitol and proline, respectively. In optimal conditions for the elimination of levofloxacin, sorbitol- and proline-treated laccase led to 82.9 % and 76.2 % bio-removal of the applied fluoroquinolone in 1 M urea solution, respectively. Biotransformation products of the parent antibiotic were spectroscopically analyzed that assigned to different reaction pathways including demethylation, defluorination, decarboxylation, deamination, and hydroxylation. A micro-toxicity study concerning the growth of some Gram+ and Gram– bacteria exhibited decreasing in inhibition of laccase-treated levofloxacin after a 10-h incubation at 37 °C.

Oxidation of antibiotics by ferrate(VI) in water: Evaluation of their removal efficiency and toxicity changes

Antibiotics in water and wastewater have been determined extensively. The treatment of antibiotics in water needs evaluation of possible harmful effects on aquatic ecosystems and human health. This paper presents the toxicity evaluation of antibiotics after their treatment with ferrate (VI) (FeVIO42−, Fe(VI)) in water. The antibiotics (sulfamethoxazole (SMX), erythromycin (ERY), ofloxacin (OFL), ciprofloxacin (CIP), tetracycline (TET), oxytetracycline (OXY), and trimethoprim (TMP)) were treated at pH 8.0 by applying two concentrations of Fe(VI) to have molar ratios of 5:1 and 10:1 ([Fe(VI)]:[antibiotic]). Under the studied conditions, incomplete removal of antibiotics was observed, suggesting that the treated solutions contained parent antibiotics and their transformation products. The toxicity of antibiotics without Fe(VI) treatment was tested against freshwater green alga Raphidocelis subcapitata and cyanobacterium Synechococcus elongatus, which were determined to be generally sensitive to antibiotics, with EC50 < 1.0 mg/L. The toxicity of Fe(VI) treated solution was tested against R. subcapitata. Results found no toxicity for the treated solutions of OFL, CIP, and OXY. However, SMX, ERY, and TET remained toxic after Fe(VI) treatment (i.e., more than 75% growth inhibition of R. subcapitata). Results demonstrated that R. subcapitata may be applied to test the toxicity of antibiotics after oxidative treatments.

Conjugation to Enterobactin and Salmochelin S4 Enhances the Antimicrobial Activity and Selectivity of β-Lactam Antibiotics against Nontyphoidal Salmonella.

The pathogen Salmonella enterica is a leading cause of infection worldwide. Nontyphoidal Salmonella (NTS) serovars typically cause inflammatory diarrhea in healthy individuals, and can cause bacteremia in immunocompromised patients, children, and the elderly. Management of NTS infection poses a challenge because antibiotic treatment prolongs fecal shedding of the pathogen and is thus not recommended for most patients. In recent years, the emergence of antibiotic resistance in NTS has also become a major issue. Thus, new therapeutic strategies to target NTS are needed. Here, we evaluated whether six siderophore-β-lactam conjugates based on enterobactin (Ent) and salmochelin S4 (digulcosylated Ent, DGE) provide antimicrobial activity against the two highly prevalent NTS serovars Typhimurium and Enteritidis by targeting the siderophore receptors FepA and/or IroN. The conjugates showed 10- to 1000-fold lower minimum inhibitory concentrations against both serovars Typhimurium and Enteritidis compared to the parent antibiotics under iron limitation and were recognized and transported by FepA and/or IroN. NTS treated with the Ent/DGE-β-lactam conjugates exhibited aberrant cellular morphologies suggesting inhibition of penicillin-binding proteins, and the conjugates selectively killed NTS in coculture with Staphylococcus aureus. Lastly, the DGE-based conjugates proved to be effective at inhibiting growth of NTS in the presence of the Ent-sequestering protein lipocalin-2. This work describes the successful use of siderophore-antibiotic conjugates against NTS and highlights the opportunity for narrowing the activity spectrum of antibiotics by using Ent and DGE to target enteric bacterial pathogens.

Enterobactin- and salmochelin-β-lactam conjugates induce cell morphologies consistent with inhibition of penicillin-binding proteins in uropathogenic Escherichia coli CFT073.

The design and synthesis of narrow-spectrum antibiotics that target a specific bacterial strain, species, or group of species is a promising strategy for treating bacterial infections when the causative agent is known. In this work, we report the synthesis and evaluation of four new siderophore-β-lactam conjugates where the broad-spectrum β-lactam antibiotics cephalexin (Lex) and meropenem (Mem) are covalently attached to either enterobactin (Ent) or diglucosylated Ent (DGE) via a stable polyethylene glycol (PEG3) linker. These siderophore-β-lactam conjugates showed enhanced minimum inhibitory concentrations against Escherichia coli compared to the parent antibiotics. Uptake studies with uropathogenic E. coli CFT073 demonstrated that the DGE-β-lactams target the pathogen-associated catecholate siderophore receptor IroN. A comparative analysis of siderophore-β-lactams harboring ampicillin (Amp), Lex and Mem indicated that the DGE-Mem conjugate is advantageous because it targets IroN and exhibits low minimum inhibitory concentrations, fast time-kill kinetics, and enhanced stability to serine β-lactamases. Phase-contrast and fluorescence imaging of E. coli treated with the siderophore-β-lactam conjugates revealed cellular morphologies consistent with the inhibition of penicillin-binding proteins PBP3 (Ent/DGE-Amp/Lex) and PBP2 (Ent/DGE-Mem). Overall, this work illuminates the uptake and cell-killing activity of Ent- and DGE-β-lactam conjugates against E. coli and supports that native siderophore scaffolds provide the opportunity for narrowing the activity spectrum of antibiotics in clinical use and targeting pathogenicity.

Bi-Functional Alginate Oligosaccharide-Polymyxin Conjugates for Improved Treatment of Multidrug-Resistant Gram-Negative Bacterial Infections.

The recent emergence of resistance to colistin, an antibiotic of last resort with dose-limiting toxicity, has highlighted the need for alternative approaches to combat infection. This study aimed to generate and characterise alginate oligosaccharide (“OligoG”)–polymyxin (polymyxin B and E (colistin)) conjugates to improve the effectiveness of these antibiotics. OligoG–polymyxin conjugates (amide- or ester-linked), with molecular weights of 5200–12,800 g/mol and antibiotic loading of 6.1–12.9% w/w, were reproducibly synthesised. In vitro inflammatory cytokine production (tumour necrosis factor alpha (TNFα) ELISA) and cytotoxicity (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) of colistin (2.2–9.3-fold) and polymyxin B (2.9–27.2-fold) were significantly decreased by OligoG conjugation. Antimicrobial susceptibility tests (minimum inhibitory concentration (MIC), growth curves) demonstrated similar antimicrobial efficacy of ester- and amide-linked conjugates to that of the parent antibiotic but with more sustained inhibition of bacterial growth. OligoG–polymyxin conjugates exhibited improved selectivity for Gram-negative bacteria in comparison to mammalian cells (approximately 2–4-fold). Both OligoG–colistin conjugates caused significant disruption of Pseudomonas aeruginosa biofilm formation and induced bacterial death (confocal laser scanning microscopy). When conjugates were tested in an in vitro “time-to-kill” (TTK) model using Acinetobacter baumannii, only ester-linked conjugates reduced viable bacterial counts (~2-fold) after 4 h. Bi-functional OligoG–polymyxin conjugates have potential therapeutic benefits in the treatment of multidrug-resistant (MDR) Gram-negative bacterial infections, directly reducing toxicity whilst retaining antimicrobial and antibiofilm activities.

Synthesis and biochemical evaluation of cephalosporin analogues equipped with chemical tethers.

Molecular probes typically require structural modifications to allow for the immobilisation or bioconjugation with a desired substrate but the effects of these changes are often not evaluated. Here, we set out to determine the effects of attaching functional handles to a first-generation cephalosporin. A series of cephalexin derivatives was prepared, equipped with chemical tethers suitable for the site-selective conjugation of antibiotics to functionalised surfaces. The tethers were positioned remotely from the β-lactam ring to ensure minimal effect to the antibiotic's pharmacophore. Herein, the activity of the modified antibiotics was evaluated for binding to the therapeutic target, the penicillin binding proteins, and shown to maintain binding interactions. In addition, the deactivation of the modified drugs by four β-lactamases (TEM-1, CTX-M-15, AmpC, NDM-1) was investigated and the effect of the tethers on the catalytic efficiencies determined. CTX-M-15 was found to favour hydrolysis of the parent antibiotic without a tether, whereas AmpC and NDM-1 were found to favour the modified analogues. Furthermore, the antimicrobial activity of the derivatives was evaluated to investigate the effect of the structural modifications on the antimicrobial activity of the parent drug, cephalexin.

Dissipation of antibiotics by microalgae: Kinetics, identification of transformation products and pathways

Dissipation potential of four algae viz. Haematococcus pluvialis, Selenastrum capricornutum, Scenedesmus quadricauda and Chlorella vulgaris was investigated against ten antibiotics (sulfamerazine, sulfamethoxazole, sulfamonomethoxine, trimethoprim, clarithromycin, azithromycin, roxithromycin, lomefloxacin, levofloxacin and flumequine) in a series of synthetic wastewater batch culture experiments, maintained at 20, 50 and 100 μg L−1 initial concentration levels and incubated over a period of 40 days. Generally, the antibiotic removal was achieved with overall dissipation percentage (%) varying among the algal species and different antibiotics. Biodegradation was the major antibiotic removal mechanism from the dissolved fraction, with minor contributions of bioadsorption, bioaccumulation, and abiotic factors. The antibiotics dissipation followed the pseudo-first-order-kinetics with the fastest antibiotic degradation rate achieved by H. pluvialis. The Monod kinetics was successfully applied to explain the relationship between the algal growth and the removal of antibiotics and nutrients in the batch cultures. S. capricornutum and C. vulgaris showed more affinity for the macrolides and fluoroquinolones than sulfonamides, while, H. pluvialis and S. quadiricauda showed relatively higher preference for sulfonamides than the other antibiotic groups. A total of 10 transformation products were identified and the transformation pathway was proposed, accordingly. Most of the transformation products had lower toxicity compared with their parent antibiotics.

Removal of veterinary antibiotics from swine wastewater using anaerobic and aerobic biodegradation

High amounts of antibiotics, used in animal farms for the prevention of diseases, are released back into the natural environment with a possible risk of chronic toxicity to other organisms and the development of antibiotic-resistant genes. The antibiotics, including sulfonamides and β-lactams, detected in swine wastewater were between 99.2 and 339.3 μg/L. The typical on-site swine wastewater treatment process turned out to be inadequate, reflected by the high conventional contaminant and antibiotic residuals even under a long hydraulic residence time (HRT, around 2–3 months). The lab-scale combined anaerobic and aerobic biological process showed that anaerobic digestion was mainly responsible for chemical oxygen demand (COD) reduction and aerobic biodegradation contributed significantly to antibiotic removal, with overall removal efficiencies of 95% for COD and 92% for antibiotics under a short HRT of 3.3 days. The removal of selected antibiotics could be a combined result of biodegradation, the balance between adsorption and desorption, and the transformation between antibiotic metabolites and their parent antibiotics. The current work provides valuable insights into the appropriate selection and optimisation of biological processes for the treatment of typical wastewater with high COD and trace antibiotics.

Insights into degradation pathways and toxicity changes during electro-catalytic degradation of tetracycline hydrochloride

The removal of antibiotics has attracted much attention due to their extremely high adverse impacts on the environment. However, the potential risks of degradation intermediates are seldom reported. In this work, the influence of different factors on the electro-catalytic degradation efficiency of tetracycline hydrochloride (TCH) by the prepared carbon nanotubes/agarose/indium tin oxide (CNTs/AG/ITO) electrode was investigated. Under optimal conditions (10 wt% CNTs dosage, pH = 7), the maximum degradation efficiency for TCH (10 mg L−1) reached up to 96% within 30 min treatment with 4 V potential. Superoxide anions (•O2−) played an important role in the electro-catalytic degradation. Totally 10 degradation intermediates were identified using HPLC-MS/MS, and the degradation pathway was proposed. Toxicities of the parent antibiotic and the identified intermediates were calculated using the ECOSAR (Ecological Structure Activity Relationship) program in EPISuite, and results showed that more toxic intermediates were generated. The maximal chronic toxicity for green algae of the intermediate increased 1439.92 times. Furthermore, antimicrobial activity was further verified by disk agar biocidal tests with Escherichia coli ATCC25922 and higher biotoxicity intermediates compared with parent compounds were confirmed to be formed. Therefore, more attention should be paid on the potential risk of degradation intermediates in the treatment of wastewater containing antibiotics.

Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone-dichloroacetic acid hybrids.

A series of new fluoroquinolone conjugates 8a-g and 9a-f were synthesized via benzotriazole-mediated synthetic approach with good yield and purity. Some of the synthesized analogs exhibited significant antibacterial properties against Escherichia coli and Staphylococcus aureus with potency higher than that of the parent drugs through in vitro standard bioassay procedure (conjugates 8c and 8d reveal antimicrobial properties with potency 1.9, 61.9, 20.7 and 2.4, 37.1, 8.3 folds relative to the parent antibiotic 6 against E.coli, S.aureus, and Enterococcus faecalis, respectively). The observed experimental data were supported by enzymatic DNA gyrase inhibitory property. Developed BMLR-QSAR model validates the observed experimental data and recognizes the parameters responsible for the enhanced antibacterial properties.

Reactivity of unactivated peroxymonosulfate with nitrogenous compounds

A recent investigation has demonstrated that peroxymonosulfate (PMS), a peroxide commonly applied as a radical precursor during advanced oxidation processes (AOPs), can degrade organic contaminants without the involvement of radicals. However, little is known about this non-radical reaction mechanism. In this study, the reactivity of PMS with several nitrogenous compounds was investigated. Fluoroquinolone antibiotics (except for flumequine) were rapidly degraded by direct PMS oxidation, followed by aliphatic amines (e.g., metoprolol and venlafaxine) and nitrogenous heterocyclic compounds (e.g., adenine and caffeine) at pH 8. The degradation rate of fluoroquinolones followed a second-order kinetic and was highly pH and structure-dependent. Unlike the radical-based AOPs, the direct degradation of contaminants by PMS was less influenced by the scavenging effect of the water matrix. High-Resolution Mass Spectrometry (HRMS) analysis demonstrated that the piperazine ring of fluoroquinolones was the main reaction site. Results showed that the direct electron-transfer from nitrogenous moieties (piperazine ring) to PMS can produce amide and aldehyde compounds. An amide-containing transformation product of ciprofloxacin (m/z 320), showing the highest signal intensity on HRMS, was previously recorded during ozonation. Moreover, the hydroxylamine analogue of ciprofloxacin and enrofloxacin N-oxide were tentatively identified, and the formation of the latter was not impacted by the dissolved oxygen in water. These results suggested that PMS also reacts with nitrogenous compounds via oxygen transfer pathway. Agar disk-diffusion tests indicated that PMS treatment efficiently removed the antibacterial activity of ciprofloxacin with the complete degradation of parent antibiotic, except for the transformation products in an earlier stage, which might still exert antibacterial potency.

Uptake and metabolism of clarithromycin and sulfadiazine in lettuce

Antibiotics are introduced into agricultural fields by the application of manure or biosolids, or via irrigation using reclaimed wastewater. Antibiotics can enter the terrestrial food chains through plant uptake, which forms an alternative pathway for human exposure to antibiotics. However, previous studies mainly focused on detecting residues of the parent antibiotics, while ignoring the identification of antibiotics transformation products in plants. Here, we evaluated the uptake and metabolism of clarithromycin (CLA) and sulfadiazine (SDZ) in lettuce under controlled hydroponic conditions. The antibiotics and their metabolites were identified by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-QToF-MS/MS) and ultra-performance liquid chromatograph Micromass triple quadrupole mass spectrometry (UPLC−QqQ−MS/MS). The structure of CLA, SDZ and N-acetylated SDZ were confirmed with synthesized standards, verifying the reliability of the identification method. Eight metabolites of CLA and two metabolites of SDZ were detected in both the leaves and roots of lettuce. The metabolites of CLA included phases I and II transformation products, while only phase II metabolites of SDZ were observed in lettuce. The proportion of CLA metabolites was estimated to be greater than 70%, indicating that most of the CLA was metabolized in plant tissues. The proportion of SDZ metabolites was lower than 12% in the leaves and 10% in the roots. Some metabolites might have the ability to increase or acquire antibacterial activity. Therefore, in addition to the parent compounds, metabolites of antibiotics in edible vegetables are also worthy of study for risk assessment and to determine the consequences of long-term exposure.

Synthesis and evaluation of biological activity for dual-acting antibiotics on the basis of azithromycin and glycopeptides

One of the promising directions of the combined approach is the design of dual-acting antibiotics – heterodimeric structures on the basis of antimicrobial agents of different classes. In this study a novel series of azithromycin-glycopeptide conjugates were designed and synthesized. The structures of the obtained compounds were confirmed using NMR spectroscopy and mass spectrometry data including MS/MS analysis. All novel hybrid antibiotics were found to be either as active as azithromycin and vancomycin against Gram-positive bacterial strains or have superior activity in comparison with their parent antibiotics. One compound, eremomycin-azithromycin conjugate 16, demonstrated moderate activity against Enterococcus faecium and Enterococcus faecalis strains resistant to vancomycin, and equal to vancomycin’s activity for the treatment of mice with Staphylococcus aureus sepsis.

Derivatives of Ribosome-Inhibiting Antibiotic Chloramphenicol Inhibit the Biosynthesis of Bacterial Cell Wall.

Here, we describe the preparation and evaluation of α,β-unsaturated carbonyl derivatives of the bacterial translation inhibiting antibiotic chloramphenicol (CAM). Compared to the parent antibiotic, two compounds containing α,β-unsaturated ketones (1 and 4) displayed a broader spectrum of activity against a panel of Gram-positive pathogens with a minimum inhibitory concentration range of 2-32 μg/mL. Interestingly, unlike the parent CAM, these compounds do not inhibit bacterial translation. Microscopic evidence and metabolic labeling of a cell wall peptidoglycan suggested that compounds 1 and 4 caused extensive damage to the envelope of Staphylococcusaureus cells by inhibition of the early stage of cell wall peptidoglycan biosynthesis. Unlike the effect of membrane-disrupting antimicrobial cationic amphiphiles, these compounds did not rapidly permeabilize the bacterial membrane. Like the parent antibiotic CAM, compounds 1 and 4 had a bacteriostatic effect on S.aureus. Both compounds 1 and 4 were cytotoxic to immortalized nucleated mammalian cells; however, neither caused measurable membrane damage to mammalian red blood cells. These data suggest that the reported CAM-derived antimicrobial agents offer a new molecular scaffold for development of novel bacterial cell wall biosynthesis inhibiting antibiotics.

Pore-forming activity of new conjugate antibiotics based on amphotericin B.

A series of amides of the antifungal antibiotic amphotericin B (AmB) and its conjugates with benzoxaboroles was tested to determine whether they form pores in lipid bilayers and to compare their channel characteristics. The tested derivatives produced pores of larger amplitude and shorter lifetime than those of the parent antibiotic. The pore conductance was related to changes in the partial charge of the hydrogens of the hydroxyl groups in the lactone ring that determined the anion coordination in the channel. Neutralization of one of the polar group charges in the AmB head during chemical modification produced a pronounced effect by diminishing the dwell time of the polyene channel compared to modification of both groups. In this study, compounds that had a modification of one carboxyl or amino group were less effective in initializing phase separation in POPC-membranes compared to derivatives that had modifications of both polar groups as well as the parent antibiotic. The effects were attributed to the restriction of the aggregation process by electrical repulsion between charged derivatives in contrast to neutral compounds. The significant correlation between the ability of derivatives to increase the permeability of model membranes—causing the appearance of single channels in lipid bilayers or inducing calcein leakage from unilamellar vesicles—and the minimal inhibitory concentration indicated that the antifungal effect of the conjugates was due to pore formation in the membranes of target cells.

Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates

A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.

Redox-mediator-free degradation of sulfathiazole and tetracycline using Phanerochaete chrysosporium

ABSTRACTThe removal of two of the most commonly used antibiotics, tetracycline (TC) and sulfathiazole (STZ), using laccase-producing Phanerochaete chrysosporium was studied in liquid-phase batch experiments in the absence of any synthetic redox mediator. The removal of STZ and TC from single antibiotic spikes varied from 97.8% to 15.4% and 98.8% to 31%, respectively, with increasing initial doses of 10–250 mg L−1 within 14 days of incubation. The enzyme activity of P. chrysosporium was only minimally influenced by the concentrations of these antibiotics. The degradation of antibiotics initiated before an appreciable extracellular enzyme activity was noted in the fungal culture. The appearance of low-molecular weight molecular fragments from parent antibiotics in liquid chromatography–mass spectrometry confirmed the biodegradation process.