Synthetic Antibacterial Agents Research Articles

8-Amino-7-(aryl/hetaryl)fluoroquinolones. An emerging set of synthetic antibacterial agents.

This study reports the synthesis of seven new 8-amino-7-(aryl/hetaryl)fluoroquinolones and their antibacterial activity against 10 bacteria associated with microbial infections and foodborne illnesses. These fluoroquinolones are prepared via the reactions of selected aryl(hetaryl)boronic acids with ethyl-7chloro-6-fluoro-8-nitroquinolone-3-carboxylate, under Suzuki-Miyaura cross-coupling conditions. Nitro group reduction of the latter resulted in the corresponding 8-aminoquinolone-3-esters which upon hydrolysis formed the respective 8-amino-7-(aryl/hetaryl)-quinolone-3-carboxylic acids. The latter compounds were tested against selected Gram-negative bacteria (Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumonia) and Gram-positive bacteria (Enterococcus feacalis, Listeria monocytogenes, Streptococcus agalactiae, Staphylococcus epidermidis, and Staphylococcus aureus). The tested fluoroquinolones showed a significant antimicrobial activity against most of the tested bacterial strains. The antimicrobial activity of some of the tested compounds were comparable to or higher than a wide range of standard antibiotics including ampicillin, ciprofloxacin, and imipenem. The results highlight the new synthesized 8-amino-7-(aryl/hetaryl)fluroquinolones as promising candidates for new antimicrobial drugs to treat bacterial infections. This study highlights that the newly synthetic 8-amino-7-(aryl/hetaryl)fluroquinolones are promising candidates for new antimicrobial drugs to treat human diseases including foodborne illnesses.

Recent advances in oxazolidinones as antituberculosis agents.

Tuberculosis (TB) is an infectious and fatal disease caused by Mycobacterium tuberculosis (Mtb) and remains a serious public health threat; therefore, the development of new antitubercular agents is a priority for the World Health Organization's End TB strategy and the United Nations' Sustainable Development Goals to eradicate TB. Oxazolidinones are a class of synthetic antibacterial agents with a distinct mode of action developed for the treatment of Gram-positive bacterial infections. Many oxazolidinones exhibit good activity against Mtb, and some are currently in clinical trials for multidrug-resistant TBand extensively drug-resistant TBtherapy. In this review, the mechanism of action, activityand toxicity of oxazolidinonesand recent progress in the research and development of oxazolidinones as anti-TB agentsare summarized.

New Potential Pharmacological Targets of Plant-Derived Hydroxyanthraquinones from Rubia spp.

The increased use of polyphenols nowadays poses the need for identification of their new pharmacological targets. Recently, structure similarity-based virtual screening of DrugBank outlined pseudopurpurin, a hydroxyanthraquinone from Rubia cordifolia spp., as similar to gatifloxacin, a synthetic antibacterial agent. This suggested the bacterial DNA gyrase and DNA topoisomerase IV as potential pharmacological targets of pseudopurpurin. In this study, estimation of structural similarity to referent antibacterial agents and molecular docking in the DNA gyrase and DNA topoisomerase IV complexes were performed for a homologous series of four hydroxyanthraquinones. Estimation of shape- and chemical feature-based similarity with (S)-gatifloxacin, a DNA gyrase inhibitor, and (S)-levofloxacin, a DNA topoisomerase IV inhibitor, outlined pseudopurpurin and munjistin as the most similar structures. The docking simulations supported the hypothesis for a plausible antibacterial activity of hydroxyanthraquinones. The predicted docking poses were grouped into 13 binding modes based on spatial similarities in the active site. The simultaneous presence of 1-OH and 3-COOH substituents in the anthraquinone scaffold were emphasized as relevant features for the binding modes’ variability and ability of the compounds to strongly bind in the DNA-enzyme complexes. The results reveal new potential pharmacological targets of the studied polyphenols and help in their prioritization as drug candidates and dietary supplements.

Evaluation of New Antimicrobial Agents Based on tris(1H-Indol-3-yl)methylium Salts: Activity, Toxicity, Suppression of Experimental Sepsis in Mice.

The antimicrobial activity and toxicity of three novel synthetic antibacterial agents containing tris(1H-indol-3-yl)methylium fragment were studied in vitro and in vivo. All compounds in vitro revealed high activity (minimal inhibitory concentration (MIC) 0.13–1.0 µg/mL) against bacteria that were either sensitive or resistant to antibiotics, including multidrug-resistant clinical isolates. The derivatives combining high antimicrobial activity with relatively low cytotoxicity against human donor fibroblasts HPF-hTERT were subjected to further testing on mice. In vivo they revealed fairly good tolerance and relatively low toxicity. Acute toxicity was evaluated, and the main indicators of toxicity, including LD50 and LD10, were determined. A study of compounds in vivo showed their efficiency in the model of staphylococcal sepsis in mice. The efficiency of compounds may be due to the ability of indolylmethylium salts to form pores in the cytoplasmic membrane of microbial cells and thereby facilitate the penetration of molecules into the pathogen.

Discovery of a novel class of small-molecule antibacterial agents against Staphylococcus aureus.

Background: With constantly increasing resistance against the known antibiotics, the search for novel antibacterial compounds is a challenge. The number of synthetic antibacterial agents is limited. Materials & methods: We discovered novel small-molecule antibacterial agents that are accessible via a simple two-step procedure. The evaluation against Staphylococcus aureus showed antibacterial effects depending on the substituent positioning at the residues of the molecular scaffold. Additionally, we investigated the potential of the compounds to increase the antibacterial activity of tetracycline. Results: The most effective antibacterial compounds possessed a 3-methoxy function at an aromatic residue. In combination with tetracycline, we found a strong effect for a few compounds in boosting the antibacterial activity, so the first promising lead compounds with dual activities could be identified.

Bio colourants from the waste leaves of Ginkgo biloba L. tree: Wool dyeing and antimicrobial functionalization against some antibiotic-resistant bacterial strains

This research focuses on flavonoid-based natural dyes for the coloration and antibacterial finishing of wool fabrics. In the present study, we accessed the suitability of biocolorants from Gingko biloba L. waste/fallen leaves extract to develop colored antibacterial wool fabrics to reduce the environmental pollution and dependency of the textile industry on the synthetic antibacterial agents. Specifically, we present a novel method to counteract the growing antibiotic resistance using G. biloba L. leaves extract as a potent antibacterial agent in conjunction with ampicillin. Natural colorants were extracted in 50% aqueous ethanol at 70 °C for 60 min under acid conditions of pH 3. Before dyeing procedures, the extracted dye powder was assessed for thermal stability by TGA analysis. Structural characterization of the extracted dye was done by UV–visible and FT-IR spectral analysis. Optimal dyeing results were achieved at 90 °C for 70 min with a dye concentration of 50% (o.w.f.). Additionally, dye adsorption (Isotherm constants) and dye performances were effectively reported during this study. Pseudo-second order and sips isotherm model provided the best fitting of experimental data with high regression coefficient (R2 = 0.99). Valuated indicators (color strength (K/S), color characteristics, and fastness properties) of dyed wool fabric were effectively reported in response to washing pretreated with different metallic and natural mordants. The antibacterial potential of extracted natural dye was enhanced in combination with ampicillin (synergism) which can be correlated with the significant reduction in the corresponding MIC values. Fe2+ and Sn2+ salts demonstrated negative effects on the antibacterial performance of the dyed wool fabric, whereas most of the biomordants showed enhanced antibacterial performances. The effective use of the extracted yellow dye from G. biloba L. fallen/waste leaves in textile dyeing and finishing will enhance the industrial applications of the green waste over its normal applications.

An insight into non-covalent interactions in binary, ternary and quaternary copper (II) complexes: Synthesis, X-ray structure, DFT calculations, antimicrobial activity and molecular docking studies

Levofloxacin is a synthetic antibacterial agent that effectively inhibits DNA replication and is commonly used for the treatment of genitourinary, respiratory, and gastrointestinal tract infections. Metallodrugs interact with DNA, RNA, proteins, receptors, and lipids, making them unique and more effective as chemotherapy agents than their parent drugs. On this basis, herein four copper(II) complexes assembled from antibacterial levofloxacin ligand were synthesized and characterized using different analytical and spectroscopic measurements. X- ray perceived the formation of a ternary dimer and a ternary monomer complexes both in distorted square pyramidal geometry, with the existence of levofloxacin in a zwitterionic form. The other two complexes were verified, as binary and quaternary complexes having distorted octahedral geometry. Structure elucidation of these complexes was also explored by density functional theory methods and optimized geometrical parameters. Ternary dimer complex demonstrated higher stability than the ternary monomer complex. Natural bond orbital (NBO) analysis and molecular electrostatic potential (MESP)were investigated. Electronic absorption spectra of the optimized structure were performed using the time-dependent density functional theory (TD-DFT)/CAM-B3LYP method with LANL2DZ basis set in the gas phase. Binary copper complex exhibited significant antimicrobial activity and ternary monomer complex was more potent than ternary dimer complex. Interestingly levofloxacin and ternary copper complexes were completely devoid of antifungal activity, whereas octahedral binary and quaternary copper complexes displayed antifungal activity. In-silico molecular docking studies were accomplished with 3T88 (E-Coli) and 2GNP (S. pneumonia) receptors. Results proved powerful interaction at the docked site through the formation of hydrogen bond and van der wall interactions.

FORMULATION, OPTIMIZATION AND EVALUATION OF MOXIFLOXACIN HYDROCHLORIDE GASTRO RETENTIVE TABLETS

The objective of the current study was to develop gastro retentive formulation of moxifloxacin. HCl using various drug release modifiers and performing in vitro and in in vivo evaluations. Moxifloxacin is a novel synthetic fluoro quinolone antibacterial agent. Floating, muco adhesive tablets of moxifloxacin. HCl were prepared using variable amounts of HPMCK100M, Lannea coromandelica gum by direct compression technique and wet granulation technique, respectively. Formulations were developed, optimized and checked for pharmacopoeial tests. Results show that all the batches lie within the standard limits. Dissolution parameters of all formulations were sy=ubjected to kinetic fitting and various statistical parameters were determined. Formulation (FS5 ) containing 50 mg of HPMCK100M and 50 mg of LCG, is the best formulation showing similarity f2 =71.734, f1 = 4.271 with the marketed product (Avelox). It follows Higuchi's kinetics, non-fickian diffusion first order kinetics(n=0.717). In vivo studies were performed for the FS5 with 6 healthy rabbits and pharmacokinetic parameters were determined, compared with Avelox and it was found that FS5 produced similar results. Stability studies were performed for FS5 as per ICH guidelines. Results were found to be satisfactory. FS5 is expected to improve patient compliance by means of providing good clinical outcome

Recent Advances in the Use of the Dimerization Strategy as a Means to Increase the Biological Potential of Natural or Synthetic Molecules.

The design of C2-symmetric biologically active molecules is a subject of interest to the scientific community. It provides the possibility of discovering medicine with higher biological potential than the parent drugs. Such molecules are generally produced by classic chemistry, considering the shortness of reaction sequence and the efficacy for each step. This review describes and analyzes recent advances in the field and emphasizes selected C2-symmetric molecules (or axial symmetric molecules) made during the last 10 years. However, the description of the dimers is contextualized by prior work allowing its development, and they are categorized by their structure and/or by their properties. Hence, this review presents dimers composed of steroids, sugars, and nucleosides; known and synthetic anticancer agents; polyphenol compounds; terpenes, known and synthetic antibacterial agents; and natural products. A special focus on the anticancer potential of the dimers transpires throughout the review, notwithstanding their structure and/or primary biological properties.

The Application of Triclosan in antibacterial finishing on 100% cotton fabric

The demand for antibacterial fabric has been recently increasing in the medical textiles. The fibers used in textile products, especially those made from natural fibers with a large surface area and good moisture-retention capacity, provide a favorable condition for microbial growth. They are present almost everywhere and multiply rapidly, depending on moisture, nutrients, and the environment in which they live. The growth of microorganisms on textile products has caused a series of undesirable effects, not only on the product but also on the user of the products. Cotton fabric is easy to wrinkle. When exposed to a humid environment, it is susceptible to damage caused by microorganisms. Therefore, antibacterial treatment for Cotton fabric 100% is a important requirement in the textiles and garments depending on the intended use and is a prerequisite for fabric products in the medical field. Many antibacterial agents for textiles are already known such as organo-metallics, phenols, quaternary ammonium salts. Triclosan is a popular antibacterial chemical. Triclosan is present everywhere in life from consumer products such as toothpaste, soap, detergents, toys, household appliances to cosmetics. Especially Triclosan is an antibacterial agent used quite a lot in the textile industry. Triclosan with chlorinated phenol, a synthetic chemical, is common and potential antibacterial agent. In this study, The technical parameters were investigated include Triclosan concentration, dipping time, drying temperature, citric acid concentration to evaluate the effects of treated parameters on the antimicrobial efficiencies of the 100% cotton fabrics. The results show that cotton fabrics after finishing treatment with Triclosan and applying citric acid (CA) as important bonding chemical have good antibacterial ability and also have improved durable antibacterial properties after 5 launderings. The antibacterial properties of treated cotton fabrics was evaluated based on ASTM E2149-01 standard, the experiment was done with E.Coli ATCC 25922 and S. Aureus ATCC 6538.

Formulation Development and evaluation of mucoadhesive tablets for vaginal delivery of metronidazole

Vaginitis is a very common gynecological problem in women of all age groups. Metronidazole is a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class and used against protozoa such as Trichomonas vaginalis, amebiasis, and giardiasis. The present study was aimed with the application of chitosan in combination with anionic polymers for the design and development of mucoadhesive tablets for vaginal delivery of Metronidazole. Matrix tablets of metronidazole were prepared in combination with polyelectrolyte complex by wet granulation method and further characterized for various formulation parameters, in-vitro muco adhesion and antimicrobial activity. The developed formulation showed significant mucoadhesion due to presence of chitosan or carrageenan and ionisation of amino groups of chitosan at pH 5.2. The developed formulation showed desirable characteristics in terms of FTIR, DSC, SEM, in vitro drug release, swelling behaviour as well for mucoadhesion and antimicrobial potential compared with the marketed formulation. In overall developed dosage form imparts desirable characteristics in formulation for vaginal delivery of metronidazole with enhanced therapeutic effects. Thus, this dosage form can be further investigated for therapeutic applications of metronidazole in vaginal drug delivery.

Selective delivery of silver nanoparticles for improved treatment of biofilm skin infection using bacteria-responsive microparticles loaded into dissolving microneedles

The treatment of infected chronic wounds has been hampered by development of bacterial biofilms and the low penetration of antibacterial compounds delivered by conventional dosage forms. Numerous bacterial biofilm formers have shown resistance to synthetic antibacterial agents. In this study, we explore the potential of silver nanoparticles (NPs) synthesized using green tea extract as antibiofilm agents against Staphylococcus aureus (SA) and Pseudomonas aeruginosa (PA) biofilms. Due to the toxicity of silver NPs, for the first time, silver NPs were incorporated into bacteria-responsive microparticles (MPs) prepared from poly (Ɛ-caprolactone) decorated with chitosan. The in vitro release of silver NPs from MPs increased up to 9-times in the presence of SA and PA, showing the selectivity of this approach. Incorporation of the MPs into dissolving microneedles (DMNs) could enhance the dermatokinetic profiles of silver NPs compared to DMNs containing silver NPs without MP formulations and conventional cream formulations. Furthermore, 100% of bacterial bioburdens were eradicated on ex vivo biofilm model in rat skin following 60 h of the administration of this system. The findings revealed here confirmed the feasibility of the loading of silver NPs into responsive MPs for improved antibiofilm activities when delivered using DMNs. Following on from these promising results, toxicity and in vivo pharmacodynamic studies should now be carried out in an appropriate model.

Exploration into the origins and mobilization of di-hydrofolate reductase genes and the emergence of clinical resistance to trimethoprim.

Trimethoprim is a synthetic antibacterial agent that targets folate biosynthesis by competitively binding to the di-hydrofolate reductase enzyme (DHFR). Trimethoprim is often administered synergistically with sulfonamide, another chemotherapeutic agent targeting the di-hydropteroate synthase (DHPS) enzyme in the same pathway. Clinical resistance to both drugs is widespread and mediated by enzyme variants capable of performing their biological function without binding to these drugs. These mutant enzymes were assumed to have arisen after the discovery of these synthetic drugs, but recent work has shown that genes conferring resistance to sulfonamide were present in the bacterial pangenome millions of years ago. Here, we apply phylogenetics and comparative genomics methods to study the largest family of mobile trimethoprim-resistance genes (dfrA). We show that most of the dfrA genes identified to date map to two large clades that likely arose from independent mobilization events. In contrast to sulfonamide resistance (sul) genes, we find evidence of recurrent mobilization in dfrA genes. Phylogenetic evidence allows us to identify novel dfrA genes in the emerging pathogen Acinetobacter baumannii , and we confirm their resistance phenotype in vitro. We also identify a cluster of dfrA homologues in cryptic plasmid and phage genomes, but we show that these enzymes do not confer resistance to trimethoprim. Our methods also allow us to pinpoint the chromosomal origin of previously reported dfrA genes, and we show that many of these ancient chromosomal genes also confer resistance to trimethoprim. Our work reveals that trimethoprim resistance predated the clinical use of this chemotherapeutic agent, but that novel mutations have likely also arisen and become mobilized following its widespread use within and outside the clinic. Hence, this work confirms that resistance to novel drugs may already be present in the bacterial pangenome, and stresses the importance of rapid mobilization as a fundamental element in the emergence and global spread of resistance determinants.

Inhibition of Breast Cancer Resistance Protein (BCRP) by Ko143 Can Affect Pharmacokinetics of Enrofloxacin in Exopalaemon carinicauda

Adenosine triphosphate-binding cassette transporter breast cancer resistance protein (BCRP) exists highly in the apical membranes of epithelia, and is involved in drug availability. Ko143 is a typical inhibitor of BCRP in rodents. The synthetic antibacterial agent enrofloxacin (ENRO) is a fluoroquinolone employed as veterinary and aquatic medicine, and also a substrate for BCRP. BCRP gene highly expressed in the hepatopancreas and intestine of Exopalaemon carinicauda as was determined with real-time quantitative reverse transcription-polymerase chain reaction (RT-qPCR) method. The effects of Ko143 on the abundance of BCRP mRNA and ENRO pharmacokinetics in E. carinicauda were studied. The mRNA abundance of BCRP decreased significantly in hepatopancreas and intestine (P <0.05) after Ko143 treatment. Co-administration of Ko143 significantly changed the pharmacokinetics of orally administered enrofloxacin, which was supported by higher distribution half-life (t1/2α), elimination half-life (t1/2β), area under the curve up to the last measurable concentration (AUC0-t), peak concentration (Cmax) and lower clearance (CL/F). These findings revealed that Ko143 downregulates BCRP expression in hepatopancreas and intestine, thus affects the pharmacokinetics of orally administered enrofloxacin in E. carinicauda. The drug-drug interaction can be caused by the change in BCRP activity if ENRO is used in combination with other drugs in shrimp.

Disposition of cyadox in domesticated cats following oral, intramuscular, and intravenous administration.

Cyadox (CYX) is a synthetic antibacterial agent of quinoxaline with much lower toxic effects. A safety criterion of CYX for clinical use was established by studying the pharmacokinetics and metabolism of CYX after oral (PO), intramuscular (IM), and intravenous (IV) administration. CYX was administered in six domesticated cats (three males and three females) by PO (40mg/kg.b.w.), IM (10mg/kg.b.w.), and IV (10mg/kg.b.w.) routes in a crossover pattern. Highly sensitive liquid chromatography with ultraviolet detection (HPLC-UV) method was developed for detection of CYX and its metabolites present in plasma, urine, and feces. The bioavailability of CYX after PO and IM routes was 4.37% and 84.4%. The area under curves (AUC), mean resident time (MRT), and clearance (CL) of CYX and its metabolites revealed that CYX quickly metabolized into its metabolites. The total recovery of CYX and its main metabolites was >60% after each route. PO delivery suggesting first pass effect in cats that might make this route suitable for intestinal infection and IM injection could be better choice for systemic infections. Less ability of glucuronidation did not show any impact on CYX metabolism. The findings of present study provide detailed information for evaluation of CYX.

Biological activity tuning of antibacterial urotropineviaco-crystallization: synthesis, biological activity evaluation and computational insight

Urotropine (1) is a synthetic heterocyclic antibacterial agent.

Outline of Animals and Plants-Basedantimicrobial agents (NAA) in Antimicrobial food packaging(AFP):Anew paradigm in food industry

Natural compounds due to their less toxicity for human health are desired for antimicrobial food packaging. Natural compounds derived from plants, animals and microorganisms such as oils, phenols, terpenes, aliphatic compounds, aldehydes, organic acids and glucosinolates. Polyphenol around food inhibits gas exchange, moisture, flavor and other soluble transfer, hence, increase shelf life. Less use of phenols in food is enhanced by using polyphenols in the food industry, that maintain superficial expression, lowering bacterial activity at upper surfaced of vegetables, fruits and raw muscle food. From hypothetical studies, it is estimated that synthetic or artificial antibacterial agents are more beneficial as compared to the natural. Microbe’s free food is an innovative demand of the food industry and it is need of the hour to use cheaper safer and healthy ways for the preservation of food. The meat industry is dependent on the antimicrobial packaging which is necessary for the safety of the meat. Efficient packaging and antimicrobial agents are the main aspects of the best quality and safety of meat and meat products. This review gives new insight into natural compounds used for antimicrobial food packaging and the application of antimicrobial food packaging.

Development and Evaluation of In-situ gel containing Linezolid and Diclofenac Sodium in the treatment of Periodontitis

Periodontal treatment aims at reduction of infection and inflammation. Linezolid is a synthetic antibacterial agent of a new class of antibiotics, the oxazolidinones, which has clinical utility in the treatment of infections caused by aerobic and anaerobic bacteria susceptible organisms methicillin and vancomycin-resistant in the treatment of periodontitis. Diclofenac sodium is anti-inflammatory agent and in-situ gel containing Linezolid and Diclofenac sodium in this study may have a potential additive effect. Hence, there is broad scope for research in local application of antimicrobial and anti-inflammatory combination drug (s) in periodontitis. Linezolid and Diclofenac sodium. In-situ gel containing Linezolid in combination with Diclofenac sodium was prepared using combination of carbopol-HPMC and carbopol-NaCMC. The prepared in-situ gel formulation showed satisfactory results for in-vitro gelling capacity, rheology, and other physical properties. In-vitro drug release profile was dependent up on the concentration of polymer, i.e. drug release was decreased with increase in polymer concentration and vice versa. The formulations of batches LDCF1, LDCF2, LDCF3, LDSF1, LD SF2 and LDSF3 failed to extend the drug release up to 12 hours. Thus, the formulation of batches LDCF4 and LDSF4 containing carbopol: HPMC and carbopol: NaCMC in 1: 2 ratios were considered as optimum formulation on the basis of optimum viscosity, gelation time, gelation temperature, gelling capacity, and their capacity to extend the in-vitro drug release up to 12 hours. Hence, prepared formulations showed sustain drug release behaviour.

Co-delivery of Diverse Therapeutic Compounds Using PEG–PLGA Nanoparticle Cargo against Drug-Resistant Bacteria: An Improved Anti-biofilm Strategy

Controlling biofilms of bacteria is a challenging aspect because of their drug-resistance potentials against a range of antibiotics, demanding the development of active anti-biofilm agents. Rutin(R), a natural antioxidant, and benzamide(B), a synthetic antibacterial agent, have several pharmacological and antibacterial abilities. Herein, we developed PEG-PLGA NPs that synergistically carried rutin and benzamide as drug candidates, while displaying therapeutic and anti-biofilm functions. These drug delivery NPs were synthesized by the oil-in-water emulsion (O/W) solvent evaporation technique. The obtained NPs were characterized by UV-vis, FT-IR, SEM, TEM, and DLS measurements. Confocal laser scanning microscopy was employed to evaluate theanti-biofilmcapabilities against Staphylococcus aureus and Pseudomonas aeruginosa and further quantified the levels of residual biofilm constituents such as protein and exopolysaccharide (EPS). Drug release experiments showed the controlled release of rutin-benzamide (RB)for several days. Antibacterial analyses showed that the minimum inhibitory concentration (MIC) of NPs was at least two times lower than that of the free drugs. RB-PEG-PLGA NPs revealed that they targeted biofilm-forming bacteria through the disruption of the membrane and biofilm surface and were observed to be nontoxic when tested using human erythrocytes and human cell lines. In vivo evaluations in zebrafish showed that the NPs did not alter the antioxidant functions and histological features of tissues. On the basis of results obtained, it is substantiated that the rutin-benzamide-loaded nanocarrier offers potential anti-biofilm therapy due to its high anti-biofilmactivity and biocompatibility.

Antibacterial based on IPBCC.08.610 glucose oxidase against UDP-N-acetyl glucosamine enolpyruvyl transferase and elongation factor G enzymes in silico

The use of a synthetic antibacterial agent as food preservatives could develop several health problems thus the user should be reduced. Enzyme-based antibacterial is a natural antibacterial that could substitute the latter antibacterials. Enzyme-based antibacterials have several ways that can be used to inactivate microbes, one of them utilize enzyme catalysis products. The aim of this research is to study the interaction between IPBCC.08.610 glucose oxidase (NCBI accession number MH593586) catalysis product against MurA and EFG enzymes using computational investigation. We confirmed that the gene sequence from previous research is truly encoding the IPBCC.08.610 glucose oxidase. Gluconolactone and gluconic acid are less effectively absorbed by microbes. Gluconolactone and gluconic acid are capable to interact with Cys115 and Asp305 of MurA, meanwhile, it does not interact with Phe90 and Thr84 of EFG. Gluconolactone and gluconic acid can inhibit MurA effectively but not on EFG.