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  1. Huang M, Ma Y, Qian J, Sokolova IM, Zhang C, Waiho K, et al.
    J Hazard Mater, 2024 Apr 15;468:133801.
    PMID: 38377908 DOI: 10.1016/j.jhazmat.2024.133801
    Pollution with anthropogenic contaminants including antibiotics and nanoplastics leads to gradual deterioration of the marine environment, which threatens endangered species such as the horseshoe crab Tachypleus tridentatus. We assessed the potential toxic mechanisms of an antibiotic (norfloxacin, 0, 0.5, 5 μg/L) and polystyrene nanoparticles (104 particles/L) in T. tridentatus using biomarkers of tissue redox status, molting, and gut microbiota. Exposure to single and combined pollutants led to disturbance of redox balance during short-term (7 days) exposure indicated by elevated level of a lipid peroxidation product, malondialdehyde (MDA). After prolonged (14-21 days) exposure, compensatory upregulation of antioxidants (catalase and glutathione but not superoxide dismutase) was observed, and MDA levels returned to the baseline in most experimental exposures. Transcript levels of molting-related genes (ecdysone receptor, retinoic acid X alpha receptor and calmodulin A) and a molecular chaperone (cognate heat shock protein 70) showed weak evidence of response to polystyrene nanoparticles and norfloxacin. The gut microbiota T. tridentatus was altered by exposures to norfloxacin and polystyrene nanoparticles shown by elevated relative abundance of Bacteroidetes. At the functional level, evidence of suppression by norfloxacin and polystyrene nanoparticles was found in multiple intestinal microbiome pathways related to the genetic information processing, metabolism, organismal systems, and environmental information processing. Future studies are needed to assess the physiological and health consequences of microbiome dysbiosis caused by norfloxacin and polystyrene nanoparticles and assist the environmental risk assessment of these pollutants in the wild populations of the horseshoe crabs.
    Matched MeSH terms: Norfloxacin/toxicity
  2. Gorajana A, Kit WW, Dua K
    Recent Pat Drug Deliv Formul, 2015;9(2):167-82.
    PMID: 25714525
    OBJECTIVE: Norfloxacin has a low aqueous solubility which leads to poor dissolution. Keeping this fact in mind the purpose of the present study is to formulate and evaluate norfloxacin solid dispersion.

    METHODS: Solid dispersions were prepared using hydrophilic carriers like polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974pNF (CP) in various ratios using solvent evaporation technique. These formulations were evaluated using solubility studies, dissolution studies; Fourier transmitted infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetery (DSC). The influence of polymer type and drug to polymer ratio on the solubility and dissolution rate of norfloxacin was also evaluated.

    RESULTS: FTIR analysis showed no interaction of all three polymers with norfloxacin. The results from XRD and DSC analyses of the solid dispersion preparations showed that norfloxacin existsin its amorphous form. Among the Norfloxacin: PEG solid dispersions, Norfloxacin: PEG 1:14 ratio showed the highest dissolution rate at pH 6.8. For norfloxacin: PVP solid dispersions, norfloxacin: PVP 1:10 ratio showed the highest dissolution rate at pH 6.8. For Norfloxacin: CP solid dispersions, norfloxacin: P 1:2 ratio showed the highest dissolution rate at pH 6.8.

    CONCLUSION: The solid dispersion of norfloxacin with polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974p NF (CP), lends an ample credence for better therapeutic efficacy.

    Matched MeSH terms: Norfloxacin/pharmacokinetics; Norfloxacin/chemistry*
  3. Cheong YM, Joseph PG, Koay AS
    PMID: 3477872
    The current drugs recommended for treatment of melioidosis are tetracycline, chloramphenicol and cotrimoxazole. Unfortunately these drugs are not the drug of choice in an acutely ill patient with septicaemia prior to the availability of laboratory results. With the discovery of the new cephalosporins which have a broad spectrum of activity clinicians are using them either alone or in combination with other antibiotics in such critical situations. Hence, an in-vitro study was carried out on the susceptibility of 41 strains of P. pseudomallei isolated in Malaysia, to these new cephalosporins and a new quinolone. The results showed that all the cephalosporins tested had some activity on the strains tested, with ceftazidime being the most active drug. Pefloxacin had very poor activity. However, further clinical studies are required to determine the duration, dosage and in-vivo activity of the antibiotics.
    Matched MeSH terms: Norfloxacin/analogs & derivatives*; Norfloxacin/pharmacology
  4. Ma Y, Gao Y, Xu R, Li D, Waiho K, Wang Y, et al.
    Mar Environ Res, 2024 Jan;193:106277.
    PMID: 38040551 DOI: 10.1016/j.marenvres.2023.106277
    Nanoplastics (NPs) and antibiotics (ABs) are two of the emerging marine contaminants that have drawn the most attention in recent years. Given the necessity of figuring out the effects of plastic and antibiotic contamination on marine organism life and population in the natural environment, it is essential to apply rapid and effective biological indicators to evaluate their comprehensive toxic effects. In this study, using mussel (Mytilus coruscus) as a model, we investigated the combined toxic effects of NP (80 nm polystyrene beads) and AB (Norfloxacin, NOR) at environmental-relevant concentrations on antioxidant and immune genes. In terms of the antioxidant genes, NPs significantly increased the relative expression of Cytochrome P450 3A-1 (CYP3A-1) under various concentrations of NOR conditions, but they only significantly increased the relative expression of CYP3A-2 in the high concentration (500 μg L-1 NOR) co-exposure group. In the NP-exposure group which exposed to no or low concentrations of NOR, nuclear factor erythroid 2-related factor 2 (Nrf2) was upregulated. In terms of the immune genes, interleukin-1 receptor-associated kinase (IRAK) -1 showed a significant increase in the low-concentration NOR group while a significant inhibition in the high-concentration NOR group. Due to the presence of NPs, exposure to NOR resulted in a significant increase in both IRAK-4 and heat shock protein (HSP) 70. Our findings indicate that polystyrene NPs can exacerbate the effects of NOR on the anti-oxidant and immune defense performance of mussels. This study delves into the toxic effects of NPs and ABs from a molecular perspective. Given the expected increase in environmental pollution due to NPs and ABs, future research is needed to investigate the potential synergistic effect of NPs and ABs on other organisms.
    Matched MeSH terms: Norfloxacin/metabolism; Norfloxacin/toxicity
  5. Loh GO, Tan YT, Peh KK
    Carbohydr Polym, 2014 Jan 30;101:505-10.
    PMID: 24299805 DOI: 10.1016/j.carbpol.2013.09.084
    The effect of hydroxypropyl methylcellulose (HPMC) concentration on β-cyclodextrin (β-CD) solubilization of norfloxacin was examined. The solubility and dissolution of norfloxacin/β-CD and norfloxacin/β-CD/HPMC inclusion complexes were studied. The presence of β-CD increased significantly the solubility and dissolution of norfloxacin. The addition of HPMC until 5% (w/w) improved the solubilization of norfloxacin but further addition above 5% (w/w), decreased norfloxacin solubilization. Fourier transformed Infra-red (FTIR) showed that norfloxacin was successfully included into β-CD. Differential scanning calorimetry (DSC) showed that the norfloxacin endothermic peak shifted to a lower temperature with reduced intensity indicating the formation of inclusion complex. The addition of HPMC reduced further the intensity of norfloxacin endothermic peak. Most of the sharp and intense peaks of norfloxacin disappeared with the addition of HPMC. In conclusion, the concentration of hydrophilic polymer used to enhance β-CD solubilization of poorly soluble drugs is very critical.
    Matched MeSH terms: Norfloxacin/chemistry*
  6. Walayat K, Ahmad M, Rasul A, Aslam S, Anjum MN, Sultan S, et al.
    Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):855-860.
    PMID: 32863262
    The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon. Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work, norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the treatment with hydrazine hydrate to result in corresponding acetohydrazide 3. A range of substituted benzaldehydes were reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.
    Matched MeSH terms: Norfloxacin/chemical synthesis*; Norfloxacin/pharmacology*
  7. Barman M, Mahmood S, Augustine R, Hasan A, Thomas S, Ghosal K
    Int J Biol Macromol, 2020 Nov 01;162:1849-1861.
    PMID: 32781129 DOI: 10.1016/j.ijbiomac.2020.08.060
    Applying nanotechnology to deliver drug could result in several benefits such as prolong duration of action, enhancement in overall bioavailability, targeting to specific site, low initial loading dose require, systemic stability enhancement etc. Halloysite is one of those clay minerals showing maximum effectiveness when consider as a nano drug carriers for different kind applications. Here, we have used norfloxacin as the model drug for loading into halloysite nanotube (HNT) for its anti-bacterial activity. Norfloxacin was loaded into halloysites by vacuum operation and sonication. The nanotubes were evaluated using X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), scanning electron microscopy (SEM), optical microscopy, water absorption studies, cytotoxicity studies, antimicrobial studies and in vitro diffusion studies. SEM, FT-IR and XRD analysis data showed that the norfloxacin was successfully loaded into nanotubes. TEM analysis confirmed loading of norfloxacin in halloysites' lumen. The halloysite/chitosan nanocomposites were prepared by solvent casting and freeze-drying method. SEM analysis revealed compact and rugged surface of nanocomposites due to existing norfloxacin loaded halloysite. FTIR and XRD confirmed formation of nanocomposite. The nanocomposites showed good antimicrobial effect and good biocompatibility in cytotoxicity study. The in-vitro release studies revealed that halloysite/chitosan nanocomposites were able to sustain the drug release. Also, the nanocomposites were stable in various humidity conditions. Therefore, all the outcomes suggest that the prepared nanocomposites can provide enhanced therapeutic benefits and they can be very potential nano vehicle for sustaining drug delivery.
    Matched MeSH terms: Norfloxacin/administration & dosage*; Norfloxacin/pharmacology
  8. Vashist N, Sambi SS, Narasimhan B, Kumar S, Lim SM, Shah SAA, et al.
    Chem Cent J, 2018 Dec 01;12(1):125.
    PMID: 30506405 DOI: 10.1186/s13065-018-0498-y
    BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities.

    RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug.

    CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil.

    Matched MeSH terms: Norfloxacin
  9. Samuel, L., Marian, M.M.,, Apun, K., Lesley, M.B., Son, R.
    MyJurnal
    Antibiotic susceptibility and genetic diversity of E. coli isolated from cultured catfish and their surrounding environment were determined. The levels of resistance of the E. coli isolates towards six different antibiotics tested differed considerably. Though the isolates displayed resistance towards some of the antibiotics tested, none of the isolates showed resistant towards norfloxacin, sulphametoxazole/trimethoprim and chloramphenicol. RAPD-PCR analysis using single primer and primers combination clustered the E. coli isolates into 3 and 5 groups, respectively. The results of this study suggest that the E. coli isolates from the catfish and their surrounding environment derived from a mixture of sensitive and resistant strains with diverse genetic contents. The use of the RAPD analysis is sufficiently discriminatory for the typing of the E. coli isolates.
    Matched MeSH terms: Norfloxacin
  10. Gan IN, Tan HS
    BMC Res Notes, 2019 Feb 21;12(1):97.
    PMID: 30791948 DOI: 10.1186/s13104-019-4124-4
    OBJECTIVES: Shigella is a human pathogen that causes shigellosis, an acute invasive intestinal infection. Recent studies in the model bacterium Escherichia coli (E. coli) provided evidence that small regulatory RNAs (sRNAs) can contribute to antimicrobial resistance or susceptibility. One of the sRNAs is SdsR, which increases sensitivity of E. coli against fluoroquinolone by repressing the drug efflux pump, TolC. However, no reports exist about the effect of SdsR on fluoroquinolone resistance in Shigella sonnei (S. sonnei). In this study, we established the effect of SdsR on the sensitivity of S. sonnei to norfloxacin.

    DATA DESCRIPTION: We tested the effects of SdsR and SdsRv2 on fluoroquinolone resistance in S. sonnei in vivo. SdsRv2 is a synthetic version which promotes higher binding stability to tolC mRNA. Overexpression of either SdsR or SdsRv2 lowers the expression of tolC mRNA. Interestingly, SdsR and SdsRv2 promote the growth of S. sonnei in the presence of a sub-inhibitory concentration of norfloxacin. Mutant carrying SdsRv2 showed the highest growth advantage. This phenotype is opposite to the effect of SdsR reported in E. coli. This study is an example that demonstrates the difference in the phenotypic effect of a highly conserved sRNA in two closely related bacteria.

    Matched MeSH terms: Norfloxacin/pharmacology*
  11. Lee YY, Tee HP, Mahadeva S
    World J Gastroenterol, 2014 Feb 21;20(7):1790-6.
    PMID: 24587656 DOI: 10.3748/wjg.v20.i7.1790
    Bacterial infections are common in cirrhotic patients with acute variceal bleeding, occurring in 20% within 48 h. Outcomes including early rebleeding and failure to control bleeding are strongly associated with bacterial infection. However, mortality from variceal bleeding is largely determined by the severity of liver disease. Besides a higher Child-Pugh score, patients with hepatocellular carcinoma are particularly susceptible to infections. Despite several hypotheses that include increased use of instruments, greater risk of aspiration pneumonia and higher bacterial translocation, it remains debatable whether variceal bleeding results in infection or vice versa but studies suggest that antibiotic prophylaxis prior to endoscopy and up to 8 h is useful in reducing bacteremia and spontaneous bacterial peritonitis. Aerobic gram negative bacilli of enteric origin are most commonly isolated from cultures, but more recently, gram positives and quinolone-resistant organisms are increasingly seen, even though their clinical significance is unclear. Fluoroquinolones (including ciprofloxacin and norfloxacin) used for short term (7 d) have the most robust evidence and are recommended in most expert guidelines. Short term intravenous cephalosporin (especially ceftriaxone), given in a hospital setting with prevalent quinolone-resistant organisms, has been shown in studies to be beneficial, particularly in high risk patients with advanced cirrhosis.
    Matched MeSH terms: Norfloxacin/therapeutic use
  12. Takkinsatian P, Silpskulsuk C, Prommalikit O
    Med J Malaysia, 2020 11;75(6):672-676.
    PMID: 33219176
    INTRODUCTION: Salmonella is a common organism, causing intestinal and extraintestinal infections among Thai children, especially infants, and leading to overwhelming antibiotic use.

    MATERIALS AND METHODS: In this retrospective review, data collected during 2006-2015 from the medical charts of patients with evidence of infection, caused by any Salmonella serogroup or clinical form, were examined. We aimed to assess the clinical manifestations, antibiotic susceptibility, and antibiotic use in children with Salmonella gastroenteritis over the ten years' period.

    RESULTS: A total of 419 patients had non-typhoidal Salmonella infection. Four-hundred (95.5%) patients were diagnosed with acute gastroenteritis, which was common in children aged <12 months (72.3%). The clinical features of patients with gastroenteritis included fever (74.5%), diarrhoea with bloody mucus (60.5%), watery diarrhoea (39.5%), and vomiting (19.8%). Serogroup B was most commonly detected in the stool specimens. The susceptibility of non-typhoidal Salmonella to ampicillin, norfloxacin, and co-trimoxazole was 36.3%, 98.0%, and 80.5%, respectively. Serogroup B was the most resistant strain, which was sensitive to ampicillin in only 21.6% of specimens, while it showed high susceptibility to norfloxacin and co-trimoxazole (98.1 and 84.0%, respectively). Third-generation cephalosporin and fluoroquinolone were most commonly prescribed.

    CONCLUSIONS: Acute gastroenteritis is the most common form of Salmonella infection. Gastroenteritis caused by serogroup B is still the most common infection, which mostly occurs among infants under one year of age. The majority of stool specimens were still susceptible to antimicrobial agents, especially fluoroquinolone and cotrimoxazole; however, there was an overuse of antibiotics without proper indications.

    Matched MeSH terms: Norfloxacin
  13. Sharma D, Kumar S, Narasimhan B, Ramasamy K, Lim SM, Shah SAA, et al.
    BMC Chem, 2019 Dec;13(1):60.
    PMID: 31384808 DOI: 10.1186/s13065-019-0575-x
    In order to overcome the challenges of microbial resistance as well as to improve the effectiveness and selectivity of chemotherapeutic agents against cancer, a novel series of 4-(4-bromophenyl)-thiazol-2-amine derivatives was synthesized and its molecular structures were confirmed by physicochemical and spectral characteristics. The synthesized compounds were further evaluated for their in vitro antimicrobial activity using turbidimetric method and anticancer activity against oestrogen receptor positive human breast adenocarcinoma cancer cell line (MCF7) by Sulforhodamine B (SRB) assay. The antimicrobial activity results revealed that compound p2, p3, p4 and p6 exhibited promising antimicrobial activity that are comparable to standard norfloxacin (antibacterial) and fluconazole (antifungal). Anticancer screening results demonstrated that compound p2 was found to be the most active one against cancer cell line when compared to the rest of the compounds and comparable to the standard drug (5-fluorouracil). The molecular docking study demonstrated that compounds, p2, p3, p4 and p6 displayed good docking score within binding pocket of the selected PDB ID (1JIJ, 4WMZ and 3ERT) and showed promising ADME properties.
    Matched MeSH terms: Norfloxacin
  14. Usha, M.R., Fauziah, M., Tunung, R., Chai, L.C., Cheah, Y.K., Farinazleen, M.G., et al.
    MyJurnal
    Broiler part samples (80 fresh and 80 chilled) were examined for the prevalence and numbers of C. jejuni and C. coli by employing most-probable-number (MPN) and polymerase chain reaction (PCR) techniques. The prevalence of the bacteria was high where C. jejuni was detected in 92.5% fresh and 53.8% chilled samples while C. coli in 80.0% fresh and 56.3% chilled. The number of these bacteria in the positive fresh and chilled samples was from 3 to more than 2400 MPN/g and from 3 to 290 MPN/g, respectively. Antibiotic resistance test (using Kirby-Bauer disc diffusion method) on 10 C. jejuni and 13 C. coli isolates toward ampicillin, tobramycin, enrofloxacin, ciprofloxacin, tetracycline, cephalothin, gentamicin and norfloxacin revealed high resistance toward all antibiotics (20.0% - 100.0%). All isolates were resistant to at least two antibiotics. This study highlights the potential of multidrug-resistant C. jejuni and C. coli transmission to humans through fresh and chilled broiler parts. Consecutive studies with bigger sample sizes and covering all over Malaysia are warranted in future.
    Matched MeSH terms: Norfloxacin
  15. Tang, J.Y.H., Wan-Rosli, W.F., Abdul-Razak, N.H., Yeo, C.C., Abu Bakar, C.A., Son, R.
    MyJurnal
    This study aimed to investigate the prevalence and antibiogram of Vibrio parahaemolyticus in processed bivalve molluscs in Kuala Terengganu. A total of 80 seafood samples, namely mussels (n=20), carpet clams (n=20), cockles (n=20) and scallops (n=20), were subjected to PCR and conventional plating method for the detection of V. parahaemolyticus. V. parahaemolyticus was found in green mussels (55%), carpet clam (80%), cockles (40%) and scallops (55%). Fifty-five V. parahaemolyticus isolates were subjected to 9 types antibiotic sensitivity test using discs diffusion method. All isolates were susceptible to Tetracycline and Gentamycin. Isolates showed high resistance towards Vancomycin (52.73%), Penicillin (45.45%) and Amplicillin (32.73%). Resistance towards Amikacin, Ciprofloxacin and Norfloxacin were found to be 1.82%. It can be concluded that local bivalve molluscs were contaminated with V. parahaemolyticus and isolates showed resistance towards certain antibiotics. Therefore, consumption of raw or semi-cooked bivalve molluscs is not advisable.
    Matched MeSH terms: Norfloxacin
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