Displaying publications 61 - 80 of 256 in total

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  1. Fulltext Antibacterial Activity of Clay Soils against Food-Borne Salmonella typhimurium and Staphylococcus aureus
    Azmi NN, Mahyudin NA, Wan Omar WH, Mahmud Ab Rashid NK, Ishak CF, Abdullah AH, et al.
    Molecules, 2021 Dec 28;27(1).
    PMID: 35011396 DOI: 10.3390/molecules27010170
    Natural clays have recently been proven to possess antibacterial properties. Effective natural antimicrobial agents are needed to combat bacterial contamination on food contact surfaces, which are increasingly more prevalent in the food chain. This study sought to determine the antibacterial activity of clays against the food-borne pathogens Salmonella typhimurium ATCC 14028 and Staphylococcus aureus ATCC 13565. Soils were processed to yield leachates and suspensions from untreated and treated clays. Soil particle size, pH, cation-exchange capacity, metal composition and mineralogy were characterized. Antibacterial screening was performed on six Malaysian soils via the disc diffusion method. In addition, a time-kill assay was conducted on selected antibacterial clays after 6 h of exposure. The screening revealed that Munchong and Carey clays significantly inhibit Salmonella typhimurium (11.00 ± 0.71 mm) and S. aureus (7.63 ± 0.48 mm), respectively. Treated Carey clay leachate and suspension completely kill Salmonella typhimurium, while S. aureus viability is reduced (2 to 3 log10). The untreated Carey and all Munchong clays proved ineffective as antibacterials. XRD analysis confirmed the presence of pyrite and magnetite. Treated Carey clays had a higher soluble metal content compared to Munchong; namely Al (92.63 ± 2.18 mg/L), Fe (65.69 ± 3.09 mg/L) and Mg (88.48 ± 2.29 mg/L). Our results suggest that metal ion toxicity is responsible for the antibacterial activity of these clays.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  2. Fulltext Bactericidal Properties of Plants-Derived Metal and Metal Oxide Nanoparticles (NPs)
    Teow SY, Wong MM, Yap HY, Peh SC, Shameli K
    Molecules, 2018 06 06;23(6).
    PMID: 29882775 DOI: 10.3390/molecules23061366
    Nanoparticles (NPs) are nano-sized particles (generally 1⁻100 nm) that can be synthesized through various methods. The wide range of physicochemical characteristics of NPs permit them to have diverse biological functions. These particles are versatile and can be adopted into various applications, particularly in biomedical field. In the past five years, NPs’ roles in biomedical applications have drawn considerable attentions, and novel NPs with improved functions and reduced toxicity are continuously increasing. Extensive studies have been carried out in evaluating antibacterial potentials of NPs. The promising antibacterial effects exhibited by NPs highlight the potential of developing them into future generation of antimicrobial agents. There are various methods to synthesize NPs, and each of the method has significant implication on the biological action of NPs. Among all synthetic methods, green technology is the least toxic biological route, which is particularly suitable for biomedical applications. This mini-review provides current update on the antibacterial effects of NPs synthesized by green technology using plants. Underlying challenges in developing NPs into future antibacterials in clinics are also discussed at the present review.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  3. Fulltext ZnO-NPs embedded biodegradable thiolated bandage for postoperative surgical site infection: In vitro and in vivo evaluation
    Arshad R, Sohail MF, Sarwar HS, Saeed H, Ali I, Akhtar S, et al.
    PLoS One, 2019;14(6):e0217079.
    PMID: 31170179 DOI: 10.1371/journal.pone.0217079
    Post-operative surgical site infections (SSI) present a serious threat and may lead to complications. Currently available dressings for SSI lack mucoadhesion, safety, efficacy and most importantly patient compliance. We aimed to address these concerns by developing a bioactive thiolated chitosan-alginate bandage embedded with zinc oxide nanoparticles (ZnO-NPs) for localized topical treatment of SSI. The FTIR, XRD, DSC and TGA of bandage confirmed the compatibility of ingredients and modifications made. The porosity, swelling index and lysozyme degradation showed good properties for wound healing and biodegradation. Moreover, in-vitro antibacterial activity showed higher bactericidal effect as compared to ZnO-NPs free bandage. In-vivo wound healing in murine model showed significant improved tissue generation and speedy wound healing as compared to positive and negative controls. Over all, thiolated bandage showed potential as an advanced therapeutic agent for treating surgical site infections, meeting the required features of an ideal surgical dressing.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  4. Synthesis, spectral analysis and biological evaluation of 2-{[(morpholin-4-yl)ethyl]thio}-5-phenyl/aryl-1,3,4-oxadiazole derivatives
    Ur-Rehman A, Khan SG, Naqvi SAR, Ahmad M, Akhtar N, Bokhari TH, et al.
    Pak J Pharm Sci, 2021 Jan;34(1(Special)):441-446.
    PMID: 34275792
    A series of new derivatives of 4-(2-chloroethyl)morpholine hydrochloride (5) were efficiently synthesized. Briefly, different aromatic organic acids (1a-f) were refluxed to acquire respective esters (2a-f) using conc. H2SO4 as catalyst. The esters were subjected to nucleophillic substitution by monohydrated hydrazine to acquire hydrazides (3a-f). The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Finally, the derivatives, 6a-f, were prepared by reacting oxadiazoles (4a-f) with 5 using NaH as activator. Structures of all the derivatives were elucidated through 1D-NMR EI-MS and IR spectral data. All these molecules were subjected to antibacterial and hemolytic activities and showed good antibacterial and hemolytic potential relative to the reference standards.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  5. Fulltext A new strategy for taste masking of azithromycin antibiotic: development, characterization, and evaluation of azithromycin titanium nanohybrid for masking of bitter taste using physisorption and panel testing studies
    Amin F, Khan S, Shah SMH, Rahim H, Hussain Z, Sohail M, et al.
    Drug Des Devel Ther, 2018;12:3855-3866.
    PMID: 30510401 DOI: 10.2147/DDDT.S183534
    Background: The obnoxious bitter taste of orally taken antibiotics is one of the biggest problems in the treatment of children. The pediatric population cannot tolerate the bitter taste of drugs and vomit out which ultimately leads to suboptimal therapeutic value, grimace and mental stress so it is the challenging task for the formulation scientists to formulate a palatable formulation particularly to overcome address the issue.

    Purpose of study: The study aimed to mask and evaluate the unpleasant bitter taste of azithro-mycin (AZ) in the dry suspension dosage form by physisorption technique.

    Materials and methods: AZ was selected as an adsorbent and titanium dioxide nanoparticles as adsorbate. The AZ nanohybrids (AZN) were prepared by treating fixed amount of adsorbent with a varied amount of adsorbate, prepared separately by dispersing it in an aqueous medium. The mixture was sonicated, stirred followed by filtration and drying. The AZN produced were characterized by various techniques including scanning electron microscopy (SEM), energy dispersive X-rays (EDX), powder X-ray diffraction (PXRD), HPLC and Fourier-transformed infrared (FTIR). The optimized nanohybrid was blended with other excipients to get stable and taste masked dry suspension dosage form.

    Results: The results confirmed the adsorption of titanium dioxide nanoparticles on the surface of AZ. The fabricated optimized formulation was subjected for taste masking by panel testing and accelerated stability studies. The results showed a remarkable improvement in bitter taste masking, inhibiting throat bite without affecting the dissolution rate. The product showed an excellent stability both in dry and reconstituted suspension. The optimized formulation of AZN and was found stable when subjected to physical and chemical stability studies, this is because of short and single step process which interns limits the exposure of the product to various environmental factors that could potentially affect the stability of the product. The dissolution rate of the optimized formulation of AZN was compared with its marketed counterpart, showing the same dissolution rate compared to its marketed formulation.

    Conclusion: The current study concludes that, by fabricating AZ-titanium nanohybrids using physisorption can effectively mask the bitter taste of the drug. The palatability and stability of azithromycin formulation was potentially enhanced without affecting its dissolution rate.

    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  6. 2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line
    Tahlan S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA
    Mini Rev Med Chem, 2019;19(13):1080-1092.
    PMID: 30306865 DOI: 10.2174/1389557518666181009151008
    BACKGROUND: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer.

    OBJECTIVE: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole.

    METHODS: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively.

    RESULTS: Compounds 8 (MICpa, an = 2.41, 1.20 µM/ml), 10 (MICse, sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity.

    CONCLUSION: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents.

    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  7. Synthesis, spectral analysis and biological evaluation of sulfamoyl and 1,3,4-oxadiazole derivatives of 3-pipecoline
    Rehman A, Aslam SJ, Abbasi MA, Siddiqui SZ, Rasool S, Shah SAA
    Pak J Pharm Sci, 2019 May;32(3):987-996.
    PMID: 31278711
    Heterocyclic chemistry is an important field of organic chemistry due to therapeutic potential. The minor modification in the structure of poly-functional compounds has great effect on therapeutic ability. In the presented research work, substituted 1,3,4-oxadiazole derivatives, 8a-p, have been synthesized by the reaction of 1-(4-bromomethylbenzenesulfonyl)-3-methylpiperidine (7) and 5-substituted-1,3,4-oxadiazole-2-thiol (4a-p). The 5-substituted-1,3,4-oxadiazole-2-thiol were synthesized by converting carboxylic acids correspondingly into esters, hydrazides and oxadiazoles. Secondly the electrophile, 1-(4-Bromomethylbenzenesulfonyl)-3-methylpiperidine (7), was prepared by the reaction of 3-methylpiperidine with 4-bromomethylbenzenesulfonyl chloride in the presence of water and Na2CO3 under pH of 9-10. The compounds were structurally corroborated through spectroscopic data analysis of IR, EI-MS and 1H-NMR. The screening for antibacterial activity revealed the compounds to be moderate to excellent inhibitors against bacteria under study. Anti-enzymatic activity was assessed against urease enzyme and 1-{[4-({[5-(3-nitrophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}methyl)phenyl]sulfonyl}-3-methylpiperidine (8d) was the most active one.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  8. Oritavancin - a new semisynthetic lipoglycopeptide agent to tackle the challenge of resistant gram positive pathogens
    Das B, Sarkar C, Schachter J
    Pak J Pharm Sci, 2013 Sep;26(5):1045-55.
    PMID: 24035967
    Natural glycopeptide antibiotics like vancomycin and teicoplanin have played a significant role in countering the threat posed by Gram-positive bacterial infections. The emergence of resistance to glycopeptides among enterococci and staphylococci has prompted the search for second-generation drugs of this class and semi-synthetic derivatives are currently under clinical trials. Antimicrobial resistance among Gram-positive organisms has been increasing steadily during the past several decades and the current development of antibiotics falls short of meeting the needs. Oritavancin (LY-333328 diphosphate), a promising novel second-generation semisynthetic lipoglycopeptide, has a mechanism of action similar to that of other glycopeptides. It has concentration-dependent activity against a variety of Gram-positive organisms specially methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate resistant Staphylococcus aureus (VISA), Streptococcus pneumoniae and vancomycin-resistant enterococcus. It is rapidly bactericidal against many species and in particular for enterococci where vancomycin and teicoplanin are only bacteriostatic even against susceptible strains. The pharmacokinetic profile of oritavancin has not been fully described; however, oritavancin has a long half-life of about 195.4 hours and is slowly eliminated by renal means. Oritavancin is not metabolized by the liver in animals. Oritavancin will most probably be prescribed as a once-daily dose and it demonstrates concentration-dependent bactericidal activity. Oritavancin has demonstrated preliminary safety and efficacy in Phase I and II clinical trials. In a Phase III clinical trial, oritavancin has achieved the primary efficacy end point in the treatment of complicated Gram-positive skin and skin-structure infections. To date, adverse events have been mild and limited; the most common being administration site complaints, headache, rhinitis, dry skin, pain, increases in liver transaminases and accumulation of free cholesterol and phospholipids in phagocytic (macrophages) and nonphagocytic (fibroblast) cells. Oritavancin appears to be a promising antimicrobial alternative to vancomycin (with additional activity against Staphylococcus and Enterococcus resistant to vancomycin) for the treatment of complicated Gram-positive skin and skin-structure infections. Additional clinical data are required to fully explore its use.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  9. Fulltext Antioxidant and antibacterial activity of different parts of Leucas aspera
    Chew AL, Jessica JJ, Sasidharan S
    Asian Pac J Trop Biomed, 2012 Mar;2(3):176-80.
    PMID: 23569893 DOI: 10.1016/S2221-1691(12)60037-9
    To evaluate antioxidant, antimicrobial and cytotoxic activity of different parts (root, flower, leaf and stem) of Leucas aspera (L. aspera) (Labiatae).
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  10. Fulltext The Antimicrobial efficacy of Elaeis guineensis: characterization, in vitro and in vivo studies
    Vijayarathna S, Zakaria Z, Chen Y, Latha LY, Kanwar JR, Sasidharan S
    Molecules, 2012 Apr 26;17(5):4860-77.
    PMID: 22538489 DOI: 10.3390/molecules17054860
    The urgent need to treat multi-drug resistant pathogenic microorganisms in chronically infected patients has given rise to the development of new antimicrobials from natural resources. We have tested Elaeis guineensis Jacq (Arecaceae) methanol extract against a variety of bacterial, fungal and yeast strains associated with infections. Our studies have demonstrated that E. guineensis exhibits excellent antimicrobial activity in vitro and in vivo against the bacterial and fungal strains tested. A marked inhibitory effect of the E. guineensis extracts was observed against C. albicans whereby E. guineensis extract at ½, 1, or 2 times the MIC significantly inhibited C. albicans growth with a noticeable drop in optical density (OD) of the bacterial culture. This finding confirmed the anticandidal activity of the extract on C. albicans. Imaging using scanning (SEM) and transmission (TEM) electron microscopy was done to determine the major alterations in the microstructure of the extract-treated C. albicans. The main abnormalities noted via SEM and TEM studies were the alteration in morphology of the yeast cells. In vivo antimicrobial activity was studies in mice that had been inoculated with C. albicans and exhibited good anticandidal activity. The authors conclude that the extract may be used as a candidate for the development of anticandidal agent.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  11. Fulltext Cassia spectabilis (DC) Irwin et Barn: a promising traditional herb in health improvement
    Jothy SL, Torey A, Darah I, Choong YS, Saravanan D, Chen Y, et al.
    Molecules, 2012 Aug 29;17(9):10292-305.
    PMID: 22932211 DOI: 10.3390/molecules170910292
    The genus Cassia, comprising about 600 species widely distributed worldwide is well known for its diverse biological and pharmacological properties. Cassia spectabilis (sin Senna spectabilis) (DC) Irwin et Barn (Fabaceae) is widely grown as an ornamental plant in tropical and subtropical areas. C. spectabilis has been commonly used in traditional medicine for many years. Information in the biomedical literature has indicated the presence of a variety of medicinally-important chemical constituents in C. spectabilis. Pharmacological studies by various groups of investigators have shown that C. spectabilis possesses significant biological activity, such as antibacterial, antibiofilm, antifungal and antioxidant properties. Beside this, toxicity studies of this plant have revealed no toxic effect on mice. In view of the immense medicinal importance of C. spectabilis, this review aimed at compiling all currently available information on C. spectabilis’s botany, phytochemistry, pharmacology, and mechanism of actions, toxicology and its ethnomedicinal uses.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  12. Recent Update on the Anti-infective Potential of β-carboline Analogs
    Faheem, Kumar BK, Sekhar KVGC, Kunjiappan S, Jamalis J, Balaña-Fouce R, et al.
    Mini Rev Med Chem, 2021;21(4):398-425.
    PMID: 33001013 DOI: 10.2174/1389557520666201001130114
    β-Carboline, a naturally occurring indole alkaloid, holds a momentous spot in the field of medicinal chemistry due to its myriad of pharmacological actions like anticancer, antiviral, antibacterial, antifungal, antileishmanial, antimalarial, neuropharmacological, anti-inflammatory and antithrombotic among others. β-Carbolines exhibit their pharmacological activity via diverse mechanisms. This review provides a recent update (2015-2020) on the anti-infective potential of natural and synthetic β-carboline analogs focusing on its antibacterial, antifungal, antiviral, antimalarial, antileishmanial and antitrypanosomal properties. In cases where enough details are available, a note on its mechanism of action is also added.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  13. Fulltext Detection of secreted antimicrobial peptides isolated from cell-free culture supernatant of Paenibacillus alvei AN5
    Alkotaini B, Anuar N, Kadhum AA, Sani AA
    J Ind Microbiol Biotechnol, 2013 Jun;40(6):571-9.
    PMID: 23508455 DOI: 10.1007/s10295-013-1259-5
    An antimicrobial substance produced by the Paenibacillus alvei strain AN5 was detected in fermentation broth. Subsequently, cell-free culture supernatant (CFCS) was obtained by medium centrifugation and filtration, and its antimicrobial activity was tested. This showed a broad inhibitory spectrum against both Gram-positive and -negative bacterial strains. The CFCS was then purified and subjected to SDS-PAGE and infrared spectroscopy, which indicated the proteinaceous nature of the antimicrobial compound. Some de novo sequencing using an automatic Q-TOF premier system determined the amino acid sequence of the purified antimicrobial peptide as Y-S-K-S-L-P-L-S-V-L-N-P (1,316 Da). The novel peptide was designated as peptide AN5-1. Its mode of action was bactericidal, inducing cell lysis in E. coli ATCC 29522 and S. aureus, and non-cell lysis in both S. marcescens and B. cereus ATCC 14579. Peptide AN5-1 displayed stability at a wide range of pH values (2-12) and remained active after exposure to high temperatures (100 °C). It also maintained its antimicrobial activity after incubation with chemicals such as SDS, urea and EDTA.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  14. Fulltext Biosynthesis of zinc oxide nanoparticles by cell-biomass and supernatant of Lactobacillus plantarum TA4 and its antibacterial and biocompatibility properties
    Mohd Yusof H, Abdul Rahman N, Mohamad R, Zaidan UH, Samsudin AA
    Sci Rep, 2020 Nov 17;10(1):19996.
    PMID: 33204003 DOI: 10.1038/s41598-020-76402-w
    This study aims to utilize the cell-biomass (CB) and supernatant (CFS) of zinc-tolerant Lactobacillus plantarum TA4 as a prospective nanofactory to synthesize ZnO NPs. The surface plasmon resonance for the biosynthesized ZnO NPs-CFS and ZnO NPs-CB was 349 nm and 351 nm, respectively, thereby confirming the formation of ZnO NPs. The FTIR analysis revealed the presence of proteins, carboxyl, and hydroxyl groups on the surfaces of both the biosynthesized ZnO NPs that act as reducing and stabilizing agents. The DLS analysis revealed that the poly-dispersity indexes was less than 0.4 for both ZnO NPs. In addition, the HR-TEM micrographs of the biosynthesized ZnO NPs revealed a flower-like pattern for ZnO NPs-CFS and an irregular shape for ZnO NPs-CB with particles size of 291.1 and 191.8 nm, respectively. In this study, the biosynthesized ZnO NPs exhibited antibacterial activity against pathogenic bacteria in a concentration-dependent manner and showed biocompatibility with the Vero cell line at specific concentrations. Overall, CFS and CB of L. plantarum TA4 can potentially be used as a nanofactory for the biological synthesis of ZnO NPs.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  15. Fulltext Surfactant-mediated synthesis of polyhydroxybutyrate (PHB) nanoparticles for sustained drug delivery
    Pachiyappan S, Shanmuganatham Selvanantham D, Kuppa SS, Chandrasekaran S, Samrot AV
    IET Nanobiotechnol, 2019 Jun;13(4):416-427.
    PMID: 31171747 DOI: 10.1049/iet-nbt.2018.5053
    In this study, polyhydroxybutyrate (PHB) nanoparticles were synthesised following nanoprecipitation method having different solvents and surfactant (Tween 80) concentrations. In this study, PHB nanoparticles were encapsulated with curcumin and subjected for sustained curcumin delivery. Both the curcumin loaded and unloaded PHB nanoparticles were characterised using FTIR, SEM, and AFM. Sizes of the particles were found to be between 60 and 300 nm. The drug encapsulation efficiency and in vitro drug release of the nanoparticles were analysed. Antibacterial activity and anticancer activity were also evaluated. The LC50 values of most of the nanoparticles were found to be between 10 and 20 µg/100 µl, anticancer activity of curcumin loaded PHB nanoparticles were further confirmed by AO/PI staining and mitochondrial depolarisation assay.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  16. Immobilization of antibacterial chlorhexidine on stainless steel using crosslinking polydopamine film: Towards infection resistant medical devices
    Mohd Daud N, Saeful Bahri IF, Nik Malek NA, Hermawan H, Saidin S
    Colloids Surf B Biointerfaces, 2016 Sep 01;145:130-9.
    PMID: 27153117 DOI: 10.1016/j.colsurfb.2016.04.046
    Chlorhexidine (CHX) is known for its high antibacterial substantivity and is suitable for use to bio-inert medical devices due to its long-term antibacterial efficacy. However, CHX molecules require a crosslinking film to be stably immobilized on bio-inert metal surfaces. Therefore, polydopamine (PDA) was utilized in this study to immobilize CHX on the surface of 316L type stainless steel (SS316L). The SS316L disks were pre-treated, modified with PDA film and immobilized with different concentrations of CHX (10mM-50mM). The disks were then subjected to various surface characterization analyses (ATR-FTIR, XPS, ToF-SIMS, SEM and contact angle measurement) and tested for their cytocompatibility with human skin fibroblast (HSF) cells and antibacterial activity against Escherichia coli and Staphylococcus aureus. The results demonstrated the formation of a thin PDA film on the SS316L surface, which acted as a crosslinking medium between the metal and CHX. CHX was immobilized via a reduction process that covalently linked the CHX molecules with the functional group of PDA. The immobilization of CHX increased the hydrophobicity of the disk surfaces. Despite this property, a low concentration of CHX optimized the viability of HSF cells without disrupting the morphology of adherent cells. The immobilized disks also demonstrated high antibacterial efficacy against both bacteria, even at a low concentration of CHX. This study demonstrates a strong beneficial effect of the crosslinked PDA film in immobilizing CHX on bio-inert metal, and these materials are applicable in medical devices. Specifically, the coating will restrain bacterial proliferation without suffocating nearby tissues.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  17. Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels
    Sheshala R, Quah SY, Tan GC, Meka VS, Jnanendrappa N, Sahu PS
    Drug Deliv Transl Res, 2019 04;9(2):434-443.
    PMID: 29392681 DOI: 10.1007/s13346-018-0488-6
    The objectives of present research were to develop and characterize thermosensitive and mucoadhesive polymer-based sustained release moxifloxacin in situ gels for the treatment of periodontal diseases. Poloxamer- and chitosan-based in situ gels are in liquid form at room temperature and transform into gel once administered into periodontal pocket due to raise in temperature to 37 °C. Besides solution-to-gel characteristic of polymers, their mucoadhesive nature aids the gel to adhere to mucosa in periodontal pocket for prolonged time and releases the drug in sustained manner. These formulations were prepared using cold method and evaluated for pH, solution-gel temperature, syringeability and viscosity. In vitro drug release studies were conducted using dialysis membrane at 37 °C and 50 rpm. Antimicrobial studies carried out against Aggregatibacter actinomycetemcomitans (A.A.) and Streptococcus mutans (S. Mutans) using agar cup-plate method. The prepared formulations were clear and pH was at 7.01-7.40. The viscosity of formulations was found to be satisfactory. Among the all, formulations comprising of 21% poloxamer 407 and 2% poloxamer 188 (P5) and in combination with 0.5% HPMC (P6) as well as 2% chitosan and 70% β-glycerophosphate (C6) demonstrated an ideal gelation temperature (33-37 °C) and sustained the drug release for 8 h. Formulations P6 and C6 showed promising antimicrobial efficacy with zone of inhibition of 27 mm for A.A. and 55 mm for S. Mutans. The developed sustained release in situ gel formulations could enhance patient's compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  18. Langkolide, a 32-membered macrolactone antibiotic produced by Streptomyces sp. Acta 3062
    Helaly SE, Kulik A, Zinecker H, Ramachandaran K, Tan GY, Imhoff JF, et al.
    J Nat Prod, 2012 Jun 22;75(6):1018-24.
    PMID: 22642587 DOI: 10.1021/np200580g
    A new 32-membered macrolactone antibiotic, named langkolide, was isolated from the mycelium of Streptomyces sp. Acta 3062. The langkolide structure was determined by HR-MS and 1D and 2D NMR as a 32-membered macrolactone connected from an overhanging polyketide tail to a naphthoquinone unit mediated by two carbohydrate moieties. The producing strain was isolated from a rhizosphere soil of Clitorea sp. collected at Burau Bay, Langkawi, Malaysia, and was characterized by its morphological and chemotaxonomic features in addition to its 16S rRNA gene sequence. It was identified as a member of the Streptomyces galbus clade. Langkolide exhibited various bioactivities including antimicrobial and antiproliferative activities. Furthermore, langkolide inhibited human recombinant phosphodiesterase 4 with an IC(50) value of 0.48 μM.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  19. Cytotoxicity evaluation of vancomycin and its complex with beta-cyclodextrin on human glial cell line
    Sofian ZM, Abdullah JM, Rahim AA, Shafee SS, Mustafa Z, Razak SA
    Pak J Pharm Sci, 2012 Oct;25(4):831-7.
    PMID: 23010001
    The possible cytotoxic effects of vancomycin and its complex with beta-cyclodextrin (β-CD) on human glial cell line (CRL 8621) were studied accordingly by means of MTS assay. The cultured cells were incubated with various concentrations of vancomycin, β-CD as well as β-CD/vancomycin complex ranging from 4.69 to 300 ug/ml. A linear dose-dependency cytotoxicity followed by hermetic-like biphasic dose-dependence was observed after incubation period of 72 hours. In general, significant increase (p<0.001) of cell proliferation was observed at lower concentrations: <18.75 μg/ml for cells treated with β-CD and their complex while < 9.38 μg/ml for cells treated with vancomycin. In contrary, regardless of the treatments given, significant (p<0.001) reduce in cell survival was found at higher concentrations >150 μg/ml. In particular, 50 % inhibitory in vitro was achieved at the concentrations of 115.95 μg/ml (for β-CD), 116.48 μg/ml (for vancomycin) and 115.44 μg/ml (for β-CD/vancomycin complex).
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  20. A facile ultrasonic-aided biosynthesis of ZnO nanoparticles using Vaccinium arctostaphylos L. leaf extract and its antidiabetic, antibacterial, and oxidative activity evaluation
    Bayrami A, Alioghli S, Rahim Pouran S, Habibi-Yangjeh A, Khataee A, Ramesh S
    Ultrason Sonochem, 2019 Jul;55:57-66.
    PMID: 31084791 DOI: 10.1016/j.ultsonch.2019.03.010
    The synthesis of nanoparticles often result in the generation of harmful chemical pollutants. As such, many researchers have focused on developing green processes, which include the biosynthesis. In this research, ZnO nanoparticles were prepared using the leaf extract of whortleberry (Vaccinium arctostaphylos L.) via a simple ultrasonic-assisted method. The morphology, crystal size and structure, surface, thermal, and optical properties of the bio-mediated ZnO sample (ZnOext) were analyzed and compared with that produced without incorporating the extract (ZnOchem). The ZnO samples were evaluated for their antidiabetic, antibacterial, as well as their sono- and photo-catalytic performances. Initially, the samples were intraperitoneal injected to alloxan-diabetic rats to examine their treatment efficiency in terms of effects on fasting blood glucose, insulin, cholesterol, high-density lipoprotein, and total triglyceride levels. The ZnOext showed significantly higher efficiency for improving the health status of alloxan-diabetic rats in contrast with other tested treatments, vis. ZnOchem, insulin, and only leaf extract. In addition, both the ZnO samples were assessed against gram-negative and gram-positive bacteria and through sono- and photo-catalytic processes for removing rhodamine B, respectively. The results of this study indicated that not only the ZnOext sample was pollution free, it also exhibited higher potentials for treating diabetic rats, bacterial decontamination, and also oxidative removal of organic compounds under the influences of ultrasound and UV irradiations when compared with ZnOchem sample.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
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