Displaying publications 21 - 40 of 257 in total

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  1. A Glance on the Role of Bacterial Siderophore from the Perspectives of Medical and Biotechnological Approaches
    AlMatar M, Albarri O, Makky EA, Var I, Köksal F
    Curr Drug Targets, 2020;21(13):1326-1343.
    PMID: 32564749 DOI: 10.2174/1389450121666200621193018
    Iron, which is described as the most basic component found in nature, is hard to be assimilated by microorganisms. It has become increasingly complicated to obtain iron from nature as iron (II) in the presence of oxygen oxidized to press (III) oxide and hydroxide, becoming unsolvable at neutral pH. Microorganisms appeared to produce organic molecules known as siderophores in order to overcome this condition. Siderophore's essential function is to connect with iron (II) and make it dissolvable and enable cell absorption. These siderophores, apart from iron particles, have the ability to chelate various other metal particles that have collocated away to focus the use of siderophores on wound care items. There is a severe clash between the host and the bacterial pathogens during infection. By producing siderophores, small ferric iron-binding molecules, microorganisms obtain iron. In response, host immune cells produce lipocalin 2 to prevent bacterial reuptake of siderophores loaded with iron. Some bacteria are thought to produce lipocalin 2-resistant siderophores to counter this risk. The aim of this article is to discuss the recently described roles and applications of bacterial siderophore.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  2. Pluronic-F127 composite film loaded with erythromycin for wound application: formulation, physicomechanical and in vitro evaluations
    Alavi T, Rezvanian M, Ahmad N, Mohamad N, Ng SF
    Drug Deliv Transl Res, 2019 04;9(2):508-519.
    PMID: 29181832 DOI: 10.1007/s13346-017-0450-z
    Composite film dressings composed of pluronic F127 (PL)-pectin (PC) and pluronic (PL) F127-gelatin (GL) were investigated as potential drug delivery system for wound healing. Composite films were solvent cast by blending PL with PC or GL in different ratios using glycerol (2.5%) as plasticizer. Erythromycin (ER) (0.1%) was incorporated in films as model hydrophobic antibiotic. The optimized composite films were characterized for physical appearance, morphology, mechanical profile, and thermal behavior. In addition, drug release, antibacterial activity, and cytocompatibility of the films were investigated to assess their potential as drug delivery system. The composite films exhibited excellent wound dressing characters in terms of appearance, stability, and mechanical profile. Moreover, ER-loaded composite films released ER in controlled manner, exhibited antibacterial activity against Staphylococcus aureus, and were non-toxic to human skin fibroblast. These findings demonstrate that these composite films hold the potential to be formulated as antibacterial wound dressing.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  3. Enhanced nanocurcumin toxicity against (PC3) tumor and microbial by using magnetic field in vitro
    Aldahoun MA, Jaafar MS, Al-Akhras MH, Bououdina M
    Artif Cells Nanomed Biotechnol, 2017 Jun;45(4):843-853.
    PMID: 27137748 DOI: 10.1080/21691401.2016.1178137
    Curcumin is more soluble in ethanol, dimethylsulfoxide, methanol and acetone than in water. In this study, nanocurcumin combined with 8 mT AC static magnetic field was used to enhance cellular uptake, bioavailability, and ultimate efficiency of curcumin against prostate cancer cell line (PC3), four bacteria strains (two Gram positive: Micrococcus luteus ATCC 9341, Staphylococcus aureus ATCC 29213 and two Gram negative: Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853), mammalian cell line (HEK) and human erythrocytes (RBC). The efficiency (E%) between IC50 of nanocurcumin combined with magnetic field (NANOCUR-MF) and control against PC3 was 35.93%, which is three times higher compared to curcumin combined with magnetic field (CUR-MF); i.e., 10.77%. However, their E% against HEK was not significant; 1.4% for NANOCUR-MF and 1.95% for CUR-MF. Moreover, depending in minimum bacterial concentration (MBC), the use of MF leads to a reduction of MBCs for all tested bacteria compared with control. The obtained results established the applicability of (MF) in enhancing cellular uptake for PC3 and tested bacteria strains by increasing the penetration of drug (nanocurcumin and parent curcumin) into cell with fixing mild cytotoxic profile for HEK and RBC.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  4. Fulltext Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities
    Aldawsari MF, Ahmed MM, Fatima F, Anwer MK, Katakam P, Khan A
    Mar Drugs, 2021 Aug 20;19(8).
    PMID: 34436306 DOI: 10.3390/md19080467
    The objective of this work was to develop sustained-release Ca-alginate beads of apigenin using sodium alginate, a natural polysaccharide. Six batches were prepared by applying the ionotropic gelation technique, wherein calcium chloride was used as a crosslinking agent. The beads were evaluated for particle size, drug loading, percentage yield, and in vitro drug release. Particle size was found to decrease, and drug entrapment efficiency was enhanced with an increase in the polymer concentration. The dissolution study showed sustained drug release from the apigenin-loaded alginate beads with an increase in the polymer proportion. Based on the dissolution profiles, BD6 formulation was optimized and characterized for FTIR, DSC, XRD, and SEM, results of which indicated successful development of apigenin-loaded Ca alginate beads. MTT assay demonstrated a potential anticancer effect against the breast cancer MCF-7 cell lines. The antimicrobial activity exhibited effective inhibition in the bacterial and fungal growth rate. The DPPH measurement revealed that the formulation had substantial antioxidant activity, with EC50 value slightly lowered compared to pure apigenin. A stability study demonstrated that the BD6 was stable with similar (f2) drug release profiles in harsh condition. In conclusion, alginate-based beads could be used for sustaining the drug release of poorly water-soluble apigenin while also improving in vitro antitumor, antimicrobial, and antioxidant activity.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  5. Antimycobacterial activity: synthesis of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues
    Ali MA, Ismail R, Choon TS, Pandian S, Hassan Ansari MZ
    J Enzyme Inhib Med Chem, 2011 Aug;26(4):598-602.
    PMID: 21714764 DOI: 10.3109/14756366.2010.529805
    In this study, a series of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues were synthesized and evaluated for antimycobacterial activity against Mycobacterium tuberculosis (MTB) H(37)Rv and isoniazid resistant M. tuberculosis (INHR-MTB). All the newly synthesized compounds were showing moderate to high inhibitory activities. The compound 6,7-dimethoxy-3-(4-chloro phenyl)-4H-indeno[1,2-c]isoxazole (4b) was found to be the most promising compound, active against MTB H(37)Rv and INHR-MTB with minimum inhibitory concentrations of 0.22 and 0.34 μM.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  6. Sodium carboxymethyl cellulose hydrogels containing reduced graphene oxide (rGO) as a functional antibiofilm wound dressing
    Ali NH, Amin MCIM, Ng SF
    J Biomater Sci Polym Ed, 2019 06;30(8):629-645.
    PMID: 30896336 DOI: 10.1080/09205063.2019.1595892
    Biofilms comprise bacteria attached to wound surfaces and are major contributors to non-healing wounds. It was found that the increased resistance of biofilms to antibiotics allows wound infections to persist chronically in spite of antibiotic therapy. In this study, the reduced form of graphene oxide (rGO) was explored as plausible antibiofilm agents. The rGO was synthesized via reducing the functional groups of GO. Then, rGO were characterized using zetasizer, X-ray photoelectron spectroscopy, UV-Vis spectroscopy and FESEM. The rGO were then formulated into sodium carboxymethyl cellulose (NaCMC) hydrogels to form rGO hydrogel and tested for antibiofilm activities in vitro using XTT test, and in vivo biofilm formation assay using nematodes C. elegans. Reduced GO hydrogel was successfully formed by reducing the functional groups of GO, and a reduction of up to 95% of functional groups was confirmed with X-ray photoelectron spectroscopy analysis. XTT tests confirmed that rGO hydrogels reduced biofilm formation by S. aureus (81-84%) and P. aeruginosa (50-62%). Fluorescence intensity also confirmed that rGO hydrogel can inhibit biofilm bacteria in C. elegans experiments. This study implied that rGO hydrogel is an effective antibiofilm agent for infected wounds.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  7. Identification and characterization of antibacterial compound(s) of cockroaches (Periplaneta americana)
    Ali SM, Siddiqui R, Ong SK, Shah MR, Anwar A, Heard PJ, et al.
    Appl Microbiol Biotechnol, 2017 Jan;101(1):253-286.
    PMID: 27743045 DOI: 10.1007/s00253-016-7872-2
    Infectious diseases remain a significant threat to human health, contributing to more than 17 million deaths, annually. With the worsening trends of drug resistance, there is a need for newer and more powerful antimicrobial agents. We hypothesized that animals living in polluted environments are potential sources of antimicrobials. Under polluted milieus, organisms such as cockroaches encounter different types of microbes, including superbugs. Such creatures survive the onslaught of superbugs and are able to ward off disease by producing antimicrobial substances. Here, we characterized antibacterial properties in extracts of various body organs of cockroaches (Periplaneta americana) and showed potent antibacterial activity in crude brain extract against methicillin-resistant Staphylococcus aureus and neuropathogenic Escherichia coli K1. The size-exclusion spin columns revealed that the active compound(s) are less than 10 kDa in molecular mass. Using cytotoxicity assays, it was observed that pre-treatment of bacteria with lysates inhibited bacteria-mediated host cell cytotoxicity. Using spectra obtained with LC-MS on Agilent 1290 infinity liquid chromatograph, coupled with an Agilent 6460 triple quadruple mass spectrometer, tissues lysates were analysed. Among hundreds of compounds, only a few homologous compounds were identified that contained the isoquinoline group, chromene derivatives, thiazine groups, imidazoles, pyrrole-containing analogs, sulfonamides, furanones, and flavanones and known to possess broad-spectrum antimicrobial properties and anti-inflammatory, anti-tumour, and analgesic properties. Further identification, characterization, and functional studies using individual compounds can act as a breakthrough in developing novel therapeutics against various pathogens including superbugs.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  8. Mechanical, antibacterial, and biocompatibility mechanism of PVD grown silver-tantalum-oxide-based nanostructured thin film on stainless steel 316L for surgical applications
    Alias R, Mahmoodian R, Genasan K, Vellasamy KM, Hamdi Abd Shukor M, Kamarul T
    Mater Sci Eng C Mater Biol Appl, 2020 Feb;107:110304.
    PMID: 31761210 DOI: 10.1016/j.msec.2019.110304
    Surgical site infection associated with surgical instruments has always been a factor in delaying post-operative recovery of patients. The evolution in surface modification of surgical instruments can be a potential choice to overcome the nosocomial infection mainly caused by bacterial populations such as Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. A study was, therefore, conducted characterising the morphology, hydrophobicity, adhesion strength, phase, Nano-hardness, surface chemistry, antimicrobial and biocompatibility of SS 316L steel deposited with a Nano-composite layer of Silver (Ag) and Tantalum oxide (Ta2O5) using physical vapour deposition magnetron sputtering. The adhesion strength of Ag/AgTa2O5 coating on SS 316L and treated at 250-850 °C of thermal treatment was evaluated using micro-scratch. The Ag/Ag-Ta2O5-400 °C was shown a 154% improvement in adhesion strength on SS 316L when compared with as-sputtered layer or Ag/Ag-Ta2O5-250, 550, 700 and 850 °C. The FESEM, XPS, and XRD indicated the segregation of Ag on the surface of SS 316L after the crystallization. Wettability and Nano-indentation tests demonstrated an increase in hydrophobicity (77.3 ± 0.3°) and Nano-hardness (1.12 ± 0.43 GPa) when compared with as-sputtered layer, after the 400 °C of thermal treatment. The antibacterial performance on Ag/Ag-Ta2O5-400 °C indicated a significant zone of inhibition to Staphylococcus aureus (A-axis: 16.33 ± 0.58 mm; B-axis: 25.67 ± 0.58 mm, p 
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  9. Superhydrophobic nanocarbon-based membrane with antibacterial characteristics
    Aljumaily MM, Alsaadi MA, Binti Hashim NA, Mjalli FS, Alsalhy QF, Khan AL, et al.
    Biotechnol Prog, 2020 05;36(3):e2963.
    PMID: 31943942 DOI: 10.1002/btpr.2963
    To overcome the biofouling challenge which faces membrane water treatment processed, the novel superhydrophobic carbon nanomaterials impregnated on/powder activated carbon (CNMs/PAC) was utilized to successfully design prepare an antimicrobial membrane. The research was conducted following a systematic statistical design of experiments technique considering various parameters of composite membrane fabrication. The impact of these parameters of composite membrane on Staphylococcus aureus growth was investigated. The bacteria growth was analyzed through spectrophotometer and SEM. The effect of CNMs' hydrophobicity on the bacterial colonies revealed a decrease in the abundance of bacterial colonies and an alteration in structure with increasing the hydrophobicity. The results revealed that the optimum preparative conditions for carbon loading CNMs/PAC was 363.04 mg with a polymer concentration of 22.64 g/100 g, and a casting knife thickness of 133.91 μm. These conditions have resulted in decreasing the number of bacteria colonies to about 7.56 CFU. Our results provided a strong evidence on the antibacterial effect and consequently on the antibiofouling potential of CNMs/PAC in membrane.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  10. 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
  11. Fulltext Acute toxicity evaluation, antibacterial, antioxidant and immunomodulatory effects of Melastoma malabathricum
    Alnajar ZA, Abdulla MA, Ali HM, Alshawsh MA, Hadi AH
    Molecules, 2012;17(3):3547-59.
    PMID: 22433579 DOI: 10.3390/molecules17033547
    Melastoma malabathricum (MM) is a well-known plant in Malaysian traditional medicine, locally known as senduduk. Its ethanol and aqueous extracts have been used in the present investigation to study the immunomodulatory role on human peripheral blood mononuclear cell (PBMC), and the DPPH, ABTS and FRAP free radical scavenging activities were also measured. Total flavonoids and total phenolic contents were assayed and the antibacterial effect was tested against four species of bacteria; two Gram-positive (Staphylococcus aureus and Streptococcus agalactiae) and two Gram-negative (Escherichia coli and Klebsilla pneumonia). The tests were carried out using the disc diffusion, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methods. Moreover, the acute toxicity was evaluated in vivo on the ethanol extract of MM to establish its safety when administered orally. In our results, both extracts of MM showed abilities to scavenge DPPH and ABTS free radicals, IC(50) values: (11.599 ± 0.84, 10.573 ± 0.58 µmol/L) and (62.657 ± 0.78, 63.939 ± 0.48 µmol/L) for ethanol and aqueous extracts respectively. Indeed the ethanol extract evidenced high phenolic content (384.33 ± 0.005 mg/g), flavonoids contents (85.8 ± 0.009 mg/g) and ferric reducing antioxidant power (33,590 ± 0.038 mmol/g), with high activity against S. aureus and S. agalactiae (11 ± 0.3 and 12 ± 0.6 mm inhibition zones). Likewise, the percentage of peripheral blood mononuclear cells (PBMC) viability was increased in response to MM, IC(50) values (1.781 ± 1.2 and 6.545 ± 0.93 µg/mL) for ethanol and aqueous extracts, respectively. In addition, our results showed that the MM extract is safe even at a high dose of 5,000 mg/kg and has no oral toxicity. These findings suggest the excellent medicinal bioactivity of MM and explain the popularity of this plant in the folk medicine as a remedy for different illnesses.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  12. Martynia annua safety and efficacy: heavy metal profile, in silico and in vitro approaches on antibacterial and antidiabetic activities
    Alrabie A, Al-Rabie NA, Al Saeedy M, Al Adhreai A, Al-Qadsy I, Farooqui M
    Nat Prod Res, 2023 Mar;37(6):1016-1022.
    PMID: 35801965 DOI: 10.1080/14786419.2022.2097227
    Liquid Chromatography-Mass Spectrometry (LC-MS) analysis of methanol extract of Martynia annua seed revealed the presence of haploperozide and austricine. For safety, heavy metals content investigation of plant powder using the Inductively Coupled Plasma-Mass Spectrometry (ICP-MS) technique showed that the toxic metals (Pb: 2.07 mg/kg; Cd: 0.07 mg/kg; and As: 0.18 mg/kg) concentrations were found to be below the permissible limit. The extract demonstrated significant antibacterial activity against E. coli (MIC value 125 g/mL). Furthermore, it was effective in inhibiting both α-glucosidase and α-amylase enzymes with a high percentage and IC50 values were 42.28 ± 0.39 µg/mL and 34.11 ± 0.31 µg/mL, respectively. These findings were supported by a molecular docking study, some of the phytochemicals showed higher docking score values than references. However, Martynia annua seeds are safe to consume because they contain low levels of toxic heavy metals and possess antibacterial and anti-diabetic properties.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  13. An integrative GC-MS and LC-MS metabolomics platform determination of the metabolite profile of Bombax ceiba L. root, and in silico & in vitro evaluation of its antibacterial & antidiabetic activities
    Alrabie A, Alrabie NA, AlSaeedy M, Al-Adhreai A, Al-Qadsy I, Al-Horaibi SA, et al.
    Nat Prod Res, 2023 Jul;37(13):2263-2268.
    PMID: 36441059 DOI: 10.1080/14786419.2022.2149519
    The Bombax ceiba L. tree is a member of the family Bombacaceae and the genus Bombax. Both Chinese and Indian traditional medicine have made extensive use of it in the treatment of sickness. Its chemical composition is still a mystery. B. ceiba roots methanol extract (BCRME) was analyzed by different chromatographic analytical techniques in order to identify its major chemical constituents. Twelve compounds and six compounds were identified from GC-MS and LC-MS analysis, respectively. This is the first report on the presence of lathodoratin, cedrene, 4H-1-benzopyran-4-one,8-[{dimethylamino} methyl]-7-methoxy-3-methyl-2-phenyl, asiatic acid, and (E)-2,4,4'-trihydroxylchalcone in B. ceiba roots. Methanol extract demonstrated noteworthy antibacterial activity against Staphylococcus aureus (MTCC96) (MIC: 100 µg/mL) compare to antibiotic ampicillin (MIC: 250 µg/mL) as well as the highest α-amylase inhibition (IC50=26.91 µg/mL) and α-glucosidase inhibition (IC50=21.21 µg/mL) effects, molecular docking study confirmed these findings, with some compounds having a very high docking score.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  14. Fulltext Isolation and characterization of cyclo-(tryptophanyl-prolyl) and chloramphenicol from Streptomyces sp. SUK 25 with antimethicillin-resistant Staphylococcus aureus activity
    Alshaibani MM, Jalil J, Sidik NM, Edrada-Ebel R, Zin NM
    Drug Des Devel Ther, 2016;10:1817-27.
    PMID: 27330275 DOI: 10.2147/DDDT.S101212
    BACKGROUND: Zingiber spectabile, commonly known as Beehive Ginger, is used as an ethnobotanical plant in many countries as an appetizer or to treat stomachache, toothache, muscle sprain, and as a cure for swelling, sores and cuts. This is the first report of isolation of Streptomyces strain from the root of this plant. Strain Universiti Kebangsaan 25 (SUK 25) has a very high activity to produce secondary metabolites against methicillin-resistant Staphylococcus aureus (MRSA), which is associated with high morbidity and mortality rates due to acquired multidrug resistance genes and causes medication failure in some clinical cases worldwide. Phylogenetic analysis based on the 16S ribosomal RNA gene sequence exhibited that the most closely related strain was Streptomyces omiyaensis NBRC 13449T (99.0% similarity).

    AIM: This study was conducted to carry out the extraction, identification, and biological evaluation of active metabolites isolated from SUK 25 against three MRSA strains, namely, MRSA ATCC 43300, MRSA ATCC 33591, and MRSA ATCC 49476.

    MATERIALS AND METHODS: The production of secondary metabolites by this strain was optimized through Thronton's media. Isolation, purification, and identification of the bioactive compounds were carried out using reversed-phase high-performance liquid chromatography, high-resolution mass spectrometry, Fourier transform infrared, and one-dimensional and two-dimensional nuclear magnetic resonance.

    RESULTS: During screening procedure, SUK 25 exhibited good antimicrobial potential against several strains of MRSA. The best biological activity was shown from fraction number VII and its subfractions F2 and F3 with minimum inhibitory concentration values at 16 µg/mL and 8 µg/mL, respectively. These two subfractions were identified as diketopiperazine cyclo-(tryptophanyl-prolyl) and chloramphenicol.

    CONCLUSION: On the basis of obtained results, SUK 25 isolated from Z. spectabile can be regarded as a new valuable source to produce secondary metabolites against bacteria, especially MRSA.

    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  15. Fulltext Free radical scavenging, antimicrobial and immunomodulatory activities of Orthosiphon stamineus
    Alshawsh MA, Abdulla MA, Ismail S, Amin ZA, Qader SW, Hadi HA, et al.
    Molecules, 2012;17(5):5385-95.
    PMID: 22569417 DOI: 10.3390/molecules17055385
    Orthosiphon stamineus is considered an important traditional folk medicine. In this study ethanol and aqueous extracts of O. stamineus were evaluated in vitro for their antioxidant, antimicrobial as well as for their immunomodulatory properties on human peripheral blood mononuclear cells (PBMCs). The DPPH radical scavenging method was used for the determination of antioxidant activity, while the antibacterial efficacy was investigated by both disc diffusion method and Minimum Inhibitory Concentration (MIC) against four bacterial strains (Gram-positive and Gram-negative). Furthermore, the immunomodulatory potential of the extracts was investigated through the MTT assay. Aqueous extract of O. stamineus exhibited significant free radical scavenging activity with IC₅₀ 50 9.6 µg/mL, whereas the IC₅₀ for the ethanol extract was 21.4 µg/mL. The best antimicrobial activity was shown by the aqueous extract of O. stamineus against Staphylococcus aureus, with inhibition zone of 10.5 mm and MIC value 1.56 mg/mL. Moreover, the results observed from the MTT assay showed that both plant extracts stimulated the PBMCs proliferation in vitro in a concentration-dependent manner, but the aqueous extract has remarkable activity against PBMCs. These findings indicate that O. stamineus showed high antioxidant activity and may be considered as an immunomodulatory agent.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  16. 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
  17. A dual-action chitosan-based nanogel system of triclosan and flurbiprofen for localised treatment of periodontitis
    Aminu N, Chan SY, Yam MF, Toh SM
    Int J Pharm, 2019 Oct 30;570:118659.
    PMID: 31493495 DOI: 10.1016/j.ijpharm.2019.118659
    This study aimed to develop a dual action, namely anti-inflammatory and antimicrobial, nanogels (NG) for the treatment of periodontitis using triclosan (TCS) and flurbiprofen (FLB). Triclosan, an antimicrobial drug, was prepared as nanoparticles (NPs) using poly-ε-caprolactone (PCL), while flurbiprofen, an anti-inflammatory drug, was directly loaded in a chitosan (CS) based hydrogel. The entwinement of both NPs and hydrogel loaded systems resulted in the NG. The characterisation data confirmed that the developed formulation consists of nanosized spherical structures and displays pH-dependent swelling/erosion and temperature-responsiveness. Besides, the NG exhibited adequate bioadhesiveness using the chicken pouch model and displayed antibacterial activity through the agar plate method. An in-vivo study of the NG on experimental periodontitis (EP) rats confirmed the dual antibacterial and anti-inflammatory effects which revealed an excellent therapeutic outcome. In conclusion, a dual action NG was successfully developed and proved to have superior therapeutic effects in comparison to physical mixtures of the individual drugs.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  18. Fulltext Antimicrobial activities of green synthesized gums-stabilized nanoparticles loaded with flavonoids
    Anwar A, Masri A, Rao K, Rajendran K, Khan NA, Shah MR, et al.
    Sci Rep, 2019 02 28;9(1):3122.
    PMID: 30816269 DOI: 10.1038/s41598-019-39528-0
    Herein, we report green synthesized nanoparticles based on stabilization by plant gums, loaded with citrus fruits flavonoids Hesperidin (HDN) and Naringin (NRG) as novel antimicrobial agents against brain-eating amoebae and multi-drug resistant bacteria. Nanoparticles were thoroughly characterized by using zetasizer, zeta potential, atomic force microscopy, ultravoilet-visible and Fourier transform-infrared spectroscopic techniques. The size of these spherical nanoparticles was found to be in the range of 100-225 nm. The antiamoebic effects of these green synthesized Silver and Gold nanoparticles loaded with HDN and NRG were tested against Acanthamoeba castellanii and Naegleria fowleri, while antibacterial effects were evaluated against methicillin-resistant Staphylococcus aureus (MRSA) and neuropathogenic Escherichia coli K1. Amoebicidal assays revealed that HDN loaded Silver nanoparticles stabilized by gum acacia (GA-AgNPs-HDN) quantitatively abolished amoeba viability by 100%, while NRG loaded Gold nanoparticles stabilized by gum tragacanth (GT-AuNPs-NRG) significantly reduced the viability of A. castellanii and N. fowleri at 50 µg per mL. Furthermore, these nanoparticles inhibited the encystation and excystation by more than 85%, as well as GA-AgNPs-HDN only completely obliterated amoeba-mediated host cells cytopathogenicity. Whereas, GA-AgNPs-HDN exhibited significant bactericidal effects against MRSA and E. coli K1 and reduced bacterial-mediated host cells cytotoxicity. Notably, when tested against human cells, these nanoparticles showed minimal (23%) cytotoxicity at even higher concentration of 100 µg per mL as compared to 50 µg per mL used for antimicrobial assays. Hence, these novel nanoparticles formulations hold potential as therapeutic agents against infections caused by brain-eating amoebae, as well as multi-drug resistant bacteria, and recommend a step forward in drug development.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  19. 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
  20. Synthesis and characterization of nitrile functionalized silver(I)-N-heterocyclic carbene complexes: DNA binding, cleavage studies, antibacterial properties and mosquitocidal activity against the dengue vector, Aedes albopictus
    Asekunowo PO, Haque RA, Razali MR, Avicor SW, Wajidi MFF
    Eur J Med Chem, 2018 Apr 25;150:601-615.
    PMID: 29550733 DOI: 10.1016/j.ejmech.2018.03.029
    A series of four benzimidazolium based nitrile-functionalized mononuclear-Ag(I)-N-heterocyclic carbene and binuclear-Ag(I)-N-heterocyclic carbene (Ag(I)-NHC) hexafluorophosphate complexes (5b-8b) were synthesized by reacting the corresponding hexafluorophosphate salts (1b-4b) with Ag2O in acetonitrile, respectively. These compounds were characterized by 1H NMR, 13C NMR, IR, UV-visible spectroscopic techniques, elemental analyses and molar conductivity. Additionally, 8b was structurally characterized by single crystal X-ray diffraction technique. Preliminary in vitro antibacterial evaluation was conducted for all the compounds against two standard bacteria; gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacterial strains. Most of the Ag(I)-NHC complexes (5b-8b) showed moderate to good antibacterial activity with MIC values in the range of 12.5-100 μg/mL. Especially, compound 8b exhibited promising anti-Staphylococcus aureus activity with a low MIC value (12.5 μg/mL). However, all the hexafluorophosphate salts (1b-4b) were inactive against the bacteria strains. The preliminary interactive investigation revealed that the most active compound, 8b, could effectively intercalate into DNA to form 8b-DNA complex which shows a better binding ability for DNA (Kb = 3.627 × 106) than the complexes 5b-7b (2.177 × 106, 8.672 × 105 and 6.665 × 105, respectively). Nuclease activity of the complexes on plasmid DNA and Aedes albopictus genomic DNA was time-dependent, although minimal. The complexes were larvicidal to the mosquito, with 5b, 6b and 8b being highly active. Developmental progression from the larval to the adult stage was affected by the complexes, progressively being toxic to the insect's development with increasing concentration. These indicate the potential use of these complexes as control agents against bacteria and the dengue mosquito Ae. albopictus.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
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