Displaying publications 101 - 120 of 278 in total

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  1. Designing potential lead compounds targeting aminoglycoside N (6')-acetyltransferase in Serratia marcescens: A drug discovery strategy
    Prabhu D, Shankari G, Rajamanikandan S, Jeyakanthan J, Velusamy P, Gopinath SCB, et al.
    Int J Biol Macromol, 2024 Nov;281(Pt 1):136976.
    PMID: 39490491 DOI: 10.1016/j.ijbiomac.2024.136976
    Serratia marcescens is an opportunistic human pathogen that causes urinary tract infections, ocular lens infections, and respiratory tract infections. S. marcescens employs various defense mechanisms to evade antibiotics, one of which is mediated by aminoglycoside N-acetyltransferase (AAC). In this mechanism, the enzyme AAC facilitates the transfer and linkage of the acetyl moiety from the donor substrate acetyl-coenzyme A to specific positions on antibiotics. This modification alters the antibiotic's structure, leading to the inactivation of aminoglycoside antibiotics. In the current scenario, antibiotic resistance has become a global threat, and targeting the enzymes that mediate resistance is considered crucial to combat this issue. The study aimed to address the increasing global threat of antibiotic resistance in Serratia marcescens by targeting the aminoglycoside N-acetyltransferase (AAC (6')) enzyme, which inactivates aminoglycoside antibiotics through acetylation. Due to the absence of experimental structure, we constructed a homology model of aminoglycoside N (6')-acetyltransferase (AAC (6')) of S. marcescens using the atomic structure of aminoglycoside N-acetyltransferase AAC (6')-Ib (PDB ID: 1V0C) as a template. The stable architecture and integrity of the modelled AAC (6') structure were analyzed through a 100 ns simulation. Structure-guided high-throughput screening of four small molecule databases (Binding, Life Chemicals, Zinc, and Toslab) resulted in the identification of potent inhibitors against AAC (6'). The hits obtained from screening were manually clustered, and the five hit molecules were shortlisted based on the docking score, which are observed in the range of -17.09 kcal/mol to -11.95 kcal/mol. These selected five molecules displayed acceptable pharmacological properties in ADME predictions. The binding free energy calculations, and molecular dynamics simulations of ligand bound AAC (6') complexes represented higher affinity and stable binding. The selected molecules demonstrated stable binding with AAC (6'), indicating their strong potential to hamper the binding of aminoglycoside in the respective site. and thereby inhibit. This process mitigates enzyme mediated AAC (6') activity on aminoglycosides and reverse the bactericidal function of aminoglycosides, and also this method could serve as a platform for the development of potential antimicrobials.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  2. How Important is the Metal-free Catalytic Knoevenagel Reaction in Medicinal Chemistry? An Updated Review
    Johari S, Johan MR, Khaligh NG
    Curr Med Chem, 2024;31(27):4286-4311.
    PMID: 38243980 DOI: 10.2174/0109298673260463231122074253
    The Knoevenagel condensation is a powerful and primary step for the development of carbon-carbon bond transformations. These condensations offer versatile products/ intermediates for diverse uses in polymers, cosmetics, chemical industries, and medicinal chemistry. Various homogenous and heterogenous catalysts have been found to promote the Knoevenagel condensation reaction, both environmentally and economically. Due to their attractive use in the production of pharmaceutical drugs, they are proven to be the main force that drives the synthesis involving numerous multi-component and multistep reactions. The present study, therefore, aims to summarise reported Knoevenagel condensation reactions using metal-free catalysts resulting in pharmaceutically useful compounds with anti-cancer, anti-tumor, anti-oxidant, anti-malarial, anti-diabetic, and anti- bacterial activities. By considering factors like their structure-activity relationships (SARs), the reaction conditions, and the steps involved, as well as the advantages and limitations of the particular approach, we also provide a general framework and direction in order to achieve superior characteristics of the catalyst.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  3. Development and Characterization of Fusidic Acid-Loaded Alginate-Aloe vera Based Hydrogel Film
    Dayoob M, Kee YWY, Bahrin WH, Alrimawi BH, Kumarasamy V, Subramaniyan V, et al.
    J Vis Exp, 2024 Dec 13.
    PMID: 39760405 DOI: 10.3791/67068
    A new fusidic acid-loaded hydrogel film was prepared via the solvent casting technique using alginate and Aloe vera. The hydrogel films were optimized using different ratios of sodium alginate, Aloe vera, and glycerin. The films containing 10% glycerin (w/w of alginate) exhibited the best appearance. Incorporating Aloe vera influenced the thickness, swelling behavior, water vapor permeability, and drug release profile of the hydrogel films. Higher Aloe vera content resulted in thicker films (up to a certain ratio), increased swelling, reduced water vapor permeability, and a prolonged drug release of up to 93% over 12 h. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the presence of key functional groups and the interaction between the hydrogel components. The study suggests that the combination of sodium alginate, Aloe vera, and glycerin can improve the mechanical properties and drug release profiles of hydrogel films, making them a promising option for enhanced topical drug delivery and wound healing applications.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  4. Glycyrrhizic Acid-Loaded Poloxamer and HPMC-Based In Situ Forming Gel of Acacia Honey for Improved Wound Dressing: Formulation Optimization and Characterization for Wound Treatment
    Jha B, Majie A, Roy K, Lim WM, Gorain B
    ACS Appl Bio Mater, 2025 Jan 20;8(1):310-328.
    PMID: 39657741 DOI: 10.1021/acsabm.4c01212
    The present study aims to formulate a stimuli-responsive in situ hydrogel system to codeliver acacia honey and glycyrrhizic acid for topical application that will aid in absorbing wound exudates, control microbial infestation, and produce angiogenic and antioxidant effects to accelerate wound healing. Therefore, both the natural active constituents were incorporated within an in situ hydrogel composed of poloxamer and hydroxypropyl methylcellulose (HPMC), where the concentrations of the polymers were optimized using Design-Expert software considering optimum values of the dependent variables, gelation temperature (34-37 °C), gelation time (<10 min), and the viscosity (2000-3500 cPs). The optimized formulation showed improved physicochemical properties such as mucoadhesiveness, porosity, swelling, and spreadability, which makes it suitable for wound application. Additionally, the in situ hydrogel exhibited potent in vitro and ex vivo antioxidant effects, in vitro antimicrobial activities, and ex ovo angiogenic effects. Furthermore, the optimized formulation was found to be nontoxic while tested in the HaCaT cell line and acute dermal irritation and corrosion study. The findings of the in vivo wound-healing studies in experimental animal models showed complete wound closure within 15 days of treatment and accelerated development of the extracellular matrix. In addition, the antioxidant, antimicrobial, angiogenic, and wound-healing properties of acacia honey and glycyrrhizic acid coloaded in situ hydrogel were also found to be promising when compared to the standard treatments. Overall, it can be concluded that the optimized stimuli-responsive in situ hydrogel containing two natural compounds could be an alternative to existing topical formulations for acute wounds.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  5. 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
  6. Fulltext Studies on properties of rice straw/polymer nanocomposites based on polycaprolactone and Fe₃O₄ nanoparticles and evaluation of antibacterial activity
    Khandanlou R, Ahmad MB, Shameli K, Saki E, Kalantari K
    Int J Mol Sci, 2014;15(10):18466-83.
    PMID: 25318051 DOI: 10.3390/ijms151018466
    Modified rice straw/Fe3O4/polycaprolactone nanocomposites (ORS/Fe3O4/ PCL-NCs) have been prepared for the first time using a solution casting method. The RS/Fe3O4-NCs were modified with octadecylamine (ODA) as an organic modifier. The prepared NCs were characterized by using X-ray powder diffraction (XRD), Scanning electron microscopy (SEM), Transmission electron microscopy (TEM), Thermogravimetric analysis (TGA) and Fourier transform infrared spectroscopy (FT-IR). The XRD results showed that as the intensity of the peaks decreased with the increase of ORS/Fe3O4-NCs content in comparison with PCL peaks, the Fe3O4-NPs peaks increased from 1.0 to 60.0 wt. %. The TEM and SEM results showed a good dispersion of ORS/Fe3O4-NCs in the PCL matrix and the spherical shape of the NPs. The TGA analysis indicated thermal stability of ORS/Fe3O4-NCs increased after incorporation with PCL but the thermal stability of ORS/Fe3O4/PCL-NCs decreased with the increase of ORS/Fe3O4-NCs content. Tensile strength was improved with the addition of 5.0 wt. % of ORS/Fe3O4-NCs. The antibacterial activities of the ORS/Fe3O4/PCL-NC films were examined against Gram-negative bacteria (Escherichia coli) and Gram-positive bacteria (Staphylococcus aureus) by diffusion method using nutrient agar. The results indicated that ORS/Fe3O4/PCL-NC films possessed a strong antibacterial activity with the increase in the percentage of ORS/Fe3O4-NCs in the PCL.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  7. Fulltext The effect of various media and hormones via suspension culture on secondary metabolic activities of (Cape Jasmine) Gardenia jasminoides Ellis
    Farzinebrahimi R, Mat Taha R, Rashid K, Syafawati Yaacob J
    ScientificWorldJournal, 2014;2014:407284.
    PMID: 24967432 DOI: 10.1155/2014/407284
    The leaf of Gardenia jasminoides Ellis was used as explants and was cultured on MS and WPM media supplemented with various concentrations of NAA, IAA, 2,4-D, IBA, TDZ, and Kn (0 to 5 mg L(-1) with 0.5 increment). After six months, the higher percentage of callus (100%) and the best dry and fresh weight of callus were formed on WPM medium supplemented with 2,4-D and NAA (2.0-3.0 mg L(-1)) and this amount was decreased from (84%) to (69%) when this media supplemented with Kinetin and TDZ (1 mg L(-1)) respectively were used. Leaf segments cultured on WPM media added with Kn (1 mg L(-1)) and TDZ (2 mg L(-1)) yielded the least amount of callus. It was found that WPM media added with IAA (4.5-5.0 mg L(-1)) were optimum for root induction from G. jasminoides plantlets. Antibacterial screening of leaf extracts (in vivo) showed no inhibitory effect against E. coli, P. aeruginosa, S. aureus, and B. cereus, in contrast to callus extracts from leaf cultures supplemented with NAA, which showed inhibition activity against E. coli and B. cereus. The callus extracts from leaf cultures grown on both MS and WPM media showed higher antioxidant and superoxide dismutase activities than leaf extracts.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  8. Fulltext Novel kojic acid-polymer-based magnetic nanocomposites for medical applications
    Hussein-Al-Ali SH, El Zowalaty ME, Hussein MZ, Ismail M, Dorniani D, Webster TJ
    Int J Nanomedicine, 2014;9:351-62.
    PMID: 24453486 DOI: 10.2147/IJN.S53847
    Iron oxide magnetic nanoparticles (MNPs) were synthesized by the coprecipitation of iron salts in sodium hydroxide followed by coating separately with chitosan (CS) and polyethylene glycol (PEG) to form CS-MNPs and PEG-MNPs nanoparticles, respectively. They were then loaded with kojic acid (KA), a pharmacologically bioactive natural compound, to form KA-CS-MNPs and KA-PEG-MNPs nanocomposites, respectively. The MNPs and their nanocomposites were characterized using powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetric analysis, vibrating sample magnetometry, and scanning electron microscopy. The powder X-ray diffraction data suggest that all formulations consisted of highly crystalline, pure magnetite Fe3O4. The Fourier transform infrared spectroscopy and thermogravimetric analysis confirmed the presence of both polymers and KA in the nanocomposites. Magnetization curves showed that both nanocomposites (KA-CS-MNPs and KA-PEG-MNPs) were superparamagnetic with saturation magnetizations of 8.1 emu/g and 26.4 emu/g, respectively. The KA drug loading was estimated using ultraviolet-visible spectroscopy, which gave a loading of 12.2% and 8.3% for the KA-CS-MNPs and KA-PEG-MNPs nanocomposites, respectively. The release profile of the KA from the nanocomposites followed a pseudo second-order kinetic model. The agar diffusion test was performed to evaluate the antimicrobial activity for both KA-CS-MNPs and KA-PEG-MNPs nanocomposites against a number of microorganisms using two Gram-positive (methicillin-resistant Staphylococcus aureus and Bacillus subtilis) and one Gram-negative (Salmonella enterica) species, and showed some antibacterial activity, which could be enhanced in future studies by optimizing drug loading. This study provided evidence for the promise for the further investigation of the possible beneficial biological activities of KA and both KA-CS-MNPs and KA-PEG-MNPs nanocomposites in nanopharmaceutical applications.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  9. Fulltext Chemical analysis, inhibition of biofilm formation and biofilm eradication potential of Euphorbia hirta L. against clinical isolates and standard strains
    Perumal S, Mahmud R
    BMC Complement Altern Med, 2013;13:346.
    PMID: 24321370 DOI: 10.1186/1472-6882-13-346
    The frequent occurrences of antibiotic-resistant biofilm forming pathogens have become global issue since various measures that had been taken to curb the situation led to failure. Euphorbia hirta, is a well-known ethnomedicinal plant of Malaysia with diverse biological activities. This plant has been used widely in traditional medicine for the treatment of gastrointestinal, bronchial and respiratory ailments caused by infectious agents.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  10. Synthesis and biological evaluation of novel substituted 1,3,4-thiadiazole and 2,6-di aryl substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives
    Chandrakantha B, Isloor AM, Shetty P, Fun HK, Hegde G
    Eur J Med Chem, 2014 Jan;71:316-23.
    PMID: 24321835 DOI: 10.1016/j.ejmech.2013.10.056
    A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a-l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a-l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-ylamine. The synthesized compounds were characterized by IR, NMR, mass spectral and elemental analysis. All the compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by well plate method (zone of inhibition). Compounds 4a, 4c and 6e, 6g displayed appreciable activity at the concentration 0.5-1.0 mg/mL.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  11. Fulltext Improvement of medium chain fatty acid content and antimicrobial activity of coconut oil via solid-state fermentation using a Malaysian Geotrichum candidum
    Khoramnia A, Ebrahimpour A, Ghanbari R, Ajdari Z, Lai OM
    Biomed Res Int, 2013;2013:954542.
    PMID: 23971051 DOI: 10.1155/2013/954542
    Coconut oil is a rich source of beneficial medium chain fatty acids (MCFAs) particularly lauric acid. In this study, the oil was modified into a value-added product using direct modification of substrate through fermentation (DIMOSFER) method. A coconut-based and coconut-oil-added solid-state cultivation using a Malaysian lipolytic Geotrichum candidum was used to convert the coconut oil into MCFAs-rich oil. Chemical characteristics of the modified coconut oils (MCOs) considering total medium chain glyceride esters were compared to those of the normal coconut oil using ELSD-RP-HPLC. Optimum amount of coconut oil hydrolysis was achieved at 29% moisture content and 10.14% oil content after 9 days of incubation, where the quantitative amounts of the modified coconut oil and MCFA were 0.330 mL/g of solid media (76.5% bioconversion) and 0.175 mL/g of solid media (53% of the MCO), respectively. MCOs demonstrated improved antibacterial activity mostly due to the presence of free lauric acid. The highest MCFAs-rich coconut oil revealed as much as 90% and 80% antibacterial activities against Staphylococcus aureus and Escherichia coli, respectively. The results of the study showed that DIMOSFER by a local lipolytic G. candidum can be used to produce MCFAs as natural, effective, and safe antimicrobial agent. The produced MCOs and MCFAs could be further applied in food and pharmaceutical industries.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  12. Fulltext Synthesis, characterization, X-ray structure and biological activities of C-5-bromo-2-hydroxyphenylcalix[4]-2-methyl resorcinarene
    Abosadiya HM, Hasbullah SA, Mackeen MM, Low SC, Ibrahim N, Koketsu M, et al.
    Molecules, 2013;18(11):13369-84.
    PMID: 24172244 DOI: 10.3390/molecules181113369
    C-5-bromo-2-hydroxyphenylcalix[4]-2-methylresorcinarene (I) was synthesized by cyclocondensation of 5-bromo-2-hydroxybenzaldehyde and 2-methylresorcinol in the presence of concentrated HCl. Compound I was characterized by infrared and nuclear magnetic resonance spectroscopic data. X-ray analysis showed that this compound crystallized in a triclinic system with space group of Pī, a = 15.9592(16)Å, b = 16.9417(17)Å, c = 17.0974(17)Å, α = 68.656(3)°, β = 85.689(3)°, γ = 81.631(3)°, Z = 2 and V = 4258.6(7)Å3. The molecule adopts a chair (C2h) conformation. The thermal properties and antioxidant activity were also investigated. It was strongly antiviral against HSV-1 and weakly antibacterial against Gram-positive bacteria. Cytotoxicity testing on Vero cells showed that it is non-toxic, with a CC50 of more than 0.4 mg/mL.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  13. Sterically tuned Ag(I)- and Pd(II)-N-heterocyclic carbene complexes of imidazol-2-ylidenes: synthesis, crystal structures, and in vitro antibacterial and anticancer studies
    Haque RA, Salman AW, Budagumpi S, Abdullah AA, Majid AM
    Metallomics, 2013 Jun;5(6):760-9.
    PMID: 23645390 DOI: 10.1039/c3mt00051f
    Unsymmetrically substituted sterically tuned Pd(II)–NHC complexes of the general formula [PdCl2(NHC)2] (NHC = 1-allyl-3-methylimidazolin-2-ylidene, 7; 1-allyl-3-butylimidazol-2-ylidene, 8; 1-benzyl-3-butyl imidazolin-2-ylidene, 9) were prepared through transmetallation from their corresponding Ag(I)–NHC complexes. The Pd complexes were structurally characterized by different spectroscopic and X-ray diffraction methods. Complexes 7 and 9 adopted a trans–anti arrangement of the NHC ligands, whereas complex 8 adopted a cis–syn arrangement. Preliminary antibiogram studies using Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria showed that Ag(I)–NHC complexes demonstrate higher activity compared with Pd(I)–NHC complexes. Furthermore, Pd(II)–NHC complexes were evaluated for their anticancer potential using the human colorectal cancer cell line. A higher anticancer activity was observed for complexes 8 and 9, with 26.5 and 6.6 mM IC50 values, respectively.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  14. 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
  15. 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
  16. Purification and characterisation of antibacterial peptide-containing compound derived from palm kernel cake
    Tan YN, Ayob MK, Wan Yaacob WA
    Food Chem, 2013 Jan 1;136(1):279-84.
    PMID: 23017424 DOI: 10.1016/j.foodchem.2012.08.012
    Palm kernel cake (PKC), the most useful by-product resulted from palm kernel oil production. In this study, PKC-derived protein product was found suitable for use as an antimicrobial agent with potent antibacterial activity, particularly against Bacillus species, after enzymatic hydrolysis with alcalase. The hydrolysate was further purified by gel filtration chromatography. The purified fraction was found to have 14.63±0.70% (w/w) protein, a molecular mass of 2.4kDa and low hemolytic activity (<50% hemolysis of human erythrocytes at concentration of 1000μg/ml). The presence of lysine and the major component lauric acid derivative, as indicated by electrospray ionisation-mass spectrometry (ESI-MS) direct infusion and nuclear magnetic resonance (NMR) spectroscopy, may have contributed to the antibacterial effect of purified PKC fraction. This study suggests that the antibacterial PKC compound may be not a pure peptide but instead a peptide-containing compound high in lauric acid derivative.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  17. Essential oil composition, cytotoxic and antibacterial activities of five Etlingera species from Borneo
    Vairappan CS, Nagappan T, Palaniveloo K
    Nat Prod Commun, 2012 Feb;7(2):239-42.
    PMID: 22474969
    Essential oils obtained by hydrodistillation from the rhizomes of Etlingera pyramidosphaera (K. Schum.) R. M. Sm, E. megalocheilos (Griff.) A.D. Poulsen, comb. nov., E. coccinea (Blume) S. Sakai & Nagam, E. elatior (Jack) R. M. Sm, and E. brevilabrum (Valeton) R. M. Sm were analyzed by GCMS. The highest oil yield was obtained from E. pyramidosphaera (0.45%), followed by E. elatior (0.38%), E. coccinea (0.30%), E. brevilabrum (0.28%) and E. megalocheilos (0.25%). The major constituents of the essential oils were oxygenated monoterpenes, followed by sesquiterpenes, oxygenated sesquiterpenes, oxygenated diterpenes and diterpenes. The essential oils from E. pyramidosphaera and E. brevilabrum exhibited the best cytotoxicity against MCF 7 (LC50: 7.5 +/- 0.5 mg mL(-1)) and HL 60 (LC50: 5.0 mg mL(-1)), respectively. Strong inhibition was also observed for the essential oils of E. coccinea and E. megalocheilos against Staphylococcus aureus (MIC: 8.0 +/- 0.5 mg mL(-1), and 5.0 +/- 0.5 mg mL(-1)) and Streptococcus pyrogenes (MIC: 6.0 +/- 0.5 mg mL(-1) and 8.0 +/- 0.5 mg mL(-1)).
    Matched MeSH terms: Anti-Bacterial Agents/chemistry*
  18. Synthesis and anti-microbial potencies of 1-(2-hydroxyethyl)-3-alkylimidazolium chloride ionic liquids: microbial viabilities at different ionic liquids concentrations
    Hossain MI, El-Harbawi M, Alitheen NB, Noaman YA, Lévêque JM, Yin CY
    Ecotoxicol Environ Saf, 2013 Jan;87:65-9.
    PMID: 23107478 DOI: 10.1016/j.ecoenv.2012.09.020
    Three 1-(2-hydroxyethyl)-3-alkylimidazolium chloride room temperature ionic liquids (ILs) [2OHimC(n)][Cl]; (n=0, 1, 4) have been synthesized from the appropriate imidazole precursors and characterized by IR and NMR spectroscopies and elemental analysis. Their anti-microbial activities were investigated using the well-diffusion method. The viabilities of Escherichia coli, Aeromonas hydrophila, Listeria monocytogenes and Salmonella enterica as a function of IL concentrations were studied. The minimal inhibitory concentrations (MICs) and EC₅₀ values for the present ILs were within the concentration range from 60 to 125 mM and 23 to 73 mM. The anti-microbial potencies of the present ILs were compared to a standard antibiotic, gentamicin. The finding affords additional perspective on the level of ILs toxicity to aquatic lifeforms and yet, this characteristic can be readily harnessed to detect microbial growth and activity.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  19. Search for antibacterial agents from Malaysian rainforest and tropical plants
    Othman M, Genapathy S, Liew PS, Ch'ng QT, Loh HS, Khoo TJ, et al.
    Nat Prod Res, 2011 Nov;25(19):1857-64.
    PMID: 21838540 DOI: 10.1080/14786419.2010.537274
    The world's rainforests hold untold potential for drug discovery. Rainforest plants are thought to contain evolved defensive active metabolites of greater diversity compared to plants from temperate regions. In recent years, the interest and overall output from pharmaceutical companies on novel antibacterial agents has diminished at a time when there is a critical need for them to fight the threat of resistance. In this study, we have investigated the antimicrobial properties of 21 flowering plants from 16 different families against six bacterial strains consisting of two Gram negative and four Gram positive. Using the pour plate disc diffusion technique, almost all extracts from these plants were found to be active against some of the bacterial strains tested. The most interesting and active plants with broad spectrum activities include Duabanga grandiflora, Acalypha wilkesiana and Pseuduvaria macrophylla where the minimum inhibitory concentration, minimum bactericidal concentration and phytochemical analysis were carried out. This is the first report describing the antimicrobial and phytochemical properties of D. grandiflora and P. macrophylla. Our findings support the utilisation of higher plant species in the search for new antimicrobial molecules to combat new emerging infective diseases and the problem of drug resistant pathogens.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry
  20. 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
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