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  1. Baig U, Gondal MA, Alam MF, Wani WA, Younus H
    J. Photochem. Photobiol. B, Biol., 2016 Nov;164:244-255.
    PMID: 27710872 DOI: 10.1016/j.jphotobiol.2016.09.034
    Cancer and pathogenic microbial diseases have terribly affected human health over a longer period of time. In response to the increasing casualties due to cancer and microbial diseases, unique poly(3-methylthiophene) and poly(3-methylthiophene)-titanium(IV)phosphate composite were prepared via in-situ oxidative chemical polymerization in this work. The poly(3-methylthiophene) and poly(3-methylthiophene)-titanium(IV)phosphate composite were well characterized by Fourier transform infrared spectroscopy and field emission scanning electron microscopy. DNA binding studies by UV-Visible and fluorescence spectroscopic investigations indicated strong binding affinities of poly(3-methylthiophene) and poly(3-methylthiophene)-titanium(IV)phosphate nanocomposite; leading to structural damage of DNA. Poly(3-methylthiophene)-titanium(IV)phosphate nanocomposite showed stronger interactions with DNA as compared to poly(3-methylthiophene) and from dye displacement assay it was confirmed that mode of binding of both the formulations was intercalative. The antimicrobial screening revealed that polymer and its composite displayed stronger antibacterial effects than ampicillin against Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhimurium. Besides, the poly(3-methylthiophene) and poly(3-methylthiophene)-titanium(IV)phosphate nanocomposite showed dose dependent effects towards estrogen receptor positive breast cancer (MCF-7) and estrogen receptor negative breast cancer (MDA-MB-231) cell lines; with poly(3-methylthiophene)-titanium(IV)phosphate nanocomposite showing better activities against both cell lines. In all in-vitro biological investigations, poly(3-methylthiophene)-titanium(IV)phosphate composite showed superior properties to that of the pure poly(3-methylthiophene), which encouraged us to suggest its potential as future therapeutic gear in drug delivery and other allied fields.
    Matched MeSH terms: Polymers/pharmacology*; Thiophenes/pharmacology*; Titanium/pharmacology*
  2. Tayyab S, Izzudin MM, Kabir MZ, Feroz SR, Tee WV, Mohamad SB, et al.
    J. Photochem. Photobiol. B, Biol., 2016 Sep;162:386-94.
    PMID: 27424099 DOI: 10.1016/j.jphotobiol.2016.06.049
    Binding characteristics of a promising anticancer drug, axitinib (AXT) to human serum albumin (HSA), the major transport protein in human blood circulation, were studied using fluorescence, UV-vis absorption and circular dichroism (CD) spectroscopy as well as molecular docking analysis. A gradual decrease in the Stern-Volmer quenching constant with increasing temperature revealed the static mode of the protein fluorescence quenching upon AXT addition, thus confirmed AXT-HSA complex formation. This was also confirmed from alteration in the UV-vis spectrum of HSA upon AXT addition. Fluorescence quenching titration results demonstrated moderately strong binding affinity between AXT and HSA based on the binding constant value (1.08±0.06×10(5)M(-1)), obtained in 10mM sodium phosphate buffer, pH7.4 at 25°C. The sign and magnitude of the enthalpy change (∆H=-8.38kJmol(-1)) as well as the entropy change (∆S=+68.21Jmol(-1)K(-1)) clearly suggested involvement of both hydrophobic interactions and hydrogen bonding in AXT-HSA complex formation. These results were well supported by molecular docking results. Three-dimensional fluorescence spectral results indicated significant microenvironmental changes around Trp and Tyr residues of HSA upon complexation with AXT. AXT binding to the protein produced significant alterations in both secondary and tertiary structures of HSA, as revealed from the far-UV and the near-UV CD spectral results. Competitive drug displacement results obtained with phenylbutazone (site I marker), ketoprofen (site II marker) and hemin (site III marker) along with molecular docking results suggested Sudlow's site I, located in subdomain IIA of HSA, as the preferred binding site of AXT.
    Matched MeSH terms: Antineoplastic Agents/pharmacology; Imidazoles/pharmacology; Indazoles/pharmacology
  3. Taha M, Ismail NH, Imran S, Wadood A, Rahim F, Al Muqarrabin LM, et al.
    Bioorg Chem, 2016 10;68:15-22.
    PMID: 27414468 DOI: 10.1016/j.bioorg.2016.07.002
    Novel series of disulfide and sulfone hybrid analogs (1-20) were synthesized and characterized through EI-MS and (1)H NMR and evaluated for β-glucuronidase inhibitory potential. All synthesized analogs except 13 and 15 showed excellent β-glucuronidase inhibitory potential with IC50 value ranging in between 2.20-88.16μM as compared to standard d-saccharic acid 1,4 lactone (48.4±1.25μM). Analogs 19, 16, 4, 1, 17, 6, 10, 3, 18, 2, 11, 14 and 5 showed many fold potent activity against β-glucuronidase inhibitor. Structure activity relationship showed that substitution of electron withdrawing groups at ortho as well as para position on phenyl ring increase potency. Electron withdrawing groups at meta position on phenyl ring showed slightly low potency as compared to ortho and para position. The binding interactions were confirmed through molecular docking studies.
    Matched MeSH terms: Disulfides/pharmacology*; Glycoproteins/pharmacology*; Sulfones/pharmacology*
  4. Rengarajan T, Yaacob NS
    Eur J Pharmacol, 2016 Oct 15;789:8-16.
    PMID: 27377217 DOI: 10.1016/j.ejphar.2016.07.001
    Epidemiological studies show that consumption of diets rich in fruits and vegetables is associated with lower risks of cancer. This evidence has kindled interest into research on bioactive food components and has till date resulted in the identification of many compounds with cancer preventive and therapeutic potential. Among such compounds is fisetin (3,7,3,4-tetrahydroxyflavone), a flavonol that is commonly found in many fruits and vegetables such as apples, persimmons, grapes, kiwis, strawberries, onions and cucumbers. Fisetin has been shown to inhibit or retard the growth of various cancer cells in culture and implanted tumors in vivo. Fisetin targets many components of intracellular signaling pathways including regulators of cell survival and apoptosis, tumor angiogenic and metastatic switches by modulating a distinct set of upstream kinases, transcription factors and their regulators. Current evidence supports the idea that fisetin is a promising agent for cancer treatment. This review summarizes reported anticancer effects of fisetin, and re-emphasizes its potential therapeutic role in the treatment of cancer.
    Matched MeSH terms: Antineoplastic Agents/pharmacology*; Antioxidants/pharmacology*; Flavonoids/pharmacology*
  5. Fazil FN, Azzimi NS, Yahaya BH, Kamalaldin NA, Zubairi SI
    ScientificWorldJournal, 2016;2016:7370536.
    PMID: 28105464 DOI: 10.1155/2016/7370536
    Clinacanthus nutans is widely grown in tropical Asia and locally known "belalai gajah" or Sabah snake grass. It has been used as a natural product to treat skin rashes, snake bites, lesion caused by herpes, diabetes, fever, and cancer. Therefore, the objectives of this research are to determine the maximum yield and time of exhaustive flavonoids extraction using Peleg's model and to evaluate potential of antiproliferative activity on human lung cancer cell (A549). The extraction process was carried out on fresh and dried leaves at 28 to 30°C with liquid-to-solid ratio of 10 mL/g for 72 hrs. The extracts were collected intermittently analysed using mathematical Peleg's model and RP-HPLC. The highest amount of flavonoids was used to evaluate the inhibitory concentration (IC50) via 2D cell culture of A549. Based on the results obtained, the predicted maximum extract density was observed at 29.20 ± 14.54 hrs of extraction (texhaustive). However, the exhaustive time of extraction to acquire maximum flavonoids content exhibited approximately 10 hrs earlier. Therefore, 18 hrs of extraction time was chosen to acquire high content of flavonoids. The best antiproliferative effect (IC50) on A549 cell line was observed at 138.82 ± 0.60 µg/mL. In conclusion, the flavonoids content in Clinacanthus nutans water extract possesses potential antiproliferative properties against A549, suggesting an alternative approach for cancer treatment.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacology*; Flavonoids/pharmacology*; Plant Extracts/pharmacology*
  6. Rahim NS, Lim SM, Mani V, Abdul Majeed AB, Ramasamy K
    Pharm Biol, 2017 Dec;55(1):825-832.
    PMID: 28118770 DOI: 10.1080/13880209.2017.1280688
    CONTEXT: Virgin coconut oil (VCO) has been reported to possess antioxidative, anti-inflammatory and anti-stress properties.

    OBJECTIVE: Capitalizing on these therapeutic effects, this study investigated for the first time the potential of VCO on memory improvement in vivo.

    MATERIALS AND METHODS: Thirty male Wistar rats (7-8 weeks old) were randomly assigned to five groups (n = six per group). Treatment groups were administered with 1, 5 and 10 g/kg VCO for 31 days by oral gavages. The cognitive function of treated-rats were assessed using the Morris Water Maze Test. Brains were removed, homogenized and subjected to biochemical analyses of acetylcholine (ACh) and acetylcholinesterase (AChE), antioxidants [superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), glutathione peroxidase (GPx) and glutathione reductase (GRx)], lipid peroxidase [malondialdehyde (MDA)] as well as nitric oxide (NO). α-Tocopherol (αT; 150 mg/kg) was also included for comparison purposes.

    RESULTS: VCO-fed Wistar rats exhibited significant (p  33%) and NO (≥ 34%). Overall, memory improvement by VCO was comparable to αT.

    DISCUSSION AND CONCLUSION: VCO has the potential to be used as a memory enhancer, the effect of which was mediated, at least in part, through enhanced cholinergic activity, increased antioxidants level and reduced oxidative stress.

    Matched MeSH terms: Antioxidants/pharmacology*; Plant Oils/pharmacology*; Cholinergic Agents/pharmacology*
  7. Yong YY, Dykes G, Lee SM, Choo WS
    Plant Foods Hum Nutr, 2017 Mar;72(1):41-47.
    PMID: 27917454 DOI: 10.1007/s11130-016-0586-x
    Betacyanins are reddish to violet pigments that can be found in red pitahaya (Hylocereus polyrhizus) and red spinach (Amaranthus dubius). This study investigated the impact of sub-fractionation (solvent partitioning) on betacyanin content in both plants. Characterization of betacyanins and evaluation of their antimicrobial activities were also carried out. Betanin was found in both plants. In addition, isobetanin, phyllocactin and hylocerenin were found in red pitahaya whereas amaranthine and decarboxy-amaranthine were found in red spinach. Sub-fractionated red pitahaya and red spinach had 23.5 and 121.5 % more betacyanin content, respectively, than those without sub-fractionation. Sub-fractionation increased the betanin and decarboxy-amaranthine content in red pitahaya and red spinach, respectively. The betacyanin fraction from red spinach (minimum inhibitory concentration [MIC] values: 0.78-3.13 mg/mL) demonstrated a better antimicrobial activity profile than that of red pitahaya (MIC values: 3.13-6.25 mg/mL) against nine Gram-positive bacterial strains. Similarly, the red spinach fraction (MIC values: 1.56-3.13 mg/mL) was more active than the red pitahaya fraction (MIC values: 3.13-6.25 mg/mL) against five Gram-negative bacterial strains. This could be because of a higher amount of betacyanin, particularly amaranthine in the red spinach.
    Matched MeSH terms: Anti-Infective Agents/pharmacology; Plant Extracts/pharmacology; Betacyanins/pharmacology
  8. Laing AB
    Med J Malaya, 1968 Sep;23(1):5-19.
    PMID: 4237560
    Matched MeSH terms: Antimalarials/pharmacology*; Pyrimethamine/pharmacology*; Sulfadiazine/pharmacology*
  9. Jagabalan JDY, Murugaiyah V, Zainal H, Mansor SM, Ramanathan S
    J Asian Nat Prod Res, 2019 Apr;21(4):351-363.
    PMID: 29667422 DOI: 10.1080/10286020.2018.1461088
    The intestinal permeability of mitragynine was investigated in situ using a single pass intestinal perfusion (SPIP) absorption model, in small intestine of rat using mitragynine in the absence/presence of the permeability markers, P-gp and/or CYP3A4 inhibitors. Mitragynine demonstrated high intestinal permeability (Peff of 1.11 × 10-4 cm/s) that is in the range of highly permeable drugs such as propranolol (Peff of 1.27 × 10-4 cm/s) indicating that it readily crosses the intestine. The addition of azithromycin (P-glycoprotein inhibitor) and ciprofloxacin (CYP3A4 inhibitor) or combination of both has no effect on intestinal permeability of mitragynine across the rat small intestine.
    Matched MeSH terms: Ciprofloxacin/pharmacology; Azithromycin/pharmacology; Cytochrome P-450 CYP3A Inhibitors/pharmacology
  10. Colagiuri S, Matthews D, Leiter LA, Chan SP, Sesti G, Marre M
    Diabetes Res Clin Pract, 2018 Sep;143:1-14.
    PMID: 29802958 DOI: 10.1016/j.diabres.2018.05.028
    The sulfonylureas are effective oral glucose-lowering agents with a long history of clinical use. While all have the same general mechanism of action, their pharmacokinetic properties are influenced by factors such as dosage, rate of absorption, duration of action, route of elimination, tissue specificity, and binding affinity for pancreatic β-cell receptor. The result is a class of agents with similar HbA1c-lowering efficacy, but well-documented differences in terms of effects on hypoglycemia, and cardiovascular and renal safety. This review examines the differences between currently available sulfonylureas with a focus on how gliclazide modified release (MR) differs from other members of this class and from newer oral antihyperglycemic agents in the form of dipeptidyl peptidase-4 (DPP4) and sodium- glucose cotransporter 2 (SGLT2) inhibitors. The first part focuses on major outcome trials that have been conducted with the sulfonylureas and new oral agents. Consideration is then given to factors important for day-to-day prescribing including efficacy and durability, weight changes, hypoglycemia, renal effects and cost. Based on current evidence, third-generation sulfonylureas such as gliclazide MR possess many of the properties desired of a type 2 diabetes drug including high glucose-lowering efficacy, once-daily oral administration, few side effects other than mild hypoglycemia, and cardiovascular safety.
    Matched MeSH terms: Gliclazide/pharmacology; Hypoglycemic Agents/pharmacology; Sulfonylurea Compounds/pharmacology
  11. Hasan MM, Ahmed QU, Mat Soad SZ, Tunna TS
    Biomed Pharmacother, 2018 May;101:833-841.
    PMID: 29635892 DOI: 10.1016/j.biopha.2018.02.137
    Diabetes mellitus is a chronic disease which has high prevalence. The deficiency in insulin production or impaired insulin function is the underlying cause of this disease. Utilization of plant sources as a cure of diabetes has rich evidence in the history. Recently, the traditional medicinal plants have been investigated scientifically to understand the underlying mechanism behind antidiabetic potential. In this regard, a substantial number of in vivo and in vitro models have been introduced for investigating the bottom-line mechanism of the antidiabetic effect. A good number of methods have been reported to be used successfully to determine antidiabetic effects of plant extracts or isolated compounds. This review encompasses all the possible methods with a list of medicinal plants which may contribute to discovering a novel drug to treat diabetes more efficaciously with the minimum or no side effects.
    Matched MeSH terms: Biological Products/pharmacology; Flavonoids/pharmacology; Hypoglycemic Agents/pharmacology
  12. Ping KS, Poobathy RR, Zakaria R, Subramaniam S
    Cryo Letters, 2018 5 8;38(4):290-298.
    PMID: 29734430
      BACKGROUND: Conservation of commercially important ornamental plants is important to maintain its unique beauty to cater the market demands.

    OBJECTIVE: The main objective is to develop an efficient cryopreservation technique for Aranda Broga Blue orchid PLBs using droplet-vitrification method.

    MATERIALS AND METHODS: Several critical factors in cryopreservation were accessed such as preculture concentrations and durations, choice of vitrification solutions, two-step or three-step vitrification, growth recovery medium and PVS2 exposure duration.

    RESULTS: The best growth regeneration percentage (5%) was obtained when 3-4mm PLBs were precultured in 0.2M sucrose for 3 days, followed by osmoprotection for 20 minutes, dehydration in PVS2 for 20 minutes at 0 degree C, LN storage, thawed and unloading for 20 minutes, and growth regeneration in VW10 medium. PLBs were found to be very sensitive to osmotic stress imposed by high molecular weight cryoprotectant such as sucrose and glycerol. Osmotic potential of growth recovery medium is one of the main factors that affect growth recovery in cryopreserved PLBs.

    CONCLUSION: Current report showed possibilities in cryopreserving Aranda Broga Blue PLBs using droplet-vitrification technique. However, further improvement of growth recovery can be done by focussing on approaches that facilitate sufficient water removal from PLBs without causing severe osmotic injuries to the plant cells.

    Matched MeSH terms: Cryoprotective Agents/pharmacology*; Glycerol/pharmacology; Sucrose/pharmacology
  13. Ibrahim SM, Kareem OH, Saffanah KM, Adamu AA, Khan MS, Rahman MBA, et al.
    Cryobiology, 2018 06;82:27-36.
    PMID: 29679551 DOI: 10.1016/j.cryobiol.2018.04.012
    The objective of this study was to evaluate the use of Afp1m as a cryopreservative agent for skin by examining the transplanted skin histological architecture and mechanical properties following subzero cryopreservation. Thirty four (34) rats with an average weight of 208 ± 31 g (mean ± SD), were used. Twenty four (n = 24) rats were equally divided into four groups: (i) immediate non-cryopreserved skin autografts (onto same site), (ii) immediate non-cryopreserved skin autografts (onto different sites), (iii) skin autografts cryopreserved with glycerol for 72 h and (iv) skin autografts cryopreserved with Afp1m for 72 h at -4 °C. Rounded shaped full-thickness 1.5-2.5 cm in diameter skin was excised from backs of rats for the autograft transplantation. Non-cryopreserved or cryopreserved auto skin graft were positioned onto the wound defects and stitched. Non-transplanted cryopreserved and non-cryopreserved skin strips from other ten rats (n = 10) were allowed for comparative biomechanical test. All skin grafts were subjected to histological and mechanical examinations at the end of day 21. Histological results revealed that tissue architecture especially the epidermal integrity and dermal-epidermal junction of the Afp1m cryopreserved skin grafts exhibited better histological appearance, good preservation of tissue architecture and structural integrity than glycerolized skin. However, there was no significant difference among these groups in other histological criteria. There were no significant differences among the 4 groups in skin graft mechanical properties namely maximum load. In conclusion, Afp1m were found to be able to preserve the microstructure as well as the viability and function of the skin destined for skin transplantation when was kept at -4 °C for 72 h.
    Matched MeSH terms: Cryoprotective Agents/pharmacology*; Glycerol/pharmacology*; Antifreeze Proteins/pharmacology*
  14. Jamaluddin N, Stuckey DC, Ariff AB, Faizal Wong FW
    Crit Rev Food Sci Nutr, 2018;58(14):2453-2465.
    PMID: 28609113 DOI: 10.1080/10408398.2017.1328658
    Bacteriocin is a proteinaceous biomolecule produced by bacteria (both Gram-positive and Gram-negative) that exhibits antimicrobial activity against closely related species, and food-borne pathogens. It has recently gained importance and attracted the attention of several researchers looking to produce it from various substrates and bacterial strains. This ushers in a new era of food preservation where the use of bacteriocin in food products will be an alternative to chemical preservatives, and heat treatment which are understood to cause unwanted side effects, and reduce sensory and nutritional quality. However, this new market depends on the success of novel downstream separation schemes from various types of crude feedstocks which are both effective and economic. This review focuses on the downstream separation of bacteriocin from various sources using both conventional and novel techniques. Finally, recommendations for future interesting areas of research that need to be pursued are highlighted.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*; Bacteriocins/pharmacology*; Food Preservatives/pharmacology*
  15. Thomas B, Gupta K
    J Esthet Restor Dent, 2017 Nov 12;29(6):435-441.
    PMID: 28703476 DOI: 10.1111/jerd.12317
    OBJECTIVE: Nano-hydroxyapatite-added GIC has been developed to improve the physical properties of conventional GIC. However, biological response of periodontal cells to this potentially useful cervical restorative material has been unexplored. The aim of this study was to investigate the in vitro response of human periodontal ligament fibroblasts to hydroxyapatite-added GIC.

    MATERIALS AND METHODS: Three categories of materials, namely, test group 1 (cGIC or type IX GIC), test group 2 (HA-GIC or hydroxyapatite-added GIC), and positive control (glass cover slips) were incubated with human periodontal ligament fibroblasts. The samples were viewed under scanning electron microscope to study the morphological characteristics of fibroblasts. Additionally, elemental analysis was performed to differentiate between the two test groups based on surface chemical composition.

    RESULTS: Test group 1 (cGIC) exhibited cells with curled up morphology, indicative of poor attachment to the substrate. Test group 2 (Ha-GIC) exhibited cells with flattened morphology and numerous cellular extensions such as lamellipodia and blebs, indicative of good attachment to the substrate. The test group 2 (Ha-GIC) demonstrated higher surface elemental percentages of calcium and phosphorus.

    CONCLUSION: Within the limitations of this study, it may be concluded that hydroxyapatite-added GIC is more biocompatible than conventional GIC (type IX), probably attributed to high elemental percentages of calcium and phosphorus.

    CLINICAL SIGNIFICANCE: The search for an ideal cervical restorative dental material has been ever elusive. Hydroxyapatite-added GIC is a simple and economical dental material to fabricate from basic conventional GIC. The results from this study strengthen its candidature for cervical and root surface restorations which may later require soft tissue augmentation. The possibility of connective tissue adhesion to this material is an exciting prospect in the field of periorestorative dentistry.

    Matched MeSH terms: Biocompatible Materials/pharmacology; Glass Ionomer Cements/pharmacology*; Durapatite/pharmacology*
  16. Ngoh YY, Gan CY
    Food Chem, 2018 Nov 30;267:124-131.
    PMID: 29934146 DOI: 10.1016/j.foodchem.2017.04.166
    Five Pinto bean peptides with α-amylase and angiotensin converting enzyme (ACE) inhibitory activities were successfully identified using the integrated bioinformatics approach. By using PEAKS studio, 511 peptide sequences were first shortlisted based on their de novo sequence property and average local confidence (ALC) yield of ≥60%. Subsequently, only five peptides were found to have high potential (score ≥0.80) for contributing bioactivy. The important sites which were potentially bound by the peptides: (a) Trp58, Trp59, Tyr 62, Asp96, Arg195, Asp197, Glu233, His299, Asp300 and His305 for α-amylase; (b) His353, Ala354, His383, Glu384, His387, Glu411, Lys511, His513, Tyr520 and Tyr523 for ACE had corresponded to the catalytic and substrate binding sites of the two enzymes. A validation assay was then conducted and IC50 values were determined. The range of the values for α-amylase inhibitory activity was 10.03-23.33mM, whereas the values for ACE inhibitory activity were of 1.52-31.88μM.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/pharmacology*; Peptides/pharmacology*; Plant Proteins/pharmacology
  17. Hu J, Lin S, Tan BK, Hamzah SS, Lin Y, Kong Z, et al.
    Food Res Int, 2018 09;111:265-271.
    PMID: 30007685 DOI: 10.1016/j.foodres.2018.05.042
    Burkholderia cepacia (B. cepacia) is an aerobic Gram-negative bacillus found in various aquatic environments and can cause food contamination. We investigated the photodynamic antibacterial effects of food additive curcumin combined with EDTA on B. cepacia. We found a ~4-log reduction in B. cepacia viability when photo-irradiated with curcumin at 50 μM by blue LED light (16 mW/cm2) for 30 min with 0.4% (w/v) EDTA. Moreover, the bacterial morphological alterations and the leakage of intracellular contents were observed after photodynamic treatment. There were also obvious genomic DNA cleavage and a general loss of bacterial proteins assigned to large-scale protein degradation after photodynamic inactivation treatment. Collectively, curcumin in combination with EDTA illuminated by blue LED is a potential candidate for photodynamic inactivation of B. cepacia.
    Matched MeSH terms: Curcumin/pharmacology*; Edetic Acid/pharmacology*; Food Additives/pharmacology*
  18. Taha M, Baharudin MS, Ismail NH, Selvaraj M, Salar U, Alkadi KA, et al.
    Bioorg Chem, 2017 04;71:86-96.
    PMID: 28160943 DOI: 10.1016/j.bioorg.2017.01.015
    Novel sulfonamides having oxadiazole ring were synthesized by multistep reaction and evaluated to check in vitro β-glucuronidase inhibitory activity. Luckily, except compound 13, all compounds were found to demonstrate good inhibitory activity in the range of IC50=2.40±0.01-58.06±1.60μM when compared to the standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Structure activity relationship was also presented. However, in order to ensure the SAR as well as the molecular interactions of compounds with the active site of enzyme, molecular docking studies on most active compounds 19, 16, 4 and 6 was carried out. All derivatives were fully characterized by 1H NMR, 13C NMR and EI-MS spectroscopic techniques. CHN analysis was also presented.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology*; Oxadiazoles/pharmacology*; Sulfonamides/pharmacology*
  19. Jafarzadeh S, Rhim JW, Alias AK, Ariffin F, Mahmud S
    J Sci Food Agric, 2019 Apr;99(6):2716-2725.
    PMID: 30350410 DOI: 10.1002/jsfa.9439
    BACKGROUND: Active food packaging films with improved properties and strong antimicrobial activity were prepared by blending mixed nanomaterials with different ratio [1:4 (40 mg:160 mg), 3:2 (120 mg: 80 mg), 0:5 (0 mg: 200 mg) and 5:0 (200 mg:0 mg)] of ZnO and kaolin with semolina using a solvent casting method and used for the packaging of low moisture mozzarella cheese to test the effect of packaging on the quality change of the cheese for long-term (up to 72 days) refrigerated storage.

    RESULTS: Compared with the neat semolina film, mechanical strength (TS) of the nanocomposite films increased significantly (increase in 21-65%) and water vapor barrier (WVP) and O2 gas barrier (OP) properties decreased significantly (decrease in 43-50% and 60-65%, respectively) depending on the blending ratio of ZnO and kaolin nanoclay. The nanocomposite films also exhibited strong antimicrobial activity against bacteria (E. coli and S. aureus), yeast (C. albicans), and mold (A. niger). The nanocomposite packaging films were effectively prevented the growth of microorganisms (coliforms, total microbial, and fungi) of the cheese during storage at low-temperature and showed microbial growth of less than 2.5 log CFU/g after 72 days of storage compared to the control group, and the quality of the packaged cheese was still acceptable.

    CONCLUSION: The semolina-based nanocomposite films, especially Sem/Z3 K2 film, were effective for packaging of low moisture mozzarella cheese to maintain the physicochemical properties (pH, moisture, and fat content) and quality (color, taste, texture, and overall acceptability) of the cheese as well as preventing microbial growth (coliforms, total microbial, and fungi). © 2018 Society of Chemical Industry.

    Matched MeSH terms: Anti-Infective Agents/pharmacology*; Kaolin/pharmacology*; Zinc Oxide/pharmacology*
  20. Md Sidek NL, Halim M, Tan JS, Abbasiliasi S, Mustafa S, Ariff AB
    Biomed Res Int, 2018;2018:5973484.
    PMID: 30363649 DOI: 10.1155/2018/5973484
    Nowadays, bacteriocin industry has substantially grown replacing the role of chemical preservatives in enhancing shelf-life and safety of food. The progress in bacteriocin study has been supported by the emerging of consumer demand on the applications of natural food preservatives. Since food is a complex ecosystem, the characteristics of bacteriocin determine the effectiveness of their incorporation into the food products. Among four commercial media (M17 broth, MRS broth, tryptic soy broth, and nutrient broth) tested, the highest growth of Pediococcus acidilactici kp10 and bacteriocin-like-inhibitory substance (BLIS) production were obtained in the cultivation with M17. BLIS production was found to be a growth associated process where the production was increased concomitantly with the growth of producing strain, P. acidilactici kp10. The antimicrobial property of BLIS against three indicator microorganisms (Listeria monocytogenes, Escherichia coli, and Staphylococcus aureus) remained stable upon heating at 100°C but not detectable at 121°C. The BLIS activity was also observed to be stable and active at a wide pH range (pH 2 to pH 7). The BLIS activity remained constant at -20°C and -80°C for 1 month of storage. However, the activity dropped after 3 and 6 months of storage at 4°C, -20°C, and -80°C with more than 80% reduction. The ability of bacteriocin from P. acidilactici kp10 to inhibit food-borne pathogens while remaining stable and active at extreme pH and temperature is of potential interest for future applications in food preservatives.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*; Bacteriocins/pharmacology*; Food Preservatives/pharmacology*
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