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https://www.readbyqxmd.com/read/27867054/thiolated-methylated-dimethylaminobenzyl-chitosan-a-novel-chitosan-derivative-as-a-potential-delivery-vehicle
#1
Shirin Hakimi, Elaheh Mortazavian, Zohreh Mohammadi, Fatemeh Yazdi Samadi, Hamidreza Samadikhah, Sadegh Taheritarigh, Niyousha Rafiee Tehrani, Morteza Rafiee-Tehrani
Chitosan is a natural mucoadhesive, biodegradable, biocompatible and nontoxic polymer which has been used in pharmaceutical industry for a lot of purposes such as dissolution enhancing, absorption enhancing, sustained releasing and protein, gene or drug delivery. Two major disadvantages of chitosan are poor solubility in physiological pH and low efficiency for protein and gene delivery. In this study thiolated methylated N-(4-N,N-dimethylaminobenzyl) chitosan was prepared for the first time in order to improve the solubility and delivery properties of chitosan...
November 17, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27852006/a-combination-of-photodynamic-therapy-and-chemotherapy-displays-a-differential-cytotoxic-effect-on-human-metastatic-melanoma-cells
#2
Fa Nsole Biteghe, L M Davids
BACKGROUND: Cutaneous melanoma represents the most lethal form of skin cancer and remains refractory to current therapies. Failure of treatment has been attributed to the over-expression of ABC transporters which efflux the drugs, below their cytotoxic threshold within cells. Therefore, this study set to investigate; the efficacy of a combinatorial approach comprising chemotherapy (Dacarbazine) and photodynamic therapy (PDT) to overcome resistance in pigmented and unpigmented metastatic melanoma and potentially identify resistant mechanisms...
November 8, 2016: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/27829440/wrn-targeted-therapy-using-inhibitors-nsc-19630-and-nsc-617145-induce-apoptosis-in-htlv-1-transformed-adult-t-cell-leukemia-cells
#3
R Moles, X T Bai, H Chaib-Mezrag, C Nicot
BACKGROUND: Human T-cell leukemia virus type 1 (HTLV-1) infection is associated with adult T-cell leukemia/lymphoma (ATLL), a lymphoproliferative malignancy with a dismal prognosis and limited therapeutic options. Recent evidence shows that HTLV-1-transformed cells present defects in both DNA replication and DNA repair, suggesting that these cells might be particularly sensitive to treatment with a small helicase inhibitor. Because the "Werner syndrome ATP-dependent helicase" encoded by the WRN gene plays important roles in both cellular proliferation and DNA repair, we hypothesized that inhibition of WRN activity could be used as a new strategy to target ATLL cells...
November 9, 2016: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/27805604/synthesis-of-thermogelling-poly-n-isopropylacrylamide-graft-chondroitin-sulfate-composites-with-alginate-microparticles-for-tissue-engineering
#4
Thomas R Christiani, Katelynn Toomer, Joseph Sheehan, Angelika Nitzl, Amanda Branda, Elizabeth England, Pamela Graney, Cristina Iftode, Andrea J Vernengo
Injectable biomaterials are defined as implantable materials that can be introduced into the body as a liquid and solidify in situ. Such materials offer the clinical advantages of being implanted minimally invasively and easily forming space-filling solids in irregularly shaped defects. Injectable biomaterials have been widely investigated as scaffolds for tissue engineering. However, for the repair of certain load-bearing areas in the body, such as the intervertebral disc, scaffolds should possess adhesive properties...
October 26, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27804852/design-synthesis-and-evaluation-of-heat-shock-protein-90-inhibitors-in-human-breast-cancer-and-its-metastasis
#5
Mehmet Gumus, Aykut Özgür, Lütfi Tutar, Ali Disli, İrfan Koca, Yusuf Tutar
In the present study, a series of benzodiazepine derivatives were designed and synthesized as novel heat shock protein 90 (Hsp90) inhibitor for target specific cancer treatment. Their anticancer activities were determined by XTT cell proliferation assay against human breast cancer cell line (MCF-7). Also, we investigated the antiangiogenic effects of the compounds on human vascular endothelium (HUVEC) cell line. In order to determine the anti-proliferative mechanism of the compounds, in silico molecular docking studies were performed between Hsp90 ATPase domain and benzodiazepine derivatives...
October 31, 2016: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/27801583/synthesis-and-antineoplastic-evaluation-of-novel-unsymmetrical-1-3-4-oxadiazoles
#6
Valentina Nieddu, Giansalvo Pinna, Irene Marchesi, Luca Sanna, Battistina Asproni, Gérard Aimè Pinna, Luigi Marco Bagella, Gabriele Murineddu
A series of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles was synthetized and evaluated for their cytotoxic activity against different cancer cell lines of various origins as in vitro tumor models. Four of 12 new compounds (2b, 2h, 2j and 2l) showed growth inhibitory activity using the XTT dye assay. The most active agent, 2-(2-methyl-1,4-dihydroindeno[1,2-b]pyrrol-3-yl)-5-phenyl-1,3,4-oxadiazole, 2j, was chosen for further studies. It showed high potency against a panel of cultured human cancer cells with IC50 ranging from 0...
November 1, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27795846/biosynthesis-of-poly-3-hydroxybutyrateco-3-hydroxy-4-methylvalerate-by-strain-azotobacter-chroococcum-7b
#7
A P Bonartsev, G A Bonartseva, V L Myshkina, V V Voinova, T K Mahina, I I Zharkova, S G Yakovlev, A L Zernov, E V Ivanova, E A Akoulina, E S Kuznetsova, V A Zhuikov, S G Alekseeva, V V Podgorskii, I V Bessonov, M N Kopitsyna, A S Morozov, E Y Milanovskiy, Z N Tyugay, G S Bykova, M P Kirpichnikov, K V Shaitan
Production of novel polyhydroxyalkanoates (PHAs), biodegradable polymers for biomedical applications, and biomaterials based on them is a promising trend in modern bioengineering. We studied the ability of an effective strain-producer Azotobacter chroococcum 7B to synthesize not only poly(3-hydroxybutyrate) homopolymer (PHB) and its main copolymer poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV), but also a novel copolymer, poly(3-hydroxybutyrate-co-3-hydroxy-4-methylvalerate) (PHB4MV). For the biosynthesis of PHB copolymers, we used carboxylic acids as additional carbon sources and monomer precursors in the chain of synthesized copolymers...
July 2016: Acta Naturae
https://www.readbyqxmd.com/read/27776997/does-biomass-production-correlate-with-metabolic-activity-in-staphylococcus-aureus
#8
Beatriz Alonso, José Lucio, María Jesús Pérez-Granda, Raquel Cruces, Carlos Sánchez-Carrillo, Emilio Bouza, María Guembe
We assessed agreement between the crystal violet binding assay and the XTT assay in the classification of biofilm production in 492 Staphylococcus aureus strains from bacteremic patients. We found that the overall correlation between the procedures was 46.5%. Biomass production and metabolic activity must be assessed simultaneously.
October 21, 2016: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/27767392/testing-of-schefflera-vinosa-extract-in-mammalian-cells-in-vitro-and-in-vivo-for-potential-toxicity-genetic-damage-and-role-of-oxidation
#9
Natália Helen Ferreira, Kelly Jacqueline Barbosa de Andrade, Luís Fernando Leandro, Nathália Oliveira Acésio, Suzana Amorim Mendes, Lucas Silva Cintra, Ana Helena Januário, Denise Crispim Tavares
The aim of this study was to examine the cytotoxic and genotoxic potential of a hydroethanolic extract of Schefflera vinosa (SV), a plant with schistosomicidal activity, as well as its influence on DNA damage induced by different mutagens, methyl methane sulfonate (MMS) and hydrogen peroxide (H2O2), in V79 cells and Swiss mice. Schefflera vinosa extract produced cytotoxicity at concentrations of 312.5 µg/ml or higher using the XTT cell proliferation assay kit. Treatment of V79 cell cultures with the highest SV concentration tested (150 µg/ml) significantly increased the frequency of micronuclei (MN) compared to controls...
October 21, 2016: Journal of Toxicology and Environmental Health. Part A
https://www.readbyqxmd.com/read/27683125/reduced-argininosuccinate-synthetase-expression-in-refractory-sarcomas-impacts-on-therapeutic-potential-and-drug-resistance
#10
Youngji Kim, Eisuke Kobayashi, Daisuke Kubota, Yoshiyuki Suehara, Kenta Mukaihara, Keisuke Akaike, Ayumu Ito, Kazuo Kaneko, Hirokazu Chuman, Akira Kawai, Shigehisa Kitano
BACKGROUND: Treating drug-resistant sarcomas remains a major challenge. The present study aimed to identify a novel therapy for drug-resistant sarcomas based on metabolic errors involving argininosuccinate synthetase1 (ASS1). RESULTS: ASS1 expression was reduced in Dox-resistant sarcoma cells. Immunohistochemistry and real-time PCR showed an inverse correlation between ASS1 and P-gp expressions. The inhibition of cellular proliferation with G1-arrest was shown to lead to autophagy with arginine deprivation...
September 23, 2016: Oncotarget
https://www.readbyqxmd.com/read/27664023/extended-wear-therapeutic-contact-lens-fabricated-from-timolol-imprinted-carboxymethyl-chitosan-g-hydroxy-ethyl-methacrylate-g-poly-acrylamide-as-a-onetime-medication-for-glaucoma
#11
T S Anirudhan, Anoop S Nair, J Parvathy
An extended wear therapeutic contact lens (TCL) for the sustained delivery of timolol maleate (TML) was fabricated based on molecular imprinting technique. The designed TCL comprised of a TML imprinted copolymer of carboxymethyl chitosan-g-hydroxy ethyl methacrylate-g-polyacrylamide (CmCS-g-HEMA-g-pAAm) embedded onto a poly HEMA matrix (pHEMA). Successful reloading of TML onto the lens was monitored using a simple and novel UV-Visible spectrophotometric method which showed an excellent reloading capacity of 6...
December 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27660214/aspergillus-fumigatus-dbm-4057-biofilm-formation-is-inhibited-by-chitosan-in-contrast-to-baicalein-and-rhamnolipid
#12
Eva Kvasničková, Vít Paulíček, Martina Paldrychová, Richard Ježdík, Olga Maťátková, Jan Masák
The biofilms of filamentous-forming fungi are a novel and still insufficiently understood research topic. We have studied Aspergillus fumigatus, an ubiquitous opportunistic pathogenic fungus, as a representative model for a study of biofilm formation by filamentous fungi and for assessing the potential anti-biofilm activity of natural substances. The activity of antibiotic amphotericin B and selected natural substances: baicalein, chitosan and rhamnolipid was studied. The minimum suspension inhibitory concentrations (MIC) were determined and the biofilm susceptibility was investigated by determining the metabolic activity of sessile cells (XTT assay) and total biofilm biomass (crystal violet staining)...
November 2016: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/27617025/holi-colours-contain-pm10-and-can-induce-pro-inflammatory-responses
#13
Katrin Bossmann, Sabine Bach, Conny Höflich, Kerttu Valtanen, Rita Heinze, Anett Neumann, Wolfgang Straff, Katrin Süring
BACKGROUND: At Holi festivals, originally celebrated in India but more recently all over the world, people throw coloured powder (Holi powder, Holi colour, Gulal powder) at each other. Adverse health effects, i.e. skin and ocular irritations as well as respiratory problems may be the consequences. The aim of this study was to uncover some of the underlying mechanisms. METHODS: We analysed four different Holi colours regarding particle size using an Electric field cell counting system...
2016: Journal of Occupational Medicine and Toxicology
https://www.readbyqxmd.com/read/27615430/the-activity-of-fungichromin-against-the-formation-of-candida-albicans-biofilm
#14
Duopeng An, Xiang Wang, Jun Li, Shanshan Jiang, XiaoJuan Ma, Hui Zhang, Hang Shi, Hongying Sun, Li Ye, Jiyang Li
The effect of fungichromin (FC) on the formation of Candida albicans biofilm was assessed using 2,3-bis(2-methoxy-4-nitro-5-sulfo-phenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction method, scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM). Results showed that FC revealed an inhibitory effect on the formation of C. albicans biofilm in a dose-dependent manner with a minimum inhibitory concentration (MIC) of 10 µg/mL. Over 80% of biofilm formation was inhibited by FC at the concentration of 40 µg/mL when compared with the control...
December 1, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27613802/the-lipopolysaccharide-of-the-crop-pathogen-xanthomonas-translucens-pv-translucens-chemical-characterization-and-determination-of-signaling-events-in-plant-cells
#15
Tim Steffens, Katarzyna Duda, Buko Lindner, Frank-Jörg Vorhölter, Hanna Bednarz, Karsten Niehaus, Otto Holst
Xanthomonas translucens pv. translucens (Xtt) is a Gram-negative pathogen of crops from the plant family Poaceae The lipopolysaccharide (LPS) of Xtt was isolated and chemically characterized. The analyses revealed the presence of rhamnose, xylose, mannose, glucose, galacturonic acid, phosphates, 3-deoxy-D-manno-oct-2-ulopyranosonic acid (Kdo) and fatty acids (10:0, 11:0, 11:0(3-OH) i/a, 11:0(3-OH), 12:0(3-OH) i/a, 12:0(3-OH), 12:0, 13:0(3-OH) i, 13:0(3-OH) a, 13:0(3-OH), 14:0(3-OH) i/a, 14:0(3-OH) and 16:0)...
September 9, 2016: Glycobiology
https://www.readbyqxmd.com/read/27613330/invitro-and-in-vivo-antitumor-activity-of-a-novel-carbonyl-ruthenium-compound-the-ct-rucl-co-dppb-bipy-pf-6-dppb-1-4-bis-diphenylphosphine-butane-and-bipy-2-2-bipyridine
#16
Andréa P Carnizello, Marília I F Barbosa, Monize Martins, Natália H Ferreira, Pollyanna F Oliveira, Geórgia M Magalhães, Alzir A Batista, Denise C Tavares
This study performed in vitro and in vivo biological assays of the ruthenium (II) compound ct-[RuCl(CO)(dppb)(bipy)]PF6 (where, dppb=1,4-bis(diphenylphosphine)butane and bipy=2,2'-bipyridine). The cytotoxic activity of this compound was evaluated against different tumor cell lines (HeLa, human cervical adenocarcinoma; MCF7, human breast adenocarcinoma; MO59J, human glioblastoma; HepG2, hepatocellular carcinoma and B16F10, murine melanoma) and healthy cell line (V79, Chinese hamster lung fibroblasts), by XTT (sodium 2,3'-bis(2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino)-carbonyl]-3,4-tetrazolium-bis(4-methoxy-6-nitro)benzene-sulfonic acid hydrate) method...
August 25, 2016: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/27612744/facile-preparation-of-ph-responsive-polyurethane-nanocarrier-for-oral-delivery
#17
Mohammad Reza Nabid, Ismail Omrani
This study reports a novel one pot synthesis of pH-responsive nanocarrier for oral delivery of hydrophobic drug under gastrointestinal tract. Triblock copolymer MPEG-HTPB-MPEG was synthesized coupling of MPEG and HTPB using hexamethylene diisocyanate(HDI) and pH-responsive carboxylic acid group was attached to polybuthadiene backbone by thiol-ene click reaction in a facile and convenient procedure. The MPEG-HTPB (g-COOH)-MPEG block copolymers were self-organized into micelle assemblies in the water. The size and shape of the micelle assemblies were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM)...
December 1, 2016: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27612733/biocompatibility-and-biomechanical-characteristics-of-loofah-based-scaffolds-combined-with-hydroxyapatite-cellulose-poly-l-lactic-acid-with-chondrocyte-like-cells
#18
Berivan Cecen, Leyla Didem Kozaci, Mithat Yuksel, Ozcan Ustun, Bekir Ugur Ergur, Hasan Havitcioglu
The current study reports the biocompatibility and biomechanical characteristics of loofah-based scaffolds combined with hydroxyapatite (HA), cellulose, poly-l-lactic acid (PLLA) with chondrocytes-like cells. Scanning electron microscope (SEM) micrographs of the scaffolds showed that the addition of PLLA usually resulted in an increase in cell's attachment on scaffolds. Mechanical and elemental analyzes were assessed using tensile test and Energy Dispersive X-ray spectrometry (EDS), respectively. In summary, we showed that the loofah+PLLA+HA scaffolds perform significantly better than other loofah-based scaffolds employed in terms of increasing a diversity of mechanical properties including tensile strength and Young's modulus...
December 1, 2016: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27610100/antifungal-effect-of-novel-2-bromo-2-chloro-2-4-chlorophenylsulfonyl-1-phenylethanone-against-candida-strains
#19
Monika Staniszewska, Małgorzata Bondaryk, Magdalena Wieczorek, Eine Estrada-Mata, Héctor M Mora-Montes, Zbigniew Ochal
We investigated the antifungal activity of novel a 2-bromo-2-chloro-2-(4-chlorophenylsulfonyl)-1-phenylethanone (compound 4). The synthesis of compound 4 was commenced from sodium 4-chlorobenzene sulfinate and the final product was obtained by treatment of α-chloro-β-keto-sulfone with sodium hypobromite. The sensitivity of 63 clinical isolates belonging to the most relevant Candida species toward compound 4 using the method M27-A3 was evaluated. We observed among most of the clinical strains of C. albicans MIC ranging from 0...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27606830/sustained-release-of-antibacterial-lipopeptides-from-biodegradable-polymers-against-oral-pathogens
#20
Lea H Eckhard, Yael Houri-Haddad, Asaf Sol, Rotem Zeharia, Yechiel Shai, Shaul Beyth, Abraham J Domb, Gilad Bachrach, Nurit Beyth
The development of antibacterial drugs to overcome various pathogenic species, which inhabit the oral cavity, faces several challenges, such as salivary flow and enzymatic activity that restrict dosage retention. Owing to their amphipathic nature, antimicrobial peptides (AMPs) serve as the first line of defense of the innate immune system. The ability to synthesize different types of AMPs enables exploitation of their advantages as alternatives to antibiotics. Sustained release of AMPs incorporated in biodegradable polymers can be advantageous in maintaining high levels of the peptides...
2016: PloS One
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