17 research outputs found

    Synthesis, physiochemical property and antimicrobial activity of novel quaternary ammonium salts

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    <p>Twenty-four novel 5-phenyl-1,3,4-oxadiazole-2-thiol (POT) analogues, benzo[<i>d</i>]oxazole-2-thiol, benzo[<i>d</i>]thiazole-2-thiol and 5-methyl-1,3,4-thiadiazole-2-thiol-substituted <i>N,N</i>-bis(2-hydroxyethyl) quaternary ammonium salts (QAS) (<b>5a-d, 6a-d, 7a-d, 10a-d, 13a-d, 16a-d</b>) were prepared and characterised by FTIR, NMR and elemental analysis. Part of target compounds (<b>5d</b>, <b>6d</b>, <b>7d</b>, <b>10d</b>, <b>13d</b>, <b>16d</b>) displayed potent antimicrobial effect against ten common pathogens (<i>S. aureus, α-H-tococcus, β-H-tococcus, E. coli, P. aeruginosa, Proteus vulgaris, Canidia Albicans, Cytospora mandshurica, Physalospora piricola, Aspergillus niger</i>) and had relatively low cytotoxity against two human cell lines (HaCat and LO2). TEM and SEM images of <i>E. coli</i> and <i>S. aureus</i> morphologies treated with <b>7d</b> showed that the antibacterial mechanism might be the QAS fixing on cell wall surfaces and puncturing to result in the release of bacterial cytoplasm. This study provides new information of QAS, which could be used to design novel antimicrobial agents applied in clinic or agriculture.</p

    Synthesis, antitumor activity evaluation of some new <i>N</i>-aroyl-<b>α</b>,<b>β</b>-unsaturated piperidones with fluorescence

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    <p>Novel <i>N</i>-aroyl-α,β-unsaturated piperidones, series <b>1</b>, series <b>2</b> and series <b>3</b> (featuring 2-bromo-4,5-dimethoxybenzylidene, 4-dimethylaminobenzylidene and 4-trifluoromethylbenzylidene, respectively), were synthesized as candidate cytotoxins. Most of the compounds displayed potent cytotoxicity against the human neoplastic cell lines SK-BR-3, PG-BE1, NCI-H460, MIA PaCa-2 and SW1990 <i>in vitro</i>, and approximately 64% of the IC<sub>50</sub> values were lower than 5 μM. Among those tested, compound <b>1b</b> of series <b>1, 3a, 3d</b> and <b>3e</b> of series <b>3</b> proved to be the most active. Importantly, <b>1b</b> displayed marked inhibitory effects on tumor growth <i>in vivo</i> and had no apparent toxicity to mice; this was evaluated by a nude mouse PG-BE1 xenograft model. In addition, the fluorescent properties of compounds series <b>1</b>–<b>3</b> were investigated. The interesting fluorescence exhibited by these compounds could be useful for their visualization in tumor cells, permitting further studies on these α,β-unsaturated piperidones as candidates for novel fluorescent antitumor agents.</p

    Additional file 1: of Doxorubicin combined with low intensity ultrasound suppresses the growth of oral squamous cell carcinoma in culture and in xenografts

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    Figure S1. Schematic diagram of the low-intensity ultrasound device and experimental setup. Figure S2. Schematic diagrams of ultrasound pressure level distribution for in vitro and in vivo experiments. Figure S3. The effects of LIUS and DOX on HT293 cell. (PPT 734 kb

    Design, Synthesis, and Anti-Osteoporotic Characterization of Arginine <i>N</i>‑Glycosylated Teriparatide Analogs via the Silver-catalyzed Solid-Phase Glycosylation Strategy

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    In spite of effective antiosteoporosis potency, teriparatide, a bone-building agent approved by the FDA (Food and Drug Administration), was proven to exhibit various side effects. In our previous work, we developed a universal strategy for synthesizing arginine N-glycosylated peptides termed silver-promoted solid-phase glycosylation (SSG) strategy. However, it is unknown whether the SSG strategy can be applied in the peptide drug design. Herein, we first reported the optimization of teriparatide via SSG strategy. Using Arg20 and/or Arg25 as the modifying positions, three series of arginine N-glycosylated teriparatide analogs were successfully synthesized, of which the introduced sugar groups included glucose, galactose, mannose, rhamnose, ribose, 2-acetamino-2-deoxy-glucose, xylose, lactose, and maltose. Among the 27 arginine N-glycosylated derivatives, Arg20-xylose and Arg25-maltose teriparatide analogs, termed PTH-1g and PTH-2i, respectively, indicated enhanced serum stability and significantly improved antiosteoporotic activities in vitro and in vivo compared with the native counterpart. They may serve as effective therapeutic candidates for treating osteoporosis

    Improved antifouling properties of photobioreactors by surface grafted sulfobetaine polymers

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    <p>To improve the antifouling (AF) properties of photobioreactors (PBR) for microalgal cultivation, using trihydroxymethyl aminomethane (tris) as the linking agent, a series of polyethylene (PE) films grafted with sulfobetaine (PE-SBMA) with grafting density ranging from 23.11 to 112 μg cm<sup>−2</sup> were prepared through surface-initiated atom transfer radical polymerization (SI-ATRP). It was found that the contact angle of PE-SBMA films decreased with the increase in the grafting density. When the grafting density was 101.33 μg cm<sup>−2</sup>, it reached 67.27°. Compared with the PE film, the adsorption of protein on the PE-SBMA film decreased by 79.84% and the total weight of solid and absorbed microalgae decreased by 54.58 and 81.69%, respectively. Moreover, the transmittance of PE-SBMA film recovered to 86.03% of the initial value after cleaning, while that of the PE film recovered to only 47.27%. The results demonstrate that the AF properties of PE films were greatly improved on polySBMA-grafted surfaces.</p
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