Synthesis and Characterization of Waterborne Polyurethane Modified by Acrylate/nano-ZnO for Dyeing of Cotton Fabrics

Waterborne polyurethane modified by acrylate/nano-ZnO (PUA/ZnO) was synthesized and used to improve the wet rubbing fastness of reactive dyed cotton fabric. The reaction conditions were optimized and the products were characterized by FT-IR, TG, DSC, SEM, and particle size distribution. The dyed cotton fabrics were finished with PUA/ZnO emulsion and the rubbing fastness, ultraviolet resistant property, and wearability of treated fabrics were measured. The wet rubbing fastness of treated fabrics was increased by about 0.5–1 rate to achieve 3–4 rate, and the ultraviolet protection factor (UPF) achieved 50+ level. The whiteness, air permeability, and elongation at break of treated fabric were not decreased significantly. SEM showed that the smooth and reticular coating on the surface of treated fabric reduced the mechanical friction force between dyed fabric and rubbing cloth, and thus improved the rubbing fastness. The decomposition temperature of finished fabric was increased by 50–80 °C.     

蔗渣基生物质炭的制备、表征及吸附性能

以甘蔗渣为前驱物,采用持续升温限氧法在350、450、550℃温度下制备生物质炭(分别标记为BC350、BC450、BC550),并对其结构和组成进行表征。结果表明,3种生物质炭的产率分别为25.27%、22.28%、18.20%,pH值分别为5.97、6.45、7.96,比表面积为110.52、160.36、298.40 m2/g,阳离子交换量为:42.87、52.69、108.53 cmol/kg。此外,通过对生物质炭进行元素分析,生物质炭中含量最高的是碳元素,通过Boehm滴定测定,生物质炭表面含氧官能团含量随着制备温度的升高而逐渐减少。在3种温度下制备的3种生物质炭对诺氟沙星具有较好的吸附性能,其log(Kf)值大小顺序为:BC550(13.74)BC450(11.47)BC350(4.52)。可用作去除水和土壤中诺氟沙星的吸附功能材料。     

Synthesis,Characterization, and Antibacterial Activity of Cross-Linked Chitosan-Glutaraldehyde

This present study deals with synthesis, characterization and antibacterial activity of cross-linked chitosan-glutaraldehyde. Results from this study indicated that cross-linked chitosan-glutaraldehyde markedly inhibited the growth of antibiotic-resistant Burkholderia cepacia complex regardless of bacterial species and incubation time while bacterial growth was unaffected by solid chitosan. Furthermore, high temperature treated cross-linked chitosan-glutaraldehyde showed strong antibacterial activity against the selected strain 0901 although the inhibitory effects varied with different temperatures. In addition, physical-chemical and structural characterization revealed that the cross-linking of chitosan with glutaraldehyde resulted in a rougher surface morphology, a characteristic Fourier transform infrared (FTIR) band at 1559 cm⁻¹, a specific X-ray diffraction peak centered at 2θ = 15°, a lower contents of carbon, hydrogen and nitrogen, and a higher stability of glucose units compared to chitosan based on scanning electron microscopic observation, FTIR spectra, X-ray diffraction pattern, as well as elemental and thermo gravimetric analysis. Overall, this study indicated that cross-linked chitosan-glutaraldehyde is promising to be developed as a new antibacterial drug.     

Synthesis and Characterization of Aqueous Chitosan-polyurethanes Dispersion for Textile Applications with Multipurpose Performance Profile

As the use of high performance textiles has grown, the need for chemical finishes to provide the fabric properties required in the special applications has grown accordingly. In this project, a series of water dispersible polyurethanes dispersion (CS-PUs) with multipurpose performance profile was developed using isophorone diisocyanate (IPDI), polyethylene glycol (PEG), 2,2-dimethylol propionic acid (DMPA) and chitosan (CS) for textile applications. In two step synthesis process, NCO functional PU prepolymers prepared by reacting IPDI, PEG, and DMPA were extended with varying molar quantities of chitosan followed by structural characterization through FTIR. The prepared CS-PU dispersions were applied onto the dyed and printed poly-cotton blend fabrics. The performance behavior of the treated fabric in terms of crease recovery, tear strength, tensile strength, and antibacterial properties was evaluated by applying standard test methods. These investigations show that the CS-PU dispersions can be applied as antibacterial textile finishes with significant improvement in the physical and mechanical properties of poly-cotton fabrics.     

壳聚糖和尿素对大麻织物染色性能的影响

将壳聚糖或尿素添加在染液中对大麻织物进行染色,使用壳聚糖或尿素对大麻织物进行整理再染色,并测定了染色织物的K/S值。结果表明,尿素和壳聚糖都能够增强活性染料对大麻织物的染色能力。在染液中添加2g/L尿素,或分子量小于1万1%的壳聚糖溶液,或使用分子量小于1万0.6%的壳聚糖溶液整理大麻织物,织物染色深度均明显提高。壳聚糖分子量越小,增色效果越明显。     

Effective Synthesis and Antifouling Activity of Dolastatin 16 Derivatives

Some derivatives of dolastatin 16, a depsipeptide natural product first obtained from the sea hare Dolabella auricularia, were synthesized through second-generation synthesis of two unusual amino acids, dolaphenvaline and dolamethylleuine. The second-generation synthesis enabled derivatizations such as functionalization of the aromatic ring in dolaphenvaline. The derivatives of fragments and whole structures were evaluated for antifouling activity against the cypris larvae of Amphibalanus amphitrite. Small fragments inhibited the settlement of the cypris larvae at potent to moderate concentrations (EC₅₀ = 0.60-4.62 μg/mL), although dolastatin 16 with a substituent on the aromatic ring (24) was much less potent than dolastatin 16.     

EGCG衍生物合成及药理活性研究进展

表没食子儿茶素没食子酸酯(EGCG)是茶叶中一类重要儿茶素,在体外细胞实验及动物体内实验中,表现出多种生物活性。但EGCG的多羟基的化学结构具有脂溶性差,生物利用率低以及稳定性差等缺点,影响其被深度利用,而分子修饰能显著的改善EGCG多种理化性质。本文综述了最近国内外EGCG结构修饰的常见方法,合成过程以及相应的药理活性研究,以期为后续EGCG的进一步研究提供参考。     

Synthesis,Characterization and Biological Evaluation of Triclosan Grafted onto Cellulosic Fibers

With the increased risk of disease transmissions and cross-infection caused by microorganisms, the control of microbial infections becomes a very important issue in modern societies. Moreover, with the emergence of antibio-resistant bacterial strains, it is necessary to control the bacterial growth. One of ways to limit the bacterial proliferation is to develop antimicrobial surfaces. The present work describes the synthesis process of a direct linking of propargyled Triclosan to a modified Kraft Pulp. Propargylated Triclosan, and azidated Kraft Pulp were linked in the presence of Cu(I) catalyst, a type of Huisgen’s 1,3-dipolar azide-alkyne cycloaddition reaction, leading to the formation of Triclosan linked to kraft Pulp fibers. The modified Kraft Pulp fibers are characterized by Fourier transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS). This novel material has been investigated for its antibacterial properties against Escherichia coli, Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa. The developed material showed an important antibacterial activity. Although Triclosan is covalently grafted onto Kraft Pulp, its antibacterial properties are maintained.     

高纯度茶氨酸的合成与特性(英文)

报道了一种改进的茶氨酸(γ-谷酰基乙胺)的合成方法,包括L-谷氨酸的去氢成为吡咯烷酮羟酸(PCA),然后再加纯的乙胺(99%,气-液)反应,得率92.6%,再在84%乙醇溶液中重结晶后,高纯度茶氨酸(A型) 的得率37.4%。其结晶在透视和扫描电镜下呈长方形棱柱,具丝光状。A型茶氨酸的融点为224℃。B型茶氨酸从L-PCA合成,为甘蓝叶状,边缘呈波浪型,融点217—218℃。用HPLC分析证明,A和B型茶氨酸是混合异构体,A型含47.9%的L-茶氨酸,B型含90.9%的L-茶氨酸,100%的L-茶氨酸的旋光度(á)为+8.57。     

Synthesis and Rheological Characterization of Water-Soluble Glycidyltrimethylammonium-Chitosan

In this study, chitosan (CS) grafted by glycidyltrimethylammonium chloride (GTMAC) to form GTMAC-CS was synthesized, chemically identified, and rheologically characterized. The Maxwell Model can be applied to closely simulate the dynamic rheological performance of the chitosan and the GTMAC-CS solutions, revealing a single relaxation time pertains to both systems. The crossover point of G′ and Gʺ shifted toward lower frequencies as the CS concentration increased but remained almost constant frequencies as the GTMAC-CS concentration increased, indicating the solubility of GTMAC-CS in water is good enough to diminish influence from the interaction among polymer chains so as to ensure the relaxation time is independent of the concentration. A frequency–concentration superposition master curve of the CS and GTMAC-CS solutions was subsequently proposed and well fitted with the experimental results. Finally, the sol-gel transition of CS is 8.5 weight % (wt %), while that of GTMAC-CS is 20 wt %, reconfirming the excellent water solubility of the latter.     

Synthesis and Bioactivities of Marine Pyran-Isoindolone Derivatives as Potential Antithrombotic Agents

2,5-Bis-[8-(4,8-dimethyl-nona-3,7-dienyl)-5,7-dihydroxy-8-methyl-3-keto-1,2,7,8-teraahydro-6H-pyran[a]isoindol-2-yl]-pentanoic acid (FGFC1) is a marine pyran-isoindolone derivative isolated from a rare marine microorganism Stachybotrys longispora FG216, which showed moderate antithrombotic(fibrinolytic) activity. To further enhance its antithrombotic effect, a series of new FGFC1 derivatives (F1–F7) were synthesized via chemical modification at C-2 and C-2′ phenol groups moieties and C-1″ carboxyl group. Their fibrinolytic activities in vitro were evaluated. Among the derivatives, F1–F4 and F6 showed significant fibrinolytic activities with EC₅₀ of 59.7, 87.1, 66.6, 82.8, and 42.3 μM, respectively, via enhancement of urokinase activity. Notably, derivative F6 presented the most remarkable fibrinolytic activity (2.72-fold than that of FGFC1). Furthermore, the cytotoxicity of derivative F6 was tested as well as expression of Fas/Apo-1 and IL-1 on HeLa cells. The results showed that, compared to FGFC1, derivative F6 possessed moderate cytotoxicity and apoptotic effect on HeLa cells (statistical significance p > 0.1), making F6 a potential antithrombotic agent towards clinical application.     

Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents

Using analogues of some marine steroidal oximes as precursors, a series of aza-B-homocholestane derivatives possessing different substituted groups at the 3-position of the steroidal nucleus were synthesized. Their biological activity against cancer cell proliferation was determined with multiple cancer cell lines. Aza-B-homocholestane derivatives possessing 3-hydroxyl, 3-hydroximino and 3-thiosemicarbazone groups displayed remarkable cytotoxicity to cancer cells via apoptosis inducing mechanism. Compounds 5, 10, 12, 15 and 18 exhibited better potency to inhibit cancer cell proliferation. In addition, compound 15 was further evaluated with three dimensional (3D) multicellular spheroids assay to determine its potency against spheroid growth. The structure-activity relationship (SAR) generated in the studies is valuable for the design of novel chemotherapeutic agents.     

Design,Synthesis and Evaluation of Novel Phorbazole C Derivatives as MNK Inhibitors through Virtual High-Throughput Screening

MNKs (mitogen-activated protein kinase-interacting protein kinases) phosphorylate eIF4E at Ser209 to control the translation of certain mRNAs and regulate the process of cell proliferation, cell migration and invasion, etc. Development of MNK inhibitors would be an effective treatment for related diseases. We used the MarineChem3D database to identify hit compounds targeting the protein MNK1 and MNK2 through high-throughput screening. Compounds from the phorbazole family showed good interactions with MNK1, and phorbazole C was selected as our hit compound. By analyzing the binding mode, we designed and synthesized 29 derivatives and evaluated their activity against MNKs, of which, six compounds showed good inhibition to MNKs. We also confirmed three interactions between this kind of compound and MNK1, which are vital for the activity. In conclusion, we report series of novel MNK inhibitors inspired from marine natural products and their relative structure–activity relationship. This will provide important information for further developing MNK inhibitors based on this kind of structure.     

Synthesis of Water-Soluble Sulfonated Chitin Derivatives for Potential Antioxidant and Antifungal Activity

Chitin is a natural renewable and useful biopolymer limited by its insolubility; chemical derivatization can enhance the solubility and bioactivity of chitin. The purpose of this study was to synthesize novel water-soluble chitin derivatives, sulfo-chitin (SCT) and sulfopropyl-chitin (SPCT), as antioxidant and antifungal agents. The target derivatives were characterized by means of elemental analysis, FTIR, ¹³C NMR, TGA and XRD. Furthermore, the antioxidant activity of the chitin derivatives was estimated by free radical scavenging ability (against DPPH-radical, hydroxyl-radical and superoxide-radical) and ferric reducing power. In addition, inhibitory effects against four fungi were also tested. The findings show that antioxidant abilities and antifungal properties were in order of SPCT > SCT > CT. On the basis of the results obtained, we confirmed that the introduction of sulfonated groups on the CT backbone would help improve the antioxidant and antifungal activity of CT. Moreover, its efficacy as an antioxidant and antifungal agent increased as the chain length of the substituents increased. This derivatization strategy might provide a feasible way to broaden the utilization of chitin. It is of great significance to minimize waste and realize the high-value utilization of aquatic product wastes.     

Contemporary Strategies for the Synthesis of Tetrahydropyran Derivatives: Application to Total Synthesis of Neopeltolide,a Marine Macrolide Natural Product

Tetrahydropyrans are structural motifs that are abundantly present in a range of biologically important marine natural products. As such, significant efforts have been paid to the development of efficient and versatile methods for the synthesis of tetrahydropyran derivatives. Neopeltolide, a potent antiproliferative marine natural product, has been an attractive target compound for synthetic chemists because of its complex structure comprised of a 14-membered macrolactone embedded with a tetrahydropyran ring, and twenty total and formal syntheses of this natural product have been reported so far. This review summarizes the total and formal syntheses of neopeltolide and its analogues, highlighting the synthetic strategies exploited for constructing the tetrahydropyran ring.     

Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin

Deoxybostrycin (1) is an anthraquinone compound derived from the marine mangrove fungus Nigrospora sp. No. 1403 and has potential to be a lead for new drugs because of its various biological properties. A series of new derivatives (2–22) of deoxybostrycin were synthesized. The in vitro cytotoxicity of all the new compounds was tested against MDA-MB-435, HepG2 and HCT-116 cancer cell lines. Most of the compounds exhibit strong cytotoxicity with IC₅₀ values ranging from 0.62 to 10 μM. Compounds 19, 21 display comparable cytotoxicity against MDA-MB-435 to epirubicin, the positive control. The primary screening results indicate that the deoxybostrycin derivatives might be a valuable source of new potent anticancer drug candidates.     

Structural Transformation and Dyeing Performance of Poly(Ethylene Terephthalate) Filament Using Dicationic Imidazolium Ionic Liquid

3,3'-[1,2-ethanediylbis (oxy-2,1-ethanediyl)]-bis[1-methyl-imidazolium]-dibromide (DImDBr), a gemini imidazolium ionic liquid, was synthesized for the modification and dyeing promotion of poly(ethylene terephthalate) (PET) filaments. The results showed that parameters such as treatment temperature, time, and DImDBr concentration played a critical role on the tensile strength and tensile strength retention of modified PET filaments. The optimal treatment parameters of the PET filaments were 120 °C for 90 min with addition of 6 % ionic liquid. The influence of disperse dyeing parameters (temperature, time, and dye concentration) on DImDBr modified PET filaments were also studied. The disperse dyed PET filaments (after treatment with DImDBr) exhibited a desirable color strength (K/S value), excellent soap washing fastness, light fastness, and rubbing fastness. Furthermore, the native PET filaments and DImDBr treated PET filaments were characterized by FT-IR, XRD, DSC, TGA, and SEM. Density functional theory (DFT) simulation showed the presence of two kinds of hydrogen bonds (C-H/O and O-H/Br) and eight strong hydrogen bonds in the DImDBr/cis-PET monomers, while only three hydrogen bonds were found in the DImDBr/trans-PET monomers. The structural transformation from the crystalline phase to the amorphous phase (FT-IR, XRD, and DFT simulation) after DImDBr modification confirmed the dyeing promotion of PET filaments at lower temperature.     

Design,Synthesis and Biological Evaluation of Novel Bromophenol Derivatives Incorporating Indolin-2-One Moiety as Potential Anticancer Agents

A series of bromophenol derivatives containing indolin-2-one moiety were designed and evaluated that for their anticancer activities against A549, Bel7402, HepG2, HeLa and HCT116 cancer cell lines using MTT assay in vitro. Among them, seven compounds (4g–4i, 5h, 6d, 7a, 7b) showed potent activity against the tested five human cancer cell lines. Wound-healing assay demonstrated that compound 4g can be used as a potent compound for inactivating invasion and metastasis by inhibiting the migration of cancer cells. The structure–activity relationships (SARs) of bromophenol derivatives had been discussed, which were useful for exploring and developing bromophenol derivatives as novel anticancer drugs.     

Total Synthesis and Anti-Inflammatory Bioactivity of (−)-Majusculoic Acid and Its Derivatives

The first total synthesis of marine natural product, (−)-majusculoic acid (1) and its seven analogs (9–15), was accomplished in three to ten steps with a yield of 3% to 28%. The strategy featured the application of the conformational controlled establishment of the trans-cyclopropane and stereochemical controlled bromo-olefination or olefination by Horner–Wadsworth–Emmons (HWE) reaction. The potential anti-inflammatory activity of the eight compounds (1 and 9–15) was evaluated by determining the nitric oxide (NO) production in the lipopolysaccharide (LPS)-induced mouse macrophages RAW264.7. (−)-Majusculoic acid (1), methyl majusculoate (9), and (1R,2R)-2-((3E,5Z)-6-bromonona-3,5-dien-1-yl)cyclopropane-1-carboxylic acid (12) showed significant effect with inhibition rates of 33.68%, 35.75%, and 43.01%, respectively. Moreover, they did not show cytotoxicity against RAW264.7 cells, indicating that they might be potential anti-inflammatory agents.     

采用高效液相色谱技术分析茶树体内维生素B6

采用高效液相色谱技术对茶树叶片等组织中维生素B₆（VB₆）的存在形态进行了分析。结果表明：叶片、嫩茎和根中VB₆的含量依次为3.36、1.27、0.18 μg/g鲜重;叶片组织中各型VB₆的构成比为：吡哆醇21%、吡哆醛2.4%、吡哆胺19.3%、磷酸吡哆醛40.8%和磷酸吡哆胺17.9%;叶片中VB₆的含量随叶片的成熟而增加,因叶老化而降低。