Advanced Materials Research Vols. 781-784

Abstract: Quinones are useful compounds as dye compounds and the 1,4-naphthoquinone structure constitutes an essential part of these classes of compounds. The process in constructing 1,4-naphthoquinone for possible screening as dyestuff is described, starting from 1,4-naphthoquinone and hydroxy acid. It provides a novel methodology for the synthesis of the 5-nitro-2-substituted 1,4-naphthoquinones. The products were characterized by IR and ¹H NMR.

Abstract: 1-(3,3-dimethylcyclohexyl) ethyl acetate was synthesized by the reaction of dihydromycene with acetic acid in the presence of sulfuric acid. The effecting factors including the amount of catalyst, the reaction temperature, the molar ratio of raw materials and the reaction time were investigated. The experimental results showed that the molar raio of the dihydromyrcene to acetic acid to sulfuric acid was 1:3:0.2, the reaction temperature is 60 °C and the reaction time was 6.5 h. The yield reached 45.3%. The structure of product was characterized by gas chromatography, mass spectrometry, infrared spectroscopy and nuclear magnetic resonance. The odor evaluation result indicated that the product had a sweet, woody, floral odor.

Abstract: Several complex esters were synthesized from phthalic anhydride, neopentyl glycol and rapeseed acid. Their rheological properties, biodegradability and tribological properties were measured. It was found that the complex esters have a wide viscosity range of 126~325mm²/s at 40°C with viscosity indices about 127~143, and solidifying points lower than-38°C. The maximum non seizure load of a complex ester with degree of polymerization 1.42 is as high as 735 N, with a wear scar diameter of 0.41mm, superior to mineral oil. The biodegradation rates are higher than 73%, and the thermal stability is good. So these complex esters are a class of green synthetic ester oils with excellent properties.

Abstract: A new and accurate chiral HPLC method was developed for the determination of Melphalan HCl, L-Phenylalanine, 4-bis (2-chloroethyl) amino hydrochloride an anti-cancer chemotherapy drug and its potential impurity namely D-Phenylalanine, 4-bis (2-chloroethyl) amino hydrochloride ( D-enantiomer) in bulk substance. HPLC separation was carried out by reverse phase chromatography on Crownpak CR (+) (5μm, 4.0x150mm) with a mobile phase composed of perchloric acid (pH 4.0): methanol in the ratio of 90:10. Melphalan and its potential impurities were baseline resolved in the optimized method. The pH of perchloric acid solution in the mobile phase has played a key role in achieving chromatographic resolution between the enantiomers and in enhancing chromatographic efficiency. The developed method was completely validated and proved to be robust. The validated method yielded good results regarding specificity, precision, linearity, accuracy, robustness, sensitivity. Melphalan HCl sample solution is found to be stable for at least 60hrs at room temperature. The proposed method was found to be suitable and accurate for quantitative determination of Melphalan HCl and its D-enantiomer in bulk substance.

Abstract: The title compounds thienopyrimidine-based S-glycoside analogues were synthesized through the nucleophilic addition/cyclization/glycosylation reactions in good yields from easily accessible starting materials under mild reaction conditions. All of compounds were characterized by NMR, MS, IR and elemental analysis. The efficient approach allowed the facial synthesis of small libraries of thienopyrimidine-based S-glycoside analogues with different structural motifs for biological screening.

Abstract: Four compounds of 7-(3- (substituted-phenoxy) propoxy) quinazoline compounds, including 7-(3-(2,4-dichlorophenoxy) propoxy)-N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 7-(3-(2-chlo-rophenoxy) propoxy)-N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 7-(3-(4-chlorophenoxy) prop-oxy)-N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine, 7-(3-(naphthalen-3-yloxy) propoxy)-N-(3-chl-orophenyl)-6-methoxyquinazolin-4-amine, were synthesized from N-(5-(3-chloropropoxy)-2-cyano-4-methoxyphen-yl)-N, N-dimethylformamidine by cyclization,etheration, in the yield of 45.9%50.6%56.34% and 80.6% respectively. Their structures were characterized by IR, ¹H NMR, ¹³C NMR, MS and elemental analysis.

Abstract: The aim of this study is the removal of endotoxin from water using a positively charged microfiltration membrane. The membrane was prepared by crosslinking a chitosan (CS) coating layer with glutaraldehyde vapor on a cellulose (CA) microporous substrate. The positively charged CS/CA membrane showed promising removal efficiency of endotoxin at a high water flux.

Abstract: 2-Hydroxy-4-methoxy acetophenone condensed the Aminobenzenearsonic Acid was synthesized by paeonol and aminobenzenearsonic acid. that is, arsanilic compounds (3b). At the same time, the compound was characterized by IR-NMR-MS, as well as four methyl thiazolyl tetrazolium (MTT) colorimetric assay the arsine compounds (3b) on growth inhibition of human hepatoma cell lines HepG2 cell at different times under different concentration. It is shown that the arsine compounds (3b) can significantly inhibit the growth of human hepatoma cell line HepG2. Its effects were dose-and time-dependent. It is indicated a potential anti-tumor activity.

Abstract: The differences of growth kinetic of urinary crystallites from patients with CaOxa stones and healthy subjects were compared. With the increase of crystal growth time (t), the size of urinary crystallites from patients increased constantly from 10±9 μm at t=1 h to 50±45 μm at t=72 h, but the number of urinary crystallites decreased gradually from 1820±610 ind./mm² at t=1 h to 220±98 ind./mm² at t=72 h, indicating that the formation process of crystallites in lithogenic urine was ascribed to growth control. In contrast, for healthy subjects, the number of crystallites increased from 1650±850 ind./mm² at t=1 h to 1800±830 ind./mm² at t=72 h. However, the particle size was slowly increased from 7±5 μm at t=1 h to 14±13 μm at t=72 h, while the sizes of most urinary crystallites were still less than 20 μm, indicating that the growth process of crystallites in healthy urine was dominated by nucleation control. The differences mentioned above are mainly attributed to that both the concentration and the activity of the inhibitors in healthy urine were higher than those in lithogenic urine, and the inhibitors in healthy urine can inhibit the growth and aggregation of urinary crystallites more effectively. This result can help to elucidate the renal-calculi formation mechanism.

Abstract: Xiao-Yan-Hua-Jie-San (XYHJS), a traditional Chinese prescription, is used as a medication recipe to clinically treat inflammation and hepatitis. In previous study, we reported the hepatoprotective effects of XYHJS by increasing an antioxidant enzyme activity in mice. In the present study, the main bioactive components of XYHJS and their antioxidant activity were further investigated by using different model systems in vitro. The total phenolics content in the extract of XYHJS was determined by the Folin-Ciocalteu method. Analysis of the major phenolic compounds in the extract of XYHYS was carried out by high-performance liquid chromatography (HPLC) and thin layer chromatographic (TLC) method. The total phenolic content of the extract was 2.84 ± 0.06 mg gallic acid equivalent (GAE)/g extract powder. The phenolic acid in XYHJS was found to be gallic acid (GA). The content of GA was 2.80 mg/ml by HPLC (n=5, RSD=1.26%). Furthermore, the antioxidant activity of XYHJS extract was determined by 1, 1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity and hydroxyl free radicals (·OH) scavenging activity assay. The radical scavenging activity of XYHJS increased significantly in a concentration-dependent manner. At a concentration of 2.5 mg/ml, the DPPH and ·OH scavenging activity was 89.94% and 91.53%, respectively. It can be concluded that the content of GA in XYHJS is very high and it is the main contributor to the antioxidant activity of XYHJS. Our study indicates that XYHJS prescription could be considered to be an effective agent in the prevention of various liver diseases associated with oxidative stress.