Synthesis and Antiradical Activity of 5-Acetyl-2-alkylthio-4-aryl-6-methyl-1,4-dihydropyridine-3-carboxylic Acid Nitriles

The alkylation of 3-cyano-1,4-dihydropyridine-2(3H)-thiones or the condensation of an aromatic aldehyde, cyanothioacetamide, acetylacetone, and methyl iodide in the presence of piperidine has given a series of novel 5-acetyl-2-alkylthio-4-aryl-6-methyl-1,4-dihydropyridine-3-carboxylic acid nitriles. A compound was obtained from 3,5-di(tert-butyl)-4-hydroxybenzaldehyde in the molecule of which were combined the active part of the antioxidant ionol and a 1,4-dihydropyridine ring. It was found that, among the compounds synthesized, the highest antiradical activity occurred in a compound having two hydroxyl groups in the 4-phenyl substituent.     

1－芳氧基乙酰基－4－邻氯苯甲酰基氨基硫脲衍生物的合成及其生物活性研究

于固－液相转移催化条件下，合成了１０个１－芳氧基乙酰基－４－邻氯苯甲酰基氨基硫脲衍生物，用元素分析、ＩＲ和￣１Ｈ－ＮＭＲ光谱确定了它们的结构。该类化合物对小麦幼苗生长具有明显的促进作用。     

示差脉冲伏安法测定乳酸脱氢酶活性及纳米微粒生物毒性检测新方法研究

采用示差脉冲伏安法，在乳酸脱氢酶(LDH)酶促体系“丙酮酸盐 + NADH +H⁺ (?) 乳酸盐 + NAD⁺”中，通过检测NAD⁺还原峰电流的变化，测定了不同条件下(不同酶用量、缓冲液pH值以及温度)LDH的活性、酶促体系的米氏常数K_m^NADH以及最大反应速率v_max。并且在最佳实验条件下，通过检测LDH活性的改变，实验考察了3种纳米物质(ZnS，TiO₂(R)和TiO₂(A))对乳酸脱氢酶酶促体系的影响。     

Chiral methylbenzylammonium salts of aryldithiophosphonic acids containing glucofuranose,allofuranose, and galactopyranose diacetonide scaffolds

Abstract

New chiral methylbenzylammonium salts of aryldithiophosphonic acids containing glucofuranose, allofuranose, and galactopyranose diacetonide substituents were obtained using (S)-(–)-α-methylbenzylamine, (R)-(+)-α-methylbenzylamine, and (R,S)-(±)-α-methylbenzylamine. Salts obtained possess antimicrobial activity.     

Inhibitory study of some novel Schiff base derivatives on Staphylococcus aureus by microcalorimetry

The effect of a series of novel Schiff base compounds on Staphylococcus aureus was studied by microcalorimetric method at 37 °C The results showed that all of the organic compounds had the capacity to inhibit the growth of S. aureus in different extent. And the extent and duration of the inhibitory effect on the growth of S. aureus, judged from the rate constant (k), varied with the different structure of the Schiff base compounds. According to the power-time curves, the multiplication rate constant and inhibition ratio were calculated. The growth rate constant of S. aureus (in log phase) in the presence of Schiff base compounds decreased with the increasing of the concentrations of these compounds regularly. The experimental results revealed that the hydrophilicity of Schiff bases had a great influence on their antibacterial activity. Of these Schiff bases, the greater their hydrophilicity, the higher their antibacterial activity. The antibacterial structure-activity relationship (SAR) of Schiff base derivatives was also briefly discussed.     

辣根过氧化物酶自组装多层膜结构形貌与活性的研究

用分子沉积自组装作制备了阳离子化和阴离子化的辣根过氧化物酶自组装膜；并用原子力显微镜（AFM）研究了不同离子化辣根过氧化物酶单层及多层自组装膜的形貌结构与自组装膜的活性变化关系。结果表明：阴离子化的辣根过氧化物酶自组装膜的表面形貌比较粗糙，均方根粗糙度（RMS）及酶分子粒径较大，且组装膜的活性比较大。     

Automatic sequential determination of the hydrogen peroxide scavenging activity and evaluation of the antioxidant potential by the 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation assay in wines by sequential injection analysis

An automatic system that performs two analytical procedures, allowing the evaluation of the relative antioxidant capacity of wine samples, was developed. Automation was carried out using a sequential injection analysis (SIA) system that allowed, thanks to its versatility, the development of two methodologies. One is based on the decolorization assay of the 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical, using a spectrophotometric detector. A second methodology allowed the evaluation of the hydrogen peroxide scavenging activity by measuring the oxidation of homovanylic acid (HVA) to its fluorescent dimer, using a fluorescent detector.The developed automatic methodologies were evaluated using trolox as standard and subsequently using other antioxidant substances as gallic acid, caffeic acid, ascorbic acid, catechin and taxifolin which are abundant in wine and whose antioxidant activities were compared to that shown by trolox. The spectrophotometric and fluorimetric assays showed linearity intervals between 0.001 and 0.01 mM, and 0.001 and 0.008 mM of trolox, respectively.The evaluation of the antioxidant power of 20 white and red wine samples, from different Portuguese wine producing regions, was carried out sequentially, in the automatic system. The results were expressed in trolox equivalent antioxidant capacity (TEAC) and presented, for the ABTS and hydrogen peroxide scavenging activity methodologies, detection limits of 8.4 × 10⁻⁷ and 1.4 × 10⁻⁴ mM and relative standard deviation (R.S.D. (%)) in the range 0.6-2.4 and 1-1.8, respectively.     

2-取代-3-芳基-4-噻唑啉(硫)酮衍生物的合成、晶体结构和生物活性

从2-取代-3-芳基-4-噻唑啉酮(4a～4e和5)合成了三个系列新型噻唑啉酮衍生物, 即5-芳基亚甲基-4-噻唑啉酮(6a～6j), 4-噻唑硫酮(7a～7e和8)和4-氰基亚胺基噻唑烷(11a～11e和12). 中间体4a～4e和5由醛、胺和巯基乙酸缩合得到. 所有化合物的结构均经元素分析和¹H NMR确证, 并且采用X射线单晶衍射分析方法测定了化合物4b的结构. 初步生物活性试验结果表明, 部分标题化合物具有一定的杀菌活性和促进黄瓜子叶生根活性.     

Target-triggered inhibiting oxidase-mimicking activity of platinum nanoparticles for ultrasensitive colorimetric detection of silver ion

The development of efficient methods for the detection of hazardous and toxic elements is extremely important for environmental security and public health. In this work, we developed a facile colorimetric assaying system for Ag⁺ detection in aqueous solution. Chitosan-stabilized platinum nanoparticles (Ch-PtNPs) were synthesized and severed as an artificial oxidase to catalyze the oxidation of the substrate 3,3′,5,5′-tetramethylbenzidine (TMB) and generate color signal. In the presence of Ag⁺, due to the strong metallophilic interactions between Ag⁺ and Pt²⁺ on the surface of Ch-PtNPs, Ag⁺ can weaken the affinity to the substrates and inactivate the catalytic activity of Ch-PtNPs, leading to decreased absorbance signal to varying degrees depending on Ag⁺ amount. Combing the specific binding between Ch-PtNPs and Ag⁺ with signal amplification procedure based on the Ch-PtNPs-catalyzed TMB oxidation, a sensitive, selective, simple, cost-effective, and rapid detection method for Ag⁺ can be realized. Ag⁺ ions in tap and lake waters have been successfully detected. We ensured that the proposed method can be a potential alternative for Ag⁺ determination in environmental samples.