Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents

Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model.     

邻苯二甲酸酯鼓泡生物降解

该课题测试了邻苯二甲酸酯类化合物的鼓泡生物降解行为。结果表明，邻苯二甲酸酯的降解速率常数（kb)与其烷基链长度之间存在良好的相关性，kb=0.0009x^2-0.019x 0.1123，相关系数r=0.9906；浓度超过500mg/L时，邻苯二甲酸二乙酯可抑制自身的生物降解；中间产物邻苯二甲酸浓度超过50mg/L时，也对邻苯二甲酸二乙酯的生物降解有明显的抑制作用。     

燃料甲酯应用研究浅析

本阐述了分别使用燃料甲酯及柴油时由柴油机以加俐到的示功图，烟度及过量空气系统等的对比结果。经分析认为：当燃料甲酯取代柴油机时，用户可不必对柴油机另作调整，因而十分方便。     

Viscoelasticity of oxidized starch/low methoxy pectin mixtures in the presence of glucose syrup

The structural properties of mixtures of pectin, oxidized starch and glucose syrup were investigated using small deformation dynamic oscillation. In the absence of added calcium, preparations of low methoxy pectin with glucose syrup formed viscous solutions, which remained crystal-free at subzero temperatures. Samples of oxidized starch and glucose syrup, on the other hand, exhibited solid-like behaviour because of the crystalline nature of the amylose-like helices. Mixtures of the two polysaccharides with the co-solute clearly showed phase inversion from liquid to solid-like behaviour with increasing amounts of starch in the formulation. The transformation was reflected in the textural properties of samples, which varied from thick solutions to firm gels. The viscoelasticity of the system was modified further by the introduction of high methoxy pectin. Preparations of high methoxy pectin and glucose syrup formed rubbery gels whose amorphous nature underwent a glass transition during cooling.     

Preparation of fatty acid methyl esters for gas-chromatographic analysis of lipids in biological materials

Theoretically, preparation of fatty acid methyl esters (FAMEs) deals with reversible chemical reactions in a complex system. Methodologically, there are numerous ways, generally characterized by the type of catalysts used and steps involved. Although there are more than a half dozen common catalysts, the majority fall into either acidic (HCl, H₂SO₄ and BF₃) or alkaline types (NaOCH₃, KOH and NaOH), with each having its own catalytic capability and application limitations. In terms of steps, many conventional methods, including those officially recognized, consist of drying, digestion, extraction, purification, alkaline hydrolysis, transmethylation/methylation and postreaction work-up. Although these methods are capable of providing reliable estimates if some precautions are taken, they are cumbersome, time-consuming and cost-inefficient. A new approach has been to transmethylate lipidsin situ. Due to its simplicity, high sensitivity, comparable reliability and capability to determine total fatty acids, the method of direct transmethylation is finding a unique place in lipid determination. Regardless of which method is used, quantitative methylation requires chemists to take precautions at every step involved, particularly during FAME formation and subsequent recovery steps. Evidently, there is an urgent need for more systematic studies, guided by the chemical principle of reactions involved and physicochemical properties of regents and end products, into factors affecting these steps. Hopefully, this will lead to an improved method, which measures lipid composition in biological materials not only with high accuracy but also with high efficiency and minimum costs.     

咪唑啉酮氧苯氧羧酸酯类化合物的合成

用含二茂铁基的叠氮化物与三苯基膦反应制得膦亚胺，再与芳基异氰酸酯、取代酚发生串连aza-Wittig反应，合成了5个新的含二茂铁基的咪唑啉酮氧苯氧羧酸酯类化合物。用元素分析、IR、^1HNMR表征了它们的结构。     

Contribution oftrans-18∶1 acids from dairy fat to european diets

Twelve commercial samples of French butter, purchased in October–November, and 12 other samples, purchased in May–June, were analyzed with particular attention to theirtrans-octadecenoic acid contents. The isomeric fatty acids were quantitated by a combination of gas-liquid chromatography (GLC) of total fatty acids as isopropyl esters on a polar capillary column (CPSil 88) and of silver nitrate-impregnated thin-layer chromatography followed by GLC of the pooled saturated (used as internal standards) andtrans-octadecenoic acid fractions. Autumn butters contained 3.22±0.44%trans-octadecenoic acids (relative to total fatty acids), whereas those collected during the spring contained 4.28±0.47% (P<0.01). Minimum and maximum values for the two sets of butters were 2.46 (autumn) and 5.10% (spring), respectively. The annual mean value for thetrans-octadecenoic acid content in all butter samples was 3.8% of total fatty acids (ca. 2% for thetrans-11 18∶1 acid). This value allows calculation of the daily individual intake oftrans-octadecenoic acids from dairy products by populations of member states of the European Economic Community (EEC). It varies from 0.57 g (Portugal) to 1.66 g (Denmark). The mean value for the twelve countries of the EEC is 1.16 g/person/d, which is close to data published for the United States. In France, the consumption oftrans octadecenoic acids from dairy fat is higher than that from margarines (ca. 1.5 vs. 1.1 g/person/d).     

Enzymatic degradation of esters of dichloropropanols: removal of chlorinated glycerides from processed foods

The esters of dichloropropanols from the byproduct of hydrolysates during food processing were degraded by the cell-free extracts of a dichloropropanol-assimilating bacterium of Pseudomonas sp. OS-K-29. 1-Acyloxy-2,3-dichloropropane was hydrolysed into the corresponding carbonic acid and 2,3-dichloropropanol, and then the dichloropropanol was dechlorinated. The esterase activity of the cell-free extracts was effective for the esters of the dichloropropanols and monoacylglycerides, but not for hydrolysing the lipase substrates such as triacylglycerides and Tween 60. A comparative study using a series of octanoyl glycerides and the esters of the dichlopropanols showed that the substrate specificities of the cell-free extracts were similar to the monoacylglyceride lipase from Penicillium camembertii.     

Process conditions for separating fatty acid esters by supercritical CO2

The solubilities of ethyl palmitate, ethyl oleate, ethyl eicosapentaenoate (EPA) and ethyl docosahexaenoate (DHA) in supercritical carbon dioxide were determined by a continuous flow method. The solubilities of fatty acid ethyl esters increased with pressure and decreased as the temperature was increased. An empirical equation, similar to Chrastil's equation, was used to describe the relationship between solute solubility and the density of carbon dioxide. The empirical equation was further used to qualitatively estimate the separation efficiency of isolating EPA and DHA ethyl esters from fatty acid esters. The operating conditions yielding high solubility gave fast extraction rate but resulted in low separation efficiency. Experiments were conducted to separate ethyl EPA and ethyl DHA from a model mixture containing four fatty acid ethyl esters and from esterified squid visceral oil. The experimental data compared closely with the calculated values.