Evaluation of Floxuridine Oligonucleotide Conjugates Carrying Potential Enhancers of Cellular Uptake

Conjugation of small molecules such as lipids or receptor ligands to anti-cancer drugs has been used to improve their pharmacological properties. In this work, we studied the biological effects of several small-molecule enhancers into a short oligonucleotide made of five floxuridine units. Specifically, we studied adding cholesterol, palmitic acid, polyethyleneglycol (PEG 1000), folic acid and triantennary N-acetylgalactosamine (GalNAc) as potential enhancers of cellular uptake. As expected, all these molecules increased the internalization efficiency with different degrees depending on the cell line. The conjugates showed antiproliferative activity due to their metabolic activation by nuclease degradation generating floxuridine monophosphate. The cytotoxicity and apoptosis assays showed an increase in the anti-cancer activity of the conjugates related to the floxuridine oligomer, but this effect did not correlate with the internalization results. Palmitic and folic acid conjugates provide the highest antiproliferative activity without having the highest internalization results. On the contrary, cholesterol oligomers that were the best-internalized oligomers had poor antiproliferative activity, even worse than the unmodified floxuridine oligomer. Especially relevant is the effect induced by palmitic and folic acid derivatives generating the most active drugs. These results are of special interest for delivering other therapeutic oligonucleotides.     

The Mystery of Extramitochondrial Proteins Lysine Succinylation

Lysine succinylation is a post-translational modification which alters protein function in both physiological and pathological processes. Mindful that it requires succinyl-CoA, a metabolite formed within the mitochondrial matrix that cannot permeate the inner mitochondrial membrane, the question arises as to how there can be succinylation of proteins outside mitochondria. The present mini-review examines pathways participating in peroxisomal fatty acid oxidation that lead to succinyl-CoA production, potentially supporting succinylation of extramitochondrial proteins. Furthermore, the influence of the mitochondrial status on cytosolic NAD⁺ availability affecting the activity of cytosolic SIRT5 iso1 and iso4—in turn regulating cytosolic protein lysine succinylations—is presented. Finally, the discovery that glia in the adult human brain lack subunits of both alpha-ketoglutarate dehydrogenase complex and succinate-CoA ligase—thus being unable to produce succinyl-CoA in the matrix—and yet exhibit robust pancellular lysine succinylation, is highlighted.     

A Facile Approach toward Thermoplastic Triple-Shape Memory Polymers

In this work, a ternary blend of polyolefin elastomer (POE), lauric acid (LA), and poly(ε-caprolactone) (PCL) with triple-shape memory effect (triple-SME) is reported. LA and PCL exhibit distinct thermal transitions and construct two reversible switching networks capable of fixing and releasing different temporary shapes under a mild condition. The ternary blend shows excellent triple-shape memory properties and good toughness. Besides, the permanent shape can be reconfigured by a simple thermal treatment. These particular features make the novel blend a competitive candidate for diverse applications. And the creative combination of crystalline small molecule and semicrystalline polymer expands the freedom for producing triple-shape memory polymers (triple-SMPs).     

The Synthesis of Covalent Triazine-Based Frameworks via Friedel–Crafts Reactions of Cyanuric Chloride with Thienyl and Carbazolyl Derivatives for Fluorescence Sensing to Picric Acid,Iodine and Capturing Iodine

A multifunctional thiophene-based covalent triazine framework (TTPATTh) with triphenylamine as core is synthesized by Friedel–Crafts reaction of cyanuric chloride with thienyl derivative for the first time. The yield of TTPATTh (99.59%) is far higher than that of the carbazole-based CTF (TTPATCz, 47.03%). TTPATTh and TTPATCz possess high BET surface areas with 1235 and 2501 m² g^–1 as well as high pore volumes with 1.60 and 2.23 cm³ g^–1, respectively. TTPATTh and TTPATCz have high thermal stability with high thermal decomposition temperatures of 514 and 598 °C in nitrogen atmosphere. With the introduction of triazine rings, the fluorescence sensing sensitivities of TTPATTh and TTPATCz to picric acid and iodine are improved significantly. Especially for TTPATTh, the K_sv values reach 5.95 × 10⁵ and 1.61 × 10⁴ L mol^–1, and LODs reach 1.02 × 10^–12 and 1.86 × 10^–12 mol L^–1. To the best of the knowledge, this is the most sensitive value among thiophene-based porous organic polymers to PA and I₂. Furthermore, TTPATTh and TTPATCz can also adsorb iodine in vapor phase, cyclohexane solution and aqueous solution, and release iodine by heating or in ethanol solution. The efficiency of controlling the release of iodine is higher than that in ethanol.     

Supplementation with Docosahexaenoic Acid and Vitamin E Improves Hepatic Triglyceride Accumulation Induced by High-Fat Diet in Mice

The study aims to investigate the effect of combined supplementation with docosahexaenoic acid (C22:6 n-3, DHA) and vitamin E (VE) on the oxidative stress and liver triglycerides (TG) accumulation induced by high-fat diet (HFD) in mice. C57BL/6J mice are fed either a control diet or an HFD for 8 weeks. Animals are supplemented with DHA, VE, or DHA + VE, respectively. Supplementation with DHA alone shows significant improvement in oxidative stress and hepatic steatosis in mice. Supplementation with DHA significantly reduces the liver TG and total cholesterol contents, and the alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels, compared with the HFD. Supplementation with DHA also significantly decreases the mRNA expression level of sterol regulatory element-binding protein 1C. However, supplementation with VE alone does not show improvement in oxidative stress and hepatic steatosis. DHA + VE supply obtains a superior effect in alleviation of hepatic steatosis than DHA supplementation alone in mice fed by HFD. The efficacy of DHA potentiated by VE can be due to that VE enhances the effect of DHA in decrease of ALT and AST levels and increase of antioxidant enzyme activity and glutathione level in mice fed by HFD. Practical Applications: Supplementation with DHA significantly improves the oxidative stress and hepatic steatosis induced by HFD in mice. The efficacy of DHA in the alleviation of hepatic steatosis induced by HFD is potentiated by VE. These findings may provide a rational basis for the use of DHA and VE co-supplementation in patients with liver steatosis.     

Feasibility Study of Microwave-Assisted Biodiesel Production from Vegetable Oil Refinery Waste

Vegetable oil refinery waste containing acid oil is used as an inexpensive feedstock for producing biodiesel by microwave-assisted esterification (MAE) method. Effects of some main variables such as free fatty acid:methanol molar ratio (1:1, 1:5, and 1:10), reaction time (5, 30, and 60 min), and catalyst concentration (1%, 2%, and 3%) on physicochemical properties of produced biodiesel are investigated. Optimum reaction conditions of MAE are free fatty acid:methanol molar ratio of 1:10, reaction time of 60 min, and a catalyst concentration of 3%, while having 95.79% conversion yield. By increasing the conversion yield of the biodiesel, density and color brightness increase, while viscosity and refractive index decrease. There are no significant differences between physicochemical and heating properties of biodiesel produced by MAE and magnetic stirrer esterification (MSE) methods. Meanwhile, energy consumption of MAE method is almost four times lower than that of MSE. MAE as a promising alternative to the conventional esterification method can be considered as an energy-efficient method for producing biodiesel from inexpensive vegetable oil refinery waste. Practical applications : Acid oil is an inexpensive by-product of alkali refining in vegetable oil plants that would pollute the environment if not rendered safely. In this study, MAE is used to convert acid oil to biodiesel as a practical process for bringing alkali refining waste into production cycle. Acid oil can provide a reduction in the cost of biodiesel production. In addition, application of energy-efficient MAE method can facilitate the economical production of biodiesel.     

Controllable synthesis of pure monodispersed zirconia nanopowders with tetragonal phase

Nanopowders of pure zirconia have been synthesized using citric acid (CA)-assisted lamellar liquid crystal template method. The microstructure of the zirconia powder prepared at the different mole ratios of CA to zirconium oxynitrate (ZN) was characterized by FT-IR, X-ray diffraction (XRD), laser particle size analyzer, Raman spectroscopy, and scanning electron microscope (SEM) methods. The phase structure of the sodium dodecyl sulfate (SDS)/C₁₀H₂₁OH/H₂O system before and after adding mixing solution CA and ZN was determined by POM (Polarizing Optical Microscope). The results show that lamellar structure of the SDS/C₁₀H₂₁OH/H₂O system after adding mixing solution CA and ZN is stable. The presence of CA inhibits agglomeration and growth of zirconia particle. The crystallite size of zirconia powders decreases and agglomerates lowly with addition of CA. Fourier transform infrared spectrometry (FI-IR) analyses reveal that the structure of chelating organic complex is maintained in zirconia structure at high-temperature calcination to cause oxygen vacancies which stabilizes the tetragonal phase of zirconia. The zirconia powders remained the single metastable tetragonal phase at the molar ratios of CA to ZN ranging from 1:3 to 5:1. The crystallite size of zirconia with spherical morphology varied from 32.2 to 20.1 nm with the increase of the molar ratio of CA to ZN in the range of 1:3 to 5:1.     

煤粉炉粉煤灰提取氧化铝活化技术研究进展

介绍了近年来采用煤粉炉粉煤灰作为原料制备氧化铝的预处理活化工艺技术,指出了粉磨法、硫酸法、氯化钙法、铵盐法、碳酸盐法、氟化盐法、物理-化学联合活化法的优缺点及在工程转化过程中需重点关注的环节。虽然部分工艺技术实现了工业化,但因成本高等因素导致项目关停,建议粉煤灰综合利用研究方向应以工程转化难点问题为导向,理论研究与工程设计相结合,逐步探索出一条经济效益好、安全环保的粉煤灰制备氧化铝工业化路线。     

Sulfuric acid recovery from rare earth sulphate solutions by diffusion dialysis

1 Introduction As an important industrial chemical, sulfuric acids are widely used in metallurgical and chemical processes, in which some waste solutions containing free sulfuric acids and metallic ions are therefore produced[1, 2]. If these waste acids …     

水质稳定剂HPDP缓蚀阻垢性能评定

用静态阻垢，旋转挂片失得法实验研究了ＨＰＤＰ对ＣａＣＯ３，Ｃａ３（ＰＯ４）２等的阻垢性能以及对Ｑ２３５碳钢的缓蚀性能等。试验证明，ＨＰＤＰ是一种优良的阻垢缓蚀剂，适用于高温，高碱，高ＰＨ，高浓缩倍数的循环冷却水处理，具有广阔的应用前景。