Photoregulation of Gene Expression with Ligand-Modified Caged siRNAs through Host/Guest Interaction

Small interfering RNA (siRNA) can effectively silence target genes through Argonate 2 (Ago2)-induced RNA interference (RNAi). It is very important to control siRNA activity in both spatial and temporal modes. Among different masking strategies, photocaging can be used to regulate gene expression through light irradiation with spatiotemporal and dose-dependent resolution. Many different caging strategies and caging groups have been reported for light-activated siRNA gene silencing. Herein, we describe a novel caging strategy that increases the blocking effect of RISC complex formation/process through host/guest (including ligand/receptor) interactions, thereby enhancing the inhibition of caged siRNA activity until light activation. This strategy can be used as a general approach to design caged siRNAs for the photomodulation of gene silencing of exogenous and endogenous genes.     

Effect of select parameters on the properties of edible film from water-soluble fish proteins in surimi wash-water

Edible film from water-soluble fish proteins were developed by casting film solution on leveled trays and effects of pH (9.5, 10.0 and 10.5), heating temperature (60, 70 and 80 °C), and heating time (10, 20 and 30 min) of the film solution on various film properties were determined using Response Surface Methodology (RSM). The impact of pH and heating temperature of film solution was more significant, overall, on the film's properties than heating time. Contour plots of tensile strength and elongation at break was highest at pH of 10.0 at 70 °C (2.75-3.02 MPa) but low in elongation at break (6.35-9.16%), while water vapor permeability and oxygen permeability were at their lowest (58.55-65.96 g mm/m² d kPa and 351.33-624.18 cm³ μm/m² d kPa). There was a direct correlation between the films’ and proteins’ solubility on one hand, and heating temperature of film solution on the other, which reversed with change in pH of film solution. Film color was darker and more yellowish with increase in the pH of film solution.     

水溶性防氧化剂在SMT用印制板上的应用

水溶性的防氧化剂是一种有机可焊性保护剂。其方法是在印制板完全阻焊、字符层的印刷，并经电检之后，通过表面浸渍在裸铜的贴片位或通孔内形成一种耐热性的有机可焊性膜层。这种有机、可焊、耐热的膜层，膜厚可达0.3-0.5mm，其分解的温度可达约300℃，传统的印制板的热风整平法亦无法满足QFP愈来愈密集的需求，同时也无法满足SMD表面平整度的要求，更无法适应PCB薄型化生产。烷基苯并咪唑的OSP法能弥补这项缺陷，因而在PCB业乃至SMT产业中得到了广泛的应用。     

Comparison between the binding of chlorpheniramine maleate to poly(sodium 4-styrenesulfonate) and the binding to other polyelectrolytes

The interactions of the antihistaminic drug chlorpheniramine maleate (CPM) with the negatively charged polyelectrolytes poly(sodium 4-styrenesulfonate) (PSS) and poly(acrylic acid) (PAA) are studied by the washing method of the diafiltration technique at conditions simulating those of the small intestine such as pH 7.5 and 0.13 M NaCl. The results are compared with those already reported involving other pharmacologically important polyelectrolytes such as alginic acid (ALG), carboxymethylcellulose (CMC), and κ- and ι-carrageenan (κ- and ι-CAR). As in the case of ALG, CMC, and CAR, interactions of CPM with PAA appear to be electrostatic and are cleaved in the presence of 0.13 M NaCl. On the contrary, apart from electrostatic interactions, additional interactions are found with PSS and residual interactions are kept in the presence of 0.13 M NaCl, a fact that may be attributed to π-π interactions and hydrophobic forces. The effect of the addition of 4 M urea, branched poly(ethyleneimine) (BPEI), and poly(vinylpyrrolidone) (PVP) is also studied. The addition of urea 4 M or 0.001 M BPEI produces a decrease on the amounts of counterions bound to PSS at infinite elution, while the addition of PVP does not produce any change on the diafiltration profiles.     

Production and structural features of a water-soluble polysaccharide from a mutant strain of Agrobacterium sp.

We have developed a mutant strain derived from Agrobacterium sp. ATCC 31750, which produces a water-soluble polysaccharide having potential utility to the food, feed, pharmaceutical and cosmetic industries. A high concentration of product (15 g/L) is obtained by 48 h cultivation of the mutant strain under optimized fermentation conditions. The water-soluble polysaccharide obtained from cultures of the mutant strain beta82 has Glc:Man:Gal in approximate molar ratios of 5.8:6.7:1.0. The molecular weight of the polysaccharide was determined to be approximately 1000 kDa by HPSEC analysis. Linkage analysis contained 3-Glcp, 3-Manp, terminal Glcp and terminal Manp, as well as a small proportion of 3- and 3,4-Galp, and 4,6-Manp residues. Based on analyses using FT-IR and ¹³C NMR spectrometers, most glycosidic bonds joining these sugar residues are of the α-type, and acetyl groups are apparently attached to the polymer chain at random.     

川中地区上三叠统天然气地球化学特征及成藏过程探讨

川中地区上三叠统是一套自生自储的天然气成藏系统，天然气中甲烷含量为88%～96％，重烃（C2＋）含量一般在6％～9％之间，二氧化碳和硫化氢等非烃气体含量普遍较低；天然气干燥系数（C1／C2＋）为5～15，并且随深度增加而呈现升高的趋势；天然气和凝析油轻烃中的甲基环己烷、庚烷和异庚烷值变化表明天然气主要来源于腐殖型母质；天然气甲烷和乙烷碳同位素分别为-39．00‰～-41．00‰和-25．00‰～-27．00‰，具有典型煤成气特征。川中地区上三叠统烃源岩在燕山期持续沉降埋藏过程中，达到高成熟早期阶段；在喜山期，该地区大约2500m地层的剥蚀，使地层温度和压力大幅度降低，故储层中早期低成熟残余天然气的卸压膨胀作用和水溶气的脱溶作用为晚期天然气聚集成藏提供了重要的气源，同时也使气藏中甲烷碳同位素变轻。     

Enantioselective extraction of mandelic acid enantiomers based on chiral ligand exchange

Based on the chiral ligand exchange, the distribution behavior of mandelic acid enantiomers, and the partition of Cu^2 at different pH values were studied in a water/alcohol two-phase system containing Cu^2 and N-ndodecyl-L-proline(A). The influences of the solvent sort, the pH value, the concentrations of Cu^2 and chiral ligand on the partition coefficient(K) and separation factor(α) were discussed. The experimental results show that the A formed has more stable ternary complex with D-mandelic acid enantiomer than with L-mandelic acid enantiomer. There is an important influence of the pH value on K and a. When the pH values are less than 3.5, the formation of binary complexes is thermodynamically unfavourable. K and a become maximum when pH values are above 3.5 and the molar ratio of the chiral ligand to Cu^2 is 2:1.     

Synthesis,Characterization and Luminescent Properties of Complexes of Rare Earth Nitrates with Tris{2-[N-(pyridine-methanoyl)amino]ethyl} amine

Duringthelastdecade ,thedesignandsynthesisoftripodalligandsandtheirmetalcomplexeshaveattractedconsiderableattentionduetotheirpotentialusesaslumi nescentprobesinmedicineandbiochemistry[1～ 7] ,ascatalysts[8] andelectrochemicalmaterials[9] .However ,thecomplexesofrareearthmetalwithtripodalligandshavefewreported[10 ] .Asanextensionofourstudiesoncomplexesofmetalwithtripodalligands ,anewtripodalligand (tris { 2 [N (pyridine methanoyl)amino]ethyl}amine ,L)anditscomplexeswithrareearthnitratesweresyn…     

Rational Design of CYP3A4 Inhibitors: A One-Atom Linker Elongation in Ritonavir-Like Compounds Leads to a Marked Improvement in the Binding Strength

Inhibition of the major human drug-metabolizing cytochrome P450 3A4 (CYP3A4) by pharmaceuticals and other xenobiotics could lead to toxicity, drug–drug interactions and other adverse effects, as well as pharmacoenhancement. Despite serious clinical implications, the structural basis and attributes required for the potent inhibition of CYP3A4 remain to be established. We utilized a rational inhibitor design to investigate the structure–activity relationships in the analogues of ritonavir, the most potent CYP3A4 inhibitor in clinical use. This study elucidated the optimal length of the head-group spacer using eleven (series V) analogues with the R₁/R₂ side-groups as phenyls or R₁–phenyl/R₂–indole/naphthalene in various stereo configurations. Spectral, functional and structural characterization of the inhibitory complexes showed that a one-atom head-group linker elongation, from pyridyl–ethyl to pyridyl–propyl, was beneficial and markedly improved K_s, IC₅₀ and thermostability of CYP3A4. In contrast, a two-atom linker extension led to a multi-fold decrease in the binding and inhibitory strength, possibly due to spatial and/or conformational constraints. The lead compound, 3h, was among the best inhibitors designed so far and overall, the strongest binder (K_s and IC₅₀ of 0.007 and 0.090 µM, respectively). 3h was the fourth structurally simpler inhibitor superior to ritonavir, which further demonstrates the power of our approach.