Data_Sheet_1_Morin Protects Channel Catfish From Aeromonas hydrophila Infection by Blocking Aerolysin Activity.PDF

Aeromonas hydrophila (A. hydrophila) is an opportunistic bacterial pathogen widely distributed in the environments, particular aquatic environment. The pathogen can cause a range of infections in both human and animals including fishes. However, the application of antibiotics in treatment of A. hydrophila infections leads to the emergence of resistant strains. Consequently, new approaches need to be developed in fighting this pathogen. Aerolysin, the chief virulence factor produced by pathogenic A. hydrophila strains has been employed as target identifying new drugs. In our present study, we found that morin, a flavonoid without anti-bacterial activity isolated from traditional Chinese medicine, could directly inhibit the hemolytic activity of aerolysin. To determine the binding sites and the action of mechanism of morin against AerA, several assays were performed. Ser36, Pro347, and Arg356 were identified as the main binding sites affecting the conformation of AerA and resulted in block of the heptameric formation. Moreover, morin could protect Vero cells from cell injury mediated by aerolysin. In vivo study showed that morin could provide a protection to channel catfish against A. hydrophila infection. These results demonstrated that morin could be developed as a promising candidate for the treatment of A. hydrophila infections by decreasing the pathogenesis of A. hydrophila.</p

Residue depletion and risk assessment of niclosamide in three species of freshwater fish

The residue depletion of niclosamide (NIC) in freshwater fish including blunt snout bream (Megalobrama amblycephala), yellow catfish (Pelteobagrus fulvidraco) and channel catfish (Ietalurus Punetaus) were investigated under laboratory conditions. NIC concentrations in fish were determined by Liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) with heated electrospray ionisation. The mean recoveries were in the range of 75.5–98.5%, with relative standard deviations ranging from 1.0 to 9.4%. The depletion results showed that the long half-life of NIC was 8.8–22.1 days. Risk assessment of NIC residue in edible tissues (muscle and skin) of the three species of freshwater fish was performed using the quotient (RQ), because of no maximum residue limit (MRL) has been set for NIC in fish. The results demonstrated that the RQ values were all significantly lower than 1. Therefore, the effect of NIC residues in the three species of freshwater fish at the immersion concentration was negligible to Chinese people.</p

Synthesis and Pharmacokinetic Study of Three Gemfibrozil Salts: An Exploration of the Structure–Property Relationship

Three salts, [H₃N­(CH₂)₂NH₃)]­[gem]₂ (<b>1</b>), [H₃N­(CH₂)₃NH₃)]­[gem]₂·2H₂O (<b>2</b>), and [H₃N­(CH₂)₄NH₃)]­[gem]₂­·2H₂O (<b>3</b>) of the minimally soluble drug gmfibrozil (Hgem), used for the treatment of hyperlipidemia have been synthesized by using a series of diamine with different carbon chain lengths and characterized by single crystal/powder X-ray diffraction, Fourier transform infrared spectroscopy, and ¹H nuclear magnetic resonance. In the three salts, two protons of two gmfibrozil molecules transfer to one diamine, and the resulting organic diammonium cation and gmfibrozil anion are assembled by hydrogen bond interactions into a two-dimensional layer. Although the apparent solubility of salts <b>1</b>–<b>3</b> is obviously improved compared to that of the original gemfibrozil, pharmacokinetic studies in rats indicate the enhancement of absorption is limited with the relative bioavailability of 104% for <b>1</b>, 154% for <b>2</b>, and 108% for <b>3</b>. It is notable that the rapid dissolution behavior of salt <b>1</b>–<b>3</b> leads to the increase of maximal plasma concentration (<i>C</i>_max) and the dramatic shortening of the time required to reach the <i>C</i>_max. The investigation of the structure–property relationship shows that there is little correlation of solubility with the carbon chain length of cation which is different from previous observations, and we speculate that both electrostatic attraction and hydrogen bond interaction contribute to the solubility order (<b>2</b> > <b>1</b> > <b>3</b>)

Electrospun-Aligned Gd-Doped In₂O₃ Nanofiber Field-Effect Transistors for Artificial DNA Detection

In view of the time-consuming and laborious problem of detecting biological genetic information by conventional methods, it is important to study high-performance deoxyribonucleic acid (DNA) biosensors. In this report, an aligned Gd-doped In2O3 nanofiber favoring carrier transport was prepared by electrospinning. When the Gd doping concentration is 0.5 mol %, the aligned In2O3 nanofiber field-effect transistors (FETs) exhibit an excellent mobility (μ = 8.7 cm2/Vs), suitable threshold voltage (VTH = 0.3 V), large on/off current ratio (Ion/Ioff = 4.1 × 107), and outstanding stability. The FET biosensor based on one-dimensional nanofibers has the advantages of simple structure, fast response, high sensitivity, and extraordinary potential for biosensor applications, where the current variation is quite pronounced at concentrations as low as 10 nM DNA immobilized in the active layer of the aligned In1.995Gd0.005O3 nanofiber FET, and this phenomenon becomes more pronounced as the concentration of immobilized DNA increases. The sensing mechanism of the current variation is mainly attributed to the oxidation of guanine nucleotides in the DNA molecular chain. The aligned Gd-doped In2O3 nanofiber FETs exhibit high sensitivity to DNA at room temperature, which provides a solution for the development of novel DNA biosensors

Sodium Salts and Solvate of Rebamipide: Synthesis, Structure, and Pharmacokinetic Study

Two sodium salts (Na­(CH₃CH₂OH) (HReb) (<b>1</b>) and Na₂(H₂O)₄(Reb) (<b>2</b>)), one methanol solvate (H₂Reb·CH₃OH (<b>3</b>)), and one methyl ester (<b>4</b>) of the minimally soluble drug, rebamipide (H₂Reb), used for the treatment of gastric ulcers and gastritis have been synthesized. For the first time the structure of rebamipide has been determined by single crystal X-ray diffraction. Although salts <b>1</b> and <b>2</b> were prepared under the similar conditions, their structures are different. In <b>1</b>, rebamipide loses the proton of the carboxyl group to interact with the sodium ion, but in <b>2</b> the drug molecule converts to its prototropic tautomer and then simultaneously loses the protons of the carboxyl and hydroxyl groups to form salt. Control experiments show that reaction temperature is the key factor influencing the formation of salts. Although all methanol was used in the synthesis of <b>3</b> and <b>4</b>, in <b>3</b> methanol acts as solvent involved in the lattice, while in <b>4</b> it reacts with rebamipide to form ester. By analyzing the mass spectra of the reaction solution, we speculate that the crystallization of <b>3</b> and <b>4</b> is controlled by the product’s solubility. Dissolution studies indicate that both the maximum solubility and dissolution rate of <b>1</b>–<b>4</b> in simulated succus gastricus are improved. Furthermore, pharmacokinetic behavior of compounds <b>1</b>–<b>4</b> was investigated in rats and the results indicate that the bioavailability of <b>1</b>, <b>3</b>, and <b>4</b> upon oral administration is enhanced compared to that of API

Structural Diversity of Diosgenin Hydrates: Effect of Initial Concentration, Water Volume Fraction, and Solvent on Crystallization

Four hemihydrates (HH-I, HH-II, HH-III, and HH-IV) and two monohydrates (MH-I, MH-II) of diosgenin, a steroid sapogenin, have been prepared. Hydrates HH-I, HH-III, HH-IV, MH-I, and MH-II have been thoroughly characterized by single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. Although in these cases diosgenin has a similar conformation, hydrogen bonding interactions connect diosgenin and the lattice water molecule into different supermolecular structures. More importantly, three controlling factors, including initial concentration, water volume fraction, and solvent, have been investigated in the crystallization of diosgenin hydrates. The control experiments in ethanol display that as the initial concentration increases, HH-III, HH-I, and HH-II appear in order, and with the increase of water content, HH-I, HH-III, MH-I, and MH-II are obtained correspondingly. When acetone is used as solvent, HH-IV was synthesized. Moreover, we observed that stick-like crystals of HH-III gradually transform to plate-like ones of MH-I in solution at ambient conditions. This transformation is prevented by lowering temperature and is accelerated by adding water

In-hospital clinical outcomes after upper gastrointestinal surgery: Data from an international observational study

AIMS: Previous research suggests that patients undergoing upper gastrointestinal surgery are at high risk of poor postoperative outcomes. The aim of our study was to describe patient outcomes after elective upper gastrointestinal surgery at a global level. METHODS: Prospective analysis of data collected during an international seven-day cohort study of 474 hospitals in 27 countries. Patients undergoing elective upper gastrointestinal surgery were recruited. Outcome measures were in-hospital complications and mortality at 30-days. Results are presented as n(%) and odds ratios with 95% confidence intervals. RESULTS: 2139 patients were included, of whom 498 (23.2%) developed one or more postoperative complications, with 30 deaths (1.4%). Patients with complications had longer median hospital stay 11 (6-18) days vs. 5 (2-10) days. Infectious complications were most frequent, affecting 368 (17.2%) patients. 328 (15.3%) patients were admitted to critical care postoperatively, of whom 161 (49.1%) developed a complication with 14 deaths (4.3%). In a multivariable logistic regression model we identified age (OR 1.02 [1.01-1.03]), American Society of Anesthesiologists physical status III (OR 2.12 [1.44-3.16]) and IV (OR 3.23 [1.72-6.09]), surgery for cancer (OR 1.63 [1.27-2.11]), open procedure (OR 1.40 [1.10-1.78]), intermediate surgery (OR 1.75 [1.12-2.81]) and major surgery (OR 2.65 [1.72-4.23]) as independent risk factors for postoperative complications. Patients undergoing major surgery for upper gastrointestinal cancer experienced twice the rate of complications compared to those undergoing other procedures (224/578 patients [38.8%] versus 274/1561 patients [17.6%]). CONCLUSIONS: Complications and death are common after upper gastrointestinal surgery. Patients undergoing major surgery for cancer are at greatest risk