Design, Synthesis, and Anticancer Activity of Cinnamoylated Barbituric Acid Derivatives.

This work deals with the design and synthesis of 18 barbituric acid derivatives bearing 1,3-dimethylbarbituric acid and cinnamic acid scaffolds to find potent anticancer agents. The target molecules were obtained through Knoevenagel condensation and acylation reaction. The cytotoxicity was assessed by the MTT assay.

Piperlongumine Analogs Promote A549 Cell Apoptosis through Enhancing ROS Generation.

Chemotherapeutic agents, which contain the Michael acceptor, are potent anticancer molecules by promoting intracellular reactive oxygen species (ROS) generation. In this study, we synthesized a panel of (piperlongumine) analogs with chlorine attaching at C2 and an electron-withdrawing/electron-donating group attaching to the aromatic ring. The results displayed that the strong electrophilicity group at the C2-C3 double bond of PL analogs plays an important role in the cytotoxicity whereas the electric effect of substituents, which attached to the aromatic ring, partly contributed to the anticancer activity.

Cocrystallization with syringic acid presents a new opportunity for effectively reducing the hepatotoxicity of isoniazid.

With the aim of surmounting the severe hepatotoxicity induced by antituberculosis drug isoniazid (INH), a novel cocrystal of INH with hepatoprotective nutraceutical syringic acid (SYA), namely INH-SYA, was designed and prepared through cocrystallization strategy, which is an intriguing attempt to reduce the toxic side effects of INH. The study not only provides new thinking for inhibiting toxic side effects of drugs through cocrystallization strategy, but also opens a new pathway for the application of nutraceuticals in the pharmacy. INH and SYA were successfully crystallized into the same crystal lattice through combining volatilization with solvent assisted methods.

Coumarin and 3,4-dihydroquinolinone derivatives: Synthesis, antidepressant activity, and molecular docking studies.

Background: Coumarin and 3,4-dihydroquinolinone nuclei are two heterocyclic rings that are important and widely exploited for the development of bioactive molecules. Here, we designed and synthesized a series of 3,4-dihydroquinolinone and coumarin derivatives (Compounds 8, 9, 11, 14, 15, 18-20, 23, 24 and 28 are new compounds) and studied their antidepressant activities.

Methods: Forced swimming test (FST) and tail suspension test (TST) were used to evaluate the antidepressant activity of the target compounds.

Blockade of Extracellular High-Mobility Group Box 1 Attenuates Systemic Inflammation and Coagulation Abnormalities in Rats with Acute Traumatic Coagulopathy.

BACKGROUND As an extracellularly released mediator, high-mobility group box 1 (HMGB1) initiates sterile inflammation following severe trauma. Serum HMGB1 levels correlate well with acute traumatic coagulopathy (ATC) in trauma patients, which is independently associated with higher mortality. We investigated the involvement of HMGB1 in ATC through blocking extracellular HMGB1.

Evaluation the value of markers for prediction of portal vein thrombosis after devascularization.

Aim: To evaluate the value of D-dimer and P-selectin in cirrhotic portal hypertension (PHT) patients for prediction of portal vein thrombosis (PVT) after devascularization.

Material And Methods: 137 patients with cirrhotic PHT who undergone devascularization from January 2012 to April 2014 were retrospectively reviewed, all of them were divided into two groups (PVT group and non-PVT group) by Doppler ultrasonography (DU) examination. The level of D-dimer and P-selectin was tested during the peri-operative period.

Fast-track protocols in devascularization for cirrhotic portal hypertension.

Introduction/objective: fast-tract surgery (FTS) has been rapidly embraced by surgeons as a mechanism for improving patient care and driving down complications and costs. The aim of this study was to determine if any improvement in outcomes occurred after FTS protocol for selective double portazygous disconnection with preserving vagus (SDPDPV) compared with non-FTS postoperative care.

Methods: patients eligible for SDPDPV in the period January 2012-April 2014 were randomly selected for the FTS group or non-FTS group.

Comparison of effects of devascularization versus shunt on patients with portal hypertension: a meta-analysis.

Background/aims: To systematically evaluate the effectiveness of devascularization and shunt on patients with portal hypertension.

Methodology: Relevant studies compared devascularization and shunt for the treatment of portal hypertension were identified searching the PubMed, Embase, Elsevier, CNKI (China National Knowledge Infrastructure) database and Cochrane Trial Register searches until December 2013. Data of interest for devascularization and shunt including postoperative recurrent bleeding, postoperative hepatic encephalopathy, ascites, operative mortality rate, and long term survival rate were subjected to meta-analysis.

Evaluation of the Value of d-Dimer, P-Selectin, and Platelet Count for Prediction of Portal Vein Thrombosis After Devascularization.

Background/aim: To evaluate the value of d-dimer, P-selectin, and platelet count in patients with cirrhotic portal hypertension (PHT) for prediction of portal vein thrombosis (PVT) after devascularization.

Methods: A total of 137 patients with cirrhotic PHT who undergone devascularization from January 2012 to April 2014 were retrospectively reviewed, all of them were divided into 2 groups (PVT group and non-PVT group) by Doppler ultrasonography (DU) examination. The level of d-dimer, P-selectin, and platelet count was tested during the perioperative period.

Effects of selective double portazygous disconnection and devascularization on hemodynamics of the portal venous system.

Aim: Selective double portazygous disconnection with preserving vagus (SDPDPV) is currently used for the therapy of portal hypertension. Doppler ultrasonography (DU) has been proposed for non-invasive evaluation of splanchnic hemodynamics, but the effect of SDPDPV on portal vein (PV) hemodynamics has not been analyzed with DU. This was the aim of the study.

[Chemical constituents of Trichosanthes kirilowii peels].

Objective: To study the chemical constituents of the peels of Trichosanthes kirilowii.

Methods: Many chromatographic techniques were used including repeated silica column chromatography, polyamide resin and semi-preparative high performance liquid chromatography. According to the physical and chemical properties and spectral analysis, the chemical structures of the compounds were determined.

Rapid pretreatment and determination of bisphenol A in water samples based on vortex-assisted liquid-liquid microextraction followed by high-performance liquid chromatography with fluorescence detection.

A method for the rapid pretreatment and determination of bisphenol A in water samples based on vortex-assisted liquid-liquid microextraction followed by high-performance liquid chromatography with fluorescence detection was proposed in this paper. A simple apparatus consisting of a test tube and a cut-glass dropper was designed and applied to collect the floating extraction drop in liquid-liquid microextraction when low-density organic solvent was used as the extraction solvent. Solidification and melting steps that were tedious but necessary once the low-density organic solvent used as extraction solvent could be avoided by using this apparatus.

Selective double disconnection for cirrhotic portal hypertension.

Background: To evaluate the effect of selective double portazygous disconnection with preserving vagus (SDPDPV) for patients with portal hypertension (PHT) in the authors' hospital.

Methods: Patients (453) with cirrhotic PHT who underwent either SDPDPV or pericardial devascularization with splenectomy (PDS) for variceal bleeding from February 2007 to January 2013 were retrospectively reviewed. The operation-relevant information, change of lavatory examination data, postoperative complications, and clinical outcomes were analyzed.

Electrochemical performance of 8-hydroxy-2'-deoxyguanosine and its detection at poly(3-methylthiophene) modified glassy carbon electrode.

8-Hydroxy-2'-deoxyguanosine (8-OH-dG) has attracted enormous attention in recent years because it has been acknowledged as a typical biomarker of oxidative DNA damage. In this paper, the electrochemical performance of 8-OH-dG at the poly(3-methylthiophene) (P3MT) modified glassy carbon electrode (GCE) was investigated by cyclic voltammetry (CV) and linear sweep voltammetry (LSV). The conducting polymer P3MT can effectively decrease the oxidation peak potential of 8-OH-dG and greatly enhance its peak current.

[Separation and identification of alkaloids in Stephania tetrandra by capillary electrophoresis electrospray-MS/MS].

Aim: To establish a method for separation and identification of alkaloids in Stephania tetrandra S. Moore methanol extracts by using non-aqueous capillary electrophoresis interfaced with electrospray ionization ion trap mass spectrometry.

Methods: The molecular ions or adducts of alkaloids and fragments of specific parent ions were used for the identification.