I-catalyzed synthesis of 3-aminopyrrole with homopropargylic amines and nitrosoarenes.

The synthesis of 3-aminopyrrole using the amination reagent nitrosoarenes and homopropargylic amines catalyzed by I through cyclization and amination has been developed. This protocol features excellent functional group tolerance and mild reaction conditions, yielding 3-aminopyrroles in moderate to good yields without a metal catalyst. This method realizes the construction and amination of the 3-aminopyrroles in which nitrosoarenes serve as the amine source and oxidant.

Mechanical and microstructural properties of recycling granite residual soil reinforced with glass fiber and liquid-modified polyvinyl alcohol polymer.

Glass fiber and liquid-modified polyvinyl alcohol polymer (SH Polymer) are used to reinforce granite residual soil. In this paper, scanning electron microscopy (SEM) tests and drop-weight tests were used to study the microscopic interaction mechanism and impact resistance of granite residual soil specimens reinforced by glass fiber and SH Polymer. Combined with the equivalent confining pressure theory, Mohr-Coulomb intensity lines were used to quantitatively analyze the reinforcement effect of glass fiber.

Cu-Catalyzed Tandem Aerobic Oxidative Cyclization for the Synthesis of 3,3'-Bipyrroles from the Homopropargylic Amines.

A Cu-catalyzed method for the synthesis of 3,3'-bipyrroles from homopropargylic amines through tandem aerobic oxidative cyclization involving the formation of C-C bond has been developed. The features of this reaction are a small number of Cu catalysis and simple starting substrates. Moreover, this procedure exhibits good functional group tolerance and a series of 3,3'-bipyrroles derivatives are obtained in moderate to good yields.

AgNO as the NO Source for the Synthesis of Substituted Pyrazole N-Oxides from N-Propargylamines.

A straightforward method for synthesizing the pyrazole N-oxides from N-propargylamines and AgNO through oxidation/cyclization reaction had been developed. AgNO was used as the NO source for the first time to synthesize pyrazole N-oxides. Various substituted groups on N-propargylamines proceeded smoothly, and the desired products were obtained in good yields.

Protamine zinc insulin combined with sodium selenite improves glycometabolism in the diabetic KKAy mice.

Long-term, high dosage protamine zinc insulin (PZI) treatments produce adverse reactions. The trace element selenium (Se) is a candidate for the prevention of diabetes due to anti-oxidative stress activity and the regulation of glycometabolism. In this study, we aimed to investigate the anti-diabetic effects of a combination of PZI and Se on type 2 diabetes.

Effect of passive pile on 3D ground deformation and on active pile response.

Using a series of model tests, this study investigated the effect of a passive pile on 3D ground deformation around a laterally loaded pile and on that laterally loaded pile's response in sand. The active pile head was subjected to lateral loads, and the passive pile was arranged in front of the active pile. In the model tests, the distance between the two pile centers was set to zero (i.

Liraglutide Exerts Antidiabetic Effect via PTP1B and PI3K/Akt2 Signaling Pathway in Skeletal Muscle of KKAy Mice.

Background. Liraglutide (a glucagon-like peptide 1 analog) was used for the treatment of type 2 diabetes (T2DM) which could produce glucose-dependent insulin secretion. Aim.

Liraglutide ameliorates glycometabolism and insulin resistance through the upregulation of GLUT4 in diabetic KKAy mice.

Liraglutide, a long-lasting glucagon‑like peptide‑1 analogue, has been used for the treatment of patients with type 2 diabetes mellitus since 2009. In this study, we investigated the anti-diabetic effects and mechanisms of action of liraglutide in a spontaneous diabetic animal model, using KK/Upj-Ay/J (KKAy) mice. The KKAy mice were divided into 2 groups, the liraglutide group (mice were treated with 250 µg/kg/day liraglutide) and the model group (treated with an equivalent amount of normal saline).

Optimizing the parameters of vagus nerve stimulation by uniform design in rats with acute myocardial infarction.

Vagus nerve stimulation (VNS) has been shown to improve left ventricular function and survival in rats with acute myocardial infarction (AMI), and this maneuver has also been adopted clinically for the treatment of patients with chronic heart failure (CHF). Recent in vitro and in vivo studies have suggested that VNS can modulate the level of pro-inflammatory factors. Despite the beneficial effects of VNS, the stimulation parameters for obtaining favorable outcomes appear highly variable.

[Effect of combination of insulin and selenium on insulin signal transduction in cardiac muscle of STZ-induced diabetic rats].

This study is to investigate the effect of low doses of insulin (1 u x kg(-1)) and selenium (180 microg x kg(-1)) in combination on general physiological parameters and insulin signal molecules in cardiac muscle of STZ-induced diabetic rats. The levels of blood glucose were estimated using One Touch SureStep Blood Glucose meter. HbA1c levels were estimated using microcolumn assay.

Transfusion of autologous late-outgrowth endothelial cells reduces arterial neointima formation after injury.

Aims: Late-outgrowth endothelial cells (OECs) exist in blood and other organs. We aimed to explore whether and how OECs participate in re-endothelialization and prevent vascular neointima formation after injury.

Methods And Results: Rabbit bone marrow OECs were cultured for 4 weeks to increase their numbers.

Lipid soluble smoke particles upregulate endothelin receptors in rat basilar artery.

The present study examines the effect of dimethylsulphoxide-soluble particles (DSP) from cigarette smoke on endothelin (ET) receptors in the basilar artery. The contractile responses to ET-1 (ET(A) and ET(B) receptors agonist) and sarafotoxin 6c (ET(B) receptor agonist) were studied using a sensitive myograph. The mRNA levels of ET receptors were determined with real-time PCR, while the protein level was evaluated by immunohistochemistry.

Experimental diabetes mellitus down-regulates large-conductance Ca2+-activated K+ channels in cerebral artery smooth muscle and alters functional conductance.

Cerebral vascular dysfunction and associated vascular complications often develop over time in type-2 diabetes, but the underlying mechanisms are not wholly understood. The aim of the present study was to investigate whether large-conductance Ca(2+)-activated K(+) (BKCa) channels in cerebral artery smooth muscle cells (CASMCs) were impaired in experimental model of type-2 diabetes, and the changes could account for cerebral vascular complication in type-2 diabetes. Sprague-Dawley rats were fed with high fat and glucose diet for 8 weeks and then injected with streptozotocin (STZ/30 mg/kg i.

The influence of chirality, physicochemical properties, and permeation enhancers on the transdermal permeation of amlodipine across rat skin.

Purpose: This study was aimed at investigating the possible relationship between the physical properties and the permeation of S-amlodipine and RS-amlodipine and studying the possible enantioselectivity of permeation of amlodipine in the presence and absence of enhancers, such as terpene enhancers and ethanol.

Method: The solubility of S-amlodipine and RS-amlodipine was measured using the shake-flask method. The thermodynamic properties were investigated by differential scanning calorimetry (DSC).

[A method for improving the accuracy and sensitivity of cell membrane chromatography].

Objective: To improve the accuracy and sensitivity of cell membrane chromatography (CMC) and evaluate the feasibility of CMC in the study of subtype receptors.

Methods: Plasmids were used to transfer alpha(1B)-AR cDNA into human embryonic kidney 293 (HEK293) cell lines to obtain cell lines stably overexpressing the subtype receptors. HEK293 alpha(1B) cell membrane stationary phase (CMSP) was prepared by immobilizing the cell membrane on silica.

The effect of insulin in combination with selenium on blood glucose and GLUT4 expression in the cardiac muscle of streptozotocin-induced diabetic rats.

We evaluated the effect of a combination of low doses of insulin (1 U/kg/day) and selenium (180 microg/kg/day) on general physiological parameters and the level of glucose transporter (GLUT4) in the cardiac muscle of streptozotocin-induced diabetic rats. Diabetic rats were treated with insulin, selenium and a combination of insulin and selenium for 4 weeks. The levels of blood glucose and hemoglobin A1c were estimated; the level of the GLUT4 in the cardiac muscle was examined by immunoblotting and immunohistochemistry.

Influence of sodium dodecyl sulfate on swelling, erosion and release behavior of HPMC matrix tablets containing a poorly water-soluble drug.

The effect of sodium dodecyl sulfate (SDS) on the swelling, erosion and release behavior of HPMC matrix tablets was examined. Swelling and erosion of HPMC matrix tablets were determined by measuring the wet and subsequent dry weights of matrices. The rate of uptake of the dissolution medium by the matrix was quantified using a square root relationship whilst the erosion of the polymer was described using the cube root law.

Frontal analysis of cell-membrane chromatography for determination of drug-alpha(1D) adrenergic receptor affinity.

The aim of the present study was to determine drug-alpha(1D) adrenergic receptor (AR) affinity by frontal analysis of cell-membrane chromatography (CMC). The cell-membrane stationary phase (CMSP) was prepared by immobilizing rat aorta cell membranes on porous silica, and the resulting CMSP was used to determine drug binding affinity to alpha(1D)-AR by frontal analysis. The CMSP of rat aorta was stable and reproducible.

Characterization of calcium signaling pathways in human preadipocytes.

Intracellular free Ca2+ (Ca(i)2+) is an important regulator of many cellular activities; however, Ca2+ signaling is not well studied in human preadipocytes. The purpose of the present study was to characterize Ca2+ signal pathways using a confocal scanning technique and RT-PCR. It was found that spontaneous Ca(i)2+ oscillations were observed in 12.

Characterization of ion channels in human preadipocytes.

Ion channels participate in regulation of cell proliferation. However, though preadipocyte (the progenitor of fat cell) is a type of highly proliferating cells, ion channel expression and their role in proliferation is not understood in human preadipocytes. The present study was designed to characterize ion channels using whole-cell patch clamp technique, RT-PCR, and Western blotting.

[Sedative, hypnotic and antiseizure effects of compound gardenia oil and jujube seed oil in mice].

Objective: To study the sedative, hypnotic and antiseizure effects of the compound preparation of gardenia oil and jujube seed oil in mice and investigate the interaction of the two drugs in this preparation.

Methods: The compound preparation was administered intragastrically in mice, whose spontaneous activity was observed along with their tolerance of the preparation after long-term administration. The hypnotic effect of the compound was assessed by investigating the changes in the pentobarbital sodium-induced sleeping.

[Pentoxifylline promotes learning and memory function of aging rats and mice with induced memory impairment].

Objective: To investigate the effects of pentoxifylline on rats and mice with learning and memory dysfunctions.

Methods: Morris water maze test was used to observe the effects of pentoxifylline on learning and memory of naturally aging rats, and jumping stand test was performed to examine its effects in promoting the learning and memory functions in mice with scopolamine- and ethanol-induced memory dysfunctions.

Results: In aging rats, pentoxifylline at high, moderate and low doses all significantly reduced the latency of platform finding in the place navigation test (P<0.

Tanshinone IIA downregulates the CD40 expression and decreases MMP-2 activity on atherosclerosis induced by high fatty diet in rabbit.

Tanshinone IIA (Tan IIA) is a member of the major lipophilic components abstracted from the root of Salvia miltiorrhiza Bunge and has the capacity of anti-atherosclerosis. To investigate the potential mechanism, we established an animal model by giving high fatty diet to rabbits and Tan IIA was given in different dose. Then, superoxide dismutase (SOD) activity and the malondialdehyde (MDA) level in serum were detected using spectrophotometry; cluster of differentiation 40 (CD40) expression of cellular membrane fraction of aortas and matrix metalloproteinase-2 (MMP-2) activity of total protein extract of aortas were detected by Western Blotting and Zymography, respectively.

Tanshinone IIA inhibits atherosclerotic plaque formation by down-regulating MMP-2 and MMP-9 expression in rabbits fed a high-fat diet.

Tanshinone IIA (Tan IIA) is one of the major lipophilic components of Salvia miltiorrhiza Bunge (SM) and has an anti-atherosclerotic effect. To investigate the potential mechanism of this effect, we established an atherosclerotic animal model by feeding rabbits a high-fat diet, and Tan IIA was given at different doses. Intimal area of the aorta was measured by image analysis, serum levels of vascular adhesion molecule-1 (VCAM-1) and interleukin (IL-1beta) were measured by ELISA, while matrix metalloproteinase-2 and-9 (MMP-2, MMP-9) expression and their activities in atherosclerotic lesions were assessed by Western blotting and zymography respectively.