Resveratrol, a red wine constituent, blocks the antimitogenic effects of estradiol on human female coronary artery smooth muscle cells.

Context: Antimitogenic effects of estradiol on vascular smooth muscle cells (VSMCs) may be cardioprotective, and these effects are mediated by estrogen receptor-alpha-dependent and -independent mechanisms, with the latter involving the conversion of estradiol to 2-hydroxyestradiol/2-methoxyestradiol by CYP450. Because resveratrol inhibits CYP450 and is an estrogen-receptor-alpha antagonist, resveratrol may abrogate the antimitogenic effects of estradiol.

Objective: The objective of the study was to examine the interaction of pharmacologically relevant concentrations of resveratrol with estradiol, 2-hydroxyestradiol, and 2-methoxyestradiol in human female coronary artery VSMCs.

Extracellular 2,3-cyclic adenosine monophosphate is a potent inhibitor of preglomerular vascular smooth muscle cell and mesangial cell growth [corrected].

Recently we discovered that intact kidneys release into the extracellular compartment 2',3'-cAMP (a positional isomer of 3',5'-cAMP with unknown pharmacology) and metabolize 2',3'-cAMP to 2'-AMP, 3'-AMP, and adenosine. Because adenosine inhibits growth of vascular smooth muscle cells and mesangial cells, we tested the hypothesis that extracellular 2',3'-cAMP attenuates growth of preglomerular vascular smooth muscle and mesangial cells via production of adenosine. For comparison, all of the experiments were performed with both 2',3'-cAMP and 3',5'-cAMP.

Extracellular 3',5'-cAMP-adenosine pathway inhibits glomerular mesangial cell growth.

Abnormal growth of glomerular mesangial cells (GMCs) contributes to the pathophysiology of many types of nephropathy. Because adenosine is an autocrine/paracrine factor that potentially could regulate GMC proliferation and because the extracellular 3',5'-cAMP-adenosine pathway (i.e.

Simultaneous RP-HPLC Estimation of Cefpodoxime Proxetil and Clavulanic Acid in Tablets.

A new, simple, precise, rapid and accurate RP-HPLC method has been developed for the simultaneous estimation of cefpodoxime proxetil and clavulanic acid from pharmaceutical dosage forms. The method was carried out on a Zorbax Eclipse XDB 5 mu C 18 (150x4.6 mm) column with a mobile phase consisting of acetonitrile:50 mM potassium dihydrogen phosphate buffer (pH 3.

Enantioselective organocatalytic alpha-sulfenylation of substituted diketopiperazines.

The asymmetric organocatalytic alpha-sulfenylation of substituted piperazine-2,5-diones is reported, with cinchona alkaloids as chiral Lewis bases and electrophilic sulfur transfer reagents. Catalyst loadings, the type of sulfur transfer reagent, temperature and solvent were investigated in order to optimize the reaction conditions. The effects of ring substitution and the type of catalyst on the yield and enantioselectivity of the reaction are reported.

Efficient Organocatalytic alpha-Sulfenylation of Substituted Piperazine-2,5-diones.

Organocatalytic alpha-sulfenylation of substituted piperazine-2,5-diones is reported through the use of cinchona alkaloids as Lewis bases and electrophilic sulfur transfer reagents. 1-Phenylsulfanyl[1,2,4]triazole, a novel sulfur transfer reagent, gave excellent product yields with a number of substituted piperazine-2,5-diones under mild conditions. Catalyst loading, stoichiometry of sulfur electrophile, temperature and solvent were optimized to achieve high product yields.

Crossed four-bar mechanism for improved prosthetic grasp.

Passive linkages were developed to improve grasp functionality and minimize a prosthetic terminal device's number of user-controlled inputs. The linkages act to stabilize grasped objects and substitute for the palp of normal anatomical fingers. The Southampton Hand Assessment Procedure was used to compare the normal anatomical hand, this prototype, and a commercially available (Hosmer) hook.

Adenosine A1 receptor activation as a brake on the microglial response after experimental traumatic brain injury in mice.

We reported that adenosine A(1) receptor (A(1)AR) knockout (KO) mice develop lethal status epilepticus after experimental traumatic brain injury (TBI), which is not seen in wild-type (WT) mice. Studies in epilepsy, multiple sclerosis, and neuro-oncology suggest enhanced neuro-inflammation and/or neuronal death in A(1)AR KO. We hypothesized that A(1)AR deficiency exacerbates the microglial response and neuronal damage after TBI.

Development and characterization of colon specific drug delivery system bearing 5-ASA and Camylofine dihydrochloride for the treatment of ulcerative colitis.

The treatment of ulcerative colitis (inflammatory bowel disease, IBD) has been achieved by using colon specific drug delivery system bearing 5-ASA and Camylofine dihydrochloride. Chitosan microspheres were prepared separately for both the drugs using emulsion method followed by enteric coating with EudragitS-100. The in vitro drug release was investigated in different simulated GIT medium.

Inhibition of hypoxia inducible factor 1-transcription coactivator interaction by a hydrogen bond surrogate alpha-helix.

Designed ligands that inhibit hypoxia-inducible gene expression could offer new tools for genomic research and, potentially, drug discovery efforts for the treatment of neovascularization in cancers. We report a stabilized alpha-helix designed to target the binding interface between the C-terminal transactivation domain (C-TAD) of hypoxia-inducible factor 1alpha (HIF-1alpha) and cysteine-histidine rich region (CH1) of transcriptional coactivator CBP/p300. The synthetic helix disrupts the structure and function of this complex, resulting in a rapid downregulation of two hypoxia-inducible genes (VEGF and GLUT1) in cell culture.

Direct inhibition of hypoxia-inducible transcription factor complex with designed dimeric epidithiodiketopiperazine.

Selective blockade of hypoxia-inducible gene expression by designed small molecules would prove valuable in suppressing tumor angiogenesis, metastasis and altered energy metabolism. We report the design, synthesis, and biological evaluation of a dimeric epidithiodiketopiperazine (ETP) small molecule transcriptional antagonist targeting the interaction of the p300/CBP coactivator with the transcription factor HIF-1alpha. Our results indicate that disrupting this interaction results in rapid downregulation of hypoxia-inducible genes critical for cancer progression.

A comparison of two methods for the segmentation of masses in the digital mammograms.

An accurate and standardized technique for breast tumor segmentation is a critical step for monitoring and quantifying breast cancer. The fully automated tumor segmentation in mammograms presents many challenges related to characteristics of an image. In this paper, a comparison of two different semi-automated methods, viz.

Stem cell-like human endothelial progenitors show enhanced colony-forming capacity after brief sevoflurane exposure: preconditioning of angiogenic cells by volatile anesthetics.

Background: Endothelial progenitor cells play a pivotal role in tissue repair, and thus are used for cell replacement therapies in "regenerative medicine." We tested whether the anesthetic sevoflurane would modulate growth or mobilization of these angiogenic cells.

Methods: In an in vitro model, mononuclear cells isolated from peripheral blood of healthy donors were preconditioned with sevoflurane (3 times 30 min at 2 vol% interspersed by 30 min of air).

Potential vascular actions of 2-methoxyestradiol.

2-Methoxyestradiol (2-ME) is a biologically active metabolite of 17beta-estradiol that appears to inhibit key processes associated with cell replication in vitro. The molecule has been suggested to have potent growth-inhibitory effects on proliferating cells, including smooth muscle cells and endothelial cells, and may be antiangiogenic. Because of these potential roles for 2-ME, its lack of cytotoxicity and low estrogenic activity, we hypothesize that 2-ME could be a valuable therapeutic molecule for prevention and treatment of cardiovascular diseases.

Kinematic comparison of myoelectric and body powered prostheses while performing common activities.

This study examined the kinematic differences of a bilateral transradial amputee using myoelectric and body-powered prostheses during select activities of daily living. First in harness suspended, body powered then self-suspended externally powered prostheses, the subject's shoulder and elbow joint movements were calculated and compared while completing an elbow range of motion test, simulated drinking from an empty cup, and opening a door. In this case, body-powered prostheses allowed for greater range of elbow flexion but required more shoulder flexion to complete the tasks that required continuous grasp.

Ketorolac tromethamine transdermal gel: development, in vitro and in vivo evaluation.

The authors developed and evaluated a transdermal gel formulation of ketorolac tromethamine (ketorolac) for the treatment of nociceptive somatic pain. The formulation was optimized for skin permeation enhancers, pH of the system, and dosage strength using in vitro and in vivo techniques. Of the various permeation enhancers evaluated, dimethyl sulfoxide (DMSO) and oleic acid were found to significantly increase skin permeation flux of ketorolac.

Design and implementation of visual-haptic assistive control system for virtual rehabilitation exercise and teleoperation manipulation.

This paper describes the design and implementation of a control system that integrates visual and haptic information to give assistive force feedback through a haptic controller (Omni Phantom) to the user. A sensor-based assistive function and velocity scaling program provides force feedback that helps the user complete trajectory following exercises for rehabilitation purposes. This system also incorporates a PUMA robot for teleoperation, which implements a camera and a laser range finder, controlled in real time by a PC, were implemented into the system to help the user to define the intended path to the selected target.

Interaction of APC/C-E3 ligase with Swi6/HP1 and Clr4/Suv39 in heterochromatin assembly in fission yeast.

Heterochromatin assembly in fission yeast is initiated by binding of Swi6/HP1 to the Lys-9-dimethylated H3 followed by spreading via cooperative recruitment of Swi6/HP1. Recruitment of Cohesin by Swi6/HP1 further stabilizes the heterochromatin structure and integrity. Subsequently, polyubiquitylation of Cut2 by anaphase-promoting complex-cyclosome (APC/C)-ubiquitin-protein isopeptide ligase (E3 ligase) followed by degradation of Cut2 releases Cut1, which cleaves the Rad21 subunit of Cohesin, facilitating sister chromatid separation during mitosis.

Excimer laser irradiation effects on soft magnetic properties of sputtered iron nitride thin films.

Effect of pulse laser irradiation on soft magnetic properties of reactively sputtered iron nitride thin film has been studied. The as-deposited films exhibit large coercivity in the range 54 Oe to 148 Oe. Laser irradiation results in remarkable decrease in the coercivity of the films, the minimum value achieved being 8 Oe.

Differential pulse polarographic determination of trace amounts of vanadium and molybdenum in various standard alloys and environmental samples after preconcentration of their morpholine-4-carbodithioates on microcrystalline naphthalene or morpholine-4-dithiocarbamate cetyltrimethyl-ammonium bromide-naphthalene adsorbent.

A highly selective, sensitive, and fairly rapid and economical differential pulse polarographic (DPP) method has been reported for the determination of trace amounts of vanadium and molybdenum in standard alloys and various environmental samples. The morpholine-4-carbodithioates of these metals were retained (>99% recovery) quantitatively on microcrystalline naphthalene in the pH range 4.5-6.

Beneficial effects of fluorescent pseudomonads on seed germination, growth promotion, and suppression of charcoal rot in groundnut (Arachis hypogea L.).

Rhizobacteria are used as inoculants to enhance crop yield and for biological control of fungal pathogens. Fluorescent pseudomonads isolated from the rhizosphere of groundnut showed suppression of the phytopathogen Macrophomina phaseolina that causes charcoal rot of groundnut, an economically important agroproduct. Two strains of fluorescent pseudomonads, designated as PS1 and PS2, were selected as a result of in vitro antifungal activity.