Design and synthesis of novel 5-phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivatives as potential antitumor agents.

A series of novel 5-phenyl-N-piperidine ethanone-4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassays demonstrated that compounds 4d, 4f, 7a and 7b occupied high antiproliferative activities against SGC-7901, MGC-803 and Bcap-37 cell lines. By a modified TRAP assay, some titled compounds were tested against telomerase, and compound 7b showed the most potent inhibitory activity with IC(50) value at 2.

Leonurine protects against tumor necrosis factor-α-mediated inflammation in human umbilical vein endothelial cells.

Objective: Leonurine, a bioactive alkaloid compound in Herba leonuri, has various pharmacological activities, including antioxidant and anti-apoptotic capacities. This study was conducted to test the hypothesis that leonurine was able to attenuate tumor necrosis factor (TNF)-α-induced human umbilical vein endothelial cells (HUVEC) activation and the underlying molecular mechanisms.

Methods: Mitogen-activated protein kinases (MAPK) activation, nuclear factor-κB (NF-κB) activation, and inflammatory mediators expression were detected by Western blot or enzyme-liked immunosorbent assay, intracellular reactive oxygen species (ROS) and NF-κB p65 translocation were measured by immunofluorescence, endothelial cell-monocyte interaction was detected by microscope.

Novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxoethoxy)-2-substituted-phenyl-4H-chromen-4-one: synthesis and anticancer activity.

Ten novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxo-ethoxy)-2-substituted-phenyl-4H-chromen-4-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 6af exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 4.

Classification accuracy and cut point selection.

In biomedical research and practice, quantitative tests or biomarkers are often used for diagnostic or screening purposes, with a cut point established on the quantitative measurement to aid binary classification. This paper introduces an alternative to the traditional methods based on the Youden index and the closest-to-(0, 1) criterion for threshold selection. A concordance probability evaluating the classification accuracy of a dichotomized measure is defined as an objective function of the possible cut point.

Manganese exposure from drinking water and children's academic achievement.

Drinking water manganese (WMn) is a potential threat to children's health due to its associations with a wide range of outcomes including cognitive, behavioral and neuropsychological effects. Although adverse effects of Mn on cognitive function of the children indicate possible impact on their academic achievement little evidence on this issue is available. Moreover, little is known regarding potential interactions between exposure to Mn and other metals, especially water arsenic (WAs).

Prostatic acid phosphatase is expressed in human prostate cancer bone metastases and promotes osteoblast differentiation.

Prostate cancer (PCa) bone metastases are a major cause of morbidity and mortality. There are no effective therapies for PCa bone metastases that prolong survival. Prostatic acid phosphatase (PAP) is a secretory protein expressed by PCa cells.

Torrefaction of sawdust in a fluidized bed reactor.

In the present work, stable fluidization of sawdust was achieved in a bench fluidized bed with an inclined orifice distributor without inert bed materials. A solids circulation pattern was established in the bed without the presence of slugging and channeling. The effects of treatment severity and weight loss on the solid product properties were identified.

[Association of methylenetetrahydrofolate reductase A1298C polymorphisms with non-syndromic cleft lip with or without cleft palate].

Objective: To investigate the association between a polymorphism of methylenetetrahydrofolate reductase with Non-syndromic cleft lip with or without cleft palate (NSCL/P) in Chinese population.

Methods: The polymerase chain reaction (PCR)-based restriction fragment length polymorphism (RFLP) technique was used to detect a single nucleotide polymorphism (SNP), rs1801131, at the methylenetetrahydrofolate reductase (MTHFR) gene in both 158 patients with NSCL/P and 192 healthy individuals. The Hardy-Weinberg equilibrium for genotypic distributions was estimated by the goodness-of-fit test.

Nandrolone reduces activation of Notch signaling in denervated muscle associated with increased Numb expression.

Nandrolone, an anabolic steroid, slows denervation-atrophy in rat muscle. The molecular mechanisms responsible for this effect are not well understood. Androgens and anabolic steroids activate Notch signaling in animal models of aging and thereby mitigate sarcopenia.

Palladium-catalyzed desulfitative C-H arylation of azoles with sodium sulfinates.

A palladium-catalyzed desulfitative C-H arylation of azoles with sodium sulfinates using Cu(OAc)(2)·H(2)O as oxidant has been discovered. The reaction proceeded well for a range of different substrates under oxidative conditions. A series of aryl-substituted azoles have been synthesized in moderate to good yields.

Maternal prenatal urinary phthalate metabolite concentrations and child mental, psychomotor, and behavioral development at 3 years of age.

Background: Research suggests that prenatal phthalate exposures affect child executive function and behavior.

Objective: We evaluated associations between phthalate metabolite concentrations in maternal prenatal urine and mental, motor, and behavioral development in children at 3 years of age.

Methods: Mono-n-butyl phthalate (MnBP), monobenzyl phthalate (MBzP), monoisobutyl phthalate (MiBP), and four di-2-ethylhexyl phthalate metabolites were measured in a spot urine sample collected from 319 women during the third trimester.

Novel anti-diabetic effect of SCM-198 via inhibiting the hepatic NF-κB pathway in db/db mice.

There are reports of early evidence that suggest the involvement of chronic low-grade inflammation in the pathogenesis of Type 2 diabetes. Thus, substances that have effects in reducing inflammation could be potential drugs for Type 2 diabetes. Leonurine (4-guanidino-n-butyl syringate; SCM-198) is an alkaloid in HL (Herba leonuri), which was reported to possess anti-inflammatory properties.

Arsenic exposure and motor function among children in Bangladesh.

Background: Several reports indicate that drinking water arsenic (WAs) and manganese (WMn) are associated with children's intellectual function. Very little is known, however, about possible associations with other neurologic outcomes such as motor function.

Methods: We investigated the associations of WAs and WMn with motor function in 304 children in Bangladesh, 8-11 years of age.

Ecstasy use and associated risk factors among Asian-American youth: findings from a national survey.

This study examined ecstasy use and associated risk and protective factors among Asian American youth. Data from 996 Asian American adolescents and 1,108 Asian American young adults were used. Ecstasy use was relatively common among Asian American youth.

Functional impairment in elderly patients with mild cognitive impairment and mild Alzheimer disease.

Context: The original mild cognitive impairment (MCI) criteria exclude substantial functional deficits, but recent reports suggest otherwise. Identifying the extent, severity, type, and correlates of functional deficits that occur in MCI and mild Alzheimer disease (AD) can aid in early detection of incipient dementia and can identify potential mechanistic pathways to disrupted instrumental activities of daily living (IADLs).

Objectives: To examine the number, type, and severity of functional impairments and to identify the clinical characteristics associated with functional impairment across patients with amnestic MCI (aMCI) and those with mild AD.

Hydrogen sulfide attenuated tumor necrosis factor-α-induced inflammatory signaling and dysfunction in vascular endothelial cells.

Background: Hydrogen sulfide (H(2)S), the third physiologically relevant gaseous molecule, is recognized increasingly as an anti-inflammatory mediator in various inflammatory conditions. Herein, we explored the effects and mechanisms of sodium hydrosulfide (NaHS, a H(2)S donor) on tumor necrosis factor (TNF)-α-induced human umbilical vein endothelial cells (HUVEC) dysfunction.

Methodology And Principal Findings: Application of NaHS concentration-dependently suppressed TNF-α-induced mRNA and proteins expressions of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1), mRNA expression of P-selectin and E-selectin as well as U937 monocytes adhesion to HUVEC.

2,2'-(p-Phenyl-ene)bis-(4,5-dihydro-1H-imidazol-3-ium) bis-(3-nitro-benzoate).

In the title compound, C(12)H(16)N(4) (+)·2C(7)H(4)NO(4) (-), the complete 2,2'-(p-phenyl-ene)bis-(4,5-dihydro-1H-imidazol-3-ium) (bib) dication is generated by crystallographic inversion symmetry. The bib cations reside on crystallographic inversion centers, which coincide with the centroids of the respective benzene rings. In the cation, the imidazole ring adopts an envelop conformation with the flap atom displaced by 0.

Manganese exposure from drinking water and children's classroom behavior in Bangladesh.

Background: Evidence of neurological, cognitive, and neuropsychological effects of manganese (Mn) exposure from drinking water (WMn) in children has generated widespread public health concern. At elevated exposures, Mn has been associated with increased levels of externalizing behaviors, including irritability, aggression, and impulsivity. Little is known about potential effects at lower exposures, especially in children.

Depression after exposure to stressful events: lessons learned from the severe acute respiratory syndrome epidemic.

Aim: The aim of the study was to examine, among hospital employees exposed to an outbreak of severe acute respiratory syndrome (SARS), post-outbreak levels of depressive symptoms and the relationship between those depressive symptom levels and the types of outbreak event exposures experienced.

Methods: In 2006, randomly selected employees (N = 549) of a hospital in Beijing were surveyed concerning their exposures to the city's 2003 SARS outbreak and the ways in which the outbreak had affected their mental health. Subjects were assessed on sociodemographic factors, on types of exposure to the outbreak, and on symptoms of posttraumatic stress disorder and depression.

Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents.

A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric cancer cell SGC-7901, liver cancer Hep-G2 and human prostate PC-3 cell lines with IC(50) values of 21.23±0.

Tremor severity and age: a cross-sectional, population-based study of 2,524 young and midlife normal adults.

Mild action tremor occurs in most normal people. Yet this tremor mainly has been studied within the context of advanced age rather than among the vast bulk of adults who are not elderly. Whether this tremor worsens during young and middle age is unknown.

A new hope for neurodegeneration: possible role of hydrogen sulfide.

For hundreds of years, hydrogen sulfide (H2S) has been known solely as a toxic gas with the smell of rotten eggs. Nevertheless, the notoriety of H2S as a toxic gas is experiencing a transformation, with an increasing amount of research showing that it regulates a range of physiological and pathological processes in mammals. Hence H2S is a physiologically important molecule and has been referred to as the third gaseous mediator alongside nitric oxide and carbon monoxide.

S-Propargyl-cysteine (SPRC) attenuated lipopolysaccharide-induced inflammatory response in H9c2 cells involved in a hydrogen sulfide-dependent mechanism.

The present study attempts to investigate the effects of S-propargyl-cysteine (SPRC), a sulfur-containing amino acid, on lipopolysaccharide (LPS)-induced inflammatory response in H9c2 cardiac myocytes. We found that SPRC prevented nuclear factor-κB (NF-κB) activation assessed by NF-κB p65 phosphorylation and IκBα degradation, suppressed LPS-induced extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation and intracellular reactive oxygen species (ROS) production. Furthermore, incubation of H9c2 cells with SPRC induced phosphorylation of Akt in a time- and concentration-dependent manner.