Identification of SR2211: a potent synthetic RORγ-selective modulator.

Nuclear receptors (NRs) are ligand-regulated transcription factors that display canonical domain structure with highly conserved DNA-binding and ligand-binding domains. The identification of the endogenous ligands for several receptors remains elusive or is controversial, and thus these receptors are classified as orphans. One such orphan receptor is the retinoic acid receptor-related orphan receptor γ (RORγ).

Synthesis and antiplasmodial evaluation of novel chromeno[2,3-b]chromene derivatives.

5-Methoxyflavenes and 6-methoxyflavenes were found to undergo stereoselective acid-catalyzed rearrangement to generate a range of novel chromeno[2,3-b]chromene derivatives. When subjected to an in vitro antiplasmodial growth inhibition assay using Plasmodium falciparum (3D7 line) the chromene analogues were shown to display IC(50) values ranging from 6.8 to 39.

Satellite Remote Sensing for Developing Time and Space Resolved Estimates of Ambient Particulate in Cleveland, OH.

This article empirically demonstrates the use of fine resolution satellite-based aerosol optical depth (AOD) to develop time and space resolved estimates of ambient particulate matter (PM) ≤2.5 µm and ≤10 µm in aerodynamic diameters (PM(2.5) and PM(10), respectively).

Thiacalix[4]arene-cinnamaldehyde derivative: ICT-induced preferential nanomolar detection of Ag+ among different transition metal ions.

A new thiacalix[4]arene-cinnamaldehyde derivative 3, which undergoes red shift in the fluorescence spectrum in the presence of Ag(+) ions, has been synthesized. This emission shift is attributed to the intramolecular charge transfer process in the presence of Ag(+) ions with a detection limit in the nanomolar range.

Anti-stress effects of cilnidipine and nimodipine in immobilization subjected mice.

The present study was designed to investigate the ameliorative role of cilnidipine and nimodipine in immobilization stress-induced behavioral alterations and memory defects in the mice. Acute stress was induced by immobilizing the mice for 150 min and stress-induced behavioral changes were assessed using actophotometer, hole board, open field and social interaction tests. The learning and memory was evaluated using elevated plus maze tests and biochemically, the corticosterone levels were measured in the blood serum.

Effect of acute moderate exercise on cognitive P300 in persons having sedentary lifestyles.

Background: There are conflicting reports regarding the effect of exercise on cognition. We therefore planned to assess the acute effect of moderate exercise on cognition, studied by event-related brain potential P300, in subjects having sedentary lifestyles.

Materials And Methods: Sixty adults (40 males and 20 females) in the age-group of 18-30 years having sedentary lifestyles were included in the study.

PKMζ is essential for spinal plasticity underlying the maintenance of persistent pain.

Background: Chronic pain occurs when normally protective acute pain becomes pathologically persistent. We examined here whether an isoform of protein kinase C (PKC), PKMζ, that underlies long-term memory storage in various brain regions, also sustains nociceptive plasticity in spinal cord dorsal horn (SCDH) mediating persistent pain.

Results: Cutaneous injury or spinal stimulation produced persistent increases of PKMζ, but not other atypical PKCs in SCDH.

Highly selective fluorescence turn-on chemodosimeter based on rhodamine for nanomolar detection of copper ions.

A highly selective fluorescent chemodosimeter based on rhodamine is synthesized which undergoes Cu(2+) driven hydrolysis in aqueous media to produce fluorescence turn-on changes with a detection limit up to the nanomolar range.

Immobilization of antibacterial dihydropyrrol-2-ones on functional polymer supports to prevent bacterial infections in vivo.

Antibiotic-resistant Staphylococcus aureus is of great concern, as it causes a wide range of life-threatening infections. The current study demonstrates that dihydropyrrolone (DHP)-coated polyacrylamide substrates are effective in reducing the number of culturable clinical isolates of S. aureus in vitro in a dose-dependent manner and are able to reduce the pathogenic potential of staphylococcal infection in a subcutaneous infection model.

Variability in coconut (Cocos nucifera L.) germplasm and hybrids for fatty acid profile of oil.

Coconut oil, the main product of coconut fruit, is the richest source of glycerol and lauric acid and hence is called lauric oil. This paper reports the fatty acid profile of oil from 60 Talls, 14 Dwarfs, and 34 hybrids. These include collections from 13 countries covering a large coconut-growing area of the world, apart from the indigenous ones.

A rapidly developing lung mass diagnosed as desmoplastic small round cell tumor.

We present a case of a young male who presented with complaints of fever along with cough and sputum. He was diagnosed with having right pleural effusion. He was already taking anti-tubercular therapy for one month before presentation.

High-resolution sonography detects extraforaminal nerve pathology in patients initially diagnosed with cervical disc disease: a case series.

In patients presenting with neck and upper limb complaints, MRI changes suggestive of cervical disc disease do not exclude concomitant extraforaminal pathology, as shown in the series of three cases presented here. High-resolution ultrasound of the brachial plexus and peripheral nerves may be useful in identifying an extraforaminal pathology when (1) symptoms and signs are disproportionate to MRI findings of cervical disc disease; (2) there is obvious discordance between MRI and nerve conduction findings; (3) an entrapment neuropathy is suspected but the site of nerve lesion is unidentifiable on the basis of available investigations and clinical findings.

A review on animal models for screening potential anti-stress agents.

Stress is a state of threatened homeostasis that produces different physiological as well as pathological changes depending on severity, type and duration of stress. The animal models are pivotal for understanding the pathophysiology of stress-induced behavioral alterations and development of effective therapy for its optimal management. A battery of models has been developed to simulate the clinical pain conditions with diverse etiology.

Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation.

PPARγ is the functioning receptor for the thiazolidinedione (TZD) class of antidiabetes drugs including rosiglitazone and pioglitazone. These drugs are full classical agonists for this nuclear receptor, but recent data have shown that many PPARγ-based drugs have a separate biochemical activity, blocking the obesity-linked phosphorylation of PPARγ by Cdk5. Here we describe novel synthetic compounds that have a unique mode of binding to PPARγ, completely lack classical transcriptional agonism and block the Cdk5-mediated phosphorylation in cultured adipocytes and in insulin-resistant mice.

Synthesis and antimalarial evaluation of novel benzopyrano[4,3-b]benzopyran derivatives.

7-Methoxyflavenes and 5,7,8-trimethoxyflavenes were found to undergo stereoselective acid-catalyzed rearrangement to generate the benzopyrano[4,3-b]benzopyran ring system present in the natural product, dependensin. Dependensin and its analogs were subjected to antimalarial growth inhibition assays against Plasmodium falciparum and found to have IC(50) values ranging between 1.9 and 3.

Synthesis and evaluation of novel tetrapropoxycalix[4]arene enones and cinnamates for protection from ultraviolet radiation.

A series of novel calix[4]arene enones (5-7) and cinnamates (12-14) have been synthesized and evaluated for ensuring protection from ultraviolet radiation (UVR). Spectroscopic analyses has revealed that compound 6 absorbs ultraviolet radiations between 280 and 350 nm with an absorption maximum at 312 nm. Its molar absorption coefficient (ε) (>5 × 10(4)M(-1)cm(-1)) and bandwidth are larger than those for the commercially used sun protectants (oxybenzone (OB), 2-ethylhexyl 4-methoxycinnamate (OMC) and avobenzone).

Regional source identification using Lagrangian stochastic particle dispersion and HYSPLIT backward-trajectory models.

The main objective of this study was to investigate the capabilities of the receptor-oriented inverse mode Lagrangian Stochastic Particle Dispersion Model (LSPDM) with the 12-km resolution Mesoscale Model 5 (MM5) wind field input for the assessment of source identification from seven regions impacting two receptors located in the eastern United States. The LSPDM analysis was compared with a standard version of the Hybrid Single-Particle Lagrangian Integrated Trajectory (HYSPLIT) single-particle backward-trajectory analysis using inputs from MM5 and the Eta Data Assimilation System (EDAS) with horizontal grid resolutions of 12 and 80 km, respectively. The analysis included four 7-day summertime events in 2002; residence times in the modeling domain were computed from the inverse LSPDM runs and HYPSLIT-simulated backward trajectories started from receptor-source heights of 100, 500, 1000, 1500, and 3000 m.

Mandibular third molar angulation in extraction and non extraction orthodontic cases.

Background: The purpose of this study is to determine the angulation of mandibular third molar in orthodontic cases which are planned for extraction and non extraction.

Methods: This is a cross-sectional descriptive study in which pre-treatment panoramic radiographs of 49 patients, age range 11-26 years were taken from the OPD of Department of Orthodontics, Dr. Ishrat- ul -Ebad Khan Institute of Oral and Health Sciences (DIKIOHS), Dow University of Health Sciences.

Effect of acute moderate exercise on cognitive event-related potentials n100, p200, n200, and interpeak latencies.

Background: Effect of acute moderate exercise on cognition has been studied recently, although there are controversial reports in this context. This is the reason we performed this study, to observe the effect of acute moderate exercise on the cognitive functions of persons having a sedentary lifestyle, by measuring the latencies of event-related potentials N100, P200, N200, and the inter-peak latencies N100-P200, P200-N200, and N200-P300.

Materials And Methods: Sixty right-handed participants (34 males, 26 females) of age group 15 - 30 years, having a sedentary lifestyle, were recruited for the study.

Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.

T-helper cells that produce interleukin-17 (T(H)17 cells) are a recently identified CD4(+) T-cell subset with characterized pathological roles in autoimmune diseases. The nuclear receptors retinoic-acid-receptor-related orphan receptors α and γt (RORα and RORγt, respectively) have indispensible roles in the development of this cell type. Here we present SR1001, a high-affinity synthetic ligand-the first in a new class of compound-that is specific to both RORα and RORγt and which inhibits T(H)17 cell differentiation and function.

Seasonal and daily variation of radon at 10 m depth in borehole, Garhwal Lesser Himalaya, India.

Mostly accepted and widely reported radon (Rn(222)) measurements, a tool for earthquake precursor research, is a part of multi-parametric geophysical observation in the Garhwal Lesser Himalaya for earthquake related studies. Radon is being recorded continuously at an interval of 15 min at 10 m depth in a 68 m deep borehole. Three years high resolution 15 min data at 10 m depth shows a complex trend and has a strong seasonal effect along with some diurnal, semi-diurnal and multi-day recurring trends.

Health Effects of Air Quality Regulations in Delhi, India.

This, the first systematic study, quantifies the health effects of air quality regulations in Delhi, which adopted radical measures to improve air quality, including, for example, the conversion of all commercial vehicles to compressed natural gas (CNG), and the closure of polluting industries in residential areas from 2000 to 2002. Air pollution data, collected at 113 sites (spread across Delhi and its neighboring areas) from July-December 2003, were used to compute exposure at the place of residence of 3,989 subjects. A socio-economic and respiratory health survey was administered in 1,576 households.

Analysis of BAC-end sequences (BESs) and development of BES-SSR markers for genetic mapping and hybrid purity assessment in pigeonpea (Cajanus spp.).

Background: Pigeonpea [Cajanus cajan (L.) Millsp.] is an important legume crop of rainfed agriculture.

Nisin and class IIa bacteriocin resistance among Listeria and other foodborne pathogens and spoilage bacteria.

Food safety has been an important issue globally due to increasing foodborne diseases and change in food habits. To inactivate foodborne pathogens, various novel technologies such as biopreservation systems have been studied. Bacteriocins are ribosomally synthesized peptides or proteins with antimicrobial activity produced by different groups of bacteria, but the bacteriocins produced by many lactic acid bacteria offer potential applications in food preservation.