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Herein, an efficient and scalable synthesis of 2,4-diaryl substituted chromene [43-b] pyridine derivatives, using a multicomponent reaction strategy by microwave irradiation of 4-amino 2-oxo- 2H-chromene, aromatic aldehydes, and substituted anilines is described. This synthetic strategy was found to be very useful as it follows environment benign protocol. Also it gives a good outcome in terms of yield and requires a shorter reaction time.

Background: A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized in via an in situ procedure in high yields. The structure of synthesized compounds has been confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines, including HepG-2, SK-LU-1, and MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1, and MCF-7 with IC50 values of 8.20, 6.66, and 9.35 μM, respectively. Objective: This study aims at developing new zerumbone hydrazones as anticancer agents based on zerumbone, a natural compound wildly growing in Vietnam. Methods: A series of new zerumbone hydrazones was designed, synthesized, and evaluated for cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7, and SKLu-1, using the MTT method. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines, including HepG-2, SK-LU-1, and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1, and MCF-7 with IC50 values of 8.20, 6.66, and 9.35 μM, respectively. Conclusion: The research results suggest that some compounds could be considered as leads for the future design of zerumbone hydrazones in which bio-isosteric replacements in theortho position of the phenyl ring could be performed to improve the cytotoxic activity.

The investigation was designed to trigger the complete chemical constituents present in the methanolic extract of leaves of hair knot plant; botanically known as Pergularia daemia belongs to the family of the Asclepiadaceae one of the endemic plants of Andhra Pradesh, India by Agilent Technologies Gas Chromatography–Mass Spectrometry and components were well separated on HP-5 MS capillary column consisting of stationary phase of 5% phenyl 95% methylpolysiloxane. The resulted compounds were appropriate to the NIST (National Institute of Standards and Technology) library and the study indicated the presence of different phytochemical compounds. A total of 51 compounds were recognized in the methanolic extract of Pergularia daemia leaves. Further, five new compounds were separated and four of biological importance viz. Pentadecane, Tetratriacontane, Dibutyl phthalate and Squalene were identified. The results of the importance of biologically active phytochemicals in the study recommend, P. daemiaas as a plant of phytopharmaceutical reputation.

A selective, rapid and sensitive method was developed for the determination of genotoxic impurities (2-Amino-6-chloro purine and Bromo compound) in Penciclovir drug substance using RPUPLC-MS/MS. The chromatographic separation was performed on Kromasil C8 column (150 mm x 4.6 mm, 5 μm) maintained at 45°C using 0.1%formic acids in water as buffer and acetonitrile through gradient programme. The flow rate was maintained at 0.5mL/min with an injection volume of 10 μL. For the quantification of genotoxic impurities, positive-electrospray ionisation (ESI) mode was selected. Penciclovir and its impurities were well separated within the shortest run time of 16min. The chromatographic method was developed, and the results of all validation parameters showed that the technique is well confined to the limits of ICH guidelines. The method has high sensitivity, and the limit of detection was found to be as low as 0.15 and 0.30 ppm for 2-Amino-6-chloro purine and Bromo compound. The recovery of 2-Amino-6-chloro purine and Bromo compound are found in the range of 80-120%. The linearity of peak area versus concentration was demonstrated in the range of LOQ - 150% level of impurities with a correlation coefficient of 0.9999. The method has proved too robust by introducing minuscule changes in the chromatographic parameters. The method was successfully validated and applied for Penciclovir drug substances and their dosage forms to determine the mentioned genotoxic impurities.

A reverse phased high performance liquid (HPLC) method was developed for the determination of (TLP) drug substance and it impurities TLPRC01, TLPRC02, TLPRC03, TLPRC04, TLPRC05 and TLPC06 using an analytical column Unison UK-C18, (250mm x4.6mm, 5µ) maintained at 30oC±2oC. The wavelength was set at 265 nm. Flow rate was maintained as 1.0 ml/min with injection volume of 10 . All the could be separated with run time of 60 min. The peaks of are well resolved with the resolution of 2.0. The results of all the validation parameters showed that the developed method is well confined to the limits of ICH guidelines. Degradation studies showed that the mass balance of in all conditions is in the range of 98 to 102 %. The accuracy of six impurities TLPRC01, TLPRC02, TLPRC03, TLPRC04, TLPRC05 and TLPC06 found in the range of 80-120%. The proposed method is able to quantify the related compounds present in drug substance and also able to see the assay of drug substance in presence of degraded impurities without the loss of purity of drug substance and other impurities. The method has proved to be robust by introducing changes in the conditions.

The present study was aimed to evaluate the anti-obesity property of Tamarindus indica seed extract (TSE) on high fat-fed obese rats. TSE was prepared by cold maceration method and qualitative phytochemical studies had been carried out. In vitro cell viability assay (MTT assay) was and oil red staining for evaluating the lipid accumulation in cells was carried out using 3T3-L1 cells, and leptin levels was evaluated by ELISA. In-vivo Obesity was induced in experimental rats by administration of a high-fat diet for 04 weeks. The anti-obesity effect was screened by oral administration of TSE at two different dose levels i.e., 250 and 500mg/kg b. Wt. Along with a high-fat diet for a period of 04 weeks. The anti-obesity activity is estimated in terms of body weight gain, serum triglycerides (TG), Total cholesterol (TC). In -vitro studies revealed that the TSE has no cytotoxic effect, Administration of a high-fat diet for 04 weeks significantly increased the body weight, serum triglycerides, cholesterol. Upon treatment with TSE, a significant dose-dependent alteration in body weight, triglycerides, cholesterol levels were observed, inferring the anti-obesity property of Tamarindus seed extract.

Diabetes mellitus is a chronic metabolic disorder characterized by hyperglycemia arising from deregulation in insulin secretion, insulin action, or both. The current synthetic drugs have dose-dependent side effects which confined their uses. The phytochemicals are the natural compounds that have better therapeutic efficacy and interacts synergistically with oral hypoglycemic drugs. The addition of phytochemicals with OHDs may reduce the dose of synthetic drugs as well as their side effects and toxicity. A detailed outline about such combinations like Ferulic acid & THZ/Metformin, Ellagic acid & Pioglitazone (THZ), Chlorogenic acid & THZ/Metformin, Caffeic acid & THZ/Metformin, eugenol acid & THZ/Metformin, cinnamic acid & THZ/Metformin, p- coumaric acid & THZ/Metformin, Arecoline &Vanillic acid with the THZ/ Metformin have been illustrated. This review has also discussed the synergy and mechanism of phytochemical with the OHDs to combat hyperglycemia and other risk associated with it. A comprehensive review was conducted to pile up the information about polyphenols & synthetic drug combinations used for the treatment of diabetes mellitus, which has been carried out in-vitro or in-vivo and may contribute to identifying novel strategies in the treatment of T2D condition. This review shows the importance of the responsible bioactive agents present in medicinal plants in the drive to demonstrate their antidiabetic effects.

This article proposes an extensive experimental and microstructural analysis to study the consequences of deep cryogenic treatment (DCT) soaking duration on tungsten carbide end mill cutter on the machinability of P20 mold steel. A Box-Behnken design of response surface methodology (RSM) is utilized to collect data for the study. Cutting speed, feed rate, depth of cut and milling cutters subjected to various soaking durations are taken as important process variables which are a function of performance measures viz. tool wear rate (TWR), material removal rate (MRR) and surface roughness (Ra). It is observed that cutting speed, feed, depth of cut and cryogenic treatment exhibit a considerable effect on performance measures. In the present study, NSGA-II multi-objective optimization technique is used to obtain the optimal process parameters of end milling process to enhance the productivity of the process. For this purpose, the developed RSM model is coupled with NSGA-II in MATLAB.

Nitric oxide (NO) is a well-established signaling molecule and cytotoxic agent in mammals. NO is synthesized by nitric oxide synthase (NOS) by macrophages at high concentrations as a key part of the host immune response, and at low concentrations in endothelial and neuronal cells as a signaling agent. In endothelial cells, the primary NO receptor is soluble guanylate cyclase (sGC), which contains a heme-nitric oxide/oxygen binding domain (H-NOX). Selective binding of NO to the H-NOX domain is responsible for activation of sGC. Thus, the mammalian NO signaling system involves NO synthesis by NOS, and NO sensing by the H-NOX domain of sGC. NOS and H-NOX proteins have also been identified in a number of bacterial species, including pathogens. Putative roles for bacterial NOS proteins include protection against oxidative stress and antibiotics, while bacterial H-NOX proteins have been shown to govern processes such as biofilm formation and bioluminescence via interactions with signaling proteins such as diguanylate cyclases (DGC) or histidine kinases (HK). Here, various aspects of NO signaling from three different organisms are characterized: the marine alphaproteobacterium Silicibacter sp. TrichCH4B; the soil-dwelling gammaproteobacterium Shewanella oneidensis, and the marine cyanobacterium Synechococcus sp. PCC 7335. This work and other recent studies seek to understand not only the diverse roles for NO in bacteria, but also the molecular mechanisms of bacterial NO signaling. Silicibacter sp. TrichCH4B is the first bacterial organism discovered to contain both an NOS and H-NOX, thus capable of both NO synthesis and sensing, analogous to mammalian systems. The H-NOX protein from Silicibacter is found in an operon adjacent to an HK, forming part of a two-component phospho-relay signaling network. The response regulator of the network was identified to be a diguanylate cyclase (DGC), which is inactivated upon phosphorylation and establishes the link between NO and intracellular cyclic-di-GMP levels, and consequently biofilm formation. It was also determined that Silicibacter NOS activity is stimulated by a signaling protein from an algal symbiont, Trichodesmium erythraeum, which is a major marine nitrogen fixer. Thus, in the presence of Trichodesmium, the increase in NOS activity results in Silicibacter biofilm formation and poising the two species for nutrient exchange, revealing a novel role for NO in interspecies communication and symbiosis.Given the diverse processes governed by NO/H-NOX signaling, it is crucial to understand the molecular mechanism by which H-NOX regulates HK autophosphorylation activity, the most common outcome of a NO-bound H-NOX. Here, the interaction and signal transduction between the H-NOX-HK signaling pair from Shewanella oneidensis are characterized. Binding kinetics measurements and analytical gel filtration revealed that NO-bound H-NOX has a tighter affinity for the HK, compared with H-NOX in the unliganded state, correlating binding affinity with kinase inhibition. Kinase activity assays with a panel of binding-deficient H-NOX mutants further reveal that while formation of the H-NOX-HK protein complex is required to stabilize the HK, H-NOX conformational changes upon NO binding are necessary for HK inhibition. Characterization of H-NOX proteins has led to an increased understanding of bacterial NO sensing. However, NO production in bacteria is less well-understood, and here the NOS protein from Synechococcus sp. PCC 7335 is characterized. Mammalian NOS proteins are comprised of a P450-like heme/oxidase domain responsible for catalysis, and a reductase domain responsible for electron transfer. While most bacterial NOS proteins discovered to date contain only the heme/oxidase domain, Synechococcus NOS contains both the oxidase and reductase domains, and additionally contains a predicted globin domain resembling bacterial flavohemoglobins. Spectroscopic and biochemical characterization of the globin indicated a possible role in redox communication in this novel class of bacterial NOS enzymes.

Hyperpolarized magnetic resonance spectroscopic imaging (MRSI) of [1-13C]pyruvate metabolism has previously been used to assess the effects of traumatic brain injury (TBI) in rats. Here, we show that MRSI can be used in conjunction with dichloroacetate to measure the phosphorylation state of pyruvate dehydrogenase (PDH) following mild-to-moderate TBI, and that measurements can be repeated in a longitudinal study to monitor the course of injury progression and recovery. We found that the level of 13C-bicarbonate and the bicarbonate-to-lactate ratio decreased on the injured side of the brain four hours after injury and continued to decrease through day 7. Levels recovered to normal by day 28. Measurements following dichloroacetate administration showed that PDH was inhibited equally by PDH kinase (PDK) on both sides of the brain. Therefore, the decrease in aerobic metabolism is not due to inhibition by PDK.

Background and objectives: Lower vitamin status has been linked to cognitive deficits, pending mechanistic elucidation. Serum 25-hydroxyvitamin D [25(OH)D], folate and cobalamin were explored against brain volumes and white matter integrity (WMI). Methods: Three prospective waves from Healthy Aging in Neighborhoods of Diversity Across the Life Span (HANDLS) study were used [Baltimore, City, MD, 2004-2015, N = 183-240 urban adults (Agev1: 30-64 years)]. Serum vitamin 25-hydroxyvitamin D [25(OH)D], folate and cobalamin concentrations were measured at visits 1 (v1: 2004-2009) and 2 (v2: 2009-2013), while structural and diffusion Magnetic Resonance Imaging (sMRI/dMRI) outcomes were measured at vscan: 2011-2015. Top 10 ranked adjusted associations were corrected for multiple testing using familywise Bonferroni (FWER 50 years: +205 ± 54]; parietal WM; [overall: +251 ± 77, males: +486 ± 129 and Agev1 > 50 years: +393 ± 108] and left occipital pole volume [overall: +15.70 ± 3.83 and above poverty: 19.0 ± 4.3], findings replicated for 25(OH)D (v2-v1) annualized exposure, which was also linked with greater WMI (fractional anisotropy, FA) in the anterior limb of the internal capsule (ALIC); FWER < 0.05 [Overall: +0.0020 ± 0.0004; Whites: +0.0024 ± 0.0004] and in the cingulum (hippocampus) [Overall: +0.0016 ± 0.0004]. Only trends were detected for cobalamin exposures (q < 0.10), while serum folate (v1) was associated with lower mean diffusivity (MD) in ALIC, reflecting greater WMI, overall. Conclusions: Among urban adults, serum 25(OH)D status and increase were consistently linked to larger occipital and parietal WM volumes and greater region-specific WMI. Pending longitudinal replication of our findings, randomized controlled trials of vitamin D supplementation should be conducted against brain marker outcomes.

Monophosphate prodrug analogs of 2′-deoxy-2′-fluoro-2′-C-methylguanosine have been reported as potent inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase. These prodrugs also display potent anti-dengue virus activities in cellular assays although their prodrug moieties were designed to produce high levels of triphosphate in the liver. Since peripheral blood mononuclear cells (PBMCs) are among the major targets of dengue virus, different prodrug moieties were designed to effectively deliver 2′-deoxy-2′-fluoro-2′-C-methylguanosine monophosphate prodrugs and their corresponding triphosphates into PBMCs after oral administration. We identified a cyclic phosphoramidate, prodrug 17, demonstrating well-balanced anti-dengue virus cellular activity and in vitro stability profiles. We further determined the PBMC concentration of active triphosphate needed to inhibit virus replication by 50% (TP(50)). Compound 17 was assessed in an AG129 mouse model and demonstrated 1.6- and 2.2-log viremia reductions at 100 and 300 mg/kg twice a day (BID), respectively. At 100 mg/kg BID, the terminal triphosphate concentration in PBMCs exceeded the TP(50) value, demonstrating TP(50) as the target exposure for efficacy. In dogs, oral administration of compound 17 resulted in high PBMC triphosphate levels, exceeding the TP(50) at 10 mg/kg. Unfortunately, 2-week dog toxicity studies at 30, 100, and 300 mg/kg/day showed that “no observed adverse effect level” (NOAEL) could not be achieved due to pulmonary inflammation and hemorrhage. The preclinical safety results suspended further development of compound 17. Nevertheless, present work has proven the concept that an efficacious monophosphate nucleoside prodrug could be developed for the potential treatment of dengue virus infection.

Studies were carried out on bael (Aegle marmelos L.) seed protein concentrate (BSPC) to evaluate the proximate, mineral and amino acid composition, nitrogen extractability and functional properties. The protein content was found to be 70.8 g/100 g BSPC. Calcium and phosphorus were observed in major quantities. The bael seed meal (BSM) lipid is found to be rich in unsaturated fatty acids (75%). Essential amino acids occurred in good quantities in BSPC. Nitrogen extractability of BSPC in water was found to be higher at 1:40 (w/v) ratio and an extraction time of 40 min. Minimum nitrogen extractability (14 g/100 g protein) and maximum extractability (97 g/ 100 g protein) were observed at pH 4 and 12, respectively. In the presence of sodium chloride (0.1 and 0.5 M), the nitrogen extractability was found to be increased between pH 4-10. Protein precipitability was maximum (90 g/100 g protein) at pH 5.5. SDS-PAGE of BSM and BSPC showed different polypeptides with molecular weights from 205 kDa to 12 kDa. The lower water holding capacity and higher oil holding capacity, foam capacity and foam stability were noted in BSPC. The sorption isotherm studies showed that the BSPC was non-hygroscopic in nature.

Diabetes predisposes to cognitive decline leading to dementia and is associated with decreased brain NAD+ levels. This has triggered an intense interest in boosting nicotinamide adenine dinucleotide (NAD+) levels to prevent dementia. We tested if the administration of the precursor of NAD+, nicotinamide mononucleotide (NMN), can prevent diabetes-induced memory deficits. Diabetes was induced in Sprague-Dawley rats by the administration of streptozotocin (STZ). After 3 months of diabetes, hippocampal NAD+ levels were decreased (p = 0.011). In vivo localized high-resolution proton magnetic resonance spectroscopy (MRS) of the hippocampus showed an increase in the levels of glucose (p &lt, 0.001), glutamate (p &lt, 0.001), gamma aminobutyric acid (p = 0.018), myo-inositol (p = 0.018), and taurine (p &lt, 0.001) and decreased levels of N-acetyl aspartate (p = 0.002) and glutathione (p &lt, 0.001). There was a significant decrease in hippocampal CA1 neuronal volume (p &lt, 0.001) and neuronal number (p &lt, 0.001) in the Diabetic rats. Diabetic rats showed hippocampal related memory deficits. Intraperitoneal NMN (100 mg/kg) was given after induction and confirmation of diabetes and was provided on alternate days for 3 months. NMN increased brain NAD+ levels, normalized the levels of glutamate, taurine, N-acetyl aspartate (NAA), and glutathione. NMN-treatment prevented the loss of CA1 neurons and rescued the memory deficits despite having no significant effect on hyperglycemic or lipidemic control. In hippocampal protein extracts from Diabetic rats, SIRT1 and PGC-1&alpha, protein levels were decreased, and acetylation of proteins increased. NMN treatment prevented the diabetes-induced decrease in both SIRT1 and PGC-1&alpha, and promoted deacetylation of proteins. Our results indicate that NMN increased brain NAD+, activated the SIRT1 pathway, preserved mitochondrial oxidative phosphorylation (OXPHOS) function, prevented neuronal loss, and preserved cognition in Diabetic rats.

Organophosphorus (OP) insecticides are pest-control agents heavily used worldwide. Unfortunately, they are also well known for the toxic effects that they can trigger in humans. Clinical manifestations of an acute exposure of humans to OP insecticides include a well-defined cholinergic crisis that develops as a result of the irreversible inhibition of acetylcholinesterase (AChE), the enzyme that hydrolyzes the neurotransmitter acetylcholine (ACh). Prolonged exposures to levels of OP insecticides that are insufficient to trigger signs of acute intoxication, which are hereafter referred to as subacute exposures, have also been associated with neurological deficits. In particular, epidemiological studies have reported statistically significant correlations between prenatal subacute exposures to OP insecticides, including chlorpyrifos, and neurological deficits that range from cognitive impairments to tremors in childhood. The primary objectives of this article are: (i) to address the short- and long-term neurological issues that have been associated with acute and subacute exposures of humans to OP insecticides, especially early in life (ii) to discuss the translational relevance of animal models of developmental exposure to OP insecticides, and (iii) to review mechanisms that are likely to contribute to the developmental neurotoxicity of OP insecticides. Most of the discussion will be focused on chlorpyrifos, the top-selling OP insecticide in the United States and throughout the world. These points are critical for the identification and development of safe and effective interventions to counter and/or prevent the neurotoxic effects of these chemicals in the developing brain. This is an article for the special issue XVth International Symposium on Cholinergic Mechanisms.

Powder-mixed dielectric fluid is one of the innovations of electrode-discharge machining (EDM) which seeks to improve the process outputs by addition of Nickel powders to the dielectric during machining. In the present study, the influence of Nickel powder in kerosene dielectric fluid on EDM process outputs was investigated. Experiments were conducted with the outputs as material removal rate (MRR) and surface roughness(Ra). During the EDM, the discharge current was varied between 3 and 15 A, while powder concentration ranges between 2 and 10 g/l. Results indicate that the highest MRR of 39.888 mm3 /min was obtained with Nickel powder concentration of 6 g/l at the current of 9A, where as the lowest SR of 3.397 μm was obtained with Nickel concentration of 3 g/l at the current of 3A.

The present research was aimed to formulate aceclofenac transemulgel using Aloe vera as gel base. The prepared formulations were subjected to physical characterization, in-vitro and in-vivo assessment. Aceclofenac, a hydrophobic potential non steroidal anti inflammatory drug, causes ulceration upon chronic oral administration, could be formulated into transemulgel to enhance therapeutic efficacy and to lower the unwanted side effects. The transemulgel was prepared from aqueous Aloe vera gel and aceclofenac emulsion. The prepared transemulgel was evaluated for its pH, viscosity, drug content, skin irritation, in-vitro diffusion and accelerated stability studies. The prepared aceclofenac-Aloe vera tranemulgel and commercial aceclofenac gel were subjected to pharmacodynamic studies in albino rats of Wistar strain employing carrageenan induced left hind paw edema method to assess the anti-inflammatory effect. The transemulgel showed a pH of 6.78 and viscosity of 18 cps. In-vitro diffusion data revealed better permeation characteristics. Topical application of formulation found no skin irritation. Stability study has proved the integrity of the formulation. The prepared aceclofenac Aloe vera transemulgel showed better in-vitro drug release when compared with the commercial aceclofenac gel formulation. Anti-inflammatory activity in treated rats showed the significant paw volume reduction at p

Prenatal ethanol exposure alters brain structure, functional connectivity, and behavior in humans and rats. Behavioral changes include deficits in executive function, which requires cooperative activity between the frontal cortices and other brain regions. In this study, we analyzed the functional connectivity and neurochemical levels of the prefrontal cortex (PFC) using resting-state functional magnetic resonance imaging (rsfMRI) and proton magnetic resonance spectroscopy (1H-MRS) in ethanol-exposed (Eth) and control (Ctr) rats. Pregnant Long-Evans rats were fed a liquid diet containing ethanol (2.1–6.46% v/v ethanol) from gestational days 6 to 21 (Eth). Ctr animals received an isocaloric, isonutritive liquid diet. In young adulthood, male and female offspring underwent in vivo MRI using a 7.0-Tesla system. 1H-MRS from the PFC and whole brain rsfMRI were obtained on the animals. Seed-based functional connectivity analysis was performed with seeds placed in the PFC, matching the voxel of MRS. Male, but not female, Eth rats showed less functional connectivity between PFC and dorsal striatum than Ctr animals. In Eth males glucose levels were significantly lower, and in Eth females lower levels of phosphorylcholine but an increased gamma-aminobutyric acid/glutamate ratio were observed in the PFC compared with Ctr animals. Prenatal ethanol alters brain metabolism and functional connectivity of the PFC in a sex-dependent manner.

A field experiment was conducted to investigate the effect of nitrogen (N) fertilizer on growth, development and yield of Upland, IRHTN, DRR and other released rice groups. Six varieties from each group, a total of 18 genotypes were planted in randomized complete block design during dry (2011) and wet (2012) seasons with three replications at Indian Institute of Rice Research, Hyderabad. Group responses to the N-stress (N0; native nitrogen) and recommended nitrogen (N100; 100 kg N ha-1) for physiological, morphological and yield attributes were recorded. The average leaf rolling time was found 75.4% increased with N-100 in IRHTN group over N-0 in the same group and also found higher among the groups. Leaf temperature, SPAD was noticed higher in DRR and other released group with N-100. The highest plant height was observed in Upland group only, while number of tillers, effective booting tillers (EBT), filled grain weight and total dry matter (TDM), harvest index (HI), total nitrogen content (straw + grain) were found increased with N-100 in DRR and other released group. Key words: Leaf rolling, nitrogen, rice, SPAD, grain yield.

The finishing mechanism of the ball end Magnetorheological finishing (BEMRF) process mainly depends on the stiffened hemispherical ball of Magnetorheological polishing (MRP) fluid formed at the tool tip. MRP fluid imparts strength to the polishing spot with the effect of magnetic field strength. Behaviour of this polishing fluid mainly depends on the size and shape of its constituents, volume concentration, particle size distribution and applied magnetic field strength. Rheological properties such as yield stress and viscosity of MRP fluid play a very important role while finishing the work piece surfaces. Evaluation of the behaviour of MR polishing fluid for silicon polishing was attempted through designing and fabrication of parallel plate magnetorheometer.

Purpose This study evaluated the longitudinal metabolic alterations after neonatal hypoxia-ischemia (HI) in rats and tested the neuroprotective effect of acetyl-L-carnitine (ALCAR) using in vivo proton short-TE Point-RESolved Spectroscopy method. Methods Rice-Vannucci model was used on 7-day-old Sprague-Dawley rats. Data were acquired from contralateral and ipsilateral cortex and hippocampus, respectively at 4 time points (24-h, 72-h, 7-days, 28-days) post-HI. The effect of subcutaneous administration of ALCAR (100 mg/kg) immediately after HI, at 4-h, 24-h, and 48-h post-HI was determined. Results Significant reductions in glutathione (P < 0.005), myo-inositol (P < 0.002), taurine (P < 0.001), and total creatine (P < 0.005) were observed at 24-h postinjury compared with the control group in the ipsilateral hippocampus of the HI rat pups. ALCAR-treated-HI rats had lower levels of lactate and maintained total creatine at 24-h and had smaller lesion size compared with the HI only rats. Conclusion Severe oxidative, osmotic stress, impaired phosphorylation, and a preference for anaerobic glycolysis were found in the ipsilateral hippocampus in the HI pups at 24-h postinjury. ALCAR appeared to have a neuroprotective effect if administered early after HI by serving as an energy substrate and promote oxidative cerebral energy producing and minimize anaerobic glycolysis. Magn Reson Med 74:1530–1542, 2015. © 2014 Wiley Periodicals, Inc.

Beef Tallow Methyl Ester (BTME) was tried in an Indirect Diesel Injection (IDI) engine with super charger and secondary injection of hydrated ethyl alcohol as an additive at the suction end. The additive was injected at 3bar in to the incoming air without affecting the breathing capacity of the engine. Alcohol injection is resorted to ensure low temperature combustion. The additive starting from 2% to 8% was injected in steps of 2% increase. For all these percentages of additive, the combustion pressures and tail pipe emissions were measured to compare the engine performance in these aspects with respect to diesel fuel. The experimentation revealed that the biodiesel with 2% hydrated ethyl alcohol proved to be befitting replacement to the diesel fuel.

Objective: The research aims to formulate and develop the controlled release profile of glibenclamide by encapsulating glibenclamide into niosomes followed by incorporation into an aqueous gel base. Materials and methods: Glibenclamide incorporated niosomes were prepared by a modified ether injection technique using Span 20/Span 80 and cholesterol. The prepared niosomes were evaluated for chemical incompatibility by FT-IR, morphology, vesicle dimension, encapsulation efficiency, in-vitro diffusion and drug release kinetics. Niosomal gels were prepared by incorporating the optimized niosomes into a gel base containing Carbopol 934 and evaluated for viscosity, in-vitro diffusion and in-vivo pharmacodynamic activity. Results and discussion: The results indicated that relationship between the amount of Span and niosomal vesicular diameter was inversely proportional. Microscopic images have illustrated the sphere shape vesicles. The cumulative percentage of drug release from niosomal suspension was observed in the order GN-4>GN-2>GN- 6>GN-5>GN-3>GN-1. Glibenclamide gel showed highest percentage drug release when compared to niosomal gel. Invivo study revealed that the glibenclamide incorporated niosomal gel formulation; GNG-1 is more efficient in lowering blood glucose levels in experimental animals. Conclusion: The niosomal gel of glibenclamide had released the drug in well controlled manner which is supported by pharmacodynamic activity with evidence of consistent lowering of blood glucose levels.