An approach for predicting the occurrence of interveinal chlorosis in Anab-e-Shahi grape (Vitis vinifera L.)

With a view to evolve a criterion to predict the occurrence of interveinal chlorosis of Anab-e-Shahi at different stages of fruit development, the calcium and magnesium contents of the petioles and leaf blades at full bloom stage were compared. Hypotheses were formulated, by which a 96 percent accuracy in prediction was made possible. Versuch einer Prognose der Interkostalchlorose bei der Sorte Anab-e-Shahi Um ein Kriterium für die Vorhersage der Interkostalchlorose in den verschiedenen Phasen der Beerenentwicklung von Anab-e-Shahi zu erarbeiten, wurde der Calcium- und Magnesium-Gehalt in den Blattstielen und Blattspreiten zur Zeit der Anthesis verglichen. Es werden Hypothesen formuliert, die mit 96%iger Wahrscheinlichkeit eine Prognose ermöglichen

ANTIMICROBIAL AND IN SILICO ADMET SCREENING OF NOVEL (E)-N-(2-(1H-INDOL-3-YL-AMINO) VINYL)-3-(1-METHYL-1H-INDOL-3-YL)-3-PHENYLPROPANAMIDE DERIVATIVES

Objective: Synthesis, in silico absorption, distribution, metabolism, excretion, toxicity (ADMET) and in vitro antimicrobial screening of (E)-N-(2-(1H-indol-3-ylamino) vinyl)-3-(1-methyl-1H-indol-3-yl)-3-phenylpropanamide derivatives.Methods: (E)-N-(2-(1H-indol-3-ylamino) vinyl)-3-(1-methyl-1H-indol-3-yl)-3 phenylpropane-amide derivatives were synthesized by combining indole ethanolamine and substituted Meldrum's adduct. The synthesized compounds were subjected to in vitro antimicrobial study by cup plate method and in silico ADMET properties using ACD/I-Lab 2.0.Results: The in vitro antimicrobial screening against precarious pathogenic microorganisms viz, Pseudomonas aureginosa, Staphylococcus aureus, Escherichia coli, Vibrio cholerae, and the antifungal activity against Candida albicans, Aspergillus niger, Penicillin chrysogenum and Cladosporium oxysporum strains. The results revealed that compounds 5b, 5c, 5d and 5e showed good antimicrobial property and obeyed the in silico pharmacokinetic parameters.Conclusion: The encouraging results exhibited by the compounds (E)-N-(2-(1H-indol-3-ylamino) vinyl)-3-(1-methyl-1H-indol-3-yl)-3-phenyl propanamide derivatives, 5(a-e) can be explored as possible hits in antimicrobial therapy. The molecules obey the Lipinski rule of five when tested in silico and can be used in understanding the quantitative structure-activity relationship (QSAR) parameters

Challenges and opportunities for policy decisions to address health equity in developing health systems: case study of the policy processes in the Indian state of Orissa

<p>Abstract</p> <p>Introduction</p> <p>Achieving health equity is a pertinent need of the developing health systems. Though policy process is crucial for planning and attaining health equity, the existing evidences on policy processes are scanty in this regard. This article explores the magnitude, determinants, challenges and prospects of 'health equity approach' in various health policy processes in the Indian State of Orissa - a setting comparable with many other developing health systems.</p> <p>Methods</p> <p>A case-study involving 'Walt-Gilson Policy Triangle' employed key-informant interviews and documentary reviews. Key informants (n = 34) were selected from the departments of Health and Family Welfare, Rural Development, and Women and Child Welfare, and civil societies. The documentary reviews involved various published and unpublished reports, policy pronouncements and articles on health equity in Orissa and similar settings.</p> <p>Results</p> <p>The 'health policy agenda' of Orissa was centered on 'health equity' envisaging affordable and equitable healthcare to all, integrated with public health interventions. However, the subsequent stages of policy process such as 'development, implementation and evaluation' experienced leakage in the equity approach. The impediment for a comprehensive approach towards health equity was the nexus among the national and state health priorities; role, agenda and capacity of actors involved; and existing constraints of the healthcare delivery system.</p> <p>Conclusion</p> <p>The health equity approach of policy processes was incomprehensive, often inadequately coordinated, and largely ignored the right blend of socio-medical determinants. A multi-sectoral, unified and integrated approach is required with technical, financial and managerial resources from different actors for a comprehensive 'health equity approach'. If carefully geared, the ongoing health sector reforms centered on sector-wide approaches, decentralization, communitization and involvement of non-state actors can substantially control existing inequalities through an optimally packaged equitable policy. The stakeholders involved in the policy processes need to be given orientation on the concept of health equity and its linkage with socio-economic development.</p

ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES

Objective: The objective of the study is acetylcholinesterase (AChE) inhibitory effect of 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives by Ellman's method, physostigmine is used as positive control.Method: 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were synthesized by the addition of chalcone (0.25 g, 1 mmol), indole (0.12 g, 1 mmol) in ethanol (5 ml), and concentrated hydrochloric acid (5 mmol %). These earlier synthesized compounds were screened for AChE inhibitors by modifying Ellman's method.Results: Among the tested compounds, 3a and 3j were found to be having more potential than other compounds with half maximal inhibitory concentration values of 13.64 and 14.3 μg/ml, respectively. Whereas, compounds 3c, 3e, 3g, and 3i exhibited an average AChE inhibition of 16.4, 17.9, 17.6, and 21.1 μg/ml, respectively.Conclusion: The compounds 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were found to be possible lead molecules in AChE inhibition and even though, the molecules were structurally dissimilar to that of the standard, still they exhibited a considerable degree of inhibition and encourage the researchers to look into the mode of action of their inhibition ability against AChE

On the spectrum of weakly almost periodic solutions of certain abstract differential equations

In a sequentially weakly complete Banach space, if the dual operator of a linear operator A satisfies certain conditions, then the spectrum of any weakly almost periodic solution of the differential equation u′=Au+f is identical with the spectrum of f except at the origin, where f is a weakly almost periodic function

ANTIPROLIFERATIVE, ADME AND POTENTIAL IN SILICO G6PDH INHIBITORY ACTIVITY OF NOVEL 2-(1-BENZOFURAN-2-YL)-4-(5-PHENYL-4H-1, 2, 4-TRIAZOL-3-YL) QUINOLINE DERIVATIVES

Objectives: Synthesis of new 2-(1-benzofuran-2-yl)-4-(5-phenyl-4H-1, 2, 4-triazol-3-yl) quinoline and its derivatives for antiproliferative potential against cancer cells.Methods: The general methods were employed for the synthesis and the structures were confirmed by IR, 1H-NMR, 13C-NMR and mass spectral analysis. The antiproliferative activity was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and molecular docking study were performed by Auto Dock Tools. In silico Absorption-Distribution-Metabolism-Excretion-Toxicity (ADMET) study for the drug, likeliness was carried out on ACD/lab-2.Results: The compound 3l showed 44, 44, 38 and 37 % inhibition against MCF-7, HepG2, Colo205 and HeLa cell lines, respectively; whereas, the compounds 3i and 3j exhibited 49 and 42 % inhibition against MCF-7 cell line. The molecular docking study revealed that the compound 3i has the lowest binding energy (-8.60 Kcal mol-1), suggesting to be potentially best inhibitor of Glucose-6-phosphate dehydrogenase (G6PDH). The in silico ADME analysis also revealed that compound 3i does not violate any of the Lipinski rules of five and has the best stimulative human colonic absorption up to 95 %.Conclusion: The study reveals that the compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics.Â

Systematic prediction of DNA shape changes due to CpG methylation explains epigenetic effects on protein–DNA binding

Background DNA shape analysis has demonstrated the potential to reveal structure-based mechanisms of protein–DNA binding. However, information about the influence of chemical modification of DNA is limited. Cytosine methylation, the most frequent modification, represents the addition of a methyl group at the major groove edge of the cytosine base. In mammalian genomes, cytosine methylation most frequently occurs at CpG dinucleotides. In addition to changing the chemical signature of C/G base pairs, cytosine methylation can affect DNA structure. Since the original discovery of DNA methylation, major efforts have been made to understand its effect from a sequence perspective. Compared to unmethylated DNA, however, little structural information is available for methylated DNA, due to the limited number of experimentally determined structures. To achieve a better mechanistic understanding of the effect of CpG methylation on local DNA structure, we developed a high-throughput method, methyl-DNAshape, for predicting the effect of cytosine methylation on DNA shape. Results Using our new method, we found that CpG methylation significantly altered local DNA shape. Four DNA shape features—helix twist, minor groove width, propeller twist, and roll—were considered in this analysis. Distinct distributions of effect size were observed for different features. Roll and propeller twist were the DNA shape features most strongly affected by CpG methylation with an effect size depending on the local sequence context. Methylation-induced changes in DNA shape were predictive of the measured rate of cleavage by DNase I and suggest a possible mechanism for some of the methylation sensitivities that were recently observed for human Pbx-Hox complexes. Conclusions CpG methylation is an important epigenetic mark in the mammalian genome. Understanding its role in protein–DNA recognition can further our knowledge of gene regulation. Our high-throughput methyl-DNAshape method can be used to predict the effect of cytosine methylation on DNA shape and its subsequent influence on protein–DNA interactions. This approach overcomes the limited availability of experimental DNA structures that contain 5-methylcytosine

Ethyl 4-(4′-heptanoyloxyphenyl)-6-methyl-3,4-dihydropyrimidin-2-one-5-carboxylate Prevents Progression of Monocrotaline-induced Pulmonary Arterial Hypertension in Rats

Therapies to prevent onset and progression of pulmonary arterial pressure are not very effective yet. This study was designed to investigate the effects of a novel dihydropyrimidinone, ethyl 4-(4′-heptanoyloxyphenyl)-6-methyl-3,4-dihydropyrimidin-2-one-5-carboxylate (H-DHPM) on pathogenesis of monocrotaline (MCT)-induced pulmonary arterial hypertension (PAH). For the same purpose, rats were injected intraperitoneally (i.p.) a single dose (60 mg/kg) of MCT which led to development of PAH in 21 days. MCT insult caused high mortality, pulmonary vascular and parenchymal remodelling. Since the course of PAH pathogenesis is characterised by an early onset and progression phases, H-DHPM was administered i.p. at 30 mg/kg dosage in MCT pre-injected animals either from day 0 through day 21 or day 14 though day 21 of MCT injection in two separate treatment groups. H-DHPM significantly improved survival, prevented remodelling of pulmonary vasculature and parenchyma and subsequently ameliorated PAH pathogenesis. Moreover, we observed significant decrease in right ventricle hypertrophy, measured by wet weight of right ventricle (RV) divided by wet weight of left ventricle plus septum (LV+S), in H-DHPM treated groups as compared to MCT injected animals. These findings suggest H-DHPM not only prevented development of PAH but also treated the PAH pathogenesis in progressive phase. In conclusion, our data determines H-DHPM, might be a future drug for the prevention of PAH

Sensitization and translocation of TRPV1 by insulin and IGF-I

Insulin and insulin-like growth factors (IGFs) maintain vital neuronal functions. Absolute or functional deficiencies of insulin or IGF-I may contribute to neuronal and vascular complications associated with diabetes. Vanilloid receptor 1 (also called TRPV1) is an ion channel that mediates inflammatory thermal nociception and is present on sensory neurons. Here we demonstrate that both insulin and IGF-I enhance TRPV1-mediated membrane currents in heterologous expression systems and cultured dorsal root ganglion neurons. Enhancement of membrane current results from both increased sensitivity of the receptor and translocation of TRPV1 from cytosol to plasma membrane. Receptor tyrosine kinases trigger a signaling cascade leading to activation of phosphatidylinositol 3-kinase (PI(3)K) and protein kinase C (PKC)-mediated phosphorylation of TRPV1, which is found to be essential for the potentiation. These findings establish a link between the insulin family of trophic factors and vanilloid receptors