Designing and Synthesis of Flavonoids Derivatives and Screening of their Antioxidant Activity

The flavonoids present in red wine were responsible this low cardiovascular mortality rate. Epidemiologic studies further suggest that dietary flavonoids are useful to control and protect the CHD. The flavonoids are yellow color substance (pigments) and the name given on the basis of Latin term Flavus which means yellow color. Flavonoids are derivatives of benzo-pyrone. Banzopyrone is a group of heterocyclic aromatic oxygen containing compounds. Finely powdered zinc chloride (8.25) was dissolved in glacial acetic acid (18ml)  by heating on sand bath then dry resorcinol (appx.5.5 gm) was added with  continuous  stirring to the mixture at  1400C. Antioxidant Screening by hydrogen peroxide scavenging assays. Hydrogen peroxide solution (40 mini moles) was prepared with standard phosphate buffer of pH 7.4. Different concentration of the compound stock solution and 4ml distilled water was added to 0.6 ml of hydrogen peroxide solution. UV absorbance was determined at the wavelength of 230 nm after 10 min with a blank solution containing phosphate buffer without H2O2. Take 4 ml different concentration of sample solution and 1ml sodium nitroprusside solution, added and incubated for 2.5 hrs at 370C. After incubation baseline was taken with methanol and 1ml sodium nitroprusside solution as blank solution. Griess reagent and methanol was added immediately before recording of readings. The readings were recorded at 546nm wavelenth. In the series of synthesized and evaluated compounds of Flavanoid electron withdrawing group at position four shows good activity. 2,3-dihydroflavan-3-ol derivatives showed lower activity than that of 3- hydroxyflavone derivatives. The 4-oxo (keto double bond at position 4 of the C ring), especially in association with the J2-J3 double bond, increases scavenger activity by delocalizing electrons, 3-hydroxy group on the C ring generates an extremely active scavenger; the combination of J2-J3 double bond,3-hydroxy group and 4-oxo group appears to be the best combination for potent antioxidant activity. Keywords: Flavonoids, Antioxidant activity, Hydrogen peroxide scavenging, free radical

Detection of Congenital Heart Disease by Fetal Echocardiography and Its Correlation with Karyotype

Background: Congenital heart diseases (CHDs) account for a third of all major congenital abnormalities in children; nearly 1,80,000 children are born with heart defect each year in India. Approximately, 10% of present infant mortality in India may be attributed to CHD alone. Such high mortality is due to laying less emphasis on its prenatal diagnosis by fetal echocardiography. This study was done with objectives to find out the incidence of CHD in high risk cases and its correlation with karyotype and also evaluating the diagnostic accuracy of fetal echocardiography. Methods: Fetal echocardiography was performed in 142 high risk cases who attended antenatal clinic of Institute of Medical Sciences (IMS), Banaras Hindu University (BHU), Varanasi between July 2014 to June 2016 with maternal/fetal risk for CHD (maternal diabetes mellitus, collagen disorders, teratogen exposure, maternal TORCH infection, in vitro fertilization [IVF] conceived pregnancy, familial history of CHD, abnormal four-chamber view, monochorionic twins). Results: The incidence of major CHD was 28/1,000 live births and 56/1,000 live births for minor CHD in high risk group. Ventricular septal defect (16.6%) and hypoplastic left heart syndrome (16.6%) were the most common CHD detected. Family history of CHD increases the risk significantly. Fetal echocardiography was 75% (46.77-91.11, 95% confidence interval [CI]) sensitive and 94.5% (89.22-97.35, 95% CI) specific, with 92.91% (87.44-96.1, 95% CI) diagnostic accuracy. It was seen that 16.6% cases of CHD had aneuploidy detected on karyotyping (trisomy 21 and trisomy 18). Conclusion: Fetal echocardiography is highly sensitive and specific, when done by an experienced operator. Prenatal diagnosis of CHD and planned delivery in a cardiac facility had satisfactory immediate outcomes

Synthesis and Evaluation of Phenol Derivatives of Sulfonyl Chloride Quinoxaline

The objective of the present study was to synthesize some new 7-sulfonate of 2, 3- Diphenyl quinoxaline which are more potential as antibacterial than parent quinoxalines. The present study was synthesis of derivatives of sulfonyl chloride quinoxaline and physicochemical and spectral characterization, in vitro antimicrobial screening against gram positive and gram negative bacteria.The concentration of derivatives used as 200 and 400 microgram initially. When 200 µg concentrations was used R6 shows sensitivity towards S. aureus and R6 shows sensitivity towards gram negative E. coli organism. When 400 µg used then R3, R5, and R6 shows sensitivity in case of gram positive organism. And in case of gram negative organism R5, R6 shows sensitivity.Azithromycin is used as Reference drug and a comparative study was done. As compare to reference drug all derivatives shows less sensitivity than S- Standard and R- quinoxaline derivatives. Keywords: Diphenyl quinoxaline, QSAR, Quinoxaline, Phenol derivative

Formulation Development and Evaluation of Floating Microsphere of Famotidine for the Treatment of Peptic Ulcer

The purpose of this research was to prepare a floating drug delivery system of famotidine. The floating microspheres can be prepared for the improvement of absorption and bioavailability of famotidine by retaining the system in the stomach for prolonged period of time. Floating microspheres of famotidine were prepared using different polymers like ethyl cellulose, hydroxy propyl methyl cellulose by solvent diffusion-evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres was up to 73.32±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in 331.6 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to 73.25±0.23. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of famotidine offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved. Keywords: Famotidine, Solvent diffusion evaporation method, Ethyl cellulose, Hydroxyl propyl methyl cellulos

Real-world clinical experience of ticagrelor in Indian patients with acute coronary syndrome after discharge from a tertiary setting

Background: To understand the usage pattern of ticagrelor in real-life clinical experience in Indian patients with the acute coronary syndrome (ACS) after discharge from a tertiary care setting. Methods: A retrospective multicentric observational study conducted across Indian healthcare centers having medical records of adult patients with ACS. Patients prescribed with ticagrelor post-discharge for at least 1 month were included. The study endpoints were to determine the clinical effectiveness of ticagrelor in post-ACS patients and adverse events reported during the study period. Results: A total of 1910 patients with ACS with a mean (SD) age of 58.2 (11.3) years were enrolled in this study. The median (IQR) duration of treatment was 30.0 (30.0-90.0) days. More than half of the patients (n=1115, 58.4%) were managed with interventional therapy. The most common comorbid conditions were type-2 diabetes mellitus (46.9%), followed by hypertension (36.8%). A total of 9.7% of patients reported complaints after treatment with ticagrelor. Among them, weakness, giddiness, and body pain were the most common (3.2%). Conclusions: This real-world study revealed that ticagrelor had been used widely in patients who underwent different management strategies. History of diabetes and hypertension were the most common risk factors. There were no major adverse events reported during the follow-up, indicating ticagrelor is well-tolerated in Indian patients with ACS

Poor emotional responsiveness in clinical hypertension:Reduced accuracy in the labelling and matching of emotional faces amongst individuals with hypertension and prehypertension

Tese de Doutoramento em Engenharia Mecânica, no ramo de Gestão e Robótica Industrial, apresentada ao Departamento de Engenharia Mecânica da Faculdade de Ciências e Tecnologia da Universidade de CoimbraA presente tese foca-se na integração e avaliação de metodologias distintas com o objetivo de fazer a deteção de limões nas árvores em cenários naturais, ou seja, de cenários com iluminação não controlada. A proposta apresentada dista das restantes abordagens, discutida na revisão bibliográfica, por ser endereçada a um fruto até agora não avaliado e por apostar num sistema de visão artificial simples, passível de ser aplicado em contexto real de trabalho. De acordo com o estado da arte, os métodos de aprendizagem supervisionada são os mais eficazes na segmentação e deteção dos frutos nas condições precedentes. Com base neste pressuposto foi criada uma base de dados de referência, composta por cinco classes de elementos, para treino e avaliação dos classificadores SVM na segmentação das imagens. Adicionalmente, um outro conjunto de imagens é usado para avaliar a deteção dos frutos através de classificadores baseados nos métodos de Haar, HOG e LBP. A segmentação inicial das imagens é realizada a partir de uma árvore de decisão, em que é avaliada a resposta do modelo a um classificador SVM denominado global, treinado segundo a estratégia um contra todos, e a outros dois modelos compostos por vários classificadores SVM, treinados com a estratégia um contra um. Em qualquer um destes casos, o objetivo é separar os pixels dos limões da restante imagem, pelo que, no final, a avaliação do desempenho dos modelos de classificação é realizada considerando apenas duas classes de elementos (C=2), a classe dos limões e a classe do background. Devido à elevada quantidade de combinações possíveis de características de cor e parametrizações do SVM é proposto um método que convirja para as soluções de classificação ótimas. Além disso, este método é responsável pela determinação das características, aparentemente mais significativas para a correta segmentação dos frutos, ao longo dos vários estágios de treino em que se incrementa o número de características a analisar. Com as imagens segmentadas são avaliadas as respostas de diversos classificadores na deteção dos frutos nas árvores, onde se conclui que os métodos de Haar e HOG permitem melhores resultados do que os classificadores LBP, contrariamente ao que seria esperado, de acordo com a bibliografia revista. A metodologia de segmentação dos frutos proposta, para as 133 imagens de teste, apresenta uma taxa média de TP = 93.14 % para uma taxa de FP = 2.34 %, através da aplicação do classificador SVM, designado de global. Este processo de segmentação tem um tempo de execução, em média, de 145 ms. Relativamente à deteção dos limões, a configuração que resulta na maior deteção dos frutos visíveis nas 44 imagens apresenta como desempenho uma Precision = 80.19 % e Recall = 92.39 %, atingidos por um classificador de Haar executado, em média com uma duração de 36 ms por imagem; porém, se para a aplicação final for mais relevante a menor ocorrência de falsos-alarmes, o melhor modelo de classificação é obtido com a metodologia HOG, executada em 50 ms, onde se obtém uma Precision = 85.37 % e Recall = 76.09 %. Os resultados alcançados por um simples sistema de visão artificial, apenas com aquisição de imagens a cores no espectro visível, estão ao nível dos melhores resultados alcançados e identificados na literatura revista. Excetuam-se apenas os resultados conseguidos pela introdução de modelos de Deep Learning. Apesar dos resultados alcançados, e em função dos modelos de cor usados para atenuar os impactos das variações das condições de luz, é admissível que a metodologia proposta possa falhar em condições de iluminação deficiente. Nestes casos é recomendável a utilização de iluminação artificial, que poderá até aumentar o contraste entre os frutos e os restantes elementos captados nas imagens. Além disso é benéfica a introdução de metodologias que permitam a correta de deteção de frutos que se encontrem parcialmente sobrepostos.This thesis is focused on the integration and evaluation of several methodologies aiming to detect lemons on trees in natural outdoor scenarios, without controlled light conditions. Current approach is different from the previous ones identified on literature, because it addresses a fruit not evaluated before using a simple vision system, which only acquire RGB images, suitable for real tasks conditions. Based on state of the art review, the supervised learning methods are more effective than the unsupervised ones to segment and detect fruits in uncontrolled light scenarios. Considering such previous findings, it is created a reference database of lemons fruits scenarios to train, validate and test SVM classifiers and also to evaluate the performance of Haar, HOG and LBP classifiers. Segmentation of citrus fruits is performed by a decision tree and three different schemes of SVM classifiers: through a global classifier trained by the strategy of one vs all; and through two sets of SVM classifiers, trained differently, by the strategy one vs one. The final performance evaluation is a two class problem, because only interests to distinguish between the remaining scenario and lemons in each image. To avoid constraints from light changes on RGB color space, all simulations are performed using color components from YCbCr, HSV and chromaticity color spaces. Additionally, they were created two color indexes derived from chromaticity color space. Evaluating all combinations of color components plus SVM parameters by brute-force methods, it is an inefficient process. So, it is proposed a method based on hill-climbing algorithm that converge to the optimal configuration on SVM parametrization. After each stage of training and aiming to increase the number of features evaluated by SVM, it is proposed a method that filter the best set of features for further evaluations based on AUC (Area Under the Curve) results. Since the ground truth database is not extensive as desired and its population contains some noise, it is proposed another method to split the data to train, validate and test the classifiers, instead of traditional k-fold. According to achieved results, this proposal fits well on the presented case. Using the SVM-based segmented images, they are evaluated the Haar, HOG and LBP classifiers to perform the fruits detection. In opposition to previous findings, Haar and HOG classifiers performs better than LBP. For the 133 images used to test segmentation methods, the best response is achieved by the global classifier related to true-positive rate of 93.14 % and a false-positive rate of 2.34 %. For such configuration, the segmentation is performed by 145 ms on average. About detection, the best Recall of 92.39 % corresponds to a Precision of 80.19 % achieved by Haar classifiers, executed in 36 ms. If the precision is relevant for a specific application, the best result corresponds to the use of HOG classifiers that response with a Precision of 85.37 % to a Recall of 76.09 %, executed on 47 ms on average per image. Current results achieved by a simple vision system and by acquiring only RGB images are similar to the state of the art results, except when compared to Deep Learning methods whose perform better but also more computationally demanding to train. Notwithstanding promising results, the proposed methodology tends to fail when exposed to low light scenarios. In such conditions it is highly advisable to use controlled external light sources, not only to compensate the low light conditions, but also to enhance the contrast between fruits and the remaining scenario. Additionally, it may be useful the introduction of new methods in order to detect correctly individual fruits grouped.FCT – Fundação para a Ciência e a Tecnologia, projeto: UID/EMS/00285/201

Development of Micro-Emulsion Gel Based Topical Delivery of Salicylic Acid and Neem Oil for the Management of Psoriasis

Microemulsions (MEs) are clear, thermodynamically stable systems. They were used to solubilise drugs and to improve topical drug availability. Salicylic acid (SA) is a keratolytic agent used in topical products with antimicrobial actions. This study aimed to formulate an optimized SA micro emulsion gel for the slow, variable and incomplete oral drug absorption in patient suffering from psoriasis infection. The dispersion solubility of SA was studied in various oils, surfactants and co-surfactants and by constructing pseudo phase ternary diagram, micro emulsion area was identified. The optimized formulations of micro emulsion were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in micro emulsion, zeta Potential and vesicle size measurement and then micro emulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Labrasol was selected as surfactant, plurol oleique as co surfactant and neem oil as oil component based on solubility study. The optimized formulation contained SA 0.05 (%w/w), labrasol (24%), plurol oleique (8 %) and neem oil (8%). The in vitro drug release from SA micro emulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of micro emulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of SA can be increased by formulating into micro emulsion gel. Keywords: Salicylic Acid, Neem Oil, Micro-emulsion, In-vitro diffusion, Zeta potential, Stability, Labraso

Formulation Development and Evaluation of Lansoprazole Mucoadhesive Microsphere

Lansoprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but rather suppress gastric acid secretion by specific inhibition of the (H+,K+)-ATPase enzyme system at the secretary surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The aim of the present study was to develop lansoprazole loaded thiolated chitosan microspheres were prepared by emulsifying method using liquid paraffin light and heavy in ratio of 50:50 as a dispersing medium and glutaraldehyde used as a cross-linking agent. The prepared microspheres were evaluated for mean particle size and particle size distribution, drug content, mucoadhesion measurement and in-vitro drug release. FT-IR spectroscopic analysis was performed to ascertain drug polymer interaction. The release profiles showed first order release behavior up to 12 hours where the highest drug release was 88.89 % of the lansoprazole loaded in the thiolated chitosan microspheres, indicating a strong crosslinking between chitosan and glutaraldehyde. From the results of the present investigation it may be concluded that drug loaded chitosan microspheres can be prepared by a simple technique which avoids the use of complex apparatus and special precautions. Keywords: Lansoprazole, Thiolated chitosan, Microspheres, Glutaraldehyde, Mucoadhesion measuremen

Assessing the feasibility of integrating ecosystem-based with engineered water resource governance and management for water security in semi-arid landscapes: A case study in the Banas catchment, Rajasthan, India

Much of the developing world and areas of the developed world suffer water vulnerability. Engineering solutions enable technically efficient extraction and diversion of water towards areas of demand but, without rebalancing resource regeneration, can generate multiple adverse ecological and human consequences. The Banas River, Rajasthan (India), has been extensively developed for water diversion, particularly from the Bisalpur Dam from which water is appropriated by powerful urban constituencies dispossessing local people. Coincidentally, abandonment of traditional management, including groundwater recharge practices, is leading to increasingly receding and contaminated groundwater. This creates linked vulnerabilities for rural communities, irrigation schemes, urban users, dependent ecosystems and the multiple ecosystem services that they provide, compounded by climate change and population growth. This paper addresses vulnerabilities created by fragmented policy measures between rural development, urban and irrigation water supply and downstream consequences for people and wildlife. Perpetuating narrowly technocentric approaches to resource exploitation is likely only to compound emerging problems. Alternatively, restoration or innovation of groundwater recharge practices, particularly in the upper catchment, can represent a proven, ecosystem-based approach to resource regeneration with linked beneficial socio-ecological benefits. Hybridising an ecosystem-based approach with engineered methods can simultaneously increase the security of rural livelihoods, piped urban and irrigation supplies, and the vitality of river ecosystems and their services to beneficiaries. A renewed policy focus on local-scale water recharge practices balancing water extraction technologies is consistent with emerging Rajasthani policies, particularly Jal Swavlamban Abhiyan (‘water self-reliance mission’). Policy reform emphasising recharge can contribute to water security and yield socio-economic outcomes through a systemic understanding of how the water system functions, and by connecting goals and budgets across multiple, currently fragmented policy areas. The underpinning principles of this necessary paradigm shift are proven and have wider geographic relevance, though context-specific research is required to underpin robust policy and practical implementation

A bibliography of parasites and diseases of marine and freshwater fishes of India

With the increasing demand for fish as human food, aquaculture both in freshwater and salt water is rapidly developing over the world. In the developing countries, fishes are being raised as food. In many countries fish farming is a very important economic activity. The most recent branch, mariculture, has shown advances in raising fishes in brackish, estuarine and bay waters, in which marine, anadromous and catadromous fishes have successfully been grown and maintained