Search results for: drugs

Authors: Ľudmila Ballová, Slavomír Kurhajec, Eva Petrovová, Jarmila Eftimová

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Angiogenesis, a formation of new blood vessels from a pre-existing vasculature, plays an important role in pathologic processes such as the growth and metastasis of tumours. Tumours cannot grow beyond a few millimetres without blood supply from the newly formed blood vessels from the host tissue, a process called tumour-induced angiogenesis. The successful research of antiangiogenic treatment of cancer has focused on nutraceuticals with angiogenesis-modulating properties. Berberine, as a major active component of the bark of Phellodendron amurense Rupr., has shown antitumour activity by intervening into different steps of carcinogenesis. The influence of ethanolic extract of Phellodendron amurese bark on the angiogenesis was tested in vivo on chick chorioallantoic membrane (CAM). The irritancy of the CAM after the application of the crude bark extract dissolved in normal saline (10 mg/mL) was investigated on embryonic day 7. No significant signs of the irritancy, such as vasoconstriction, hyperaemia, haemorrhage or coagulation were observed which indicates the harmless character of the extract. A significant reduction in vessel sprouting and higher percentage of avascular zone was observed in the case of CAM treated with the extract in comparison with non-treated CAM (control), which is a proof of the antiangiogenic potential of the extract. These results could contribute to the development of novel drugs for the treatment of cancer or other diseases, in which angiogenesis plays a significant role.

Keywords: Angiogenesis, berberine, chorioallantoic membrane, Phellodendron amurense.

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Authors: Anita, Sari Septiani Tangke, Rusdina Bte Ladju, Nasrum Massi

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New diagnostic tools are urgently needed to interrupt the transmission of tuberculosis and multidrug-resistant tuberculosis. The microscopic-observation drug-susceptibility (MODS) assay is a rapid, accurate and simple liquid culture method to detect multidrug-resistant tuberculosis (MDR-TB). MODS were evaluated to determine a lower and same concentration of isoniazid and rifampin for detection of MDR-TB. Direct drug-susceptibility testing was performed with the use of the MODS assay. Drug-sensitive control strains were tested daily. The drug concentrations that used for both isoniazid and rifampin were at the same concentration: 0.16, 0.08 and 0.04μg per milliliter. We tested 56 M. tuberculosis clinical isolates and the control strains M. tuberculosis H37RV. All concentration showed same result. Of 53 M. tuberculosis clinical isolates, 14 were MDR-TB, 38 were susceptible with isoniazid and rifampin, 1 was resistant with isoniazid only. Drug-susceptibility testing was performed with the use of the proportion method using Mycobacteria Growth Indicator Tube (MGIT) system as reference. The result of MODS assay using lower concentration was significance (P<0.001) compare with the reference methods.

A lower and same concentration of isoniazid and rifampin can be used to detect MDR-TB. Operational cost and application can be more efficient and easier in resource-limited environments. However, additional studies evaluating the MODS using lower and same concentration of isoniazid and rifampin must be conducted with a larger number of clinical isolates.

Keywords: Isoniazid, MODS assay, MDR-TB, Rifampin.

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Authors: S. Nasri, G. H. Amin, A. Azimi

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The use of herbs to treat disease is accompanied with the history of human life. This research is aimed to study the anti-inflammatory and antinociceptive effects of hydroalcoholic extract of aerial parts of "Tanacetum balsamita balsamita". In the experimental studies 144 male mice are used. In the inflammatory test, animals were divided into six groups: Control, positive control (receiving Dexamethason at dose of 15mg/kg), and four experimental groups receiving Tanacetum balsamita balsamita hydroalcoholic extract at doses of 25, 50, 100 and 200mg/kg. Xylene was used to induce inflammation. Formalin was used to study the nociceptive effects. Animals were divided into six groups: control group, positive control group (receiving morphine) and four experimental groups receiving Tanacetum balsamita balsamita (Tb.) hydroalcoholic extract at doses of 25, 50, 100 and 200mg/kg. I.p. injection of drugs or normal saline was performed 30 minutes before test. The data were analyzed by using one way Variance analysis and Tukey post test. Aerial parts of Tanacetum balsamita balsamita hydroalcoholic extract decreased significantly inflammatory at dose of 200mg/kg (P<0/001) and caused a significant decrease and alleviated the nociception in both first and second phases at doses of 200mg/kg (p<0/001) and 100mg/kg (P<0/05). Tanacetum balsamita balsamita extract has the anti-inflammatory and anti-nociceptive effects which seems to be related with flavonoids especially Quercetin.

Keywords: Inflammation, nociception, Hydroalcoholic extract, aerial parts of Tanacetum balsamita balsamita L.

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Authors: Mohammad Aziz Shah Mohamed Arip, Aslina Ahmad, Fauziah Mohd Sa'ad, Samsiah Mohd Jais, Syed Sofian Syed Salim

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This experimental study evaluates the effect of using Cognitive-Behavioral Therapy (CBT) and Multidimensional Self- Concept Model (MSCM) in a drug prevention programme to increase resiliency and reduce aggression among at-risk youth in Malaysia. A number of 60 (N=60) university students who were at-risk of taking drugs were involved in this study. Participants were identified with self-rating scales, Adolescent Resilience Attitude Scale (ARAS) and Aggression Questionnaire. Based on the mean score of these instruments, the participants were divided into the treatment group, and the control group. Data were analyzed using t-test. The finding showed that the mean score of resiliency was increased in the treatment group compared to the control group. It also shows that the mean score of aggression was reduced in the treatment group compared to the control group. Drug Prevention Programme was found to help in enhancing resiliency and reducing aggression among participants in the treatment group compared to the controlled group. Implications were given regarding the preventive actions on drug abuse among youth in Malaysia.

Keywords: Drug Prevention Programme, Cognitive-Behavioral Therapy (CBT), Multidimensional Self Concept Model (MSCM), resiliency, aggression, at-risk youth.

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Authors: Deepak Kukkar, Inderpreet Kaur, Jagtar Singh, Lalit M Bharadwaj

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Polymeric microreactors have emerged as a new generation of carriers that hold tremendous promise in the areas of cancer therapy, controlled delivery of drugs, for removal of pollutants etc. Present work reports a simple and convenient methodology for synthesis of polystyrene and poly caprolactone microreactors. An aqueous suspension of carboxylated (1μm) polystyrene latex particles was mixed with toluene solution followed by freezing with liquid nitrogen. Freezed particles were incubated at -20°C and characterized for formation of voids on the surface of polymer microspheres by Field Emission Scanning Electron Microscope. The hollow particles were then overnight incubated at 40ºC with unfunctionalized quantum dots (QDs) in 5:1 ratio. QDs Encapsulated polystyrene microcapsules were characterized by fluorescence microscopy. Likewise Poly ε-caprolactone microreactors were prepared by micro-volcanic rupture of freeze dried microspheres synthesized using emulsification of polymer with aqueous Poly vinyl alcohol and freezed with liquid nitrogen. Microreactors were examined with Field Emission Scanning Electron Microscope for size and morphology. Current study is an attempt to create hollow polymer particles which can be employed for microencapsulation of nanoparticles and drug molecules.

Keywords: FE-SEM, Microreactors, Microvolcanic rupture, Poly (ε-caprolactone), Polystyrene

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Authors: Papon Thamvasupong, Kwanchanok Viravaidya-Pasuwat

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Osteoarthritis affects a lot of people worldwide. Local injection of glucosamine is one of the alternative treatment methods to replenish the natural lubrication of cartilage. However, multiple injections can potentially lead to possible bacterial infection. Therefore, a drug delivery system is desired to reduce the frequencies of injections. A hydrogel is one of the delivery systems that can control the release of drugs. Thermo-reversible hydrogels can be beneficial to the drug delivery system especially in the local injection route because this formulation can change from liquid to gel after getting into human body. Once the gel is in the body, it will slowly release the drug in a controlled manner. In this study, various formulations of Pluronic-based hydrogels were synthesized for the controlled release of glucosamine. One of the challenges of the Pluronic controlled release system is its fast dissolution rate. To overcome this problem, alginate and calcium sulfate (CaSO₄) were added to the polymer solution. The characteristics of the hydrogels were investigated including the gelation temperature, gelation time, hydrogel dissolution and glucosamine release mechanism. Finally, a mathematical model of glucosamine release from Pluronic-alginate-hyaluronic acid hydrogel was developed. Our results have shown that crosslinking Pluronic gel with alginate did not significantly extend the dissolution rate of the gel. Moreover, the gel dissolution profiles and the glucosamine release mechanisms were best described using the zeroth-order kinetic model, indicating that the release of glucosamine was primarily governed by the gel dissolution.

Keywords: Controlled release, drug delivery system, glucosamine, Pluronic® F-127, thermoreversible hydrogel.

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Authors: Herdina Indrijati

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This research aims to describe teenager delinquency behavior (Juvenile Delinquency) of senior high school students in Surabaya, Indonesia. Juvenile Delinquency is a broad range of behaviors start from socially unacceptable behavior (overreact in school), violation (escape from home) to crimes (like stealing). This research uses quantitative descriptive method using 498 students who come from 8 different schools in Surabaya as subjects. Juvenile Delinquency behavior form questionnaire has been completed by subjects and was used to measure and describe the behavior. The result of this research is presented in statistic descriptive forms. Result shows that 169 subjects skip school, 55 subjects get out of home without parent’s permission, 110 subjects engage in smoking behavior, 74 subjects damage other people properties, 32 subjects steal, 16 subjects exploit others and 7 subjects engage in drug abuse. Frequency of the top five mentioned behavior are 1-10 times. It is also found that subject’s peers are most likely to be the victim of Juvenile Delinquency. The reasons teenagers engage in Juvenile Delinquency include (1) feeling tired, bored or lazy – that contributes to their skip school behavior (2) Having a lot of problem with parents - contrives them to run away from home, (3) accidentally damage other people’s properties, (4) financial problems – force them to steal and exploit, (5) feeling like having a lot of life problems – that makes them do drugs (6) trying smoking for experience.

Keywords: Juvenile delinquency, senior high school, student.

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Authors: Sharan Badiger, Prema T. Akkasaligar, Deepak Kadeli, M. Vishok

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Neurological disorders are the most debilitating of manifestations seen in patients infected with HIV. The clinical profile of neurological manifestations in HIV patients has undergone a shift in recent years with opportunistic infections being controlled with combination anti-retroviral therapy and the advent of drugs which have higher central nervous system penetrability. The aim of this paper is to study the clinical, investigation profile and various neurological disorders in HIV patients on anti‐retroviral therapy. Fifty HIV patients with neurological manifestations were studied. A complete neurological examination including neurocognitive functioning using Montreal Cognitive Assessment and HIV Dementia scale were assessed. Apart from relevant investigations, CD4 count, cerebrovascular fluid analysis, computed tomography (CT) and magnetic resonance imaging (MRI) of brain were done whenever required. Neurocognitive disorders formed the largest group with 42% suffering from HIV associated Neurocognitive Disorders. Among them, asymptomatic neurocognitive impairment was seen in 28%; mild neurocognitive disorder in 12%, and 2% had HIV‐associated dementia. Opportunistic infections of the nervous system accounted for 32%, with meningitis being the most common. Four patients had space occupying lesions of central nervous system; four tuberculomas, and one toxoplasmosis. With the advent of highly active retroviral therapy, HIV patients have longer life spans with suppression of viral load leading to decrease in opportunistic infections of the nervous system. Neurocognitive disorders are now the most common neurological dysfunction seen and thus neurocognitive assessment must be done in all patients with HIV.

Keywords: Anti retroviral therapy, cognitive dysfunction, dementia, neurological manifestations, opportunistic infections.

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Authors: Teerapon Pirom, Ura Pancharoen

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Amoxicillin is an antibiotic which is widely used to treat various infections in both human beings and animals. However, when amoxicillin is released into the environment, it is a major problem. Amoxicillin causes bacterial resistance to these drugs and failure of treatment with antibiotics. Liquid membrane is of great interest as a promising method for the separation and recovery of the target ions from aqueous solutions due to the use of carriers for the transport mechanism, resulting in highly selectivity and rapid transportation of the desired metal ions. The simultaneous processes of extraction and stripping in a single unit operation of liquid membrane system are very interesting. Therefore, it is practical to apply liquid membrane, particularly the HFSLM for industrial applications as HFSLM is proved to be a separation process with lower capital and operating costs, low energy and extractant with long life time, high selectivity and high fluxes compared with solid membranes. It is a simple design amenable to scaling up for industrial applications. The extraction and recovery for (Amoxicillin) through the hollow fiber supported liquid membrane (HFSLM) using aliquat336 as a carrier were explored with the experimental data. The important variables affecting on transport of amoxicillin viz. extractant concentration and operating time were investigated. The highest AMOX- extraction percentages of 85.35 and Amoxicillin stripping of 80.04 were achieved with the best condition at 6 mmol/L [aliquat336] and operating time 100 min. The extraction reaction order (n) and the extraction reaction rate constant (kf) were found to be 1.00 and 0.0344 min-1, respectively.

Keywords: Aliquat336, amoxicillin, HFSLM, kinetic.

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Authors: Inas E. Darwish, Alia M. Arab, Tarek A. Azeim, Teshreen M. Zeitoun, Wafaa A. Hewedy, Moemen A. Heiba, Iman S. Emara

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Inflammatory bowel disease (IBD) is a chronic relapsing-remitting condition that afflicts millions of people throughout the world and impairs their daily functions and quality of life. Treatment of IBD depends largely on 5-aminosalicylic acid (5- ASA) and corticosteroids. The present study aimed to clarify the effects of 5-aminosalicylic acid, budesonide and currcumin on 90 male albino rats against trinitrobenzene sulfonic acid (TNB) induced colitis. TNB was injected intrarectally to 50 rats. The other 40 rats served as control groups. Both 5-ASA (in a dose of 120 mg/kg) and budesonide (in a dose of 0.1 mg/kg) were administered daily for one week whereas currcumin was injected intraperitonially (in a dose of 30 mg/kg daily) for 14 days after injection of either TNB in the colitis rats (group B) or saline in control groups (group A). The study included estimation of macroscopic score index, histological examination of H&E stained sections of the colonic tissue, biochemical estimation of myeloperoxidase (MPO), nitric oxide (NO), and caspase-3 levels, in addition to studying the effect of tested drugs on colonic motility. It was found that budesonide and curcumin improved mucosal healing, reduced both NO production and caspase- 3 level. They had the best impact on the disturbed colonic motility in TNBS-model of colitis.

Keywords: Colitis, curcumin, nitric oxide.

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Authors: Funmilola O. Omoya, Abdul O. Momoh

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Malaria constitutes one of the major health problems in Nigeria. One of the reasons attributed for the upsurge was the development of resistance of Plasmodium falciparum and the emergence of multi-resistant strains of the parasite to anti-malaria drugs. A continued search for other effective, safe and cheap plantbased anti-malaria agents thus becomes imperative in the face of these difficulties. The objective of this study is therefore to evaluate the in vivo anti-malarial efficacy of ethanolic extracts of Chromolaena odorata and Androgaphis paniculata leaves. The two plants were evaluated for their anti-malaria efficacy in vivo in a 4-day curative test assay against Plasmodium berghei strain in mice. The group treated with 500mg/ml dose of ethanolic extract of A. paniculata plant showed parasite suppression with increase in Packed Cell Volume (PCV) value except day 3 which showed a slight decrease in PCV value. During the 4-day curative test, an increase in the PCV values, weight measurement and zero count of Plasmodium berghei parasite values was recorded after day 3 of drug administration. These results obtained in group treated with A. paniculata extract showed anti-malarial efficacy with higher mortality rate in parasitaemia count when compared with Chromolaena odorata group. These results justify the use of ethanolic extracts of A. paniculata plant as medicinal herb used in folklore medicine in the treatment of malaria.

Keywords: Anti-malaria, Curative, Plant-based anti-malaria agents.

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Authors: Hassan Zarei, Ali Vahidian Kamyad, Sohrab Effati

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In this paper, a mathematical model of human immunodeficiency virus (HIV) is utilized and an optimization problem is proposed, with the final goal of implementing an optimal 900-day structured treatment interruption (STI) protocol. Two type of commonly used drugs in highly active antiretroviral therapy (HAART), reverse transcriptase inhibitors (RTI) and protease inhibitors (PI), are considered. In order to solving the proposed optimization problem an adaptive memetic algorithm with population management (AMAPM) is proposed. The AMAPM uses a distance measure to control the diversity of population in genotype space and thus preventing the stagnation and premature convergence. Moreover, the AMAPM uses diversity parameter in phenotype space to dynamically set the population size and the number of crossovers during the search process. Three crossover operators diversify the population, simultaneously. The progresses of crossover operators are utilized to set the number of each crossover per generation. In order to escaping the local optima and introducing the new search directions toward the global optima, two local searchers assist the evolutionary process. In contrast to traditional memetic algorithms, the activation of these local searchers is not random and depends on both the diversity parameters in genotype space and phenotype space. The capability of AMAPM in finding optimal solutions compared with three popular metaheurestics is introduced.

Keywords: HIV therapy design, memetic algorithms, adaptivealgorithms, nonlinear integer programming.

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Authors: Maryam Nazari, Majid Karandish, Alihossein Saberi

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Obesity as a global health challenge motivates pharmaceutical industries to produce anti-obesity drugs. However, effectiveness of these agents is remained unclear. Because of popularity of dietary supplements, the aim of this study was tp investigate the effects of Conjugated Linoleic Acid (CLA) and L-carnitine (LC) on serum glucose, triglyceride, cholesterol and weight changes in diet induced obese rats. 48 male Wistar rats were randomly divided into two groups: Normal fat diet (n=8), and High fat diet (HFD) (n=32). After eight weeks, the second group which was maintained on HFD until the end of study, was subdivided into four categories: a) 500 mg Corn Oil (as control group), b) 500 mg CLA, c) 200 mg LC, d) 500 mg CLA+ 200 mg LC.All doses are planned per kg body weights, which were administered by oral gavage for four weeks. Body weights were measured and recorded weekly by means of a digital scale. At the end of the study, blood samples were collected for biochemical markers measurement. SPSS Version 16 was used for statistical analysis. At the end of 8^th week, a significant difference in weight was observed between HFD and NFD group. After 12 weeks, LC significantly reduced weight gain by 4.2%. Trend of weight gain in CLA and CLA+LC groups was insignificantly decelerated. CLA+LC reduced triglyceride level significantly, but just CLA had significant influence on total cholesterol and insignificant decreasing effect on FBS. Our results showed that an obesogenic diet in a relative short time led to obesity and dyslipidemia which can be modified by LC and CLA to some extent.

Keywords: Conjugated linoleic acid, high fat diet, L-carnitine, obesity.

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Authors: Kheireddine El-Boubbou

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Drug delivery to target human acute myeloid leukemia (AML) using a nanoparticulate chemotherapeutic formulation that can deliver drugs selectively to AML cancer is hugely needed. In this work, we report the development of a nanoformulation made of polymeric-stabilized multifunctional magnetic iron oxide nanoparticles (PMNP) loaded with the anticancer drug Doxorubicin (Dox) as a promising drug carrier to treat AML. Dox@PMNP conjugates simultaneously exhibited high drug content, maximized fluorescence, and excellent release properties. Nanoparticulate uptake and cell death following addition of Dox@PMNPs were then evaluated in different types of human AML target cells, as well as on normal human cells. While the unloaded MNPs were not toxic to any of the cells, Dox@PMNPs were found to be highly toxic to the different AML cell lines, albeit at different inhibitory concentrations (IC₅₀ values), but showed very little toxicity towards the normal cells. In comparison, free Dox showed significant potency concurrently to all the cell lines, suggesting huge potentials for the use of Dox@PMNPs as selective AML anticancer cargos. Live confocal imaging, fluorescence and electron microscopy confirmed that Dox is indeed delivered to the nucleus in relatively short periods of time, causing apoptotic cell death. Importantly, this targeted payload may potentially enhance the effectiveness of the drug in AML patients and may further allow physicians to image leukemic cells exposed to Dox@PMNPs using MRI.

Keywords: Magnetic nanoparticles, drug delivery, acute myeloid leukemia, iron oxide, cancer nanotherapy.

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Authors: Raad Nari, Maura Moriaty, Maha T. Barakat

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Introduction: Sodium-glucose co-transporter-2 (SGLT2) inhibitors are a new class of oral anti-diabetic drugs with a unique mechanism of action. They are used to improve glycaemic control in adults with type 2 diabetes by enhancing urinary glucose excretion. In the UAE, there has been certainly an increased use of these medications. As with any new medication, there are safety considerations related to their use in patients with type two diabetes. A retrospective study was conducted at the three main centres of the Imperial College London Diabetes Centre. Methodology: All patients in electronic database (Diamond) from October 2014 to October 2017 were included with a minimum of six months usage of sodium glucose co-transporter inhibitors that comprise canagliflozin, dapagliflozin and empagliflozin. There were 15 paired sample biochemical and clinical correlations. The analysis was done at the start of the study, three months and six months apart. SPSS version 24 was used for this study. Conclusion: This study of sodium glucose co-transporter-2 inhibitors used showed significant reductions in weight, glycated haemoglobin A1C, systolic and diastolic blood pressures. As the case with systematic reviews, there were similar changes in liver enzymes, raised total cholesterol, low density lipopoptein and high density lipoprotein. There was slight improvement in estimated glomerular filtration rate too. Our analysis also showed that they increased in the incidence of urinary tract symptoms and incidence of urinary tract infections.

Keywords: SGLT2 inhibitors dapagliflozin empagliflozin canagliflozin, adverse effects, amputation diabetic ketoacidosis DKA, urinary tract infection.

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Authors: S. S. Pathak, M. A. Borkar, S. S. Patel

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To compare Healing Effects of an Ayurvedic Preparation and Silver Sulfadiazine on burn wounds in Albino Rats. Methods: Albino rats– 30 male / female rats weighing between 150-200 g were used in the study. They were individually housed and maintained on normal diet and water ad libitum. Partial thickness burn wounds were inflicted, on overnight-starved animals under pentobarbitone (30mg/kg, i.p.) anaesthesia, by pouring hot molten wax at 80oC into a plastic cylinder of 300 mm2 circular openings placed on the shaven back of the animal. Apart from the drugs under investigation no local/ systemic chemotherapeutic cover will be provided to animals. All the animals were assessed for the percentage of wound contraction, signs of infection, scab formation and histopathological examination. Results: Percentage of wound healing was significantly better in the test ointment group compared to the standard. Signs of infection were observed in more animals in the test ointment group compared to the standard. Scab formation also took place earlier in the test ointment group compared to standard. Epithelial regeneration and healing profile was better in the test ointment compared to the standard. Moreover the test ointment group did not show any raised margins in the wound or blackish discoloration as was observed in silver sulfadiazine group. Conclusion: The burn wound healing effect of the ayurvedic ointment under study is better in comparison to standard therapy of silver sulfadiazine. The problem of infection encountered with the test ointment can be overcome by changing the concentrations and proportions of the ingredients in the test ointment which constitutes the further plan of the study.

Keywords: Ayurvedic test ointment, burn wounds, Silver sulfadiazine.

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Authors: M. Jarrar, S. Behl, N. Shaheen, A. Fatima, R. Nasab

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Skin aging is a slow multifactorial process influenced by both internal as well as external factors. Ultra-violet radiations (UV), diet, smoking and personal habits are the most common environmental factors that affect skin aging. Fat contents and fibrous proteins as collagen and elastin are core internal structural components. The direct influence of UV on elastin integrity and health is central on aging of skin especially by time. The deposition of abnormal elastic material is a major marker in a photo-aged skin. Searching for compounds that may protect against cutaneous photodamage is exceedingly valued. Retinoids and alpha hydroxy acids have been endorsed by some researchers as possible candidates for protecting and or repairing the effect of UV damaged skin. For consolidating a better system of anti- and protective effects of such anti-aging agents, we evaluated the combinatory effects of various dosages of lactic acid and retinol on the dermal fibroblast’s elastin levels exposed to UV. The UV exposed cells showed significant reduction in the elastin levels. A combination of drugs with a higher concentration of lactic acid (30 -35 mM) and a lower concentration of retinol (10-15mg/mL) showed to work better in maintaining elastin concentration in UV exposed cells. We assume this preservation could be the result of increased tropo-elastin gene expression stimulated by retinol whereas lactic acid probably repaired the UV irradiated damage by enhancing the amount and integrity of the elastin fibers.

Keywords: Alpha Hydroxy Acid, Elastin, Retinol, Ultraviolet radiations.

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Authors: Surender Singh Jadav, Venkatesan Jayaprakash, Arijit Basu, Barij Nayan Sinha

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Chikungunya virus (CHICKV) is an arboviruses belonging to family Tagoviridae and is transmitted to human through by mosquito (Aedes aegypti and Aedes albopictus) bite. A large outbreak of chikungunya has been reported in India between 2006 and 2007, along with several other countries from South-East Asia and for the first time in Europe. It was for the first time that the CHICKV outbreak has been reported with mortality from Reunion Island and increased mortality from Asian countries. CHICKV affects all age groups, and currently there are no specific drugs or vaccine to cure the disease. The need of antiviral agents for the treatment of CHICKV infection and the success of virtual screening against many therapeutically valuable targets led us to carry out the structure based drug design against Chikungunya nSP2 protease (PDB: 3TRK). Highthroughput virtual screening of publicly available databases, ZINC12 and BindingDB, has been carried out using the Openeye tools and Schrodinger LLC software packages. Openeye Filter program has been used to filter the database and the filtered outputs were docked using HTVS protocol implemented in GLIDE package of Schrodinger LLC. The top HITS were further used for enriching the similar molecules from the database through vROCS; a shape based screening protocol implemented in Openeye. The approach adopted has provided different scaffolds as HITS against CHICKV protease. Three scaffolds: Indole, Pyrazole and Sulphone derivatives were selected based on the docking score and synthetic feasibility. Derivatives of Pyrazole were synthesized and submitted for antiviral screening against CHICKV.

Keywords: Chikungunya, nsP2 protease, ADME filter, HTVS, Docking, Active site.

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Authors: Teka Haile, Behailu Hawulte, Solomon Alemayehu

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Background: HIV virological failure still remains a problem in HV/AIDS treatment and care. This study aimed to describe the prevalence and identify the factors associated with viral non-suppression among HIV-positive adult patients on antiretroviral therapy in Woliso Town, Oromia, Ethiopia. Methods: A retrospective cross-sectional study was conducted among 424 HIV-positive patient’s attending antiretroviral therapy (ART) in Woliso Town during the period from August 25, 2020 to August 30, 2020. Data collected from patient medical records were entered into Epi Info version 2.3.2.1 and exported to SPSS version 21.0 for analysis. Logistic regression analysis was done to identify factors associated with viral load non-suppression, and statistical significance of odds ratios were declared using 95% confidence interval and p-value < 0.05. Results: A total of 424 patients were included in this study. The mean age (± SD) of the study participants was 39.88 (± 9.995) years. The prevalence of HIV viral load non-suppression was 55 (13.0%) with 95% CI (9.9-16.5). Second-line ART treatment regimen (Adjusted Odds Ratio (AOR) = 8.98, 95% Confidence Interval (CI): 2.64, 30.58) and routine viral load testing (AOR = 0.01, 95% CI: 0.001, 0.02) were significantly associated with virological non-suppression. Conclusion: Virological non-suppression was high, which hinders the achievement of the third global 95 target. The second-line regimen and routine viral load testing were significantly associated with virological non-suppression. It suggests the need to assess the effectiveness of antiretroviral drugs for epidemic control. It also clearly shows the need to decentralize third-line ART treatment for those patients in need.

Keywords: Virological non-suppression, HIV-positive, ART, Woliso Town, Ethiopia.

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Authors: D. Farsi, Gh. Dokhtvasi, S. Abbasi, S. Shafiee Ardestani, E. Payani

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Background and aim: It has not been well studied whether fentanyl-thiopental (FT) is effective and safe for PSA in orthopedic procedures in Emergency Department (ED). The aim of this trial was to evaluate the effectiveness of intravenous FT versus fentanyl-midazolam (FM) in patients who suffered from shoulder dislocation or distal radial fracture-dislocation. Methods: In this randomized double-blinded study, Seventy-six eligible patients were entered the study and randomly received intravenous FT or FM. The success rate, onset of action and recovery time, pain score, physicians’ satisfaction and adverse events were assessed and recorded by treating emergency physicians. The statistical analysis was intention to treat. Results: The success rate after administrating loading dose in FT group was significantly higher than FM group (71.7% vs. 48.9%, p=0.04); however, the ultimate unsuccessful rate after 3 doses of drugs in the FT group was higher than the FM group (3 to 1) but it did not reach to significant level (p=0.61). Despite near equal onset of action time in two study group (P=0.464), the recovery period in patients receiving FT was markedly shorter than FM group (P<0.001). The occurrence of adverse effects was low in both groups (p=0.31). Conclusion: PSA using FT is effective and appears to be safe for orthopedic procedures in the ED. Therefore, regarding the prompt onset of action, short recovery period of thiopental, it seems that this combination can be considered more for performing PSA in orthopedic procedures in ED.

Keywords: Procedural Sedation and Analgesia, Thiopental, Fentanyl, Midazolam, Orthopedic Procedure, Emergency Department, Pain.

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Authors: M. J. Reis Lima, J. Oliveira, M. Brito, C. Lemos, A. Mascarenhas, E. Teixeira Lemos

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Hypertension is a common condition causing cardio and cerebrovascular complications. Portugal has one of the highest mortality rates from stroke and a high prevalence of hypertension. Systolic Blood Pressure (SBP) is an important risk factor for cardiovascular events (myocardial infarction and stroke) and premature mortality, particularly in the elderly population. The present study aims to estimate the prevalence of hypertension in a Portuguese population living in a coastal city and to identify some of its determinants (namely gender, age, the body mass index and physical activity frequency). A total of 91 adults who attended three pharmacies of a coastal city in the center of Portugal, between May and August of 2013 were evaluated. Attendants who reported to have diabetes or taking antihypertensive drugs in the 2 previous weeks were excluded from the study. Sociodemographic factors, BMI, habits of exercise and BP were assessed. Hypertension was defined as blood pressure ≥140/90 mmHg. The majority of the studied population was constituted by women (75.8%), with a mean age of 54.2±1.6 years old, married or living in civil union and that had completed secondary school or had higher education (40%). They presented a mean BMI of 26.2±4.76 Kg/m2., and were sedentary. The mean BP was 127.0±17.77mmHg- 74.69 ± 9.53. In this population we found 4.3% of people with hypertension and 16.1% with normal high blood pressure. Men exhibit a tendency to present higher systolic blood pressure values than women. Of all the factors considered, SBP values also tended to be higher with age and higher BMI values. Despite the fact that the mean values of SBP did not present values higher than 140 mmHg we must be concerned because the studied population is undiagnosed for hypertension. Although this is a preliminary study, it might be a prelude to the upcoming research about the underlying factors responsible for the occurrence of SBP.

Keywords: Hypertension, age, exercise, obesity, gender.

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Authors: G. Wagner, R. Herrmann

Abstract:

Cytotoxic platinum compounds play a major role in the chemotherapy of a large number of human cancers. However, due to the severe side effects for the patient and other problems associated with their use, there is a need for the development of more efficient drugs and new methods for their selective delivery to the tumours. One way to achieve the latter could be in the use of nanoparticular substrates that can adsorb or chemically bind the drug. In the cell, the drug is supposed to be slowly released, either by physical desorption or by dissolution of the particle framework. Ideally, the cytotoxic properties of the platinum drug unfold only then, in the cancer cell and over a longer period of time due to the gradual release. In this paper, we report on our first steps in this direction. The binding properties of a series of cytotoxic Pt(II) oxadiazoline compounds to mesoporous silica particles has been studied by NMR and UV/vis spectroscopy. High loadings were achieved when the Pt(II) compound was relatively polar, and has been dissolved in a relatively nonpolar solvent before the silica was added. Typically, 6-10 hours were required for complete equilibration, suggesting the adsorption did not only occur to the outer surface but also to the interior of the pores. The untreated and Pt(II) loaded particles were characterised by C, H, N combustion analysis, BET/BJH nitrogen sorption, electron microscopy (REM and TEM) and EDX. With the latter methods we were able to demonstrate the homogenous distribution of the Pt(II) compound on and in the silica particles, and no Pt(II) bulk precipitate had formed. The in vitro cytotoxicity in a human cancer cell line (HeLa) has been determined for one of the new platinum compounds adsorbed to mesoporous silica particles of different size, and compared with the corresponding compound in solution. The IC50 data are similar in all cases, suggesting that the release of the Pt(II) compound was relatively fast and possibly occurred before the particles reached the cells. Overall, the platinum drug is chemically stable on silica and retained its activity upon prolonged storage.

Keywords: Cytotoxicity, mesoporous silica, nanoparticles platinum compounds.

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Authors: Monisha Isaac

Abstract:

Biotechnology is a discipline which explains the use of living organisms and systems to construct a product, or we can define it as an application or technology developed to use biological systems and organisms processes for a specific use. Particularly, it includes cells and its components use for new technologies and inventions. The tools developed can be further used in diverse fields such as agriculture, industry, research and hospitals etc. The 21^st century has seen a drastic development and advancement in biotechnology in India. Significant increase in Government of India’s outlays for biotechnology over the past decade has been observed. A sectoral break up of biotechnology-based companies in India shows that most of the companies are agriculture-based companies having interests ranging from tissue culture to biopesticides. Major attention has been given by the companies in health related activities and in environmental biotechnology. The biopharmaceutical, which comprises of vaccines, diagnostic, and recombinant products is the most reliable and largest segment of the Indian Biotech industry. India has developed its vaccine markets and supplies them to various countries. Then there are the bio-services, which mainly comprise of contract researches and manufacturing services. India has made noticeable developments in the field of bio industries including manufacturing of enzymes, biofuels and biopolymers. Biotechnology is also playing a crucial and significant role in the field of agriculture. Traditional methods have been replaced by new technologies that mainly focus on GM crops, marker assisted technologies and the use of biotechnological tools to improve the quality of fertilizers and soil. It may only be a small contributor but has shown to have huge potential for growth. Bioinformatics is a computational method which helps to store, manage, arrange and design tools to interpret the extensive data gathered through experimental trials, making it important in the design of drugs.

Keywords: Biotechnology, advancement, agriculture, bio-services, bio-industries, bio-pharmaceuticals.

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Authors: N. M. Sani, E. D. Jatau, O. S. Olonitola, M. Y. Gwarzo, P. Moodley, N. S. Mujahid

Abstract:

Hemoglobin (HB) indicates anemia level and by extension may reflect the nutritional level and perhaps the immunity of an individual. Some antiretroviral drugs like Zidovudine are known to cause anemia in people living with HIV/AIDS (PLWHA). A cross sectional study using demographic data and blood specimen from 218 female commercial sex workers attending antiretroviral therapy (ART) clinics was conducted between December, 2009 and July, 2011 to assess the effect of zidovudine on hematologic, and RNA viral load of female sex workers receiving antiretroviral treatment in north western Nigeria. Anemia is a common and serious complication of both HIV infection and its treatment. In the setting of HIV infection, anemia has been associated with decreased quality of life, functional status, and survival. Antiretroviral therapy, particularly the highly active antiretroviral therapy (HAART), has been associated with a decrease in the incidence and severity of anemia in HIV-infected patients who have received a HAART regimen for at least 1 year. In this study, result has shown that of the 218 patients, 26 with hemoglobin count between 5.1 – 10g/dl were observed to have the highest viral load count of 300,000 – 350,000copies/ml. It was also observed that most patients (190) with HB of 10.1 – 15.0g/dl had viral load count of 200,000 – 250,000 copies /ml. An inverse relationship therefore exists i.e. the lower the hemoglobin level, the higher the viral load count even though the test statistics did not show any significance between the two (P = 0.206). This shows that multivariate logistic regression analysis demonstrated that anemia was associated with a CD4 + cell count below 50/μL, female sex workers with a viral load above 100,000 copies/mL, who use zidovudine. Severe anemia was less prevalent in this study population than in historical comparators; however, mild to moderate anemia rates remain high. The study therefore recommends that hematological and virologic parameters be monitored closely in patients receiving first line ART regimen.

Keywords: Female sex worker, Zidovudine, Hemoglobin, Anemia.

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Authors: Huyen T. Pham, Nhue P. Nguyen, Tien Q. Phi, Phuong T. Dang, Hy G. Le

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Since the marine environmental conditions are extremely different from the other ones, marine actinomycetes might produce novel bioactive compounds. Therefore, actinomycete strains were screened from marine water and sediment samples collected from the coastal areas of Northern Vietnam. Ninety-nine actinomycete strains were obtained on starch-casein agar media by dilution technique, only seven strains, named HP112, HP12, HP411, HPN11, HP 11, HPT13 and HPX12, showed significant antibacterial activity against both gram-positive and gram-negative bacteria (Bacillus subtilis ATCC 6633, Staphylococcus epidemidis ATCC 12228, Escherichia coli ATCC 11105). Further studies were carried out with the most active HP411 strain against Candida albicans ATCC 10231. This strain could grow rapidly on starch casein agar and other media with high salt containing 7-10% NaCl at 28-30oC. Spore-chain of HP411 showed an elongated and circular shape with 10 to 30 spores/chain. Identification of the strain was carried out by employing the taxonomical studies including the 16S rRNA sequence. Based on phylogenetic and phenotypic evidence it is proposed that HP411 to be belongs to species Streptomyces variabilis. The potent of the crude extract of fermentation broth of HP411 that are effective against wide range of pathogens: both grampositive, gram-negative and fungi. Further studies revealed that the crude extract HP411 could obtain the anticancer activity for cancer cell lines: Hep-G2 (liver cancer cell line); RD (cardiac and skeletal muscle letters cell line); FL (membrane of the uterus cancer cell line). However, the actinomycetes from marine ecosystem will be useful for the discovery of new drugs in the future.

Keywords: Marine actinomycetes, antibacterial, anticancer, Streptomyces variabilis.

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Authors: Manish Kumar Gautam, Raj Kumar Goel

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Delayed wound healing in diabetes is primarily associated with hyperglycemia, over-expression of inflammatory marker, oxidative stress and delayed collagen synthesis. This unmanaged wound is producing high economic burden on the society. Thus research is required to develop new and effective treatment strategies to deal with this emerging issue. Our present study incorporates the evaluation of wound healing effects of 50% ethanol extract of Ocimum sanctum (OSE) in streptozotocin (45mg/kg)-induced diabetic rats with concurrent wound ulcer. The animals showing diabetes (Blood glucose level >140 and <250 mg/dL) will be selected for wound healing study using standard dead space wound model. Wounds were created by implanting two polypropylene tubes (0.5 x 2.5 cm2 each), one on either side in the lumbar region on the dorsal surface of each rat. On the 10th postwounding day, the animals were sacrificed and granulation tissue formed on the implanted tubes was carefully dissected out and study the status of antioxidants (Superoxide dismutase, SOD and Glutathione, GSH) free radicals (Lipid peroxidation, LPO and nitric oxide, NO) acute inflammatory marker (myeloperoxidase, MPO) connective tissue determinants, hydroxyproline, hexosamine and hexuronic acid, which play a major role in wound healing and diabetes. Besides the anti-diabetic parameters (estimation of serum blood glucose, triglycerides and total cholesterol), the above parameters for wound healing were studied both in normal, untreated and OSE treated diabetic rats. The effects of extract on above parameters will be compared with known standard antioxidant (Vitamin E) and anti-diabetic (Glybenclamide) drugs. OSE 400 mg/kg substantiated by significantly decreased serum blood glucose, triglycerides and total cholesterol. OSE also decrease granulation tissue free radicals (LPO, 58.1% and NO, 52.7%) and myeloperoxidase (MPO, 63.3%), and enhanced antioxidants (GSH, 116.4% and SOD, 201.1%)

Keywords: Wound healing, diabetes, Ocimum sanctum, Antioxidant, Free radical, Myeloperoxidase

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Authors: Rawia M. Khalil, Ahmed A. Abd El Rahman, Mahfouz A. Kassem, Mohamed S. El Ridi, Mona M. Abou Samra, Ghada E. A. Awad, Soheir S. Mansy

Abstract:

Solid lipid nanoparticles (SLNs) have gained great attention for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Our work deals with the preparation of nystatin loaded solid lipid nanoparticles (NystSLNs) using the hot homogenization and ultrasonication method. The prepared NystSLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, transmission electron microscopy, differential scanning calorimetry, rheological behavior and in vitro drug release. A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans, by counting the colonies and examining the histopathological changes induced on the skin of infected rats. The results showed that SLNs dispersions are spherical in shape with particle size ranging from 83.26±11.33 to 955.04±1.09 nm. The entrapment efficiencies are ranging from 19.73±1.21 to 72.46±0.66% with zeta potential ranging from -18.9 to -38.8 mV and shear-thinning rheological Behavior. The stability studies done for 6 months showed that nystatin (Nyst) is a good candidate for topical SLN formulations. A least number of colony forming unit/ ml (cfu/ml) was recorded for the selected NystSLN compared to the drug solution and the commercial Nystatin® cream present in the market. It can be fulfilled from this work that SLNs provide a good skin targeting effect and may represent promising carrier for topical delivery of Nyst offering the sustained release and maintaining the localized effect, resulting in an effective treatment of cutaneous fungal infection.

Keywords: Candida infections, Hot homogenization, Nystatin, Solid lipid nanoparticles, Stability, Topical delivery.

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Authors: S. Vijayakumar, M. Sasikala, T. S. Mohammed Saleem, Gurusharan, K. Gauthaman

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The main objective of our study is to collect data about the profile of the asthmatic patients in Assam and thereby have a comprehensive knowledge of the factors influencing the asthmatic patients of the state and their medication pattern. We developed a search strategy to find any publication about the community based survey asthma related and used. These to search the MEDLINE (1996 to current literature) CINAHL DOAJ pubmed databases using the key phrases, Asthma, Respiratory disorders, Drug therapy of Asthma, database decision support system and asthma. The appropriate literature was printed out from the online source and library (Journal) source. The study was conducted through a set of structured and non-structured questionnaires targeted on the asthmatic patients belonging to the rural and urban areas of Assam, during the month of Dec 2006 to July 2007, 138 cases were studied in Gauwathi Medical College & Hospital located in Bhangagarh, Assam in India. The demographic characteristics a factor in 138 patients with asthma with allergic rhinitis (cases) gives the detail profile of asthmatic patient-s distribution of Assam as classified on the basis of age and sex. It is evident from the study that male populations (66%) are more prone to asthma as compared to the females (34%).Another striking features that emerged from this survey is the maximum prevalence of asthma in the age group of 20- 30 years followed by infants belonging to the age group of 7 (0.05%) 0-10years among both male and female populations of Assam. The high incidence of asthma in the age group of 20-30 years may probably be due to the allergy arising out of sudden exposure to dust and pollen which the children face while playing and going to the school. The rural females in the age group of 30-40 years are more prone to asthma than urban females in the same age group may be due to sex differentiation among the tribal population of the state. Pharmacists should educate the asthmatics how to use inhalers considering growing menace of asthma in the state. Safer drugs should be produced in the form of aerosol so that easy administration by the asthmatic patients and physicians of the state is possible for curing asthma. The health centers should be more equipped with the medicines to cure asthma in the state like Assam.

Keywords: Asthma, Respiratory disease, Smoker.

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Authors: F. Alaa Ali, S. A. Sherein Abdelgayed, S. Osama. EL-Tawil, M. Adel Bakeer

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Tartrazine is an organic azo dyes food additive widely used in foods, drugs, and cosmetics. The present study aimed to investigate the toxic effects of tartrazine on kidneys and liver biomarkers in addition to the investigation of oxidative stress and change of histopathological structure of liver and kidneys in 30 male rats. Tartrazine was orally administrated daily at dose 200 mg/ kg bw (1/ 10 LD₅₀) for sixty days. Serum and tissue samples were collected at the end of the experiment to investigate the underlying mechanism of tartrazine through assessment oxidative stress (Glutathione (GSH), Superoxide dismutase (SOD) and malondialdehyde (MDA) and biochemical markers (alanine aminotransferase (ALT), aspartate aminotransferase (AST), Total protein and Urea). Liver and kidneys tissue were collected and preserved in 10% formalin for histopathological examination. The obtained values were statistically analyzed by one way analysis of variance (ANOVA) followed by multiple comparison test. Biochemical analysis revealed that tartrazine induced significant increase in serum ALT, AST, total protein, urea level compared to control group. Tartrazine showed significant decrease in liver GSH and SOD where their values when compared to control group. Tartrazine induced increase in liver MDA compared to control group. Histopathology of the liver showed diffuse vacuolar degeneration in hepatic parenchyma, the portal area showed sever changes sever in hepatoportal blood vessels and in the bile ducts. The kidneys showed degenerated tubules at the cortex together with mononuclear leucocytes inflammatory cells infiltration. There is perivascular edema with inflammatory cell infiltration surrounding the congested and hyalinized vascular wall of blood vessel. The present study indicates that the subchronic effects of tartrazine have a toxic effect on the liver and kidneys together with induction of oxidative stress by formation of free radicals. Therefore, people should avoid the hazards of consuming tartrazine.

Keywords: Albino rats, tartrazine, toxicity, pathology

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Authors: Pronab Ganguly, Ahmed A. Moustafa

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Holistic management of schizophrenia involves mainstream pharmacological intervention, complimentary medicine intervention, therapeutic intervention and other psychosocial factors such as accommodation, education, job training, employment, relationship, friendship, exercise, overall well-being, smoking, substance abuse, suicide prevention, stigmatisation, recreation, entertainment, violent behaviour, arrangement of public trusteeship and guardianship, day-day-living skill, integration with community, and management of overweight due to medications and other health complications related to medications amongst others. Our review shows that there is no integrated survey by combining all these factors. An international web-based survey was conducted to evaluate the significance of all these factors and present them in a unified manner. It is believed this investigation will contribute positively towards holistic management of schizophrenia. There will be two surveys. In the pharmacological intervention survey, five popular drugs for schizophrenia will be chosen and their efficacy as well as harmful side effects will be evaluated on a scale of 0 -10. This survey will be done by psychiatrists. In the second survey, each element of therapeutic intervention and psychosocial factors will be evaluated according to their significance on a scale of 0 - 10. This survey will be done by care givers, psychologists, case managers and case workers. For the first survey, professional bodies of psychiatrists in English speaking countries will be contacted to request them to ask their members to participate in the survey. For the second survey, professional bodies of clinical psychologist and care givers in English speaking countries will be contacted to request them to ask their members to participate in the survey. Additionally, for both the surveys, relevant professionals will be contacted through personal contact networks. For both the surveys, mean, mode, median, standard deviation and net promoter score will be calculated for each factor and then presented in a statistically significant manner. Subsequently each factor will be ranked according to their statistical significance. Additionally, country specific variation will be highlighted to identify the variation pattern. The results of these surveys will identify the relative significance of each type of pharmacological intervention, each type of therapeutic intervention and each type of psychosocial factor. The determination of this relative importance will definitely contribute to the improvement in quality of life for individuals with schizophrenia.

Keywords: Schizophrenia, holistic management, antipsychotics, quality of life.

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