Search results for: bacterial ring rot

Authors: Ursula D. C. Resende, Fabiano S. Bicalho, Sandro T. M. Gonçalves

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The growing demand for cheap and clean energy sources have been motivated by the study and development of distinct technologies and devices able to provide different amounts of energy. In order to supply energy for small loads, the energy from the electromagnetic spectrum can be harvested. This possibility is particularly interesting because this kind of energy is constantly available in the environment and the number of radiofrequency sources is permanently increasing, due to advances in telecommunications services. A rectenna, which is a combination of an antenna and a rectifier circuit, is an equipment that can efficiently perform the electromagnetic energy harvesting. However, since the amount of electromagnetic energy available in the environment is very small, limited values of power can be harvested by the rectenna. Therefore, several technical strategies have been investigated in order to increase this amount of power. In this work, a metamaterial electromagnetic lens is used to improve the electromagnetic energy harvesting. The rectenna investigated was designed and optimized to charge a Li-Ion battery using the electromagnetic energy from an internet Wi-Fi commercial router model TL-WR841HP operating in 2.45 GHz with maximal output power equal to 18 dBm. The rectenna consists of a high directive antenna, a double voltage rectifier circuit and a metamaterial lens. The printed antenna, constituted of two rectangular radiator elements, was projected and optimized by using the Computer Simulation Software (CST) in order to obtain high directivities and values of S11 parameter below -10 dB in 2.45 GHz. The antenna was printed over a double-sided copper fiberglass substrate, FR4, with characterized relative electric permittivity εr = 4.3 and tangent of losses δ = 0.01. The rectifier circuit, which incorporates a circuit for impedance matching and uses the Schottky diode HSMS-2852, was projected and optimized by using Advanced Design Software (ADS) and built over the same FR4 substrate. The metamaterial cell is composed of two Square Split Ring Resonator (S-SRR) and a thin wire in order to operate with negative values of εr and relative magnetic permeability in 2.45 GHz. In order to evaluate the performance of the purposed rectenna two experimental charging tests were performed, one without and other with the metamaterial lens. The result obtained demonstrate that the electromagnetic lens was able to significantly increase the levels of electric current delivered to the battery, approximately 44%.

Keywords: electromagnetic energy harvesting, electromagnetic lens, metamaterial, rectenna

Procedia PDF Downloads 125

Authors: J. Bravo, F. Cabrera Suárez, B. Vega, L. Román, M. Martel, F. Acosta

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Ciguatera fish poisoning (CFP) is the most common non-bacterial intoxication in the world caused by ingestion of fish with bio-accumulated ciguatoxins (CTXs). It is typical in tropical and subtropical areas, mainly affecting the Caribbean Sea, Polynesia and other areas in the Pacific and Indian Oceans. Interest in Europe by the CFP is increasing in recent years as more and more cases in European hospitals are appearing, usually by people who have consumed ciguatoxin imported fish or have travelled to areas of risk for this poisoning. Since 2004 a series of poisonings raised the question of a possible occurrence of ciguatoxin in Europe, especially in the area of Macaronesia in the East Atlantic temperate zone. Furthermore, some studies have identified the presence of Gambierdiscus spp. in waters surrounding the Canary Islands and Madeira, a toxic dinoflagellate related to this poisoning. The toxin accumulates and concentrates through the food chain and affects to the end of the chain, the human consumer. Fish were collected from the Canary Islands waters and the toxin has been extracted and purified by using acetone and liquid/liquid partition in order to eliminate the excess of fatty acids that may interfere with the detection of the toxin. The fish extracts were inoculated in Neuroblastoma (neuro-2a) cells. After 24-h cell viability was used as an endpoint for cytotoxic effects measurement. Since 2011 our laboratory is collecting data for species such Seriola spp., Epinephelus spp., Makaira spp., Pomatomus spp., Xiphias spp., and Acantocybium spp., from all islands and including the sports fishing and professional activities, we obtained a 8% of fish that have ciguatoxin in their muscle. With these results, we conclude that the island where fishing and fish size affects the probability of catching a fish with the ciguatoxin.

Keywords: Canary Islands, ciguatera fish poisoning, ciguatoxin, Europe

Procedia PDF Downloads 324

Authors: Arpit K. Shrivastava, Nirmal K. Mohakud, Subrat Kumar, Priyadarshi S. Sahu

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Acute diarrhea is one of the major causes of morbidity and mortality among children less than five years of age. Multiple etiologies have been implicated for infectious gastroenteritis causing acute diarrhea. In our study fecal samples (n=165) were collected from children (<5 years) presenting with symptoms of acute diarrhea. Samples were screened for viral, bacterial, and parasitic etiologies such as Rotavirus, Adenovirus, Diarrhoeagenic Escherichia coli (EPEC, EHEC, STEC, O157, O111), Shigella spp., Salmonella spp., Vibrio cholera, Cryptosporidium spp., and Giardia spp. The overall results from our study showed that 57% of children below 5 years of age with acute diarrhea were positive for at least one infectious etiology. Diarrhoeagenic Escherichia coli was detected to be the major etiological agent (29.09%) followed by Rotavirus (24.24%), Shigella (21.21%), Adenovirus (5.45%), Cryptosporidium (2.42%), and Giardia (0.60%). Among the different DEC strains, EPEC was detected significantly higher in <2 years children in comparison to >2 years age group (p =0.001). Concurrent infections with two or more pathogens were observed in 47 of 160 (28.48%) cases with a predominant incidence particularly in <2-year-old children (66.66%) compared to children of 2 to 5 years age group. Co-infection of Rotavirus with Shigella was the most frequent combination, which was detected in 17.94% cases, followed by Rotavirus with EPEC (15.38%) and Shigella with STEC (12.82%). Detection of multiple infectious etiologies and diagnosis of the right causative agent(s) can immensely help in better management of acute childhood diarrhea. In future more studies focusing on the detection of cases with concurrent infections must be carried out, as we believe that the etiological agents might be complementing each other’s strategies of pathogenesis resulting in severe diarrhea.

Keywords: children, co-infection, infectious diarrhea, Odisha

Procedia PDF Downloads 313

Authors: Natalia Moreno-Castellanos, Amaia Rodriguez, Gema Frühbeck

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Introduction: In adipocytes, the cytoskeleton undergoes important expression and distribution in adipocytes rearrangements during adipogenesis and in obesity. Indeed, a role for these proteins in the regulation of adipocyte differentiation and response to insulin has been demonstrated. Recently, septins have been considered as new components of the cytoskeletal network that interact with other cytoskeletal elements (actin and tubulin) profoundly modifying their dynamics. However, these proteins have not been characterized as yet in adipose tissue. In this work, were examined the cellular, molecular and functional features of a member of this family, septin 11 (SEPT11), in adipocytes and evaluated the impact of obesity on the expression of this protein in human adipose tissue. Methods: Adipose gene and protein expression levels of SEPT11 were analysed in human samples. SEPT11 distribution was evaluated by immunocytochemistry, electronic microscopy, and subcellular fractionation techniques. GST-pull down, immunoprecipitation and a Yeast-Two Hybrid (Y2H) screening were used to identify the SEPT11 interactome. Gene silencing was employed to assess the role of SEPT11 in the regulation of insulin signaling and lipid metabolism in adipocytes. Results: SEPT11 is expressed in human adipocytes, and its levels increased in both omental and subcutaneous adipose tissue in obesity, with SEPT11 mRNA content positively correlating with parameters of insulin resistance in subcutaneous fat. In non-stimulated adipocytes, SEPT11 immunoreactivity showed a ring-like distribution at the cell surface and associated to caveolae. Biochemical analyses showed that SEPT11 interacted with the main component of caveolae, caveolin-1 (CAV1) as well as with the fatty acid-binding protein, FABP5. Notably, the three proteins redistributed and co-localized at the surface of lipid droplets upon exposure of adipocytes to oleate. In this line, SEPT11 silencing in 3T3-L1 adipocytes impaired insulin signaling and decreased insulin-induced lipogenesis. Conclusions: Those findings demonstrate that SEPT11 is a novel component of the adipocyte cytoskeleton that plays an important role in the regulation of lipid traffic, metabolism and can thus represent a potential biomarker of insulin resistance in obesity in adipocytes through its interaction with both CAV1 and FABP5.

Keywords: caveolae, lipid metabolism, obesity, septins

Procedia PDF Downloads 180

Authors: Munish Garg, Vinni Ahuja

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In the past few years, the high consumption of soft drinks has attracted negative attention world-wide due to its possible adverse effects, leading the health conscious people to find alternative nutraceutical or herbal health drinks. In the present study, a nutraceutical soft drink was developed utilizing some easily available and well known traditional herbs having nutritional potential. The key ingredients were selected as bael, amla, lemon juice, ashwagandha and poppy seeds based on their household routine use in the summer with proven refreshing, cooling and energetic feeling since ages. After several trials made, the final composition of nutraceutical summer soft drink was selected as most suitable combination based on the taste, physicochemical, microbial and organoleptic point of view. The physicochemical analysis of the prepared drink found to contain optimum level of titratable acidity, total soluble solids and pH which were in accordance of the commercial recommendations. There were no bacterial colonies found in the product therefore found within limits. During the nine point’s hedonic scale sensory evaluation, the drink was strongly liked for colour, taste, flavour and texture. The formulation was found to contain flavonoids (80mg/100ml), phenolics (103mg/100ml), vitamin C (250mg/100ml) and has antioxidant potential (75.52%) apart from providing several other essential vitamins, minerals and healthy components. The developed nutraceutical drink provides an economical and feasible option for the consumers with very good taste combined with potential health benefits. The present drink is potentially capable to replace the synthetic soft drinks available in the market.

Keywords: herbal drink, summer drink, nutraceuticals, soft drink

Procedia PDF Downloads 400

Authors: Guillaume Caulier, Lola Brasseur, Patrick Flammang, Pascal Gerbaux, Igor Eeckhaut

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Saponins and quinones are two major groups of secondary metabolites widely distributed in the biosphere. More specifically, triterpenoid saponins and anthraquinones are mainly found in a wide variety of plants, bacteria and fungi. In the animal kingdom, these natural organic compounds are rare and only found in small quantities in arthropods, marine sponges and echinoderms. In this last group, triterpenoid saponins are specific to holothuroids (sea cucumbers) while anthraquinones are the chemical signature of crinoids (feather stars). Depending on the species, they present different molecular cocktails. Despite presenting different chemical properties, these molecules share numerous similarities. This study compares the biological distribution, the pharmacological effects and the ecological roles of holothuroid saponins and crinoid anthraquinones. Both of them have been defined as allomones repelling predators and parasites (i.e. chemical defense) and have interesting pharmacological properties (e.g. anti-bacterial, anti-fungal, anti-cancer). Our study investigates the chemical ecology of two symbiotic associations models; between the snapping shrimp Synalpheus stimpsonii associated with crinoids and the Harlequin crab Lissocarcinus orbicularis associated with holothuroids. Using behavioral experiments in olfactometers, chemical extractions and mass spectrometry analyses, we discovered that saponins and anthraquinones present a second ecological role: the attraction of obligatory symbionts towards their hosts. They can, therefore, be defined as kairomones. This highlights a new paradigm in marine chemical ecology: Chemical repellents are attractants to obligatory symbionts because they constitute host specific chemical signatures.

Keywords: anthraquinones, kairomones, marine symbiosis, saponins, attractant

Procedia PDF Downloads 179

Authors: Adnan A. Kadi, Nasser S. Al-Shakliah, Haitham Al-Rabiah

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Zorifertinib is a novel, potent, oral, a small molecule used to treat non-small cell lung cancer (NSCLC). zorifertinib is an Epidermal Growth Factor Receptor (EGFR) inhibitor and has good blood–brain barrier permeability for (NSCLC) patients with EGFR mutations. zorifertinibis currently at phase II/III clinical trials. The current research reports the characterization and identification of in vitro, in vivo and reactive intermediates of zorifertinib. Prediction of susceptible sites of metabolism and reactivity pathways (cyanide and GSH) of zorifertinib were performed by the Xenosite web predictor tool. In-vitro metabolites of zorifertinib were performed by incubation with rat liver microsomes (RLMs) and isolated perfused rat liver hepatocytes. Extraction of zorifertinib and it's in vitro metabolites from the incubation mixtures were done by protein precipitation. In vivo metabolism was done by giving a single oral dose of zorifertinib(10 mg/Kg) to Sprague Dawely rats in metabolic cages by using oral gavage. Urine was gathered and filtered at specific time intervals (0, 6, 12, 18, 24, 48, 72,96and 120 hr) from zorifertinib dosing. A similar volume of ACN was added to each collected urine sample. Both layers (organic and aqueous) were injected into liquid chromatography ion trap mass spectrometry(LC-IT-MS) to detect vivozorifertinib metabolites. N-methyl piperizine ring and quinazoline group of zorifertinib undergoe metabolism forming iminium and electro deficient conjugated system respectively, which are very reactive toward nucleophilic macromolecules. Incubation of zorifertinib with RLMs in the presence of 1.0 mM KCN and 1.0 Mm glutathione were made to check reactive metabolites as it is often responsible for toxicities associated with this drug. For in vitro metabolites there were nine in vitro phase I metabolites, four in vitro phase II metabolites, eleven reactive metabolites(three cyano adducts, five GSH conjugates metabolites, and three methoxy metabolites of zorifertinib were detected by LC-IT-MS. For in vivo metabolites, there were eight in vivo phase I, tenin vivo phase II metabolitesofzorifertinib were detected by LC-IT-MS. In vitro and in vivo phase I metabolic pathways wereN- demthylation, O-demethylation, hydroxylation, reduction, defluorination, and dechlorination. In vivo phase II metabolic reaction was direct conjugation of zorifertinib with glucuronic acid and sulphate.

Keywords: in vivo metabolites, in vitro metabolites, cyano adducts, GSH conjugate

Procedia PDF Downloads 176

Authors: I. Schäfer, B. Kohn, M. Volkmann, E. Müller

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Introduction: Blood-feeding arthropods transmit parasitic, bacterial, or viral pathogens to domestic animals and wildlife. Vector-borne infections are gaining significance due to the increase of travel, import of domestic animals from abroad, and the changing climate in Europe. Aims of the study: The main objective of this retrospective study was to assess the prevalence of vector-borne infections in cats in which a ‘Feline Travel Profile’ had been conducted. Material and Methods: This retrospective study included test results from cats for which a ‘Feline Travel Profile’ established by LABOKLIN had been requested by veterinarians between April 2012 and December 2019. This profile contains direct detection methods via polymerase chain reaction (PCR) for Hepatozoon spp. and Dirofilaria spp. as well as indirect detection methods via immunofluorescence antibody test (IFAT) for Ehrlichia spp. and Leishmania spp. This profile was expanded to include an IFAT for Rickettsia spp. from July 2015 onwards. The prevalence of the different vector-borne infectious agents was calculated. Results: A total of 602 cats were tested using the ‘Feline Travel Profile’. Positive test results were as follows: Rickettsia spp. IFAT 54/442 (12.2%), Ehrlichia spp. IFAT 68/602 (11.3%), Leishmania spp. IFAT 21/602 (3.5%), Hepatozoon spp. PCR 51/595 (8.6%), and Dirofilaria spp. PCR 1/595 cats (0.2%). Co-infections with more than one pathogen could be detected in 22/602 cats. Conclusions: 170/602 cats (28.2%) were tested positive for at least one vector-borne pathogen. Infections with multiple pathogens could be detected in 3.7% of the cats. The data emphasizes the importance of considering vector-borne infections as potential differential diagnoses in cats.

Keywords: arthopod-transmitted infections, feline vector-borne infections, Germany, laboratory diagnostics

Procedia PDF Downloads 153

Authors: Ayodeji Blessing Ajileye

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Introduction: Infertility is described as failure to conceive after one year of unprotected sexual intercourse. One of the causes of female infertility is caused by cervical abnormalities which may be due to bacterial and parasitological infections, hormonal imbalances of Lentinizing hormone, follicular stimulating hormone, oestrogen hormone and progesterone hormone. Aim of the Study: This study aimed to determine the prevalence and pattern of abnormal cervical Pap smear in women with infertility attending fertility clinics at Uniosun Teaching Hospitals Osogbo, Osun State. Methods: This study was conducted at the fertility clinic of University of Osun Teaching Hospital, Osogbo, Osun State. The study population comprised of 50 infertile women and 50 fertile women who are attending the gynecology clinic of University of Osun Teaching Hospital, Osogbo, Osun State. Questionnaire was used to obtain relevant data. Cervical sample was collected using Ayre’s spatula, two smears were prepared and stained with Papanicolaous and H&E staining techniques. Results were analyzed using frequency table. Results: This study observed the prevalence of abnormal cervical smear among infertility women to be 16(30%), while only 03(6%) were observed among the control group (fertile women). Atypical squamous cells of undetermined significance have the highest abnormalities observed in this study with 30%, about 28% of the Pap smear results were negative for inflammation, while total inflammation observed was 72% among the infertility women. Conclusion: This study concluded that abnormal pap smears in this study is significantly more often in women with infertility as compared with fertile women.

Keywords: infertility, oestrogen hormone, pap smears, progesterone hormone

Procedia PDF Downloads 54

Authors: Q. Rzina, M. Lahrouni, S. Rida, N. Saadaoui, Y. Almossaid, K. Oufdou, K. Fares

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Many organic solid wastes are produced in the world. Poultry manure (PM), municipal organic wastes (MOW) and sugar beet lime sludge (LS) are produced in large quantities in Morocco. The co-composting of these organic wastes was investigated. The recycling and the valorization of such wastes is environmentally and economically beneficial especially for PM which is known source of bacterial pathogens. The aerobic biodegradation process was carried out by using three windrows of variable compositions: C1 prepared without LS (only MOW were composted with PM), C2 prepared from MOW plus PM and10% LS; and the last one C3 from MOW plus PM and 20% LS. The main process physico-chemical parameters (temperature, pH, humidity and C/N) and microbiological populations (mesophilic and thermophilic flora, total coliform, fecal coliform, Streptococci, Staphylococcus aureus and mesophilic fungi) were monitored over three months to ascertain the compost maturity and to ensure the compost hygienic aspect. The final products were characterized by their relatively high organic matter content, and low C/N ratio of 10.6-10.9. The organic matter degradation was reached approximately 59% for C2 and C3. In addition, the monitoring of the microbial population showed that the produced composts are mature and hygienic. The agronomic valorization of the final composts was tested on radish plant with tree level of composts and poultry manure without composting. The primary results of field trial showed a growth of radish plant biomass and root development without any phytotoxicity detected which reflects the quality of the composts produced. As for poultry manure it allowed to have a better results than other composts because of its readily available nitrogen.

Keywords: compost, municipal organic wastes, poultry manure, radish crop, sugar beet lime sludge

Procedia PDF Downloads 285

Authors: F. Yılmaz, Y. Saylan, A. Derazshamshir, S. Atay, A. Denizli

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Quartz crystal microbalance (QCM), high-resolution mass-sensing technique, measures changes in mass on oscillating quartz crystal surface by measuring changes in oscillation frequency of crystal in real time. Protein adsorption techniques via hydrophobic interaction between protein and solid support, called hydrophobic interaction chromatography (HIC), can be favorable in many cases. Some nanoparticles can be effectively applied for HIC. HIC takes advantage of the hydrophobicity of proteins by promoting its separation on the basis of hydrophobic interactions between immobilized hydrophobic ligands and nonpolar regions on the surface of the proteins. Lysozyme is found in a variety of vertebrate cells and secretions, such as spleen, milk, tears, and egg white. Its common applications are as a cell-disrupting agent for extraction of bacterial intracellular products, as an antibacterial agent in ophthalmologic preparations, as a food additive in milk products and as a drug for treatment of ulcers and infections. Lysozyme has also been used in cancer chemotherapy. The aim of this study is the synthesis of hydrophobic nanoparticles for Lysozyme detection. For this purpose, methacryoyl-L-phenylalanine was chosen as a hydrophobic matrix. The hydrophobic nanoparticles were synthesized by micro-emulsion polymerization method. Then, hydrophobic QCM nanosensor was characterized by Attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy, atomic force microscopy (AFM) and zeta size analysis. Hydrophobic QCM nanosensor was tested for real-time detection of Lysozyme from aqueous solution. The kinetic and affinity studies were determined by using Lysozyme solutions with different concentrations. The responses related to a mass (Δm) and frequency (Δf) shifts were used to evaluate adsorption properties.

Keywords: nanosensor, HIC, lysozyme, QCM

Procedia PDF Downloads 331

Authors: Lemar Blake, Chris Oura, Ayanna C. N. Phillips Savage

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Improved DNA sequencing technology has greatly enhanced bacterial identification, especially for organisms that are difficult to culture. Mycobacteriosis with consistent hyphema, bilateral exophthalmia, open mouth gape and ocular lesions, were observed in various fish populations at the School of Veterinary Medicine, Aquaculture/Aquatic Animal Health Unit. Objective: To identify the species of Mycobacterium that is affecting aquarium fish at the School of Veterinary Medicine, Aquaculture/Aquatic Animal Health Unit. Method: A total of 13 fish samples were collected and analyzed via: Ziehl-Neelsen, conventional polymerase chain reaction (PCR) and real-time PCR. These tests were carried out simultaneously for confirmation. The following combination of conventional primers: 16s rRNA (564 bp), rpoB (396 bp), sod (408 bp) were used. Concatenation of the gene fragments was carried out to phylogenetically classify the organism. Results: Acid fast non-branching bacilli were detected in all samples from homogenized internal organs. All 13 acid fast samples were positive for Mycobacterium via real-time PCR. Partial gene sequences using all three primer sets were obtained from two samples and demonstrated a novel strain. A strain 99% related to Mycobacterium marinum was also confirmed in one sample, using 16srRNA and rpoB genes. The two novel strains were clustered with the rapid growers and strains that are known to affect humans. Conclusions: Phylogenetic analysis demonstrated two novel Mycobacterium strains with the potential of being zoonotic and one strain 99% related to Mycobacterium marinum.

Keywords: polymerase chain reaction, phylogenetic, DNA sequencing, zoonotic

Procedia PDF Downloads 121

Authors: Shani Brathwaite, Deborah Villarroel-Lamb

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Wave run-up may be defined as the time-varying position of the landward extent of the water’s edge, measured vertically from the mean water level position. The hydrodynamics of the swash zone and the accurate prediction of maximum wave run-up, play a critical role in the study of coastal engineering. The understanding of these processes is necessary for the modeling of sediment transport, beach recovery and the design and maintenance of coastal engineering structures. However, due to the complex nature of the swash zone, there remains a lack of detailed knowledge in this area. Particularly, there has been found to be insufficient consideration of bed porosity and ultimately infiltration/exfiltration processes, in the development of wave run-up models. Theoretically, there should be an inverse relationship between maximum wave run-up and beach porosity. The greater the rate of infiltration during an event, associated with a larger bed porosity, the lower the magnitude of the maximum wave run-up. Additionally, most models have been developed using data collected on North American or Australian beaches and may have limitations when used for operational forecasting in Trinidad. This paper aims to assess the influence and significance of infiltration and exfiltration processes on wave run-up magnitudes within the swash zone. It also seeks to pay particular attention to how well various empirical formulae can predict maximum run-up on contrasting beaches in Trinidad. Traditional surveying techniques will be used to collect wave run-up and cross-sectional data on various beaches. Wave data from wave gauges and wave models will be used as well as porosity measurements collected using a double ring infiltrometer. The relationship between maximum wave run-up and differing physical parameters will be investigated using correlation analyses. These physical parameters comprise wave and beach characteristics such as wave height, wave direction, period, beach slope, the magnitude of wave setup, and beach porosity. Most parameterizations to determine the maximum wave run-up are described using differing parameters and do not always have a good predictive capability. This study seeks to improve the formulation of wave run-up by using the aforementioned parameters to generate a formulation with a special focus on the influence of infiltration/exfiltration processes. This will further contribute to the improvement of the prediction of sediment transport, beach recovery and design of coastal engineering structures in Trinidad.

Keywords: beach porosity, empirical models, infiltration, swash, wave run-up

Procedia PDF Downloads 335

Authors: Anoff Anim, Lila Mahmoud, Maria Katsikogianni, Sanjit Nayak

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Sustained and controlled delivery of antimicrobial drugs have been largely studied recently using metal organic frameworks (MOFs)and different polymers. However, much attention has not been given to combining both MOFs and biodegradable polymers, which would be a good strategy in providing a sustained gradual release of the drugs. Herein, we report a comparative study of the sustained and controlled release of widely used antibacterial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated in biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) membranes. Cephalexin and metronidazole were separately incorporated in MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL membranes. The pristine MOF-5 and the loaded MOFs were thoroughly characterized by FT-IR, SEM, TGA and PXRD. Drug release studies were carried out to assess the release rate of the drugs in PBS and distilled water for up to 48 hours using UV-Vis Spectroscopy. Four bacterial strains from both the Gram-positive and Gram-negative types, Staphylococus aureus, Staphylococuss epidermidis, Escherichia coli, Acinetobacter baumanii, were tested against the pristine MOF, pure drugs, loaded MOFs and the drug-loaded MOF-polymer composites. Metronidazole-loaded MOF-5 composite of PLGA (PLGA-Met@MOF-5) was found to show highest efficiency to inhibit the growth of S. epidermidis compared to the other bacteria strains while maintaining a sustained minimum inhibitory concentration (MIC). This study demonstrates that the combination of biodegradable MOF-polymer composites can provide an efficient platform for sustained and controlled release of antimicrobial drugs and can be a potential strategy to integrate them in biomedical devices.

Keywords: antimicrobial resistance, biodegradable polymers, cephalexin, drug release metronidazole, MOF-5, PCL, PLGA

Procedia PDF Downloads 114

Authors: Carmen M. Gonzalez-Henriquez, Mauricio A. Sarabia-Vallejos, Juan Rodriguez-Hernandez

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DMAEMA, as a monomer, has been widely studied and used in several application fields due to their pH-sensitive capacity (tertiary amine protonation), being relevant in the biomedical area as a potential carrier for drugs focused on the treatment of genetic or acquired diseases (efficient gene transfection), among others. Additionally, the inhibition of bacterial growth and, therefore, their antimicrobial activity, can be used as dual-functional antifogging/antimicrobial polymer coatings. According to their interesting physicochemical characteristics and biocompatible properties, DMAEMA was used as a monomer to synthesize a smart pH-sensitive hydrogel, namely poly(HEMA-co-PEGDA575-co-DMAEMA). Thus, different mole ratios (ranging from 5:1:0 to 0:1:5, according to the mole ratio between HEMA, PEGDA, and DEAEMA, respectively) were used in this research. The surface patterns formed via a two-step polymerization (redox- and photo-polymerization) were first chemically studied via 1H-NMR and elemental analysis. Secondly, the samples were morphologically analyzed by using Field-Emission Scanning Electron Microscopy (FE-SEM) and Atomic Force Microscopy (AFM) techniques. Then, a particular relation between HEMA, PEGDA, and DEAEMA (0:1:5) was also characterized at three different pH (5.4, 7.4 and 8.3). The hydrodynamic radius and zeta potential of the micro-hydrogel particles (emulsion) were carried out as a possible control for morphology, exploring the effect that produces hydrogel micelle dimensions in the wavelength, height, and roughness of the wrinkled patterns. Finally, contact angle and cross-hatch adhesion test was carried out for the hydrogels supported on glass using TSM-silanized surfaces in order to measure their mechanical properties.

Keywords: wrinkled patterns, smart pH-sensitive hydrogels, hydrogel micelle diameter, adhesion tests

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Authors: Zainab Bibi, Afsheen Aman, Shah Ali Ul Qader

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Endo-β-1,4-xylanases [EC 3.2.1.8] are one of the major groups of enzymes that are involved in degradation process of xylan and have several applications in food, textile and paper processing industries. Due to broad utility of endo-β-1,4-xylanase, researchers are focusing to increase the productivity of this hydrolase from various microbial species. Harsh industrial condition, faster reaction rate and efficient hydrolysis of xylan with low risk of contamination are critical requirements of industry that can be fulfilled by synthesizing the enzyme with efficient properties. In the current study, a newly isolated thermophile Geobacillus stearothermophilus KIBGE-IB29 was used in order to attain the maximum production of endo-1,4-β-xylanase. Bacterial culture was isolated from soil, collected around the blast furnace site of a steel processing mill, Karachi. Optimization of various nutritional and physical factors resulted the maximum synthesis of endo-1,4-β-xylanase from a thermophile. High production yield was achieved at 60°C and pH-6.0 after 24 hours of incubation period. Various nitrogen sources viz. peptone, yeast extract and meat extract improved the enzyme synthesis with 0.5%, 0.2% and 0.1% optimum concentrations. Dipotassium hydrogen phosphate (0.25%), potassium dihydrogen phosphate (0.05%), ammonium sulfate (0.05%) and calcium chloride (0.01%) were noticed as valuable salts to improve the production of enzyme. The thermophilic nature of isolate, with its broad pH stability profile and reduced fermentation time indicates its importance for effective xylan saccharification and for large scale production of endo-1,4-β-xylanase.

Keywords: geobacillus, optimization, production, xylanase

Procedia PDF Downloads 295

Authors: Anoff Anim, Lila A. M. Mahmoud, Maria Katsikogianni, Sanjit Nayak

Abstract:

Sustained and controlled delivery of antimicrobial drugs have been largely studied recently using metal organic frameworks (MOFs)and different polymers. However, much attention has not been given to combining both MOFs and biodegradable polymers, which would be a good strategy in providing a sustained gradual release of the drugs. Herein, we report a comparative study of the sustained and controlled release of widely used antibacterial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated in biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) membranes. Cephalexin and metronidazole were separately incorporated in MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL membranes. The pristine MOF-5 and the loaded MOFs were thoroughly characterized by FT-IR, SEM, TGA and PXRD. Drug release studies were carried out to assess the release rate of the drugs in PBS and distilled water for up to 48 hours using UV-Vis Spectroscopy. Four bacterial strains from both the Gram-positive and Gram-negative types, Staphylococus aureus, Staphylococuss epidermidis, Escherichia coli, Acinetobacter baumanii, were tested against the pristine MOF, pure drugs, loaded MOFs and the drug-loaded MOF-polymer composites. Metronidazole-loaded MOF-5 composite of PLGA (PLGA-Met@MOF-5) was found to show highest efficiency to inhibit the growth of S. epidermidis compared to the other bacteria strains while maintaining a sustained minimum inhibitory concentration (MIC). This study demonstrates that the combination of biodegradable MOF-polymer composites can provide an efficient platform for sustained and controlled release of antimicrobial drugs and can be a potential strategy to integrate them in biomedical devices.

Keywords: antimicrobial resistance, biodegradable polymers, cephalexin, drug release metronidazole, MOF-5, PCL, PLGA

Procedia PDF Downloads 113

Authors: M. Imran Hamid, Muzammil Hussain, Yunpeng Wu, Meichun Xiang, Xingzhong Liu

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The rhizosphere microbiome elucidate multiple functioning in the soil suppressiveness against plant pathogens. Soybean rhizosphere microbial communities may involve in the natural suppression of soybean cyst nematode (SCN) populations in disease suppressive soils. To explore these ecological mechanisms of microbes, a long term monoculture suppressive soil were taken into account for further investigation to test the disease suppressive ability by using different treatments. The designed treatments are as, i) suppressive soil (S), ii) conducive soil (C), iii) conducive soil mixed with 10% (w/w) suppressive soil (CS), iv) suppressive soil treated at 80°C for 1 hr (S80), and v) suppressive soil treated with formalin (SF). By using an ultra-high-throughput sequencing approach, we identified the key bacterial and fungal taxa involved in SCN suppression. The Phylum-level investigation of bacteria revealed that Actinobacteria, Bacteroidetes, and Proteobacteria in the rhizosphere soil of soybean seedlings were more abundant in the suppressive soil than in the conducive soil. The phylum-level analysis of fungi in rhizosphere soil indicated that relative abundance of Ascomycota was higher in suppressive soil than in the conducive soil, where Basidiomycota was more abundant. Transferring suppressive soil to conducive soil increased the population of Ascomycota in the conducive soil by lowering the populations of Basidiomycota. The genera, such as, Pochonia, Purpureocillium, Fusarium, Stachybotrys that have been well documented as bio-control agents of plant nematodes were far more in the disease suppressive soils. Our results suggested that the plants engage a subset of functional microbial groups in the rhizosphere for initial defense upon nematode attack and protect the plant roots later on by nematodes to response for suppression of SCN in disease-suppressive soils.

Keywords: disease suppressive soil, high-throughput sequencing, rhizosphere microbiome, soybean cyst nematode

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Authors: Yuriy A. Knirel

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Enteric bacteria Escherichia coli is the predominant facultative anaerobe of the colonic flora, and some specific serotypes are associated with enteritis, hemorrhagic colitis, and hemolytic uremic syndrome. Shigella spp. are human pathogens that cause diarrhea and bacillary dysentery (shigellosis). They are in effect E. coli with a specific mode of pathogenicity. Strains of Salmonella enterica are responsible for a food-borne infection (salmonellosis), and specific serotypes cause typhoid fever and paratyphoid fever. All these bacteria are closely related in respect to structure and genetics of the lipopolysaccharide, including the O-polysaccharide part (O‑antigen). Being exposed to the bacterial cell surface, the O antigen is subject to intense selection by the host immune system and bacteriophages giving rise to diverse O‑antigen forms and providing the basis for typing of bacteria. The O-antigen forms of many bacteria are unique, but some are structurally and genetically related to others. The sequenced O-antigen gene clusters between conserved galF and gnd genes were analyzed taking into account the O-antigen structures established by us and others for all S. enterica and Shigella and most E. coli O-serogroups. Multiple genetic mechanisms of diversification of the O-antigen forms, such as lateral gene transfer and mutations, were elucidated and are summarized in the present paper. They include acquisition or inactivation of genes for sugar synthesis or transfer or recombination of O-antigen gene clusters or their parts. The data obtained contribute to our understanding of the origins of the O‑antigen diversity, shed light on molecular evolutionary relationships between the O-antigens of enteric bacteria, and open a way for studies of the role of gene polymorphism in pathogenicity.

Keywords: enteric bacteria, O-antigen gene cluster, polysaccharide biosynthesis, polysaccharide structure

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Authors: Faisal Nouroz, Mukaramin Mukaramin

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Of the transposable elements (TEs), the retrotransposons are the most copious elements identified from many sequenced genomes. They have played a major role in genome evolution, rearrangement, and expansions based on their copy and paste mode of proliferation. They are further divided into LTR and Non-LTR retrotransposons. The purpose of the current study was to identify the LTR REs in sequenced Phoenix dactylifera genome and to study their structural diversity. A total of 150 P. dactylifera BAC sequences with > 60kb sizes were randomly retrieved from National Center for Biotechnology Information (NCBI) database and screened for the presence of LTR retrotransposons. Seven bacterial artificial chromosomes (BAC) sequences showed full-length LTR Retrotransposons with 4 Copia and 3 Gypsy families having variable copy numbers in respective families. Reverse transcriptase (RT) domain was found as the most conserved domain among Copia and Gypsy superfamilies and was used to deduce evolutionary analysis. The amino acid residues among various RT sequences showed variability in their percentages indicating post divergence evolution. Amino acid Leucine was found in highest proportions followed by Lysine, while Methionine and Tryptophan were in lowest percentages. The phylogenetic analysis based on RT domains confirmed that although having most conserved RT regions, several evolutionary events occurred causing nucleotide polymorphisms and hence clustering of Gypsy and Copia superfamilies into their respective lineages. The study will be helpful in identification and annotation of these elements in other species and genera and their distribution patterns on chromosomes by fluorescent in situ hybridization techniques.

Keywords: transposable elements, Phoenix dactylifera, retrotransposons, phylogenetic analysis

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Authors: Shirl H. Terrell

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In the telling of mythologies, stories of cultural and religious histories, the creative arts provide an archetypal lens through which the personal and collective unconscious are viewed, thus revealing mysteries of the unknown psyche. To that end, the author of this paper, using the hermeneutic approach, proves that Carlisle Floyd’s (1955) English language opera Susannah illuminates humanity’s instinctual nature and behaviors through music, libretto, and drama. While impressive musical works such as Wagner’s Ring Cycle and Webber’s Phantom of the Opera have received extensive Jungian analyses, critics and scholars often ignore lesser esteemed works, such as Susannah, notwithstanding the fact that they have been consistently performed on the theater circuit. Such pieces, when given notice, allow viewers to grasp the soul-making depth and timeless quality of productions which may otherwise go unrecognized as culturally or psychologically significant. Although Susannah has sometimes been described as unsophisticated and simple in scope, the author demonstrates why Floyd’s 'little' opera, set in New Hope Valley, Appalachia, a cultural region in the Eastern United States known for its prevailing myths and distortions of isolation, temperament, and the judgmentally conservative behavior of its inhabitants, belongs to opera’s hallmark works. Its approach to powerful underlying archetypal themes, which give rise to the poignant and haunting depictions of the darker and destructive side of the human soul, the Shadow, provides crucial significance to the work. The Shadow’s manifestation in the form of the scapegoating complex is central to the plot of Susannah; the church’s meting out of rules, judgment, and reparation for sins point to the foreboding aspects of human behavior that evoke their intrinsic nature. The scapegoating complex is highlighted in an eight-step process gleaned from the works of Kenneth Burke and Rene Girard. In summary, through depth psychological terms and mythological motifs, the author provides an insightful approach to perceiving instinctual behaviors as they play out in an American opera that has been staged over eight-hundred times, yet, unfortunately, remains in the shadows. Susannah’s timelessness is now.

Keywords: archetypes, mythology, opera, scapegoating, Shadow, Susannah

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Authors: Claus Bier, Dennis Binder, Alexander Gruenberger, Dagmar Drobietz, Dietrich Kohlheyer, Anita Loeschcke, Karl Erich Jaeger, Thomas Drepper, Joerg Pietruszka

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Light absorbing chromophoric systems are important optogenetic tools for biotechnical and biophysical investigations. Processes such as fluorescence or photolysis can be triggered by light-absorption of chromophores. These play a central role in life science. Photocaged compounds belong to such chromophoric systems. The photo-labile protecting groups enable them to release biologically active substances with high temporal and spatial resolution. The properties of photocaged compounds are specified by the characteristics of the caging group as well as the characteristics of the linked effector molecule. In our research, we work with different types of photo-labile protecting groups and various effector molecules giving us possible access to a large library of caged compounds. As a function of the caged effector molecule, a nearly limitless number of biological systems can be directed. Our main interest focusses on photocaging carbohydrates (e.g. arabinose) and their derivatives as effector molecules. Based on these resulting photocaged compounds a precisely controlled photoinduced gene expression will give us access to studies of numerous biotechnological and synthetic biological applications. It could be shown, that the regulation of gene expression via light is possible with photocaged carbohydrates achieving a higher-order control over this processes. With the one-step cleavable photocaged carbohydrate, a homogeneous expression was achieved in comparison to free carbohydrates.

Keywords: bacterial gene expression, biotechnology, caged compounds, carbohydrates, optogenetics, photo-removable protecting group

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Authors: Ismail Mahdi, Nidal Fahsi, Mohamed Hafidi, Abdelmounaim Allaoui, Latefa Biskri

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To meet the worldwide demand for food, smart management of arable lands is needed. This could be achieved through sustainable approaches such as the use of plant growth-promoting microorganisms including bacteria. Phosphate (P) solubilization is one of the major mechanisms of plant growth promotion by associated bacteria. In the present study, we isolated and screened 14 strains from the rhizosphere of Chenopodium quinoa wild grown in the experimental farm of UM6P and assessed their plant growth promoting properties. Next, they were identified by using 16S rRNA and Cpn60 genes sequencing as Bacillus, Pseudomonas and Enterobacter. These strains showed dispersed capacities to solubilize P (up to 346 mg L−1) following five days of incubation in NBRIP broth. We also assessed their abilities for indole acetic acid (IAA) production (up to 795,3 µg ml−1) and in vitro salt tolerance. Three Bacillus strains QA1, QA2, and S8 tolerated high salt stress induced by NaCl with a maximum tolerable concentration of 8%. Three performant isolates, QA1, S6 and QF11, were further selected for seed germination assay because of their pronounced abilities in terms of P solubilization, IAA production and salt tolerance. The early plant growth potential of tested strains showed that inoculated quinoa seeds displayed greater germination rate and higher seedlings growth under bacterial treatments. The positive effect on seed germination traits strongly suggests that the tested strains are growth promoting, halotolerant and P solubilizing bacteria which could be exploited as biofertilizers.

Keywords: phosphate solubilizing bacteria, IAA, Seed germination, salt tolerance, quinoa

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Authors: Przemyslaw Nogly, Tobias Weinert, Daniel James, Sergio Carbajo, Dmitry Ozerov, Antonia Furrer, Dardan Gashi, Veniamin Borin, Petr Skopintsev, Kathrin Jaeger, Karol Nass, Petra Bath, Robert Bosman, Jason Koglin, Matthew Seaberg, Thomas Lane, Demet Kekilli, Steffen Brünle, Tomoyuki Tanaka, Wenting Wu, Christopher Milne, Thomas A. White, Anton Barty, Uwe Weierstall, Valerie Panneels, Eriko Nango, So Iwata, Mark Hunter, Igor Schapiro, Gebhard Schertler, Richard Neutze, Jörg Standfuss

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Ultrafast isomerization of retinal is the primary step in a range of photoresponsive biological functions including vision in humans and ion-transport across bacterial membranes. We studied the sub-picosecond structural dynamics of retinal isomerization in the light-driven proton pump bacteriorhodopsin using an X-ray laser. Twenty snapshots with near-atomic spatial and temporal resolution in the femtosecond regime show how the excited all-trans retinal samples conformational states within the protein binding pocket prior to passing through a highly-twisted geometry and emerging in the 13-cis conformation. The aspartic acid residues and functional water molecules in proximity of the retinal Schiff base respond collectively to formation and decay of the initial excited state and retinal isomerization. These observations reveal how the protein scaffold guides this remarkably efficient photochemical reaction.

Keywords: bacteriorhodopsin, free-electron laser, retinal isomerization mechanism, time-resolved crystallography

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Authors: Malalage Mudara Peiris

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Objectives of the study are: the biosynthesis of silver nanoparticles (AgNPs) using Escherichia coli, Acinetobacter baumannii and Staphylococcus aureus, characterization of silver nanoparticles and determination of antimicrobial activity against E. coli, P. aeruginosa, S. aureus, MRSA, and C. Albicans. Methods: E. coli (ATCC 25922), A. baumanii (clinical strain), S. aureus (clinical strain) cultured in nutrient broth medium were used for biosynthesis of AgNPs. Culture conditions (AgNO3 concentration, pH, incubation time and temperature) were optimized. Characterization of synthesized NPs was done by UV-Visible spectroscopy. The antimicrobial activity of the synthesized NPs was studied using the good diffusion assay against E. coli, S. aureus, MRSA (Methicillin-resistant Staphylococcus aureus), P. aeruginosa and C. Albicans. Results: All the selected bacteria produced silver nanoparticles at alkaline pH above 0.3 g/L AgNO3 concentration. The optimum reaction temperature was 60oC. According to the UV-Visible spectroscopy, the maximum absorbance was found to be around 420 - 430 nm indicating the presence of AgNPs. According to the good diffusion results, AgNPs produced by S. aureus resulted in the larger zone of inhibition (ZOI) against the selected pathogens, while AgNPs produced by E. coli showed comparatively smaller ZOI. In general, biosynthesized AgNPs were highly effective against gram-negative bacteria compared to gram-positive bacterial and fungal species. Conclusions: Green AgNPs produced by each bacterium show antimicrobial activity against the selected pathogens. AgNPs produced by S. aureus are the most effective NPs among tested AgNPs, while AgNPs produced by E. coli are the least effective. Further characterization of NPs is required to study the physical properties of silver NPs.

Keywords: green nanotechnology, silver nanoparticles, bacteria, antimicrobial activity

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Authors: Asmuddin Natsir, A. Mujnisa, Syahriani Syahrir, Marhamah Nadir, Nurul Purnomo

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Bacteria, protozoa, Archaea, and fungi are the dominant microorganisms found in the rumen ecosystem that has an important role in converting feed ingredients into components that can be digested and utilized by the livestock host. This study was conducted to assess the diversity of rumen bacteria of bali cattle raised under traditional farming condition. Three adult bali cattle were used in this experiment. The rumen fluid samples from the three experimental animals were obtained by the Stomach Tube method before the morning feeding. The results of study indicated that the Illumina sequencing was successful in identifying 301,589 sequences, averaging 100,533 sequences, from three rumen fluid samples of three cattle. Furthermore, based on the SILVA taxonomic database, there were 19 kinds of phyla that had been successfully identified. Of the 19 phyla, there were only two dominant groups across the three samples, namely Bacteroidetes and Firmicutes, with an average percentage of 83.68% and 13.43%, respectively. Other groups such as Synergistetes, Spirochaetae, Planctomycetes can also be identified but in relatively small percentage. At the genus level, there were 157 sequences obtained from all three samples. Of this number, the most dominant group was Prevotella 1 with a percentage of 71.82% followed by 6.94% of Christencenellaceae R-7 group. Other groups such as Prevotellaceae UCG-001, Ruminococcaceae NK4A214 group, Sphaerochaeta, Ruminococcus 2, Rikenellaceae RC9 gut group, Quinella were also identified but with very low percentages. The sequencing results were able to detect the presence of 3.06% and 3.92% respectively for uncultured rumen bacterium and uncultured bacterium. In conclusion, the results of this experiment can provide an opportunity for a better understanding of the rumen bacterial diversity of the bali cattle raised under traditional farming condition and insight regarding the uncultured rumen bacterium and uncultured bacterium that need to be further explored.

Keywords: 16S rRNA sequencing, bali cattle, rumen microbial diversity, uncultured rumen bacterium

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Authors: Arslan Masood Pirzada, Muhammad Naeem, Hafiz Haider Ali, Muhammad Latif, Aown Sammar Raza, Asad Hussain Bukhari, Muhammad Saqib, Muhammad Ijaz

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Cyperus rotundus (Cyperaceae), a medicinal herb, is being traditionally used as a home remedy for the treatment of various clinical conditions like diarrhea, diabetic, pyretic, inflammation, malaria, and for treating stomach and bowel disorders. Its current status is one of the most widespread, troublesome, and economically damaging agronomic weeds, growing wildly in various tropical and sub-tropical regions of the world. Tuber and rhizomes of Cyperus rotundus possess a higher concentration of active ingredients in the form of essential oils, phenolic acids, ascorbic acids and flavonoids, responsible for its remedial properties. Exploitation of any medicinal plant application depends on the crucial and comprehensive information about the therapeutic potential of a plant. Researchers have evaluated and characterized the significance of Cyperus rotundus as an anti-androgenic, anti-bacterial, anti-cancerous, anti-convulsant, anti-diabetic, anti-diarrheal, anti-genotoxic, anti-inflammatory, anti-lipidemic, anti-malarial, anti-mutagenic, anti-obesity, anti-oxidant, anti-uropathogenic, hepato-, cardio-, neuroprotective, and nootropic agent. This paper comprises a broad review to summarize the current state of knowledge about chemical constituents, potential economic uses and therapeutic aspects of Cyperus rotundus that will aid in the development of bioethanol and modern herbal medicine through latest technologies that will promote the ability of this plant in the cure of many clinical disorders.

Keywords: purple nutsedge, chemical composition, economic uses, therapeutic values, future directions

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Authors: Khushbu Priyadarshi, Chandramani Pathak

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Cancer cells can develop resistance to conventional therapies especially chemotherapeutic drugs. Resistance to chemotherapy is another challenge in cancer therapeutics. Therefore, it is important to address this issue. Gallic acid (GA) is a natural plant compound that exhibits various biological properties including anti-proliferative, anti-inflammatory, anti-oxidant and anti-bacterial. Despite of the wide spectrum biological properties GA has cytotoxic response and low bioavailability. To overcome this problem, GA was conjugated with the Polyamidoamine(PAMAM) dendrimer for improving the bioavailability and efficient delivery in drug-resistant HCT-116 Colon Cancer cells. Gallic acid was covalently linked to 4.0 G PAMAM dendrimer. PAMAM dendrimer is well established nanocarrier but has cytotoxicity due to presence of amphiphilic nature of amino group. In our study we have modified surface of PAMAM dendrimer with Gallic acid and examine their anti-proliferative effects in drug-resistant HCT-116 cells. Further, drug-resistant colon cancer cells were established and thereafter treated with different concentration of PAMAM-GA to examine their anti-proliferative potential. Our results show that PAMAM-GA conjugate induces apoptotic cell death in HCT-116 and drug-resistant cells observed by Annexin-PI staining. In addition, it also shows that multidrug-resistant drug transporter P-gp protein expression was downregulated with increasing the concentration of GA conjugate. After that we also observed the significant difference in Rh123 efflux and accumulation in drug sensitive and drug-resistant cancer cells. Thus, our study suggests that conjugation of anti-cancer agents with PAMAM could improve drug resistant property and cytotoxic response to treatment of cancer.

Keywords: drug resistance, gallic acid, PAMAM dendrimer, P-glycoprotein

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Authors: Omoruyi Gold Idemudia, Alexander P. Sadimenko

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The synthesis of N-heterocycles with novel properties, having broad spectrum biological activities that may become alternative medicinal drugs, have been attracting a lot of research attention due to the emergence of medicinal drug’s limitations such as disease resistance and their toxicity effects among others. Acylpyrazolones have been employed as pharmaceuticals as well as analytical reagent and their application as coordination complexes with transition metal ions have been well established. By way of a condensation reaction with amines acylpyrazolone ketones form a more chelating and superior group of compounds known as azomethines. 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one was reacted with phenylhydrazine to get a new phenylhydrazone which was further reacted with aqueous solutions of palladium and platinum salts, in an effort towards the discovery of transition metal based synthetic drugs. The compounds were characterized by means of analytical, spectroscopic, thermogravimetric analysis TGA, as well as x-ray crystallography. 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one phenylhydrazone crystallizes in a triclinic crystal system with a P-1 (No. 2) space group based on x-ray crystallography. The bidentate ON ligand formed a square planar geometry on coordinating with metal ions based on FTIR, electronic and NMR spectra as well as magnetic moments. Reported compounds showed antibacterial activities against the nominated bacterial isolates using the disc diffusion technique at 20 mg/ml in triplicates. The metal complexes exhibited a better antibacterial activity with platinum complex having an MIC value of 0.63 mg/ml. Similarly, ligand and complexes also showed antioxidant scavenging properties against 2, 2-diphenyl-1-picrylhydrazyl DPPH radical at 0.5mg/ml relative to ascorbic acid (standard drug).

Keywords: acylpyrazolone, antibacterial studies, metal complexes, phenylhydrazone, spectroscopy

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Authors: Afifa Hafidh, Hedia Chaabane

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This work mainly focused on the synthetic strategies and biological activities associated with pyrazoles. Pyrazole derivatives have been successfully synthesized by simple and facile method and studied for their antibacterial activity. These compounds were prepared from pyrazolic difunctional compounds as starting materials, by reaction with salicylic acid, paracetamol and thiosemicarbazide respectively. Structure of all the prepared compounds confirmation were proved using (FT-IR), (1H-NMR) and (13C-NMR) spectra in addition to melting points. The screening of the antimicrobial activity of the pyrazolic derivatives was examined against different microorganisms in the present study. They were screened for their antimicrobial activities against gram positive bacteria, gram negative bacteria and Candida albicans. The synthesized compounds were found to exhibit high antibacterial and antifungal efficiency against several tested bacterial strains, using agar diffusion method and filter paper disc-diffusion method. Ampicillin was used as positive control for all strains except Candida albicans for which Nystatin was used. The obtained results reveal that the antibacterial activity of some pyrazolic derivatives is comparable to that observed for the control samples (Ampicilin and Nystatin), suggesting a strong antibacterial activity. The analysis of these results shows that synthesized products react on the surfaces cell walls that are disrupted. When these products are in contact with the bacteria, they damage the membrane, leading to the perturbation of different cellular processes and then leakage of cytoplasm, resulting in the death of the cells. The results will be presented in details. The obtained products constitute effective antibacterial agents and important compounds for biological systems.

Keywords: salicylic acid, antimicrobial activities, antioxidant activity, paracetamol, pyrazole, thiosemicarbazide

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