Search results for: pharmaceutical molecules

Authors: Thi Huong Vu, Vijay Jayasena, Zhongxiang Fang, Gary Dykes

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Carob kibble has recently received attention due to the presence of high level of polyphenol antioxidants. The capacity of microorganisms to improve antioxidant activities and total phenolics in carob kibble was investigated in the study. Two types of microorganisms including lactic acid bacteria Lactobacillus plantarum (L. plantarum) and yeast Saccharomyces cerevisiae (S. cerevisiae) were used in single and in their combination as starters. The total phenolic content was determined by the Folin–Ciocalteu method. Antioxidant activities were assessed scavenging capacity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS). The study found that S. cerevisiae alone considerably improved 55% total phenolics content at 15 h, while L. plantarum caused in a loss of 20% through the process. Antioxidant capacity of the yeast-fermented samples significantly increased by 43 % and 10 % in ABTS and DPPH assays, respectively. However, reduction of 13 % and 32 % inhibition were recorded in the carob treated with L. plantarum. In the combination of S. cerevisiae and L. plantarum (1:1), both total phenolic content and antioxidant activity of carob kibble were a similar trend as these of S. cerevisiae single, but a lower improvement. The antioxidant power of the extracts was linearly correlated to their total phenolic contents (R=0.75). The results suggested that S. cerevisiae alone was the better for enhancement of both total phenolic content and antioxidant activity in carob kibble using submerged fermentation. The efficiency of fermentation reached the highest at 15h. Thus submerged fermentation with S. cerevisiae offers a tool with simple and cost effective to further increase the bioactive potential of carob kibble, which is in use for food, cosmetic and pharmaceutical industries.

Keywords: antioxidant activity, carob kibble, lactobacillus plantarum, saccharomyces cerevisiae, total phenolics

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Authors: P. Acosta-Santamaría, A. Ibatá-Soto, A. López-Vásquez

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Organic compounds in wastewaters coming from textile and pharmaceutical industry generated multiple harmful effects on the environment and the human health. One of them is the methyl orange (MeO), an azoic dye considered to be a recalcitrant compound. The heterogeneous photocatalysis emerges as an alternative for treating this type of hazardous compounds, through the generation of OH radicals using radiation and a semiconductor oxide. According to the author’s knowledge, catalysts such as TiO₂ doped with metals show high efficiency in degrading MeO; however, this presents economic limitations on industrial scale. Black sand can be considered as a naturally doped catalyst because in its structure is common to find compounds such as titanium, iron and aluminum oxides, also elements such as zircon, cadmium, manganese, etc. This study reports the photocatalytic activity of the mineral black sand used as semiconductor in the discoloration of MeO by oxidation and reduction photocatalytic techniques. For this, magnetic composites from the mineral were prepared (RM, M1, M2 and NM) and their activity were tested through MeO discoloration while TiO₂ was used as reference. For the fractions, chemical, morphological and structural characterizations were performed using Scanning Electron Microscopy with Energy Dispersive X-Ray (SEM-EDX), X-Ray Diffraction (XRD) and X-Ray Fluorescence (XRF) analysis. M2 fraction showed higher MeO discoloration (93%) in oxidation conditions at pH 2 and it could be due to the presence of ferric oxides. However, the best result to reduction process was using M1 fraction (20%) at pH 2, which contains a higher titanium percentage. In the first process, hydrogen peroxide (H₂O₂) was used as electron donor agent. According to the results, black sand mineral can be used as natural semiconductor in photocatalytic process. It could be considered as a photocatalyst precursor in such processes, due to its low cost and easy access.

Keywords: black sand mineral, methyl orange, oxidation, photocatalysis, reduction

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Authors: Antoine Villa, Moustapha Mohamedou, Florence Pilliere, Catherine Verdun-Esquer, Mathieu Molimard, Mohamed Sidatt Cheikh El Moustaph, Mireille Canal-Raffin

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Context: In Mauritania, the activity of the National Center of Oncology (NCO) has steadily risen leading to an increase in the handling of antineoplastic drugs (AD) by healthcare professionals. In this context, the AD contamination of those professionals is a major concern for occupational physicians. It has been evaluated using biological monitoring of occupational exposure (BMOE). Methods: The intervention took place in 2015, in 2 care units, and evaluated nurses preparing and/or infusing AD and agents in charge of hygiene. Participants provided a single urine sample, at the end of the week, at the end of their shift. Five molecules were sought using specific high sensitivity methods (UHPLC-MS/MS) with very low limits of quantification (LOQ) (cyclophosphamide (CP), Ifosfamide (IF), methotrexate (MTX): 2.5ng/L; doxorubicin (Doxo): 10ng/L; α-fluoro-β-alanine (FBAL, 5-FU metabolite): 20ng/L). A healthcare worker was considered as 'contaminated' when an AD was detected at a urine concentration equal to or greater than the LOQ of the analytical method or at trace concentration. Results: Twelve persons participated (6 nurses, 6 agents in charge of hygiene). Twelve urine samples were collected and analyzed. The percentage of contamination was 66.6% for all participants (n=8/12), 100% for nurses (6/6) and 33% for agents in charge of hygiene (2/6). In 62.5% (n=5/8) of the contaminated workers, two to four of the AD were detected in the urine. CP was found in the urine of all contaminated workers. FBAL was found in four, MTX in three and Doxo in one. Only IF was not detected. Urinary concentrations (all drugs combined) ranged from 3 to 844 ng/L for nurses and from 3 to 44 ng/L for agents in charge of hygiene. The median urinary concentrations were 87 ng/L, 15.1 ng/L and 4.4 ng/L for FBAL, CP and MTX, respectively. The Doxo urinary concentration was found 218ng/L. Discussion: There is no current biological exposure index for the interpretation of AD contamination. The contamination of these healthcare professionals is therefore established by the detection of one or more AD in urine. These urinary contaminations are higher than the LOQ of the analytical methods, which must be as low as possible. Given the danger of AD, the implementation of corrective measures is essential for the staff. Biological monitoring of occupational exposure is the most reliable process to identify groups at risk, tracing insufficiently controlled exposures and as an alarm signal. These results show the necessity to educate professionals about the risks of handling AD and/or to care for treated patients.

Keywords: antineoplastic drugs, Mauritania, biological monitoring of occupational exposure, contamination

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Authors: Syed Asif Hassan, Tabrej Khan

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Multiple sclerosis (MS) is a chronic demyelinating autoimmune disorder, of the central nervous system (CNS). In the present scenario, the current therapies either do not halt the progression of the disease or have side effects which limit the usage of current Disease Modifying Therapies (DMTs) for a longer period of time. Therefore, keeping the current treatment failure schema, we are focusing on screening novel analogues of the available DMTs that specifically bind and inhibit the Sphingosine1-phosphate receptor1 (S1PR1) thereby hindering the lymphocyte propagation toward CNS. The novel drug-like analogs molecule will decrease the frequency of relapses (recurrence of the symptoms associated with MS) with higher efficacy and lower toxicity to human system. In this study, an integrated approach involving ligand-based virtual screening protocol (Ultrafast Shape Recognition with CREDO Atom Types (USRCAT)) to identify the non-toxic drug like analogs of the approved DMTs were employed. The potency of the drug-like analog molecules to cross the Blood Brain Barrier (BBB) was estimated. Besides, molecular docking and simulation using Auto Dock Vina 1.1.2 and GOLD 3.01 were performed using the X-ray crystal structure of Mtb LprG protein to calculate the affinity and specificity of the analogs with the given LprG protein. The docking results were further confirmed by DSX (DrugScore eXtented), a robust program to evaluate the binding energy of ligands bound to the ligand binding domain of the Mtb LprG lipoprotein. The ligand, which has a higher hypothetical affinity, also has greater negative value. Further, the non-specific ligands were screened out using the structural filter proposed by Baell and Holloway. Based on the USRCAT, Lipinski’s values, toxicity and BBB analysis, the drug-like analogs of fingolimod and BG-12 showed that RTL and CHEMBL1771640, respectively are non-toxic and permeable to BBB. The successful docking and DSX analysis showed that RTL and CHEMBL1771640 could bind to the binding pocket of S1PR1 receptor protein of human with greater affinity than as compared to their parent compound (Fingolimod). In this study, we also found that all the drug-like analogs of the standard MS drugs passed the Bell and Holloway filter.

Keywords: antagonist, binding affinity, chemotherapeutics, drug-like, multiple sclerosis, S1PR1 receptor protein

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Authors: Ghassan Mohammad Alalawi, Abobakr Khidir Ziyada, Abdulmajeed Khan

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A potential alternative or next-generation CO₂-selective separation medium that has lately been suggested is ionic liquids (ILs). It is more facile to "tune" the solubility and selectivity of CO₂ in ILs compared to organic solvents via modification of the cation and/or anion structures. Compared to ionic liquids at ambient temperature, polymerized ionic liquids exhibited increased CO₂ sorption capacities and accelerated sorption/desorption rates. This research aims to investigate the correlation between the CO₂ sorption rate and capacity of poly ionic liquids (pILs) and the chemical structure of these substances. The dependency of sorption on the ion conductivity of the pILs' cations and anions is one of the theories we offered to explain the attraction between CO₂ and pILs. This assumption was supported by the Monte Carlo molecular dynamics simulations results, which demonstrated that CO₂ molecules are localized around both cations and anions and that their sorption depends on the cations' and anions' ion conductivities. Polymerized ionic liquids are synthesized to investigate the impact of substituent alkyl chain length, cation, and anion on CO₂ sorption rate and capacity. Three stages are involved in synthesizing the pILs under study: first, trialkyl amine and vinyl benzyl chloride are directly quaternized to obtain the required cation. Next, anion exchange is performed, and finally, the obtained IL is polymerized to form the desired product (pILs). The synthesized pILs' structures were confirmed using elemental analysis and NMR. The synthesized pILs are characterized by examining their structure topology, chloride content, density, and thermal stability using SEM, ion chromatography (using a Metrohm Model 761 Compact IC apparatus), ultrapycnometer, and TGA. As determined by the CO₂ sorption results using a magnetic suspension balance (MSB) apparatus, the sorption capacity of pILs is dependent on the cation and anion ion conductivities. The anion's size also influences the CO₂ sorption rate and capacity. It was discovered that adding water to pILs caused a dramatic, systematic enlargement of pILs resulting in a significant increase in their capacity to absorb CO₂ under identical conditions, contingent on the type of gas, gas flow, applied gas pressure, and water content of the pILs. Along with its capacity to increase surface area through expansion, water also possesses highly high ion conductivity for cations and anions, enhancing its ability to absorb CO₂.

Keywords: polymerized ionic liquids, carbon dioxide, swelling, characterization

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Authors: Ieva Bruzauskaite, Jovile Raudoniute, Karina Poliakovaite, Danguole Zabulyte, Daiva Bironaite, Ruta Aldonyte

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Introduction: Air pollution is a growing global problem which has been shown to be responsible for various adverse health outcomes. Immunotoxicity, such as dysregulated inflammation, has been proposed as one of the main mechanisms in air pollution-associated diseases. Chronic obstructive pulmonary disease (COPD) is among major morbidity and mortality causes worldwide and is characterized by persistent airflow limitation caused by the small airways disease (obstructive bronchiolitis) and irreversible parenchymal destruction (emphysema). Exact pathways explaining the air pollution induced and mediated disease states are still not clear. However, modern societies understand dangers of polluted air, seek to mitigate such effects and are in need for reliable biomarkers of air pollution. We hypothesise that post-translational modifications of structural proteins, e.g. citrullination, might be a good candidate biomarker. Thus, we have designed this study, where mice were exposed to diesel exhaust and the ongoing protein modifications and inflammation in lungs and other tissues were assessed. Materials And Methods: To assess the effects of diesel exhaust a in vivo study was designed. Mice (n=10) were subjected to everyday 2-hour exposure to diesel exhaust for 14 days. Control mice were treated the same way without diesel exhaust. The effects within lung and other tissues were assessed by immunohistochemistry of formalin-fixed and paraffin-embedded tissues. Levels of inflammation and citrullination related markers were investigated. Levels of parenchymal damage were also measured. Results: In vivo study corroborates our own data from in vitro and reveals diesel exhaust initiated inflammatory shift and modulation of lung peptidyl arginine deiminase 4 (PAD4), citrullination associated enzyme, levels. In addition, high levels of citrulline were observed in exposed lung tissue sections co-localising with increased parenchymal destruction. Conclusions: Subacute exposure to diesel exhaust renders mice lungs inflammatory and modifies certain structural proteins. Such structural changes of proteins may pave a pathways to lost/gain function of affected molecules and also propagate autoimmune processes within the lung and systemically.

Keywords: air pollution, citrullination, in vivo, lungs

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Authors: I. Wiedemann, A. R. Sharifi, A. Mählmeyer, C. Knorr

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A requirement for sperm motility is a morphologically intact flagellum with a central axoneme. The flagellar beating is caused by the varying activation and inactivation of dynein molecules which are located in the axoneme. DNAL4 (dynein, axonemal, light chain 4) is regarded as a possible functional candidate gene encoding a small subunit of the dyneins. In the present study, 5814bp of the porcine DNAL4 (GenBank Acc. No. AM284696.1, 6097 bp, 4 exons) were comparatively sequenced using three boars with a high motility (>68%) and three with a low motility (<60%). Primers were self-designed except for those covering exons 1, 2 and 3. Prior to sequencing, the PCR products were purified. Sequencing was performed with an ABI PRISM 3100 Genetic Analyzer using the BigDyeTM Terminator v3.1 Cycle Sequencing Reaction Kit. Finally, 23 SNPs were described and genotyped for 82 AI boars representing the breeds Piétrain, German Large White and German Landrace. The genotypes were used to assess possible associations with standard spermatological parameters (ejaculate volume, density, and sperm motility (undiluted (Motud), 24h (Mot1) and 48h (Mot2) after semen collection) that were regularly recorded on the AI station. The analysis included a total of 8,833 spermatological data sets which ranged from 2 to 295 sets per boar in five years. Only SNP g.1007A>G had a significant effect. Finally, the gene substitution effect using the following statistical model was calculated: Yijk= µ+αi+βj+αβij+b1Sijk+b2Aijk+b3T ijk + b4Vijk+b5(α*A)ijk +b6(β*A)ijk+b7(A*T)ijk+Uijk+eijk where Yijk is the semen characteristics, µ is the general mean, α is the main effect of breed, β is the main effect of season, S is the effect of SNP (g.1007A > G), A is the effect of age at semen collection, V is the effect of diluter, αβ, α*A, β*A, A*T are interactions between the fixed effects, b1-b7 are regression coefficients between y and the respective covariate, U is the random effect of repeated observation on animal and e is the random error. The results from the single marker regression analysis revealed highly significant effects (p < 0.0001) of SNP g.1007A > G on Mot1 resp. on Mot2, resulting in a marked reduction by 11.4% resp. 15.4%. Furthermore a loss of Motud by 4.6% was detected (p < 0.0178). Considering the SNP g.1007A > G as a main factor (dominant-recessive model), significant differences between genotypes AA and AG as well as AA and GG for Mot1 and Mot2 exist. For Motud there was a significant difference between AA and GG.

Keywords: association, DNAL4, porcine, sperm traits

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Authors: Juan C. Duran-Alvarez, Daniel Mejia, Rodolfo Zanella

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Heterogeneous photocatalysis is a promising method to achieve the complete degradation and mineralization of organic pollutants in water via their exhaustive oxidation. In order to take this advanced oxidation process towards sustainability, it is necessary to reduce the energy consumption, referred as the light sources and the post-treatment operations. For this, the synthesis of new nanostructures of low band gap semiconductors in the form of thin films is in continuous development. In this work, thin films of the low band gap semiconductor bismuth oxyiodide (BiOI) were synthesized via the Successive Ionic Layer Adsorption and Reaction (SILAR) method. For this, Bi(NO3)3 and KI solutions were prepared, and glass supports were immersed in each solution under strict rate and time immersion conditions. Synthesis was performed at room temperature and a washing step was set prior to each immersion. Thin films with an average thickness below 100 nm were obtained upon a cycle of 30 immersions, as determined by AFM and profilometry measurements. Cubic BiOI nanocrystals with average size of 17 nm and a high orientation to the 001 plane were observed by XRD. In order to optimize the synthesis method, several Bi/I ratios were tested, namely 1/1, 1/5, 1/10, 1/20 and 1/50. The highest crystallinity of the BiOI films was observed when the 1/5 ratio was used in the synthesis. Non-stoichiometric conditions also resulted in the highest uniformity of the thin layers. PVP was used as an additive to improve the adherence of the BiOI thin films to the support. The addition of 0.1 mg/mL of PVP during the washing step resulted in the highest adherence of the thin films. In photocatalysis tests, degradation rate of the antibiotic ciprofloxacin as high as 75% was achieved using visible light (380 to 700 nm) irradiation for 5 h in batch tests. Mineralization of the antibiotic was also observed, although in a lower extent; ~ 30% of the total organic carbon was removed upon 5 h of visible light irradiation. Some ciprofloxacin by-products were identified throughout the reaction; and some of these molecules displayed residual antibiotic activity. In conclusion, it is possible to obtain highly oriented BiOI thin films under ambient conditions via the SILAR method. Non-stoichiometric conditions using PVP additive are necessary to increase the crystallinity and adherence of the films, which are photocatalytically active to remove recalcitrant organic pollutants under visible light irradiation.

Keywords: bismuth oxyhalides, photocatalysis, thin films, water treatment

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Authors: Ahmed Slami, Med El Amine Brixi Nigassa, Nassima Labdelli, Sofiane Soulimane, Arnaud Pothier

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Many people suffer from diabetes, a disease marked by abnormal levels of sugar in the blood; 285 million people have diabetes, 6.6% of the world adult population (in 2010), according to the International Diabetes Federation. Insulin medicament is invented to be injected into the body. Generally, the injection requires the patient to do it manually. However, in many cases he will be unable to inject the drug, saw that among the side effects of hyperglycemia is the weakness of the whole body. The researchers designed a medical device that injects insulin too autonomously by using micro-pumps. Many micro-pumps of concepts have been investigated during the last two decades for injecting molecules in blood or in the body. However, all these micro-pumps are intended for slow infusion of drug (injection of few microliters by minute). Now, the challenge is to develop micro-pumps for fast injections (1 microliter in 10 seconds) with accuracy of the order of microliter. Recently, studies have shown that only piezoelectric actuators can achieve this performance, knowing that few systems at the microscopic level were presented. These reasons lead us to design new smart microsystems injection drugs. Therefore, many technological advances are still to achieve the improvement of materials to their uses, while going through their characterization and modeling action mechanisms themselves. Moreover, it remains to study the integration of the piezoelectric micro-pump in the microfluidic platform features to explore and evaluate the performance of these new micro devices. In this work, we propose a new micro-pump model based on piezoelectric actuation with a new design. Here, we use a finite element model with Comsol software. Our device is composed of two pumping chambers, two diaphragms and two actuators (piezoelectric disks). The latter parts will apply a mechanical force on the membrane in a periodic manner. The membrane deformation allows the fluid pumping, the suction and discharge of the liquid. In this study, we present the modeling results as function as device geometry properties, films thickness, and materials properties. Here, we demonstrate that we can achieve fast injection. The results of these simulations will provide quantitative performance of our micro-pumps. Concern the spatial actuation, fluid rate and allows optimization of the fabrication process in terms of materials and integration steps.

Keywords: COMSOL software, piezoelectric, micro-pump, microfluidic

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Authors: Erin M. Durke, Monica L. McEntee, Meilu He, Suresh Dhaniyala

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Aerosols are one of the most important and significant surfaces in the atmosphere. They can influence weather, absorption, and reflection of light, and reactivity of atmospheric constituents. A notable feature of aerosol particles is the presence of a surface charge, a characteristic imparted via the aerosolization process. The existence of charge can complicate the interrogation of aerosol particles, so many researchers remove or neutralize aerosol particles before characterization. However, the charge is present in real-world samples, and likely has an effect on the physical and chemical properties of an aerosolized material. In our studies, we aerosolized different materials in an attempt to characterize the charge imparted via the aerosolization process and determine what impact it has on the aerosolized materials’ properties. The metal oxides, TiO₂ and SiO₂, were aerosolized expulsively and then characterized, using several different techniques, in an effort to determine the surface charge imparted upon the particles via the aerosolization process. Particle charge distribution measurements were conducted via the employment of a custom scanning mobility particle sizer. The results of the charge distribution measurements indicated that expulsive generation of 0.2 µm SiO₂ particles produced aerosols with upwards of 30+ charges on the surface of the particle. Determination of the degree of surface charging led to the use of non-traditional techniques to explore the impact of additional surface charge on the overall reactivity of the metal oxides, specifically TiO₂. TiO₂ was aerosolized, again expulsively, onto a gold-coated tungsten mesh, which was then evaluated with transmission infrared spectroscopy in an ultra-high vacuum environment. The TiO₂ aerosols were exposed to O₂, H₂, and CO, respectively. Exposure to O₂ resulted in a decrease in the overall baseline of the aerosol spectrum, suggesting O₂ removed some of the surface charge imparted during aerosolization. Upon exposure to H₂, there was no observable rise in the baseline of the IR spectrum, as is typically seen for TiO₂, due to the population of electrons into the shallow trapped states and subsequent promotion of the electrons into the conduction band. This result suggests that the additional charge imparted via aerosolization fills the trapped states, therefore no rise is seen upon exposure to H₂. Dosing the TiO₂ aerosols with CO showed no adsorption of CO on the surface, even at lower temperatures (~100 K), indicating the additional charge on the aerosol surface prevents the CO molecules from adsorbing to the TiO₂ surface. The results observed during exposure suggest that the additional charge imparted via aerosolization impacts the interaction with each probe gas.

Keywords: aerosols, charge, reactivity, infrared

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Authors: Sarah K. Amer, Walaa Alaa

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Epilepsy is an important cause of mortality and morbidity, according to WHO statistics. It is characterized by the presence of frequent seizures occurring more than 24 hours apart. Carbamazepine (CBZ) is considered first-line treatment for epilepsy. However, reports have shown that CBZ oral formulations failed to achieve optimum systemic delivery, minimize side effects, and enhance patient compliance. Besides, the literature has signified the lack of therapeutically efficient CBZ transdermal formulation and the urge for its existence owing to its ease and convenient method of application and highlighted capability to attain higher bioavailability and more extended-release profiles compared to conventional oral CBZ tablets. This work aims to prepare CBZ microspheres (MS) that are embedded in a transdermal gel containing Vitamin B to be co-delivered. MS were prepared by emulsion-solvent diffusion method using Eudragit S as core forming polymer and hydroxypropyl methylcellulose (HPMC) polymer. The MS appeared to be spherical and porous in nature, offering a large surface area and high entrapment efficiency of CBZ. The transdermal gel was prepared by solvent-evaporation technique using HPMC that, offered high entrapment efficiency and Eudragit S that provided an extended-release profile. Polyethylene glycol, Span 80 and Pyridoxine were also added. Data indicated that combinations of CBZ with pyridoxine can reduce epileptic seizures without affecting motor coordination. Extended-release profiles were evident for this system. The patches were furthermore tested for thickness, moisture content, folding endurance, spreadability and viscosity measurements. This novel pharmaceutical formulation would be of great influence on seizure control, offering better therapeutic effects.

Keywords: epilepsy, carbamazepine, pyridoxine, transdermal

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Authors: Jafar Akbari

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Quinolines are very important compounds partially because of their pharmacological properties which include wide applications in medicinal chemistry. notable among them are antimalarial drugs, anti-inflammatory agents, antiasthamatic, antibacterial, antihypertensive, and tyrosine kinase inhibiting agents. Despite quinoline usage in pharmaceutical and other industries, comparatively few methods for their preparation have been reported.The Friedlander annulation is one of the simplest and most straightforward methods for the synthesis of poly substituted quinolines. Although, modified methods employing lewis or br¢nsted acids have been reported for the synthesis of quinolines, the development of water stable acidic catalyst for quinoline synthesis is quite desirable. One of the most remarkable features of ionic liquids is that the yields can be optimized by changing the anions or the cations. Recently, sulfonic acid functionalized ionic liquids were used as solvent-catalyst for several organic reactions. We herein report the one pot domino approach for the synthesis of quinoline derivatives in Friedlander manner using TSIL as a catalyst. These ILs are miscible in water, and their homogeneous system is readily separated from the reaction product, combining advantages of both homogeneous and heterogeneous catalysis. In this reaction, the catalyst plays a dual role; it ensures an effective condensation and cyclization of 2-aminoaryl ketone with second carbonyl group and it also promotes the aromatization to the final product. Various types of quinolines from 2-aminoaryl ketones and β-ketoesters/ketones were prepared in 85-98% yields using the catalytic system of SO3-H functionalized ionic liquid/H2O. More importantly, the catalyst could be easily recycled for five times without loss of much activity.

Keywords: antimalarial drugs, green chemistry, ionic liquid, quinolines

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Authors: Anita K. Kovacs, Peter Hegyes, Zsolt Bozso, Gabor Toth

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Fluorination has been used extensively by the pharmaceutical industry as a strategy to improve the pharmacokinetics of drugs due to its effectiveness in increasing the potency of antimicrobial peptides (AMPs). Multiple-fluorinated indole-ring-containing tryptophan derivatives have the potential of having better antimicrobial activity than the widely used mono-fluorinated indole-ring containing tryptophan derivatives, but they are not available commercially. Therefore, our goal is to synthesize multiple-fluorinated indole-ring containing tryptophan derivatives to incorporate them into AMPs to enhance their antimicrobial activity. During our work, we are trying several methods (classical organic synthesis, enzymic synthesis, and solid phase peptide synthesis) for the synthesis of the said compounds, with mixed results. With classical organic synthesis (four different routes), we did not get the desired results. The reaction of serin with substituted indole in the presence of acetic anhydride led to racemic tryptophane; with the reaction of protected serin with indole in the presence of nickel complex was unsuccessful; the reaction of serin containing protected dipeptide with disuccinimidyl carbonate we achieved a tryptophane containing dipeptide, its chiral purity is being examined; the reaction of alcohol with substituted indole in the presence of copper complex was successful, but it was only a test reaction, we could not reproduce the same result with serine. The undergoing tryptophan-synthase method has shown some potential, but our work has not been finished yet. The successful synthesis of the desired multiple-fluorinated indole-ring-containing tryptophan will be followed by solid phase peptide synthesis in order to incorporate it into AMPs to enhance their antimicrobial activity. The successful completion of these phases will mean the possibility of manufacturing new, effective AMPs.

Keywords: halogenation, fluorination, tryptophan, enhancement of antimicrobial activity

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Authors: Gajanan M. Sonwane

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Nowadays, the entire pharmaceutical industry is facing the challenge of increasing efficiency and innovation. The major hurdles are the growing cost of research and development and a concurrent stagnating number of new chemical entities (NCEs). Hence, the challenge is to select the most druggable targets and to search the equivalent drug-like compounds, which also possess specific pharmacokinetic and toxicological properties that allow them to be developed as drugs. The present research work includes the studies of developing new anticancer heterocycles by using molecular modeling techniques. The heterocycles synthesized through such methodology are much effective as various physicochemical parameters have been already studied and the structure has been optimized for its best fit in the receptor. Hence, on the basis of the literature survey and considering the need to develop newer anticancer agents, new phenazinamine derivatives were designed by subjecting the nucleus to molecular modeling, viz., GQSAR analysis and docking studies. Simultaneously, these designed derivatives were subjected to in silico prediction of biological activity through PASS studies and then in silico toxicity risk assessment studies. In PASS studies, it was found that all the derivatives exhibited a good spectrum of biological activities confirming its anticancer potential. The toxicity risk assessment studies revealed that all the derivatives obey Lipinski’s rule. Amongst these series, compounds 4c, 5b and 6c were found to possess logP and drug-likeness values comparable with the standard Imatinib (used for anticancer activity studies) and also with the standard drug methotrexate (used for antimitotic activity studies). One of the most notable mutations is the threonine to isoleucine mutation at codon 315 (T315I), which is known to be resistant to all currently available TKI. Enzyme assay planned for confirmation of target selective activity.

Keywords: drug design, tyrosine kinases, anticancer, Phenazinamine

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Authors: Jungkyun Im

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are effective for relieving pain and reducing inflammation. They are nonselective inhibitors of two isoforms of COX, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), and thereby inhibiting the production of hormone-like lipid compounds such as, prostaglandins and thromboxanes which cause inflammation, pain, fever, platelet aggregation, etc. In addition, recently there are many research articles reporting the neuroprotective effect of NSAIDs in neurodegenerative diseases, such as Alzheimer’s disease (AD) and Parkinson’s disease (PD). However, the clinical use of NSAIDs in these diseases is limited by low brain distribution. Therefore, in order to assist the in-depth investigation on the pharmaceutical mechanism of flurbiprofen in neuroprotection and to make flurbiprofen a more potent drug to prevent or alleviate neurodegenerative diseases, delivery of flurbiprofen to brain should be effective and sufficient amount of flurbiprofen must penetrate the BBB thus gaining access into the patient’s brain. We have recently developed several types of guanidine-rich molecular carriers with high molecular weights and good water solubility that readily cross the blood-brain barrier (BBB) and display efficient distributions in the mouse brain. The G8 (having eight guanidine groups) molecular carrier based on D-sorbitol was found to be very effective in delivering anticancer drugs to a mouse brain. In the present study, employing the same molecular carrier, we prepared the flurbiprofen conjugate and studied its BBB permeation by mouse tissue distribution study. Flurbiprofen was attached to a molecular carrier with a fluorescein probe and multiple terminal guanidiniums. The conjugate was found to internalize into live cells and readily cross the BBB to enter the mouse brain. Our novel synthetic flurbiprofen conjugate will hopefully delivery NSAIDs into brain, and is therefore applicable to the neurodegenerative diseases treatment or prevention.

Keywords: flurbiprofen, drug delivery, molecular carrier, organic synthesis

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Authors: Muslihatus Syarifah

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Introduction: Rosella flower petals can be used as an antibacterial because it contains alkaloids, flavonoids, phenolics, and terpenoids) for the . Bacteria activity is S. aureus can cause skin infections and pengobatanya most appropriate use of topical preparations. Ointment is a topical preparation comprising the active substance and ointment base. Not all the base matches the active substances or any type of disease. In this study using flavonoid active substances contained in rosella flower petals (Hibiscus sabdariffa) to be made ointment by testing a variety of different bases in order to obtain a suitable basis for the formulation of ointment extract rosella flower petals. Methods: Experimental research with research methods Post test control group design using the ointment is hydrocarbon sample, absorption, leached water and dissolved water. Then tested for bacteria S. aureus with different concentrations of 1%, 2%, 4%, 8%, 16, 32%. Data were analyzed using One Way ANOVA followed by Post Hoc test. Results: Ointment with a hydrocarbon base, absorption, leached water and dissolved water having no change in physical properties during storage. Base affect the physical properties of an ointment that adhesion, dispersive power and pH. The physical properties of the ointment with different concentrations produce different physical properties including adhesion, dispersive power and pH. The higher the concentration the higher dispersive power, but the smaller the adhesion and pH. Conclusion: Differences bases, storage time, the concentration of the extract can affect the physical properties of the ointment. Concentration of extract in the ointment extract rosella flower petals is 32%.

Keywords: rosella, physical properties, ointments, antibacterial

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Authors: Deepali Rastogi

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Natural dyes are considered to be eco-friendly as they cause no pollution and are safe to use. With the growing interest in natural dyes, new sources of natural dyes are being explored. Coconut (Cocos nucifera) is native to tropical eastern region. It is abundantly available in Asia, Africa and South America. While coconut has tremendous commercial value in food, oil, pharmaceutical and cosmetic industry, the most important use of coconut husk has been as coir which is used for making mats, ropes, etc. In the present study an attempt has been made to extract dye from the coconut husk and study its application on wool and silk. Dye was extracted from coconut husk in an aqueous medium at three different pH. The coconut husk fibres were boiled in water at different pH of 4, 7 and 9 for one hour. On visual inspection of the extracted dye solution, maximum colour was found to be extracted at pH 9. The solution was obtained in neutral medium whereas, no dye was extracted in acidic medium. Therefore, alkaline medium at pH 9 was selected for the extraction of dye from coconut husk. The extracted dye was applied on wool and silk at three different pH, viz., 4, 7 and 9. The effect of pre- and post- mordanting with alum and ferrous sulphate on the colour value of coconut husk dye was also studied. The L*a*b*/L*c*h* values were measured to see the effect of the mordants on the colour values of all the dyed and mordanted samples. Bright golden brown to dark brown colours were obtained at pH 4 on both wool and silk. The colour yield was not very good at pH 7 and 9. Mordanting with alum resulted in darker and brighter shades of brown, whereas mordanting with ferrous sulphate resulted in darker and duller shades. All the samples were tested for colourfastness to light, rubbing, washing and perspiration. Both wool and silk dyed with dye extracted from coconut husk exhibited good to excellent wash, rub and perspiration fastness. Fastness to light was moderate to good.

Keywords: coconut husk, wool, silk, natural dye, mordants

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Authors: R. Hurtado-Ortiz, D. Clermont, M. Schüngel, C. Bizet, D. Smith, E. Stackebrandt

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Microbiological resources and their derivatives are the essential raw material for the advancement of human health, agro-food, food security, biotechnology, research and development in all life sciences. Microbial resources, and their genetic and metabolic products, are utilised in many areas such as production of healthy and functional food, identification of new antimicrobials against emerging and resistant pathogens, fighting agricultural disease, identifying novel energy sources on the basis of microbial biomass and screening for new active molecules for the bio-industries. The complexity of public collections, distribution and use of living biological material (not only living but also DNA, services, training, consultation, etc.) and service offer, demands the coordination and sharing of policies, processes and procedures. The Microbial Resource Research Infrastructure (MIRRI) is an initiative within the European Strategy Forum Infrastructures (ESFRI), bring together 16 partners including 13 European public microbial culture collections and biological resource centres (BRCs), supported by several European and non-European associated partners. The objective of MIRRI is to support innovation in microbiology by provision of a one-stop shop for well-characterized microbial resources and high quality services on a not-for-profit basis for biotechnology in support of microbiological research. In addition, MIRRI contributes to the structuring of microbial resources capacity both at the national and European levels. This will facilitate access to microorganisms for biotechnology for the enhancement of the bio-economy in Europe. MIRRI will overcome the fragmentation of access to current resources and services, develop harmonised strategies for delivery of associated information, ensure bio-security and other regulatory conditions to bring access and promote the uptake of these resources into European research. Data mining of the landscape of current information is needed to discover potential and drive innovation, to ensure the uptake of high quality microbial resources into research. MIRRI is in its Preparatory Phase focusing on governance and structure including technical, legal governance and financial issues. MIRRI will help the Biological Resources Centres to work more closely with policy makers, stakeholders, funders and researchers, to deliver resources and services needed for innovation.

Keywords: culture collections, microbiology, infrastructure, microbial resources, biotechnology

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Authors: David Taillis, Oussama Becissa, Julien Gabaston, Jean-Michel Merillon, Tristan Richard, Stephanie Cluzet

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Nowadays, there is a strong pressure to reduce the phytosanitary inputs of synthetic chemistry in vineyards. It is, therefore, necessary to find viable alternatives in order to protect the vine against its major diseases. For this purpose, we suggest the use of a plant extract enriched in antimicrobial compounds. Being produced from vine trunks and roots, which are co-products of wine production, the extract produced is part of a circular economy. The antimicrobial molecules present in this plant material are polyphenols and, more particularly, stilbenes, which are derived from a common base, the resveratrol unit, and that are well known vine phytoalexins. The stilbenoids were extracted from trunks and roots (30/70, w/w) by a double extraction with ethyl acetate followed by enrichment by liquid-liquid extraction. The produced extract was characterized by UHPLC-MS, then its antimicrobial activities were tested on Plasmopara viticola and Botrytis cinerea in the laboratory and/or in greenhouse and in vineyard. The major compounds were purified, and their antimicrobial activity was evaluated on B. cinerea. Moreover, after its spraying, the effect of the stilbene extract on the plant defence status was evaluated by analysis of defence gene expression. UHPLC-MS analysis revealed that the extract contains 50% stilbenes with resveratrol, ε-viniferin and r-viniferin as major compounds. The extract showed antimicrobial activities on P. viticola with IC₅₀ and IC₁₀₀ respectively of 90 and 300 mg/L in the laboratory. In addition, it inhibited 40% of downy mildew development in greenhouse. However, probably because of the sensitivity of stilbenes to the environment, such as UV degradation, no activity has been observed in vineyard towards P. viticola development. For B. cinerea, the extract IC50 was 123 mg/L, with resveratrol and ε-viniferin being the most active stilbenes (IC₅₀ of 88 and 142 mg/L, respectively). The analysis of the expression of defence genes revealed that the extract can induce the expression of some defence genes 24, 48, and 72 hours after treatment, meaning that the extract has a defence-stimulating effect at least for the first three days after treatment. In conclusion, we produced a plant extract enriched in stilbenes with antimicrobial properties against two major grapevine pathogenic agents P. viticola and B. cinerea. In addition, we showed that this extract displayed eliciting activity of plant defences. This extract can therefore represent, after formulation development, a viable eco-friendly alternative for vineyard protection. Subsequently, the effect of the stilbenoid extract on primary metabolism will be evaluated by quantitative NMR.

Keywords: antimicrobial, bioprotection, grapevine, Plasmopara viticola, stilbene

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Authors: Zahid Hussain, Nayyab Sultan

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This study describes the preparation of zinc oxide nanoparticles and their anti-diabetic effect individually and with the combination of Momordica charantia plant extract. This plant is termed bitter melon, balsam pear, bitter gourd, or karela. Blood glucose levels in mice were monitored in their random state before and after the administration of zinc oxide nanoparticles and plant extract. The powdered form of nanoparticles and the selected plant were used as an oral treatment. Diabetes was induced in mice by using a chemical named as streptozotocin. It is an artificial diabetes-inducing chemical. In the case of zinc oxide nanoparticles (3mg/kg) and Momordica charantia plant extract (500mg/kg); the maximum anti-diabetic effect observed was 70% ± 1.6 and 75% ± 1.3, respectively. In the case of the combination of zinc oxide nanoparticles (3mg/kg) and Momordica charantia plant extract (500mg/kg), the maximum anti-diabetic effect observed was 86% ± 2.0. The results obtained were more effective as compared to standard drugs Amaryl (3mg/kg), having an effectiveness of 52% ± 2.4, and Glucophage (500mg/kg), having an effectiveness of 29% ± 2.1. Results indicate that zinc oxide nanoparticles and plant extract in combination are more helpful in treating diabetes as compared to their individual treatments. It is considered a natural treatment without any side effects rather than using standard drugs, which shows adverse side effects on health, and most probably detoxifies in liver and kidneys. More experimental work and extensive research procedures are still required in order to make them applicable to pharmaceutical industries.

Keywords: albino mice, amaryl, anti-diabetic effect, blood glucose level, Camellia sinensis, diabetes mellitus, Momordica charantia plant extract, streptozotocin, zinc oxide nanoparticles

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Authors: Paula Salazar, Rodrigo Henríquez, Pablo Zerega

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The textile, food and pharmaceutical industries are expanding daily worldwide, and they are located within the most polluting industries due to the fact that wastewater is discharged into watercourses with high concentrations of dyes and traces of drugs. Many of these compounds are stable to light and biodegradation, being considered as emerging organic contaminants. Advanced oxidation processes (AOPs) emerge as an effective alternative for the removal and elimination of this type of contaminants. Heterogeneous photocatalysis has been extensively studied as it is an efficient, low-cost and durable method. As the main photocatalyst, TiO₂ has been used for the degradation of a large number of dyes and drugs. The disadvantage of TiO₂ is its absorption in the UV region of the solar spectrum. On the other hand, quaternary chalcogenides based on Cu₂SnZnX₄ (X = S, Se) are a possible alternative due to their narrow bandgap (ca. between 0.8 to 1.5 eV depending on the phase considered), low cost, an abundance of its constituent elements in the earth's crust and its low toxicity. The objective of this research was to synthesize Cu₂SnZnS₄ (CZTS) through of a low-cost hydrothermal method and evaluate it as a potential photo-catalyst in the photo-degradation process of Congo Red. The synthesis of the nanoparticle in suspension and film onto fluorine-doped tin oxide coated glass (FTO) was carried out using a mixture of: 2 mmol CuCl₂, 1 mmol ZnCl₂, 1 mmol SnCl₂ and 4 mmol CH4N₂S in a Teflon reactor at 180⁰C for 72 h. Characterization was performed through scanning electron microscopy (SEM), X-ray diffraction (XRD) and UV VIS spectroscopy. Photo-degradation monitoring was carried out employing a UV VIS spectrophotometer. The results show that photodegradation of 55% of the dye can be obtained after 4h of exposure to polychromatic light, it should be noted that the Congo Red dye is being studied for the first time.

Keywords: CZTS, hydrothermal, photocatalysis, dye

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Authors: Moustafa Osman Mohammed

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The photocurrent generations are influencing ultra-high efficiency solar cells based on self-assembled quantum dot (QD) nanostructures. Nanocrystal quantum dots (QD) provide a great enhancement toward solar cell efficiencies through the use of quantum confinement to tune absorbance across the solar spectrum enabled multi-exciton generation. Based on theoretical predictions, QDs have potential to improve systems efficiency in approximate regular electrons excitation intensity greater than 50%. In solar cell devices, an intermediate band formed by the electron levels in quantum dot systems. The spatial architecture is exploring how can solar cell integrate and produce not only high open circuit voltage (> 1.7 eV) but also large short-circuit currents due to the efficient absorption of sub-bandgap photons. In the proposed QD system, the structure allows barrier material to absorb wavelengths below 700 nm while multi-photon processes in the used quantum dots to absorb wavelengths up to 2 µm. The assembly of the electronic model is flexible to demonstrate the atoms and molecules structure and material properties to tune control energy bandgap of the barrier quantum dot to their respective optimum values. In terms of energy virtual conversion, the efficiency and cost of the electronic structure are unified outperform a pair of multi-junction solar cell that obtained in the rigorous test to quantify the errors. The milestone toward achieving the claimed high-efficiency solar cell device is controlling the edge causes of energy bandgap between the barrier material and quantum dot systems according to the media design limits. Despite this remarkable potential for high photocurrent generation, the achievable open-circuit voltage (Voc) is fundamentally limited due to non-radiative recombination processes in QD solar cells. The orientation of voltage recovery system is compared theoretically with experimental Voc variation in mediation upper–limit obtained one diode modeling form at the cells with different bandgap (Eg) as classified in the proposed spatial architecture. The opportunity for improvement Voc is valued approximately greater than 1V by using smaller QDs through QD solar cell recovery systems as confined to other micro and nano operations states.

Keywords: nanotechnology, photovoltaic solar cell, quantum systems, renewable energy, environmental modeling

Procedia PDF Downloads 157

Authors: Yunjia Yang, Peng Li, Gordon Xu, Timothy Mahony, Bing Zhang, Neena Mitter, Karishma Mody

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Sheep flystrike is one of the most economically important diseases affecting the Australian sheep and wool industry (>356M/annually). Currently, control of Lucillia cuprina relies almost exclusively on chemicals controls and the parasite has developed resistance to nearly all control chemicals used in the past. It is therefore critical to develop an alternative solution for the sustainable control and management of flystrike. RNA interference (RNAi) technologies have been successfully explored in multiple animal industries for developing parasites controls. This research project aims to develop a RNAi based biological control for sheep blowfly. Double-stranded RNA (dsRNA) has already proven successful against viruses, fungi and insects. However, the environmental instability of dsRNA is a major bottleneck for successful RNAi. Bentonite polymer (BenPol) technology can overcome this problem, as it can be tuned for the controlled release of dsRNA in the gut challenging pH environment of the blowfly larvae, prolonging its exposure time to and uptake by target cells. To investigate the potential of BenPol technology for dsRNA delivery, four different BenPol carriers were tested for their dsRNA loading capabilities, and three of them were found to be capable of affording dsRNA stability under multiple temperatures (4°C, 22°C, 40°C, 55°C) in sheep serum. Based on stability results, dsRNA from potential targeted genes was loaded onto BenPol carriers and tested in larvae feeding assays, three genes resulting in knockdowns. Meanwhile, a primary blowfly embryo cell line (BFEC) derived from L. cuprina embryos was successfully established, aim for an effective insect cell model for testing RNAi efficacy for preliminary assessments and screening. The results of this study establish that the dsRNA is stable when loaded on BenPol particles, unlike naked dsRNA rapidly degraded in sheep serum. The stable nanoparticle delivery system offered by BenPol technology can protect and increase the inherent stability of dsRNA molecules at higher temperatures in a complex biological fluid like serum, providing promise for its future use in enhancing animal protection.

Keywords: flystrike, RNA interference, bentonite polymer technology, Lucillia cuprina

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Authors: Ajay Krishnamurthy, Mariyappan Mahesh Kumar, Sellamuthu Periyar Selvam

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Fruits are considered as functional foods due to the presence of various bioactive compounds available such as polyphenols, which are beneficial to health when consumed as part of our diet. The primary objective of this study was to analyze the various functional groups present in ethanolic extracts of Hylocereus undatus and Garcinia indica and also measure their antibacterial and antioxidant potential respectively thereby affirming its nutraceutical potential. To fulfill our objective, a Fourier - transform Infrared Spectroscopy (FTIR) was conducted for functional group analysis, Total Phenolic Content and DPPH free radical scavenging activity for measuring it anti-oxidant potential and agar-well diffusion assay for antibacterial potential. On careful observation and analysis of the spectrum it was found that both the fruit extracts contain similar compounds viz. Phenols, Alkanes, Alkenes, Aldehydes, Ketones, Carboxylic Acid and Amines. Total phenolic content of H.undatus and G.indica was estimated to be (26.85 ± 1.84 mg GAE/100g) and (32.84 ± 1.63 mg GAE/100g) respectively which corresponds to an inhibition of 84% and 81% respectively. H.undatus shows an inhibition of (3.4 ± 2.1mm) in gram-positive and (4.2 ± 2.24mm) in gram-negative organism on the other hand G.indica shows (2.1 ± 0.98mm) in gram-positive and (3.1 ± 1.44mm) in gram negative. The presence of such diverse compounds in the fruits helps us to understand the necessity for the inclusion of fruits in our daily diet and also helps the pharmaceutical industry in realizing the importance of exotic fruits as a potential nutraceutical.

Keywords: DPPH, fourier-transform infrared spectroscopy (FTIR), Hylocereus undatus, Garcinia indica

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Authors: Boutemak Khalida, Dahmani Siham

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Garden cress (Lepidium Sativum L.) belonging to the family Brassicaceae, is edible growing annual herb. Its various parts (roots, leaves and seeds) have been used to treat various human ailments. Its seed extracts have been screened for various biological activities like hypotensive, antimicrobial, bronchodilator, hypoglycaemic and antianemic. The aim of the present study is to optimize the process parameters (cellulase concentration and incubation time) of enzymatic pre-treatment of the garden cress seeds and to evaluate the effect of cellulase pre-treatment of the crushed seeds on the oil yield, physico-chemical properties and antibacterial activity and comparing to non-enzymatic method. The optimum parameters of cellulase pre-treatment were as follows: cellulase of 0,1% w/w and incubation time of 2h. After enzymatic pre-treatment, the oil was extracted by n-hexane for 1.5 h, the oil yield was 4,01% for cellulase pre-treatment as against 10,99% in the control sample. The decrease in yield might be caused a result of mucilage. Garden cress seeds are covered with a layer of mucilage which gels on contact with water. At the same time, the antibacterial activity was carried out using agar diffusion method against 4 food-borne pathogens (Escherichia coli, Salmonella typhi,Staphylococcus aureus, Bacillus subtilis). The results showed that bacterial strains are very sensitive to the oil with cellulase pre-treatment. Staphylococcus aureus is extremely sensitive with the largest zone of inhibition (40 mm), Escherichia coli and salmonella typhi had a very sensitive to the oil with a zone of inhibition (26 mm). Bacillus subtilizes is averagely sensitive which gave an inhibition of 16 mm. But it does not exhibit sensivity to the oil without enzymatic pre-treatment with a zone inhibition (< 8 mm). Enzymatic pre-treatment could be useful for antimicrobial activity of the oil, and hold a good potential for use in food and pharmaceutical industries.

Keywords: Lepidium sativum L., cellulase, enzymatic pretreatment, antibacterial activity.

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Authors: Assia Belfar, Mohamed Hadjadj, Messaouda Dakmouche, Zineb Ghiaba, Mahdi Belguidoum

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Introduction: This study aims to phytochemical screening; Extracting the active compounds and estimate the effectiveness of antioxidant in Medicinal plants desert Limoniastrum guyonianum (Zeïta) from South Algeria. Methods: Total phenolic content and total flavonoid content using Folin-Ciocalteu and aluminum chloride colorimetric methods, respectively. The total antioxidant capacity was estimated by the following methods: DPPH (1.1-diphenyl-2-picrylhydrazyl radical) and reducing power assay. Results: Phytochemical screening of the plant part reveals the presence of phenols, saponins, flavonoids and tannins. While alkaloids and Terpenoids were absent. The Methanolic extract of L. guyonianum was extracted successively with ethyl acetate and butanol. Extraction of yield varied widely in the L. guyonianum ranging from (1.315 % to 4.218%). butanol fraction had the highest yield. The higher content of phenols was recorded in butanol fraction (311.81 ± 0.02mg GAE/g DW), the higher content of flavonoids was found in butanol fraction (9.58 ± 0.33mg QE/g DW). IC50 of inhibition of radical DPPH in ethyl acetate fraction was (0.05 ± 0.01µg/ml) Equal effectiveness with BHT, All extracts showed good activity of ferric reducing power, the higher power was in butanol fraction (16.16 ± 0.05mM). Conclusions: Demonstrated this study that the Methanolic extract of L. guyonianum contain a considerable quantity of phenolic compounds and possess a good antioxidant activity. It can be used as an easily accessible source of Natural Antioxidants and as a possible food supplement and in pharmaceutical industry.

Keywords: flavonoid compound, l. guyonianum, medicinal plants, phenolic compounds, phytochemical screening

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Authors: Magdalena Diaka, Paweł Mazierski, Joanna Żebrowska, Michał Winiarski, Tomasz Klimczuk, Adriana Zaleska-Medynska

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During the last years, TiO2 nanotubes have been widely studied due to their unique highly ordered array structure, unidirectional charge transfer and higher specific surface area compared to conventional TiO2 powder. These photoactive materials, in the form of thin layer, can be activated by low powered and low cost irradiation sources (such as LEDs) to remove VOCs, microorganism and to deodorize air streams. This is possible due to their directly growth on a support material and high surface area, which guarantee enhanced photon absorption together with an extensive adsorption of reactant molecules on the photocatalyst surface. TiO2 nanotubes exhibit also lots of other attractive properties, such as potential enhancement of electron percolation pathways, light conversion, and ion diffusion at the semiconductor-electrolyte interface. Pure TiO2 nanotubes were previously used to remove organic compounds from the gas phase as well as in water splitting reaction. The major factors limiting the use of TiO2 nanotubes, which have not been fully overcome, are their relatively large band gap (3-3,2 eV) and high recombination rate of photogenerated electron–hole pairs. Many different strategies were proposed to solve this problem, however titania nanostructures containing incorporated metal oxides like Ag2O shows very promising, new optical and photocatalytic properties. Unfortunately, there is still very limited number of reports regarding application of TiO2/MxOy nanostructures. In the present work, we prepared TiO2/Ag2O nanotubes obtained by anodization of Ti-Ag alloys containing 5, 10 and 15 wt. % Ag. Photocatalysts prepared in this way were characterized by X-ray diffraction spectroscopy (XRD), scanning electron microscopy (SEM), luminescence spectroscopy and UV-Vis spectroscopy. The activities of new TiO2/Ag2O were examined by photocatalytic degradation of toluene in gas phase reaction and phenol in aqueous phase using 1000 W Xenon lamp (Oriel) and light emitting diodes (LED) as a irradiation sources. Additionally efficiency of bacteria (Pseudomonas aeruginosa) removal from the gas phase was estimated. The number of surviving bacteria was determined by the serial twofold dilution microtiter plate method, in Tryptic Soy Broth medium (TSB, GibcoBRL).

Keywords: photocatalysis, antibacterial properties, titania nanotubes, new TiO2/MxOy nanostructures

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Authors: Debajyoti Bose

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Chitosan has received much attention as a functional biopolymer for diverse applications, especially in pharmaceutics and medicine. Chitosan is a positively charged natural biodegradable and biocompatible polymer. It is a linear polysaccharide consisting of β-1,4 linked monomers of glucosamine and N-acetylglucosamine. Chitosan can be mainly obtained from fungal sources during large fermentation process. In this study,three different fungal strains Aspergillus niger NCIM 1045, Aspergillus oryzae NCIM 645 and Mucor indicus MTCC 3318 were used for the production of chitosan. The growth mediums were optimized for maximum fungal production. The produced chitosan was characterized by determining degree of deacetylation. Chitosan possesses one reactive amino at the C-2 position of the glucosamine residue, and these amines confer important functional properties to chitosan which can be exploited for biofabrication to generate various chemically modified derivatives and explore their potential for pharmaceutical field. Chitosan nanoparticles were prepared by ionic cross-linking with tripolyphosphate (TPP). The major effect on encapsulation and release of protein (e.g. enzyme diastase) in chitosan-TPP nanoparticles was investigated in order to control the loading and release efficiency. It was noted that the chitosan loading and releasing efficiency as a nanocapsule, obtained from different fungal sources was almost near to initial enzyme activity(12026 U/ml) with a negligible loss. This signify, chitosan can be used as a polymeric drug as well as active component or protein carrier material in dosage by design due to its appealing properties such as biocompatibility, biodegradability, low toxicity and relatively low production cost from abundant natural sources. Based upon these initial experiments, studies were also carried out on modification of chitosan based nanocapsules incorporated with physiologically important enzymes and nutraceuticals for target delivery.

Keywords: fungi, chitosan, enzyme, nanocapsule

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Authors: Henry Memczak, Marc Hovestaedt, Bernhard Ay, Sandra Saenger, Thorsten Wolff, Frank F. Bier

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The influenza viruses cause flu epidemics every year and serious pandemics in larger time intervals. The only cost-effective protection against influenza is vaccination. Due to rapid mutation continuously new subtypes appear, what requires annual reimmunization. For a correct vaccination recommendation, the circulating influenza strains had to be detected promptly and exactly and characterized due to their antigenic properties. During the flu season 2016/17, a wrong vaccination recommendation has been given because of the great time interval between identification of the relevant influenza vaccine strains and outbreak of the flu epidemic during the following winter. Due to such recurring incidents of vaccine mismatches, there is a great need to speed up the process chain from identifying the right vaccine strains to their administration. The monitoring of subtypes as part of this process chain is carried out by national reference laboratories within the WHO Global Influenza Surveillance and Response System (GISRS). To this end, thousands of viruses from patient samples (e.g., throat smears) are isolated and analyzed each year. Currently, this analysis involves complex and time-intensive (several weeks) animal experiments to produce specific hyperimmune sera in ferrets, which are necessary for the determination of the antigen profiles of circulating virus strains. These tests also bear difficulties in standardization and reproducibility, which restricts the significance of the results. To replace this test a peptide-based assay for influenza virus subtyping from corresponding virus samples was developed. The differentiation of the viruses takes place by a set of specifically designed peptidic recognition molecules which interact differently with the different influenza virus subtypes. The differentiation of influenza subtypes is performed by pattern recognition guided by machine learning algorithms, without any animal experiments. Synthetic peptides are immobilized in multiplex format on various platforms (e.g., 96-well microtiter plate, microarray). Afterwards, the viruses are incubated and analyzed comparing different signaling mechanisms and a variety of assay conditions. Differentiation of a range of influenza subtypes, including H1N1, H3N2, H5N1, as well as fine differentiation of single strains within these subtypes is possible using the peptide-based subtyping platform. Thereby, the platform could be capable of replacing the current antigenic characterization of influenza strains using ferret hyperimmune sera.

Keywords: antigenic characterization, influenza-binding peptides, influenza subtyping, influenza surveillance

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Authors: Orsolya Horvath, Laszlo Deres, Krisztian Eros, Katalin Ordog, Tamas Habon, Balazs Sumegi, Kalman Toth, Robert Halmosi

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Introduction: Oxidative stress induces an imbalance in mitochondrial fusion and fission processes, finally leading to cell death. The two antioxidant molecules, BGP-15 and L2286 have beneficial effects on mitochondrial functions and on cellular oxidative stress response. In this work, we studied the effects of these compounds on the processes of mitochondrial quality control. Methods: We used H9c2 cardiomyoblast and isolated neonatal rat cardiomyocytes (NRCM) for the experiments. The concentration of stressors and antioxidants was beforehand determined with MTT test. We applied 1-Methyl-3-nitro-1-nitrosoguanidine (MNNG) in 125 µM, 400 µM and 800 µM concentrations for 4 and 8 hours on H9c2 cells. H₂O₂ was applied in 150 µM and 300 µM concentration for 0.5 and 4 hours on both models. L2286 was administered in 10 µM, while BGP-15 in 50 µM doses. Cellular levels of the key proteins playing role in mitochondrial dynamics were measured in Western blot samples. For the analysis of mitochondrial network dynamics, we applied electron microscopy and immunocytochemistry. Results: Due to MNNG treatment the level of fusion proteins (OPA1, MFN2) decreased, while the level of fission protein DRP1 elevated markedly. The levels of fusion proteins OPA1 and MNF2 increased in the L2286 and BGP-15 treated groups. During the 8 hour treatment period, the level of DRP1 also increased in the treated cells (p < 0.05). In the H₂O₂ stressed cells, administration of L2286 increased the level of OPA1 in both H9c2 and NRCM models. MFN2 levels in isolated neonatal rat cardiomyocytes raised considerably due to BGP-15 treatment (p < 0.05). L2286 administration decreased the DRP1 level in H9c2 cells (p < 0.05). We observed that the H₂O₂-induced mitochondrial fragmentation could be decreased by L2286 treatment. Conclusion: Our results indicated that the PARP-inhibitor L2286 has beneficial effect on mitochondrial dynamics during oxidative stress scenario, and also in the case of directly induced DNA damage. We could make the similar conclusions in case of BGP-15 administration, which, via reducing ROS accumulation, propagates fusion processes, this way aids preserving cellular viability. Funding: GINOP-2.3.2-15-2016-00049; GINOP-2.3.2-15-2016-00048; GINOP-2.3.3-15-2016-00025; EFOP-3.6.1-16-2016-00004; ÚNKP-17-4-I-PTE-209

Keywords: H9c2, mitochondrial dynamics, neonatal rat cardiomyocytes, oxidative stress

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