Search results for: aqueous extracts

Authors: Vadim V. Yanshole, Lyudmila V. Yanshole, Alexey S. Kiryutin, Timofey D. Verkhovod, Yuri P. Tsentalovich

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Cataract, or clouding of the eye lens, is the leading cause of vision impairment in the world. The lens tissue have very specific structure: It does not have vascular system, the lens proteins – crystallins – do not turnover throughout lifespan. The protection of lens proteins is provided by the metabolites which diffuse inside the lens from the aqueous humor or synthesized in the lens epithelial layer. Therefore, the study of changes in the metabolite composition of a cataractous lens as compared to a normal lens may elucidate the possible mechanisms of the cataract formation. Quantitative metabolomic profiles of normal and cataractous human lenses were obtained with the combined use of high-frequency nuclear magnetic resonance (NMR) and ion-pairing high-performance liquid chromatography with high-resolution mass-spectrometric detection (LC-MS) methods. The quantitative content of more than fifty metabolites has been determined in this work for normal aged and cataractous human lenses. The most abundant metabolites in the normal lens are myo-inositol, lactate, creatine, glutathione, glutamate, and glucose. For the majority of metabolites, their levels in the lens cortex and nucleus are similar, with the few exceptions including antioxidants and UV filters: The concentrations of glutathione, ascorbate and NAD in the lens nucleus decrease as compared to the cortex, while the levels of the secondary UV filters formed from primary UV filters in redox processes increase. That confirms that the lens core is metabolically inert, and the metabolic activity in the lens nucleus is mostly restricted by protection from the oxidative stress caused by UV irradiation, UV filter spontaneous decomposition, or other factors. It was found that the metabolomic composition of normal and age-matched cataractous human lenses differ significantly. The content of the most important metabolites – antioxidants, UV filters, and osmolytes – in the cataractous nucleus is at least ten fold lower than in the normal nucleus. One may suppose that the majority of these metabolites are synthesized in the lens epithelial layer, and that age-related cataractogenesis might originate from the dysfunction of the lens epithelial cells. Comprehensive quantitative metabolic profiles of the human eye lens have been acquired for the first time. The obtained data can be used for the analysis of changes in the lens chemical composition occurring with age and with the cataract development.

Keywords: cataract, lens, NMR, LC-MS, metabolome

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Authors: Shengyi Huang, Chenju Liang

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Volatile organic compounds such as benzene, toluene, ethyl-benzene, and xylene (BTEX) are common contaminants in environment, which could come from asphalt concrete or exhaust emissions of vehicles. The BTEX may invade to the subsurface environment via wet and dry atmospheric depositions. If there aren’t available ways for controlling contaminants’ fate and transport, they would extensively harm natural environment. In the 1st phase of this study, various adsorbents were screened for a suitable one to be an additive in the porous asphalt mixture. In the 2nd phase, addition of the selected adsorbent was incorporated with the design of porous asphalt concrete (PAC) to produce the permeable reactive pavement (PRP), which was subsequently tested for the potential of adsorbing aqueous BTEX as compared to the PAC, in the 3rd phase. The PRP was prepared according to the following steps: firstly, the suitable adsorbent was chosen based on the analytical results of specific surface area analysis, thermal-gravimetric analysis, adsorption kinetics and isotherms, and thermal dynamics analysis; secondly, the materials of coarse aggregate, fine aggregate, filler, asphalt, and fiber were tested in order to meet regulated specifications (e.g., water adsorption, soundness, viscosity etc.) for preparing the PRP; thirdly, the amount of adsorbent additive was determined in the PRP; fourthly, the prepared PAC and PRP were examined for their physical properties (e.g., abrasion loss, drain-down loss, Marshall stability, Marshall flow, dynamic stability etc.). As a result of comparison between PRP and PAC, the PRP showed better physical performance than the traditional PAC. At last, the Marshall Specimen column tests were conducted to explore the adsorption capacities of PAC and PRPs. The BTEX adsorption capacities of PRPs are higher than those obtained from traditional PAC. In summary, PRPs showed superior physical performance and adsorption capacities, which exhibit the potential of PRP to be applied as a replacement of PAC for better controlling the transport of non-point source pollutants.

Keywords: porous asphalt concrete, volatile organic compounds, permeable reactive pavement, non-point source pollution

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Authors: Iva Blazkova, Amitava Moulick, Vedran Milosavljevic, Pavel Kopel, Marketa Vaculovicova, Vojtech Adam, Rene Kizek

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Doxorubicin is one of the most commonly used and the most effective chemotherapeutic drugs. This antracycline drug isolated from the bacteria Streptomyces peuceticus var. caesius is sold under the trade name Adriamycin (hydroxydaunomycin, hydroxydaunorubicin). Doxorubicin is used in single therapy to treat hematological malignancies (blood cancers, leukaemia, lymphoma), many types of carcinoma (solid tumors) and soft tissue sarcomas. It has many serious side effects like nausea and vomiting, hair lost, myelosupression, oral mucositis, skin reactions and redness, but the most serious one is the cardiotoxicity. Because of the risk of heart attack and congestive heart failure, the total dose administered to patients has to be accurately monitored. With the aim to lower the side effects and to targeted delivery of doxorubicin into the tumor tissue, the different nanoparticles are studied. The drug can be bound on a surface of nanoparticle, encapsulated in the inner cavity, or incorporated into the structure of nanoparticle. Among others, carbon nanoparticles (graphene, carbon nanotubes, fullerenes) are highly studied. Besides the number of inorganic nanoparticles, a great potential exhibit also organic ones mainly lipid-based and polymeric nanoparticle. The aim of this work was to perform a toxicity study of free doxorubicin compared to doxorubicin conjugated with various nanotransporters. The effect of liposomes, fullerenes, graphene, and carbon nanotubes on the toxicity was analyzed. As a first step, the binding efficacy of between doxorubicin and the nanotransporter was determined. The highest efficacy was detected in case of liposomes (85% of applied drug was encapsulated) followed by graphene, carbon nanotubes and fullerenes. For the toxicological studies, the chicken embryos incubated under controlled conditions (37.5 °C, 45% rH, rotation every 2 hours) were used. In 7th developmental day of chicken embryos doxorubicin or doxorubicin-nanotransporter complex was applied on the chorioallantoic membrane of the eggs and the viability was analyzed every day till the 17th developmental day. Then the embryos were extracted from the shell and the distribution of doxorubicin in the body was analyzed by measurement of organs extracts using laser induce fluorescence detection. The chicken embryo mortality caused by free doxorubicin (30%) was significantly lowered by using the conjugation with nanomaterials. The highest accumulation of doxorubicin and doxorubicin nanotransporter complexes was observed in the liver tissue

Keywords: doxorubicin, chicken embryos, nanotransporters, toxicity

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Authors: Pao-Huei Chen, Shu-Mei Lin, Yih-Ming Weng, Zer-Ran Yu, Be-Jen Wang

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Pancreatic α-amylase and intestinal α-glucosidase are the critical enzymes for the breakdown of complex carbohydrates into di- or mono-saccharide, which play an important role in modulating postprandial blood sugars. Angiotensin converting enzyme (ACE) converts inactive angiotensin-I into active angiotensin-II, which subsequently increase blood pressure through triggering vasoconstriction and aldosterone secretion. Thus, inhibition of carbohydrate-digestion enzymes and ACE will help the management of blood glucose and blood pressure, respectively. Studies showed Pleurotus citrinopileatus (PC), an edible mushroom and commonly cultured in oriental countries, exerted anticancer, immune improving, antioxidative, hypoglycemic and hypolipidemic effects. Previous studies also showed various molecular weights (MW) fractioned from extracts may affect biological activities due to varying contents of bioactive components. Thus, the objective of this study is to investigate the in vitro antioxidant, hypoglycemic and hypotenstive effects and distribution of active compounds of various MWs of cold water extract from P. citrinopileatus (CWEPC). CWEPC was fractioned into four various MW fractions, PC-I (＜1 kDa), PC-II (1-3.5 kDa), PC-III (3.5-10 kDa), and PC-IV (＞10 kDa), using an ultrafiltration system. The physiological activities, including antioxidant activities, the inhibition capabilities of pancreatic α-amylase, intestinal α-glucosidase, and hypertension-linked ACE, and the active components, including polysaccharides, protein, and phenolic contents, of CWEPC and four fractions were determined. The results showed that fractions with lower MW exerted a higher antioxidant activity (p<0.05), which was positively correlated to the levels of total phenols. In contrast, the inhibition effects on the activities of α-amylase, α-glucosidase, and ACE of PC-IV fraction were significantly higher than CWEPC and the other three low MW fractions (< 10 kDa), which was more related to protein contents. The inhibition capability of CWEPC and PC-IV on α-amylase activity was 1/13.4 to 1/2.7 relative to that of acarbose (positive control), respectively. However, the inhibitory ability of PC-IV on α-glucosidase (IC50 = 0.5 mg/mL) was significantly higher than acarbose (IC50 = 1.7 mg/mL). Kinetic data revealed that PC-IV fraction followed a non-competitive inhibition on α-glucosidase activity. In conclusion, the distribution of various bioactive components contribute to the functions of different MW fractions on oxidative stress prevention, and blood pressure and glucose modulation.

Keywords: α-Amylase, angiotensin converting enzyme, α-Glucosidase, Pleurotus citrinopileatus

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Authors: Kubra Ozkan, Osman Sagdic

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To better understand the benefits of these fresh and fermented fruits on human health, the consequences of human metabolism and the bioavailability must be known. In this study, brine with 10% salt content, sugar, and vinegar (5% acetic acid) was added to fruits (Prunus domestica L. and Prunus amygdalus Batsch) in different formulations. Samples were stored at 20±2˚C for their fermentation for 21 days. The effects of in vitro digestion were determined on the bioactive compounds in fresh and fermented fruits ((Prunus domestica L. and Prunus amygdalus Batsch). Total phenolic compounds, total flavonoid compounds and antioxidant capacities of post gastric (PG), IN (with small intestinal absorbers) and OUT (without small intestine absorbers) samples obtained as gastric and intestinal digestion in vitro were measured. Bioactive compounds and antioxidant capacity were determined by spectrophotometrically. Antioxidant capacity was tested by the CUPRAC methods, the total phenolic content (TPC) was determined by the Folin-Ciocalteu method, the total flavonoid content (TFC) determined by Aluminium trichloride (AlCl3) method. While the antioxidant capacity of fresh Prunus domestica L. and Prunus amygdalus Batsch samples were 2.21±0.05 mg TEAC/g, 4.39±0.02mg TEAC/g; these values for fermented fruits were found 2.37±0.08mg TEAC/g, 5.38±0.07mg TEAC/g respectively. While the total phenolic contents of fresh fruits namely, Prunus domestica L. and Prunus amygdalus Batsch samples were 0.51±0.01mg GAE/g, 5.56±0.01mg GAE/g; these values for fermented fruits were found as 0.52±0.01mg GAE/g, 6.81±0.03mg GAE/g, respectively. While the total flavonoid amounts of fresh Prunus domestica L. and Prunus amygdalus Batsch samples were 0.19±0.01mg CAE/g, 2.68±0.02mg CAE/g, these values for fermented fruits were found 0.20±0.01mg CAE/g, 2.93±0.02mg CAE/g, respectively. This study showed that phenolic, flavonoid compounds and antioxidant capacities of the samples were increased during the fermantation process. As a result of digestion, the amounts of bioactive components decreased in the stomach and intestinal environment. The bioavailability values of the phenolic compounds in fresh and fermented Prunus domestica L. fruits are 40.89% and 43.28%, respectively. The bioavailability values of the phenolic compounds in fresh and fermented Prunus amygdalus Batsch fruits 4.27% and 3.82%, respectively. The bioavailability values of the flavonoid compounds in fresh and fermented Prunus domestica L. fruits are 5.32% and 19.98%, respectively. The bioavailability values of the flavonoid compounds in fresh and fermented Prunus amygdalus Batsch fruits 2.22% and 1.53%, respectively. The bioavailability values of antioxidant capacity in fresh and fermented Prunus domestica L. fruits are 33.06% and 33.51, respectively. The bioavailability values of antioxidant capacity in fresh and fermented Prunus amygdalus Batsch fruits 14.50% and 15.31%, respectively. Fermentation process; Prunus amygdalus Batsch decreased bioavailability while Prunus domestica increased bioavailability. When two fruits are compared; Prunus domestica bioavailability is more than Prunus amygdalus Batsch.

Keywords: bioactivity, bioavailability, fermented, fruit, nutrition

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Authors: Mojtaba Noghabaei, Khashayar Asadi, Kevin Han

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Simultaneous Localization and Mapping (SLAM) technology has recently attracted the attention of construction companies for real-time performance monitoring. To effectively use SLAM for construction performance monitoring, SLAM results should be registered to a Building Information Models (BIM). Registring SLAM and BIM can provide essential insights for construction managers to identify construction deficiencies in real-time and ultimately reduce rework. Also, registering SLAM to BIM in real-time can boost the accuracy of SLAM since SLAM can use features from both images and 3d models. However, registering SLAM with the BIM in real-time is a challenge. In this study, a novel SLAM platform named Model-Based SLAM (MB-SLAM) is proposed, which not only provides automated registration of SLAM and BIM but also improves the localization accuracy of the SLAM system in real-time. This framework improves the accuracy of SLAM by aligning perspective features such as depth, vanishing points, and vanishing lines from the BIM to the SLAM system. This framework extracts depth features from a monocular camera’s image and improves the localization accuracy of the SLAM system through a real-time iterative process. Initially, SLAM can be used to calculate a rough camera pose for each keyframe. In the next step, each SLAM video sequence keyframe is registered to the BIM in real-time by aligning the keyframe’s perspective with the equivalent BIM view. The alignment method is based on perspective detection that estimates vanishing lines and points by detecting straight edges on images. This process will generate the associated BIM views from the keyframes' views. The calculated poses are later improved during a real-time gradient descent-based iteration method. Two case studies were presented to validate MB-SLAM. The validation process demonstrated promising results and accurately registered SLAM to BIM and significantly improved the SLAM’s localization accuracy. Besides, MB-SLAM achieved real-time performance in both indoor and outdoor environments. The proposed method can fully automate past studies and generate as-built models that are aligned with BIM. The main contribution of this study is a SLAM framework for both research and commercial usage, which aims to monitor construction progress and performance in a unified framework. Through this platform, users can improve the accuracy of the SLAM by providing a rough 3D model of the environment. MB-SLAM further boosts the application to practical usage of the SLAM.

Keywords: perspective alignment, progress monitoring, slam, stereo matching.

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Authors: Kazunori Nomura, Hiromichi Ogi, Masaumi Nakahara, Sou Watanabe, Atsuhiro Shibata

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Chemical Processing Facility of Japan Atomic Energy Agency is a basic research field for advanced back-end technology developments with using actual high-level radioactive materials such as irradiated fuels from the fast reactor, high-level liquid waste from reprocessing plant. In the nature of a research facility, various kinds of chemical reagents have been offered for fundamental tests. Most of them were treated properly and stored in the liquid waste vessel equipped in the facility, but some were not treated and remained at the experimental space as a kind of legacy waste. It is required to treat the waste in safety. On the other hand, we formulated the Medium- and Long-Term Management Plan of Japan Atomic Energy Agency Facilities. This comprehensive plan considers Chemical Processing Facility as one of the facilities to be decommissioned. Even if the plan is executed, treatment of the “legacy” waste beforehand must be a necessary step for decommissioning operation. Under this circumstance, we launched a collaborative research project called the STRAD project, which stands for Systematic Treatment of Radioactive liquid waste for Decommissioning, in order to develop the treatment processes for wastes of the nuclear research facility. In this project, decomposition methods of chemicals causing a troublesome phenomenon such as corrosion and explosion have been developed and there is a prospect of their decomposition in the facility by simple method. And solidification of aqueous or organic liquid wastes after the decomposition has been studied by adding cement or coagulants. Furthermore, we treated experimental tools of various materials with making an effort to stabilize and to compact them before the package into the waste container. It is expected to decrease the number of transportation of the solid waste and widen the operation space. Some achievements of these studies will be shown in this paper. The project is expected to contribute beneficial waste management outcome that can be shared world widely.

Keywords: chemical processing facility, medium- and long-term management plan of JAEA facilities, STRAD project, treatment of radioactive waste

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Authors: Mónica P. Cala, Juan S. Carreño, Roland J.W. Meesters

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Recently, collection of biological fluids on special filter papers has become a popular micro-sampling technique. Especially, the dried blood spot (DBS) micro-sampling technique has gained much attention and is momently applied in various life sciences reserach areas. As a result of this popularity, DBS are not only intensively competing with the venous blood sampling method but are at this moment widely applied in numerous bioanalytical assays. In particular, in the screening of inherited metabolic diseases, pharmacokinetic modeling and in therapeutic drug monitoring. Recently, microsampling techniques were also introduced in “omics” areas, whereunder metabolomics. For a metabolic profiling study we applied micro-sampling of biological fluids (blood and plasma) from healthy controls and from women with breast cancer. From blood samples, dried blood and plasma samples were prepared by spotting 8uL sample onto pre-cutted 5-mm paper disks followed by drying of the disks for 100 minutes. Dried disks were then extracted by 100 uL of methanol. From liquid blood and plasma samples 40 uL were deproteinized with methanol followed by centrifugation and collection of supernatants. Supernatants and extracts were evaporated until dryness by nitrogen gas and residues derivated by O-methyxyamine and MSTFA. As internal standard C17:0-methylester in heptane (10 ppm) was used. Deconvolution and alignment of and full scan (m/z 50-500) MS data were done by AMDIS and SpectConnect (http://spectconnect.mit.edu) software, respectively. Statistical Data analysis was done by Principal Component Analysis (PCA) using R software. The results obtained from our preliminary study indicate that the use of dried blood/plasma on paper disks could be a powerful new tool in metabolic profiling. Many of the metabolites observed in plasma (liquid/dried) were also positively identified in whole blood samples (liquid/dried). Whole blood could be a potential substitute matrix for plasma in Metabolomic profiling studies as well also micro-sampling techniques for the collection of samples in clinical studies. It was concluded that the separation of the different sample methodologies (liquid vs. dried) as observed by PCA was due to different sample treatment protocols applied. More experiments need to be done to confirm obtained observations as well also a more rigorous validation .of these micro-sampling techniques is needed. The novelty of our approach can be found in the application of different biological fluid micro-sampling techniques for metabolic profiling.

Keywords: biofluids, breast cancer, metabolic profiling, micro-sampling

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Authors: Gizachew Mulugeta Manahelohe, Khidmet Safarovich Shikhaliev

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There has been a significant surge in interest in the synthesis of heterocyclic compounds that contain hydroquinoline fragments. This surge can be attributed to the broad range of pharmaceutical and industrial applications that these compounds possess. The present study provides a comprehensive account of the synthesis of both linear and fused heterocyclic systems that incorporate hydroquinoline fragments. Furthermore, the pharmacological activity spectra of the synthesized compounds were assessed using the in silico method, employing the prediction of activity spectra of substances (PASS) program. Hydroquinoline nitriles 7 and 8 were prepared through the reaction of the corresponding hydroquinolinecarbaldehyde using a hydroxylammonium chloride/pyridine/toluene system and iodine in aqueous ammonia under ambient conditions, respectively. 2-Phenyl-1,3-oxazol-5(4H)-ones 9a,b and 10a,b were synthesized via the condensation of compounds 5a,b and 6a,b with hippuric acid in acetic acid in 30–60% yield. When activated, 7-methylazolopyrimidines 11a and b were reacted with N-alkyl-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline-6-carbaldehydes 6a and b, and triazolo/pyrazolo[1,5-a]pyrimidin-6-yl carboxylic acids 12a and b were obtained in 60–70% yield. The condensation of 7-hydroxy-1,2,3,4-tetramethyl-1,2-dihydroquinoline 3 h with dimethylacetylenedicarboxylate (DMAD) and ethyl acetoacetate afforded cyclic products 16 and 17, respectively. The condensation reaction of 6-formyl-7-hydroxy-1,2,2,4-tetramethyl-1,2-dihydroquinoline 5e with methylene-active compounds such as ethyl cyanoacetate/dimethyl-3-oxopentanedioate/ethyl acetoacetate/diethylmalonate/Meldrum’s acid afforded 3-substituted coumarins containing dihydroquinolines 19 and 21. Pentacyclic coumarin 22 was obtained via the random condensation of malononitrile with 5e in the presence of a catalytic amount of piperidine in ethanol. The biological activities of the synthesized compounds were assessed using the PASS program. Based on the prognosis, compounds 13a, b, and 14 exhibited a high likelihood of being active as inhibitors of gluconate 2-dehydrogenase, as well as possessing antiallergic, antiasthmatic, and antiarthritic properties, with a probability value (Pa) ranging from 0.849 to 0.870. Furthermore, it was discovered that hydroquinoline carbonitriles 7 and 8 tended to act as effective progesterone antagonists and displayed antiallergic, antiasthmatic, and antiarthritic effects (Pa = 0.276–0.827). Among the hydroquinolines containing coumarin moieties, compounds 17, 19a, and 19c were predicted to be potent progesterone antagonists, with Pa values of 0.710, 0.630, and 0.615, respectively.

Keywords: heterocyclic compound, hydroquinoline, Vilsmeier–Haack formulation, quinolone

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Authors: Monika Ksiezopolska-Gocalska, Pawel Albrycht, Robert Holyst

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Surface Enhanced Raman Spectroscopy (SERS) is a technique used to analyze very low concentrations of substances in solutions, even in aqueous solutions - which is its advantage over IR. This technique can be used in the pharmacy (to check the purity of products); forensics (whether at a crime scene there were any illegal substances); or medicine (serving as a medical test) and lots more. Due to the high potential of this technique, its increasing popularity in analytical laboratories, and simultaneously - the absence of appropriate platforms enhancing the SERS signal (crucial to observe the Raman effect at low analyte concentration in solutions (1 ppm)), we decided to invent our own SERS platforms. As an enhancing layer, we have chosen gold and silver nanoparticles, because these two have the best SERS properties, and each has an affinity for the other kind of particles, which increases the range of research capabilities. The next step was to commercialize them, which resulted in the creation of the company ‘SERSitive.eu’ focusing on production of highly sensitive (Ef = 10⁵ – 10⁶), homogeneous and reproducible (70 - 80%) substrates. SERStive SERS substrates are made using the electrodeposition of silver or silver-gold nanoparticles technique. Thanks to a very detailed analysis of data based on studies optimizing such parameters as deposition time, temperature of the reaction solution, applied potential, used reducer, or reagent concentrations using a standardized compound - p-mercaptobenzoic acid (PMBA) at a concentration of 10⁻⁶ M, we have developed a high-performance process for depositing precious metal nanoparticles on the surface of ITO glass. In order to check a quality of the SERSitive platforms, we examined the wide range of the chemical compounds and the biological substances. Apart from analytes that have great affinity to the metal surfaces (e.g. PMBA) we obtained very good results for those fitting less the SERS measurements. Successfully we received intensive, and what’s more important - very repetitive spectra for; amino acids (phenyloalanine, 10⁻³ M), drugs (amphetamine, 10⁻⁴ M), designer drugs (cathinone derivatives, 10⁻³ M), medicines and ending with bacteria (Listeria, Salmonella, Escherichia coli) and fungi.

Keywords: nanoparticles, Raman spectroscopy, SERS, SERS applications, SERS substrates, SERSitive

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Authors: Yoshio Kobayashi, Kohsuke Gonda

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In medical diagnostics, contrast agents are used to improve the performance of X-ray, magnetic resonance, and fluorescence-based imaging. A variety of contrast agents are commercially available. Typical commercial contrast agents include solutions containing iodine compounds for X-ray imaging and gadolinium complexes for magnetic resonance imaging. Metal-gold nanoparticles can also exhibit X-ray imaging capabilities. Because of their small size, these contrast agents are not strongly attracted to liquids. Therefore, they cannot remain in vivo for long periods of time, making it difficult to obtain stable images. Forming contrast agent particles and increasing their apparent particle size is expected to be a solution to this problem, as they have a larger projected area than molecules or nanoparticles and thus have a longer residence time. In addition, contrast agents can cause adverse reactions derived from iodine, metallic gold, gadolinium ions, and cadmium. Coating particles with a shell that is inert to living organisms is a candidate for suppressing side reactions because the particles cannot contact the organism. Our laboratory has recently developed a method for the preparation of colloidal solutions of core-shell particles with an imaging-competent material as the core and biologically inert silica as the shell and studied their imaging properties. The method used was based on the hydrolysis and condensation of silicon alkoxide in the presence of particles such as iodine compound nanoparticles prepared by mixing aqueous AgClO4 and KI solutions, metal Au nanoparticles prepared by reducing HAuCl4 with citric acid, gadolinium compound nanoparticles prepared by the homogeneous precipitation method, and commercial cadmium compound nanoparticles so that silica nuclei generated from silicone alkoxide deposited on the particles to form silica shells. The prepared particle colloidal solutions showed notable imaging capabilities. For example, a computed tomography value of the silica-coated Au nanoparticle colloidal solution was higher than that of a commercial X-ray contrast agent for the same Au or iodine concentrations. In this contribution, we present our studies on the imaging capability of particle colloidal solutions that we have been conducting for the past few years.

Keywords: core-shell, particles, colloid, imaging

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Authors: M. S. Abd El-Sadek, M. A. Omar, Gharib M. Taha

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In recent years, photocatalytic degradation of various kinds of organic and inorganic pollutants using semiconductor powders as photocatalysts has been extensively studied. Owing to its relatively high photocatalytic activity, biological and chemical stability, low cost, nonpoisonous and long stable life, Tin oxide materials have been widely used as catalysts in chemical reactions, including synthesis of vinyl ketone, oxidation of methanol and so on. Tin oxide (SnO₂), with a rutile-type crystalline structure, is an n-type wide band gap (3.6 eV) semiconductor that presents a proper combination of chemical, electronic and optical properties that make it advantageous in several applications. In the present work, SnO₂ nanoparticles were synthesized at room temperature by the sol-gel process and thermohydrolysis of SnCl₂ in isopropanol by controlling the crystallite size through calculations. The synthesized nanoparticles were identified by using XRD analysis, TEM, FT-IR, and Uv-Visible spectroscopic techniques. The crystalline structure and grain size of the synthesized samples were analyzed by X-Ray diffraction analysis (XRD) and the XRD patterns confirmed the presence of tetragonal phase SnO₂. In this study, Methylene blue degradation was tested by using SnO₂ nanoparticles (at different calculations temperatures) as a photocatalyst under sunlight as a source of irradiation. The results showed that the highest percentage of degradation of Methylene blue dye was obtained by using SnO₂ photocatalyst at calculations temperature 800 ᵒC. The operational parameters were investigated to be optimized to the best conditions which result in complete removal of organic pollutants from aqueous solution. It was found that the degradation of dyes depends on several parameters such as irradiation time, initial dye concentration, the dose of the catalyst and the presence of metals such as silver as a dopant and its concentration. Percent degradation was increased with irradiation time. The degradation efficiency decreased as the initial concentration of the dye increased. The degradation efficiency increased as the dose of the catalyst increased to a certain level and by further increasing the SnO₂ photocatalyst dose, the degradation efficiency is decreased. The best degradation efficiency on which obtained from pure SnO₂ compared with SnO₂ which doped by different percentage of Ag.

Keywords: SnO₂ nanoparticles, a sol-gel method, photocatalytic applications, methylene blue, degradation efficiency

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Authors: Ruth Diego, Luis M. Romeo, Antonio Morán

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In the present work, a study of the coupling of a Bioelectrochemical System together with an oxy-combustion boiler is carried out; specifically, it proposes to connect the combustion gas outlet of a boiler with a microbial electrolysis cell (MEC) where the CO2 from the gases are transformed into methane in the cathode chamber, and the oxygen produced in the anode chamber is recirculated to the oxy-combustion boiler. The MEC mainly consists of two electrodes (anode and cathode) immersed in an aqueous electrolyte; these electrodes are separated by a proton exchange membrane (PEM). In this case, the anode is abiotic (where oxygen is produced), and it is at the cathode that an electroactive biofilm is formed with microorganisms that catalyze the CO2 reduction reactions. Real data from an oxy-combustion process in a boiler of around 20 thermal MW have been used for this study and are combined with data obtained on a smaller scale (laboratory-pilot scale) to determine the yields that could be obtained considering the system as environmentally sustainable energy storage. In this way, an attempt is made to integrate a relatively conventional energy production system (oxy-combustion) with a biological system (microbial electrolysis cell), which is a challenge to be addressed in this type of new hybrid scheme. In this way, a novel concept is presented with the basic dimensioning of the necessary equipment and the efficiency of the global process. In this work, it has been calculated that the efficiency of this power-to-gas system based on MEC cells when coupled to industrial processes is of the same order of magnitude as the most promising equivalent routes. The proposed process has two main limitations, the overpotentials in the electrodes that penalize the overall efficiency and the need for storage tanks for the process gases. The results of the calculations carried out in this work show that certain real potentials achieve an acceptable performance. Regarding the tanks, with adequate dimensioning, it is possible to achieve complete autonomy. The proposed system called OxyMES provides energy storage without energetically penalizing the process when compared to an oxy-combustion plant with conventional CO2 capture. According to the results obtained, this system can be applied as a measure to decarbonize an industry, changing the original fuel of the oxy-combustion boiler to the biogas generated in the MEC cell. It could also be used to neutralize CO2 emissions from industry by converting it to methane and then injecting it into the natural gas grid.

Keywords: microbial electrolysis cells, oxy-combustion, co2, power-to-gas

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Authors: Laura Rueda-Gensini, Jader Rodríguez, Juan C. Cruz, Carolina Munoz-Camargo

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There is an emerging interest in botanicals and plant extracts for medicinal practices due to their widely reported health benefits. A large variety of phytochemicals found in plants have been correlated with antioxidant, immunomodulatory, and analgesic properties, which makes plant-derived products promising candidates for modulating the progression and treatment of numerous diseases. Non-centrifugal cane sugar (NCS), in particular, has been known for its high antioxidant and nutritional value, but composition-wise variability due to changing environmental and processing conditions have considerably limited its use in the nutraceutical and biomedical fields. This work is therefore aimed at assessing the effect of thermal exposure during NCS production over its bioactive composition and, in turn, its therapeutic value. Accordingly, two modified dehydration methods are proposed that employ: (i) vacuum-aided evaporation, which reduces the necessary temperatures to dehydrate the sample, and (ii) window refractance evaporation, which reduces thermal exposure time. The biochemical composition of NCS produced under these two methods was compared to traditionally-produced NCS by estimating their total polyphenolic and protein content with Folin-Ciocalteu and Bradford assays, as well as identifying the major phenolic compounds in each sample via HPLC-coupled mass spectrometry. Their antioxidant activities were also compared as measured by their scavenging potential of ABTS and DPPH radicals. Results show that the two modified production methods enhance polyphenolic and protein yield in resulting NCS samples when compared to traditional production methods. In particular, reducing employed temperatures with vacuum-aided evaporation demonstrated to be superior at preserving polyphenolic compounds, as evidenced both in the total and individual polyphenol concentrations. However, antioxidant activities were not significantly different between these. Although additional studies should be performed to determine if the observed compositional differences affect other therapeutic activities (e.g., anti-inflammatory, analgesic, and immunoprotective), these results suggest that reducing thermal exposure holds great promise for the production of natural products with enhanced nutritional value.

Keywords: non-centrifugal cane sugar, polyphenolic compounds, thermal processing, antioxidant activity

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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

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Authors: Gabriela D. Silva, Rodrigo L. O. R. Cunha, Mauricio D. Coutinho-Neto

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In the last four decades the biological activities of selenium compounds has received great attention, particularly for hypervalent derivates from selenium (IV) used as enzyme inhibitors. The unregulated activity of cysteine proteases are related to the development of several pathologies, such as neurological disorders, cardiovascular diseases, obesity, rheumatoid arthritis, cancer and parasitic infections. These enzymes are therefore a valuable target for designing new small molecule inhibitors such as selenuranes. Even tough there has been advances in the synthesis and design of new selenuranes based inhibitors, little is known about their mechanism of action. It is a given that inhibition occurs through the reaction between the thiol group of the enzyme and the chalcogen atom. However, several open questions remain about the nature of the mechanism (associative vs. dissociative) and about the nature of the reactive species in solution under physiological conditions. In this work we performed a theoretical investigation on model systems to study the possible routes of substitution reactions. Nucleophiles may be present in biological systems, our interest is centered in the thiol groups from the cysteine proteases and the hydroxyls from the aqueous environment. We therefore expect this study to clarify the possibility of a route reaction in two stages, the first consisting of the substitution of chloro atoms by hydroxyl groups and then replacing these hydroxyl groups per thiol groups in selenuranes. The structures of selenuranes and nucleophiles were optimized using density function theory along the B3LYP functional and a 6-311+G(d) basis set. Solvent was treated using the IEFPCM method as implemented in the Gaussian 09 code. Our results indicate that hydrolysis from water react preferably with selenuranes, and then, they are replaced by the thiol group. It show the energy values of -106,0730423 kcal/mol for dople substituition by hydroxyl group and 96,63078511 kcal/mol for thiol group. The solvatation and pH reduction promotes this route, increasing the energy value for reaction with hydroxil group to -50,75637672 kcal/mol and decreasing the energy value for thiol to 7,917767189 kcal/mol. Alternative ways were analyzed for monosubstitution (considering the competition between Cl, OH and SH groups) and they suggest the same route. Similar results were obtained for aliphatic and aromatic selenuranes studied.

Keywords: chalcogenes, computational study, cysteine proteases, enzyme inhibitors

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Authors: Fakhreldin O. Suliman, Alia H. Al-Battashi

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This work explored the interaction of three different imidazoline drugs, naphazoline nitrate (NPH), oxymetazoline hydrochloride (OXY) and xylometazoline hydrochloride (XYL) with two different synthesized cucurbit[n]urils CB[n], cucurbit[7]uril (CB[7]) and cucuribit[8]uril (CB[8]). Three binary inclusion complexes have been investigated in solution and in the solid state. The solid complexes were obtained by lyophilization, whereas the physical mixtures of guests and hosts at a stoichiometric ratio of 1:1 were obtained for each drug. 1HNMR, electrospray ionization mass spectrometry (ESI-MS), and matrix-assisted laser desorption-ionization time-of-flight (MALDI-TOF) mass spectrometry was used to study the complexes prepared in aqueous media. The lyophilized solid complexes were characterized by Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffractometry (PXRD), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC). MS, FT-IR and PXRD experimental results established in this work reveal that NPH, OXY and XYL molecules form stable inclusion complexes with the two hosts. The TGA and DSC confirmed the enhancement of the thermal stability of each drug and the production of a thermally stable solid complex. The 1HNMR has shown that the protons of the guests faced shifting in ppm and broadening of their peaks upon the formation of inclusion complexes with the selected CB[n]. The aromatic protons of the guest exhibited the highest changes in the chemical shifts and shape of the NMR peaks, suggesting their inclusion into the cavity of the CB[n]. The diffusion coefficients (D), developed from the diffusion-controlled NMR Spectroscopy (DOSY) measurements, for the complexation of the selected imidazoline drugs with CB[7] and CB[8], were decreased in the presence of hosts compared to the free guests indicating the formation of the guest-host adduct. Furthermore, we conducted molecular dynamic simulations and quantum mechanics calculations on these complexes. The results of the theoretical study corroborate the experimental findings and have also shed light on the mechanism of inclusion of the guests into the two hosts. This study generates initial data for potential drug delivery or drug formulation systems for these three selected imidazoline drug compounds based on their inclusion into the CB[n] cavities.

Keywords: cucurbit[n]urils, imidazoline, inclusion complexes, molecular dynamics, DFT calculations, mass spectrometry

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Authors: Moin Uddin, M. Masroor A. Khan, Faisal Rasheed, Tariq Ahmad Dar, Akbar Ali, Lalit Varshney

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Oligomers, obtained by exposing the natural polysaccharides (alginate, carrageenan, chitosan, etc.) to cobalt-60 generated gamma radiation may prove as potent plant growth promoters when applied as foliar sprays to the plants. They function as endogenous growth elicitors, triggering the synthesis of different enzymes and modulating various plant responses by exploiting the gene expression. Exogenous application of Jasmonic acid or of its methyl ester, methyl jasmonate (MeJ) has been reported to increase the secondary metabolites production in medicinal and aromatic plants. Keeping this in mind, three pot experiments were conducted to test whether the foliar application of irradiated-chitosan (IC) and MeJ, applied alone or in combination, could augment the active constituents as well as growth, physiological and yield attributes of Catharanthus roseus, which carries anticancer alkaloids, viz. vincristine and vinblastine, in its leaves in addition to various other useful alkaloids. Totally, 5 spray treatments, comprising various aqueous solutions of IC [20, 40, 80 and 160 mg L-1 (Experiment 1)], MeJ (10, 20, 30 and 40 mg L-1 (Experiment 2)] and those of IC+MeJ [40+20, 40+30, 80+20, 80+30, 160+20 and 160+30 mg L-1 (Experiment 3)], were applied at seven days interval. Total leaf-alkaloids content as well as growth, physiological and yield parameters, evaluated at 120 days after sowing, were significantly enhanced by IC application. IC application could not increase the leaf-content of vincristine and vinblastine; nonetheless, it significantly augmented the yield of these alkaloids owing to enhancing the dry mass of leaves per plant. MeJ application, particularly at 30 mg L-1, increased both content (17%) and yield (48%) of total leaf-alkaloids as well as the content and yield of vincristine ( 29 and 63%, respectively) and vinblastine (14 and 44%, respectively) alkaloids, though it significantly decreased most other parameters studied, particularly at higher concentrations (30 and 40 mg L-1 of MeJ). As compared to the control (water-spray treatment), collective application of IC (80 mg L-1) and MeJ (20 mg L-1) resulted in the highest values of most of the parameters studied. However, 80 mg L-1 of IC applied with 30 mg L-1 of MeJ gave the best results for the content and yield of total as well as anticancer leaf-alkaloids (vincristine and vinblastine). Comparing the control, it increased the content and yield of total leaf-alkaloids (37 and 118%, respectively) and those of vincristine (65 and 163%, respectively) and vinblastine (31 and 107%, respectively). Conclusively, the applied technique significantly enhanced the production of total as well as anticancer alkaloids of Catharanthus roseus.

Keywords: anticancer alkaloids (vincristine and vinblastine), catharanthus roseus, irradiated chitosan, methyl jasmonate

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Authors: Heba A. Hazzah, Ragwa M. Farid, Maha M. A. Nasra, Mennatallah Zakria, Magda A. El Massik, Ossama Y. Abdallah

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Introduction: Curcumin (Cur) is a polyphenol derived from the herbal remedy and dietary spice turmeric. It possesses diverse anti-inflammatory and anti-cancer properties following oral or topical administration. The buccal delivery of curcumin can be useful for both systemic and local disease treatments such as gingivitis, periodontal diseases, oral carcinomas, and precancerous oral lesions. Despite of its high activity, it suffers a limited application due to its low oral bioavailability, poor aqueous solubility, and instability. Aim: Preparation and characterization of curcumin solid lipid nanoparticles with a high loading capacity into a mucoadhesive gel for buccal application. Methodology: Curcumin was formulated as nanoparticles using different lipids, namely Gelucire 39/01, Gelucire 50/13, Precirol, Compritol, and Polaxomer 407 as a surfactant. The SLN were dispersed in a mucoadhesive gel matrix to be applied to the buccal mucosa. All formulations were evaluated for their content, entrapment efficiency, particle size, in vitro drug dialysis, ex vivo mucoadhesion test, and ex vivo permeation study using chicken buccal mucosa. Clinical evaluation was conducted on 15 cases suffering oral erythroplakia and erosive lichen planus. Results: The results showed high entrapment efficiency reaching almost 90 % using Gelucire 50, the loaded gel with Cur-SLN showed good adhesion property and 25 minutes in vivo residence time. In addition to stability enhancement for the Cur powder. All formulae did not show any drug permeated however, a significant amount of Cur was retained within the mucosal tissue. Pain and lesion sizes were significantly reduced upon topical treatment. Complete healing was observed after 6 weeks of treatment. Conclusion: These results open a room for the pharmaceutical technology to optimize the use of this golden magical powder to get the best out of it. In addition, the lack of local anti-inflammatory compounds with reduced side effects intensifies the importance of studying natural products for this purpose.

Keywords: curcumin, erythroplakia, mucoadhesive, pain, solid lipid nanoparticles

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Authors: Bunindro Nameirakpam, Sonia Sougrapakam, Shannon B. Olsson, Rajashekar Yallappa

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Natural sources for new pesticidal compounds hold promise in view of their eco-friendly nature, selectivity and mammalian safety. Despite a large number of plants that show insecticidal activity and diversity of natural chemistry with inherent eco-friendly nature, newer classes of insecticides have eluded discovery. Artemisia vulgaris, known as Mugwort, is a universal herb used for folk medicine and religious purposes throughout the ancient world. In India, the essential oils of Artemisia vulgaris are used for its insecticidal, anti parasiticidal and antimicrobial properties. Traditionally, the dried leaves of Artemisia vulgaris are used to repel insects as well as rats in and around the granaries in the North-East India. Artemisia vulgaris collected during November from different ecological sites were studied for the bio-pesticidal utility against the stored grain pests. The insecticidal activities were found in the crude extracts of n-hexane and methanol from the samples collected in Sikkim and Manipur respectively. Using silica gel column chromatography protocol, we have isolated one novel bioactive molecule from the aerial parts of Artemisia vulgaris L based on various physical-chemical and spectroscopic techniques (IR, 1H NMR, 13C NMR and mass). The novel bioactive molecule is highly toxic and very low concentration (4.35 µg/l) is needed to control the stored product insects. In additional experiment results clearly showed the involvement of sodium pumps inhibition in the insecticidal action of purified compound in the Sitophilus oryzae. The knockdown activity of the purified compound is concomitant with the in vivo inhibition of Na+/ K+- ATPase. Further, our study showed insignificant differences in the seed germination of control and the treated grains. The lack of adverse effect of the novel bioactive molecule on the seed germination is highly desirable for seed/grain protectant and showing the potential to be developed as possible natural fumigants for the control of stored grain pests. The novel bioactive molecule is selective insecticide with a high margin of safety to mammals and showed promise as novel biopesticide candidate for grain protection. It is believed that Bio-pesticides can serve as the most important pest management tools as far as global safety is concerned.

Keywords: Indian traditional plant, Artemisia vulgaris, bio-pesticides, Na+/ K+- ATPase, seed germination

Procedia PDF Downloads 191

Authors: H. Li, L. Ji, J. Su

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Forward osmosis is an emerging technology for separation and has great potential in the concentration of liquid products such as protein, pharmaceutical, and natural products. In pharmacy industry, one of the very tough talks is to concentrate the product in a gentle way since some of the key components may lose bioactivity when exposed to heating or pressurization. Therefore, forward osmosis (FO), which uses inherently existed osmosis pressure instead of externally applied hydraulic pressure, is attractive for pharmaceutical enrichments in a much efficient and energy-saving way. Recently, coordination complexes have been explored as the new class of draw solutes in FO processes due to their bulky configuration and excellent performance in terms of high water flux and low reverse solute flux. Among these coordination complexes, ferric citrate complex with lots of hydrophilic groups and ionic species which make them good solubility and high osmotic pressure in aqueous solution, as well as its low toxicity, has received much attention. However, the chemistry of ferric complexation by citrate is complicated, and disagreement prevails in the literature, especially for the structure of the ferric citrate. In this study, we investigated the chemical reaction with various molar ratio of iron and citrate. It was observed that the ferric citrate complex (Fe-CA2) with molar ratio of 1:1 for iron and citrate formed at the beginning of the reaction, then Fecit would convert to ferric citrate complex at the molar ratio of 1:2 with the proper excess of citrate in the base solution. The structures of the ferric citrate complexes synthesized were systematically characterized by X-ray diffraction (XRD), UV-vis spectroscopy, X-ray photoelectron spectroscopy (XPS), Fourier transform infrared spectroscopy (FT-IR) and Thermogravimetric analysis (TGA). Fe-CA2 solutions exhibit osmotic pressures more than twice of that for NaCl solutions at the same concentrations. Higher osmotic pressure means higher driving force, and this is preferable for the FO process. Fe-CA2 and NaCl draw solutions were prepared with the same osmotic pressure and used in FO process for BSA protein concentration. Within 180 min, BSA concentration was enriched from 0.2 to 0.27 L using Fe-CA draw solutions. However, it was only increased from 0.20 to 0.22 g/L using NaCl draw solutions. A reverse flux of 11 g/m²h was observed for NaCl draw solutes while it was only 0.1 g/m²h for Fe-CA2 draw solutes. It is safe to conclude that Fe-CA2 is much better than NaCl as draw solute and it is suitable for the enrichment of liquid product.

Keywords: draw solutes, ferric citrate complex, forward osmosis, protein enrichment

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Authors: Dorothea Voß, Tobias Esser, Michael Huber, Jakob Albert

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The growing world population and the associated increase in demand for energy and consumer goods, as well as increasing waste production, requires the development of sustainable processes. In addition, the increasing environmental awareness of our society is a driving force for the requirement that processes must be as resource and energy efficient as possible. In this context, the use of polyoxometalate catalysts (POMs) has emerged as a promising approach for the development of green processes. POMs are bifunctional polynuclear metal-oxo-anion cluster characterized by a strong Brønsted acidity, a high proton mobility combined with fast multi-electron transfer and tunable redox potential. In addition, POMs are soluble in many commonly known solvents and exhibit resistance to hydrolytic and oxidative degradation. Due to their structure and excellent physicochemical properties, POMs are efficient acid and oxidation catalysts that have attracted much attention in recent years. Oxidation processes with molecular oxygen are worth mentioning here. However, the fact that the POM catalysts are homogeneous poses a challenge for downstream processing of product solutions and recycling of the catalysts. In this regard, nanofiltration membranes have gained increasing interest in recent years, particularly due to their relative sustainability advantage over other technologies and their unique properties such as increased selectivity towards multivalent ions. In order to establish an efficient downstream process for the highly selective separation of homogeneous POM catalysts from aqueous solutions using nanofiltration membranes, a laboratory-scale membrane system was designed and constructed. By varying various process parameters, a sensitivity analysis was performed on a model system to develop an optimized method for the recovery of POM catalysts. From this, process-relevant key figures such as the rejection of various system components were derived. These results form the basis for further experiments on other systems to test the transferability to serval separation tasks with different POMs and products, as well as for recycling experiments of the catalysts in processes on laboratory scale.

Keywords: downstream processing, nanofiltration, polyoxometalates, homogeneous catalysis, green chemistry

Procedia PDF Downloads 85

Authors: J. H. Bang, H. J. Baek, K. I. Kim, B. J. Lee, H. J. Jung, H. J. Jang, S. K. Jung

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Asthma is a chronic inflammatory lung disease characterized by airway hyper responsiveness (AHR), airway obstruction and airway wall remodeling responsible for significant morbidity and mortality worldwide. Genetic and environment factors may result in asthma, but there are no the exact causes of asthma. Chungpye-tang (CPT) has been prescribed as a representative aerosol agent for patients with dyspnea, cough and phlegm in the respiratory clinic at Kyung Hee Korean Medicine Hospital. This Korean herbal medicines have the effect of dispelling external pathogen and dampness pattern. CPT is composed of 4 species of herbal medicines. The 4 species of herbal medicines are Ephedrae herba, Pogostemonis(Agatachis) herba, Caryophylli flos and Zingiberis rhizoma crudus. CPT suppresses neutrophil infiltration and the production of pro-inflammatory cytokines in lipopolysaccharide (LPS)-induced acute lung injury (ALI) mouse model. Moreover, the anti-inflammatory effects of CPT on a mouse model of Chronic Obstructive Pulmonary Disease (COPD) was proved. Activation of the NF-κB has been proven that it plays an important role in inflammation via inducing transcription of pro-inflammatory genes. Over-expression of NF-κB has been believed be related to many inflammatory diseases such as arthritis, gastritis, asthma and COPD. So we firstly hypothesize whether CPT has an anti-inflammatory effect on asthmatic human airway epithelial tissue via inhibiting NF-κB pathway. In this study, CPT was extracted with distilled water for 3 hours at 100°C. After process of filtration and evaporation, it was freeze dried. And asthmatic human lung tissues were provided by MatTek Corp. We investigated the precise mechanism of the anti-inflammatory effect of CPT by western blotting analysis. We observed whether the decoction extracts could reduce NF-κB activation, COX-2 protein expression and NF-κB-mediated pro-inflammatory cytokines such as TNF-α, eotaxin, IL-4, IL-9 and IL-13 in asthmatic human lung tissue. As results of this study, there was a trend toward decreased NF-κB expression in asthmatic human airway epithelial tissue. We found that the inhibition effects of CPT on COX-2 expression was not determined. IL-9 and IL-13 secretion was significantly reduced in the asthmatic human lung tissue treated with CPT. Overall, our results indicate that CPT has an anti-inflammatory effect through blocking the signaling pathway of NF-κB, thereby CPT may be a potential remedial agent for allergic asthma.

Keywords: Chungpye-tang, allergic asthma, asthmatic human airway epithelial tissue, nuclear factor kappa B (NF-κB) pathway, COX-2

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Authors: Brahim Sow

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Background: Throughout West Africa, Balanites aegyptiaca (BA), or Zygophyllaceae, is widely used in traditional medicine to treat diabetes, hypertension, inflammation, malaria and liver disorders. In our recent research, we found that BA has nephroprotective potential against diabetes mellitus, hypertension and kidney disorders. However, to our knowledge, no systematic studies have been carried out on its derivative (toxicity) profile. Aim of the study: The study was conducted to assess the potential potency of the hydroalcoholic extract of BA bark in rats by the acute and sub-acute oral route. Materials and methods: Male and female rats in the acute depression study received BA extract orally at single doses of 500 mg/kg, 2000 mg/kg, 3000 mg/kg and 5000 mg/kg (n = 6 per group/sex). To assess acute depression, abnormal behaviour, toxic symptoms, weight and death were observed for 14 consecutive days. For the subacute impairment study, Wistar rats received the extract orally at doses of 125, 250 and 500 mg/kg (n=6 per group/sex) per day for 28 days. Behaviour and body weight were monitored daily. At the end of the treatment period, biochemical, haematological and histopathological examinations were performed, and gross and histopathological examinations of several organs were carried out. To determine the presence or absence of phytochemicals, the BA extract was subjected to gage phage chromatographic examination. Results: The absence of absorption chromatography of BA indicates the absence of cyanide groups. This suggests that the BA extract does not contain toxic substances. No mortality or adverse effects were observed at 5000 mg/kg in the acute depression test. With regard to body weight, general behaviour, relative organ weights, haematological and biochemical parameters, BA extract did not induce any mortality or potentially treatment-related effects in the sub-acute study. The normal architecture of the vital organs was revealed by histopathological examination, indicating the absence of morphological alterations. Conclusion: BA extract administered orally for 28 days at doses up to 500 mg/kg did not cause toxicological damage in rats in the present study. The median lethal dose (LD50) of the extract was estimated to be over 5000 mg/kg in an acute hyperglycaemia study.

Keywords: Balanites aegyptiaca L Delile, haematology, biochemistry, rat

Procedia PDF Downloads 72

Authors: F. Pires, V. Geraldo, O. N. Oliveira Jr., M. Raposo

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Catechins are powerful antioxidants which have attractive properties useful for tumor therapy. Considering their antioxidant activity, these molecules can act as a scavenger of the reactive oxygen species (ROS), alleviating the damage of cell membrane induced by oxidative stress. The complexity and dynamic nature of the cell membrane compromise the analysis of the biophysical interactions between drug and cell membrane and restricts the transport or uptake of the drug by intracellular targets. To avoid the cell membrane complexity, we used biomimetic systems as liposomes and Langmuir monolayers to study the interaction between catechin and membranes at the molecular level. Liposomes were formed after the dispersion of anionic 1,2-dipalmitoyl-sn-glycero-3-[phospho-rac-(1-glycerol)(sodium salt) (DPPG) phospholipids in an aqueous solution, which mimic the arrangement of lipids in natural cell membranes and allows the entrapment of catechins. Langmuir monolayers were formed after dropping amphiphilic molecules, DPPG phospholipids, dissolved in an organic solvent onto the water surface. In this work, we mixed epigallocatechin-3-gallate (EGCG) with DPPG liposomes and exposed them to ultra-violet radiation in order to evaluate the antioxidant potential of these molecules against oxidative stress induced by radiation. The presence of EGCG in the mixture decreased the rate of lipid peroxidation, proving that EGCG protects membranes through the quenching of the reactive oxygen species. Considering the high amount of hydroxyl groups (OH groups) on structure of EGCG, a possible mechanism to these molecules interact with membrane is through hydrogen bonding. We also investigated the effect of EGCG at various concentrations on DPPG Langmuir monolayers. The surface pressure isotherms and infrared reflection-absorption spectroscopy (PM-IRRAS) results corroborate with absorbance results preformed on liposome-model, showing that EGCG interacts with polar heads of the monolayers. This study elucidates the physiological action of EGCG which can be incorporated in lipid membrane. These results are also relevant for the improvement of the current protocols used to incorporate catechins in drug delivery systems.

Keywords: catechins, lipid membrane, anticancer agent, molecular interactions

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Authors: Omoruyi G. Idemudia, Alexander P. Sadimenko

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The need for the development of new sustainable bioactive compounds with unique properties that can become potential replacement for commonly used medicinal drugs has continued to gain tremendous research concerns because of the problems of disease resistant to these medicinal drugs and their toxicity effects. NOS-donor heterocycles are particularly of interest as they have showed good pharmacological activities in the midst of their interesting chelating properties towards metal ions, an important characteristic for transition metal based drugs design. These new compounds have also gained application as dye sensitizers in solar cell panels for the generation of renewable solar energy, as greener water purification polymer for supply and management of clean water and as catalysts which are used to reduce the amount of pollutants from industrial reaction processes amongst others, because of their versatile properties. Di-ketone acylpyrazolones and their azomethine schiff bases have been employed as pharmaceuticals as well as analytical reagents, and their application as transition metal complexes have being well established. In this research work, a new 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one-thiosemicarbazone was synthesized from the reaction of 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one and thiosemicarbazide in methanol. The pure isolate of the thiosemicarbazone was further reacted with aqueous solutions of palladium and platinum salts to obtain their metal complexes, in an effort towards the discovery of transition metal based synthetic drugs. These 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 thiosemicarbazone crystallizes in a triclinic crystal system with a P-1 (No. 2) space group according to x-ray crystallography. The tridentate NOS ligand formed a tetrahedral geometry on coordinating with metal ions. Reported compounds showed varying antioxidant free radical scavenging activities against 2, 2-diphenyl-1-picrylhydrazyl DPPH radical at 100, 200, 300, 400 and 500 µg/ml concentrations. The platinum complex have shown a very good antioxidant property against DPPH with an IC50 of 76.03 µg/ml compared with standard ascorbic acid (IC50 of 74.66 µg/ml) and as such have been identified as a potential anticancer candidate.

Keywords: acylpyrazolone, free radical scavenging activities, tridentate ligand, x-ray crystallography

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Authors: Nataša Todorović, Jovana Nikolov, Ivana Stojković, Milan Vraneš, Jovana Panić, Slobodan Gadžurić

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The detection of ²¹⁰Pb levels in aquatic environments evokes interest in various scientific studies. Its precise determination is important not only for the radiological assessment of drinking waters but also ²¹⁰Pb, and ²¹⁰Po distribution in the marine environment are significant for the assessment of the removal rates of particles from the ocean and particle fluxes during transport along the coast, as well as particulate organic carbon export in the upper ocean. Measurement techniques for ²¹⁰Pb determination, gamma spectrometry, alpha spectrometry, or liquid scintillation counting (LSC) are either time-consuming or demand expensive equipment or complicated chemical pre-treatments. However, one other possibility is to measure ²¹⁰Pb on an LS counter if it is in equilibrium with its progeny ²¹⁰Bi - through the Cherenkov counting method. It is unaffected by the chemical quenching and assumes easy sample preparation but has the drawback of lower counting efficiencies than standard LSC methods, typically from 10% up to 20%. The aim of the presented research in this paper is to investigate the possible increment of detection efficiency of Cherenkov counting during ²¹⁰Pb/²¹⁰Bi detection on an LS counter Quantulus 1220. Considering naturally low levels of ²¹⁰Pb in aqueous samples, the addition of ionic liquids to the counting vials with the analysed samples has the benefit of detection limit’s decrement during ²¹⁰Pb quantification. Our results demonstrated that ionic liquid, 1-butyl-3-methylimidazolium salicylate, is more efficient in Cherenkov counting efficiency increment than the previously explored 2-hydroxypropan-1-amminium salicylate. Consequently, the impact of a few other ionic liquids that were synthesized with the same cation group (1-butyl-3-methylimidazolium benzoate, 1-butyl-3-methylimidazolium 3-hydroxybenzoate, and 1-butyl-3-methylimidazolium 4-hydroxybenzoate) was explored in order to test their potential influence on Cherenkov counting efficiency. It was confirmed that, among the explored ones, only ionic liquids in the form of salicylates exhibit a wavelength shifting effect. Namely, the addition of small amounts (around 0.8 g) of 1-butyl-3-methylimidazolium salicylate increases the detection efficiency from 16% to >70%, consequently reducing the detection threshold by more than four times. Moreover, the addition of ionic liquids could find application in the quantification of other radionuclides besides ²¹⁰Pb/²¹⁰Bi via Cherenkov counting method.

Keywords: liquid scintillation counting, ionic liquids, Cherenkov counting, ²¹⁰PB/²¹⁰BI in water

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Authors: M. N. Ofokansi, Onyemelukwe Chisom, Amauche Chukwuemeka, Ezema Onyinye

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The leaves of Clerodendrumcapitatum(Lamiaceae) is mostly used in the treatment of gastric ulcer in Nigerian folk medicine. The aim of this study was to evaluate the antiulcer activity of its crude methanol leaf extract and its ethyl acetate fraction in white albino rats. The effect of crude methanol leaf extract and its ethyl acetate fraction(250mg/kg, 500mg/kg) was evaluated using an absolute ethanol induced ulcer model. Crude methanol leaf extract and the ethyl acetate fraction was treated with distilled water and 6% Tween 80, respectively. crude methanol leaf extract was further investigated using a pylorus ligation induced ulcer model. Omeprazole was used as the standard treatment. Four groups of five albino rats of either sex were used. Parameters such as mean ulcer index and percentage ulcer protection were assessed in the ethanol-induced ulcer model, while the gastric volume, pH, and total acidity were assessed in the pyloric ligation induced ulcer model. Crude methanol leaf extract of Clerodendrumcapitatum(500mg/kg) showed a very highly significant reduction in mean ulcer index(p<0.001) in the absolute ethanol-induced model. ethyl acetate fraction of crude methanol leaf extract of Clerodendrumcapitatum(250mg/kg,500mg/kg) showed a very highly significant dose-dependent reduction in mean ulcer indices (p<0.001) in the absolute ethanol-induced model. The mean ulcer indices (1.6,2.2) with dose concentration (250mg/kg, 500mg/kg) of ethyl acetate fraction increased with ulcer protection (82.85%,76.42%) respectively when compared to the control group in the absolute ethanol-induced ulcer model. Crude methanol leaf extract of Clerodendrumcapitatum(250mg/kg, 500mg/kg) treated animals showed a highly significant dose-dependent reduction in mean ulcer index(p<0.01) with an increase in ulcer protection (56.77%,63.22%) respectively in pyloric ligated induced, ulcer model. Gastric parameters such as volume of gastric juice, pH, and total acidity were of no significance in the different doses of the crude methanol leaf extract when compared to the control group. The phytochemical investigation showed that the crude methanol leaf extracts Possess Saponins and Flavonoids while its ethyl acetate fraction possess only Flavonoids. The results of the study indicate that the crude methanol leaf extract and its ethyl acetate fraction is effective and has gastro protective and ulcer healing capacity. Ethyl acetate fraction is more potent than crude methanol leaf extract against ethanol-induced This result provides scientific evidence as a validation for its folkloric use in the treatment of gastric ulcer.

Keywords: gastroprotective, herbal medicine, anti-ulcer, pharmacology

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Authors: Reena Aggarwal

Abstract:

The use of textile chemicals in the various pre and post-textile manufacturing processes has made the textile industry conscious of its negative contribution to environmental pollution. Popular environmentally friendly fibers such as recycled polyester and organic cotton have been now increasingly used by fabrics and apparel manufacturers. However, after these textiles or the finished apparel are manufactured, they have to be dyed in the same chemical dyes that are harmful and toxic to the environment. Dyeing is a major area of concern for the environment as well as for people who have chemical sensitivities as it may cause nausea, breathing difficulties, seizures, etc. Ayurvastra or herbal medical textiles are one step ahead of the organic lifestyle, which supports the core concept of holistic well-being and also eliminates the impact of harmful chemicals and pesticides. There is a wide range of herbs that can be used not only for dyeing but also for providing medicinal properties to the textiles like antibacterial, antifungal, antiseptic, antidepressant and for treating insomnia, skin diseases, etc. The concept of herbal dyeing of fabric is to manifest herbal essence in every aspect of clothing, i.e., from production to end-use, additionally to eliminate the impact of harmful chemical dyes and chemicals which are known to result in problems like skin rashes, headache, trouble concentrating, nausea, diarrhea, fatigue, muscle and joint pain, dizziness, difficulty breathing, irregular heartbeat and seizures. Herbal dyeing or finishing on textiles will give an extra edge to the textiles as it adds an extra function to the fabric. The herbal extracts can be applied to the textiles by a simple process like the pad dry cure method and mainly acts on the human body through the skin for aiding in the treatment of disease or managing the medical condition through its herbal properties. This paper, therefore, delves into producing Ayurvastra, which is a perfect amalgamation of cloth and wellness. The aim of the paper is to design and create herbal disposable and non-disposable medical textile products acting mainly topically (through the skin) for providing medicinal properties/managing medical conditions. Keeping that in mind, a range of antifungal socks and antibacterial napkins treated with turmeric and aloe vera were developed, which are recommended for the treatment of fungal and bacterial infections, respectively. Both Herbal Antifungal socks and Antibacterial napkins have proved to be efficient enough in managing and treating fungal and bacterial infections of the skin, respectively.

Keywords: ayurvastra, ayurveda, herbal, pandemic, sustainable

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Authors: Marius Sebastian Secula, Mihaela Darie, Gabriela Carja

Abstract:

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAIDs) and is among the most frequently detected pharmaceuticals in environmental samples and among the most widespread drug in the world. Its concentration in the environment is reported to be between 10 and 160 ng L-1. In order to improve the abatement efficiency of this compound for water source prevention and reclamation, the development of innovative technologies is mandatory. AOPs (advanced oxidation processes) are known as highly efficient towards the oxidation of organic pollutants. Among the promising combined treatments, photo-Fenton processes using layered double hydroxides (LDHs) attracted significant consideration especially due to their composition flexibility, high surface area and tailored redox features. This work presents the self-supported Fe, Mn or Ti on ZnFeAl LDHs obtained by co-precipitation followed by reconstruction method as novel efficient photo-catalysts for Fenton-like catalysis. Fe, Mn or Ti/ZnFeAl LDHs nano-hybrids were tested for the degradation of a model pharmaceutical agent, the anti-inflammatory agent ibuprofen, by photocatalysis and photo-Fenton catalysis, respectively, by means of a lab-scale system consisting of a batch reactor equipped with an UV lamp (17 W). The present study presents comparatively the degradation of Ibuprofen in aqueous solution UV light irradiation using four different types of LDHs. The newly prepared Ti/ZnFeAl 4:1 catalyst results in the best degradation performance. After 60 minutes of light irradiation, the Ibuprofen removal efficiency reaches 95%. The slowest degradation of Ibuprofen solution occurs in case of Fe/ZnFeAl 4:1 LDH, (67% removal efficiency after 60 minutes of process). Evolution of Ibuprofen degradation during the photo Fenton process is also studied using Ti/ZnFeAl 2:1 and 4:1 LDHs in the presence and absence of H2O2. It is found that after 60 min the use of Ti/ZnFeAl 4:1 LDH in presence of 100 mg/L H2O2 leads to the fastest degradation of Ibuprofen molecule. After 120 min, both catalysts Ti/ZnFeAl 4:1 and 2:1 result in the same value of removal efficiency (98%). In the absence of H2O2, Ibuprofen degradation reaches only 73% removal efficiency after 120 min of degradation process. Acknowledgements: This work was supported by a grant of the Romanian National Authority for Scientific Research and Innovation, CNCS - UEFISCDI, project number PN-II-RU-TE-2014-4-0405.

Keywords: layered double hydroxide, advanced oxidation process, micropollutant, heterogeneous Fenton

Procedia PDF Downloads 227