Search results for: marine sponge cytotoxicity
658 High Impact Ecostratigraphic and Biostratigrapgic Study of Amama-1 and Bara-1 Wells in Parts of Anambra Basin
Authors: J. O. Njoku, G. C. Soronnadi-ononiwu, E. J. Acrra, C. C. Agoha, T. C. Anyawu
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The High Impact Ecostratigraphic And Biostratigrapgic Study of parts of Anambra basin was carried out using samples from two exploration wells (Amama-1 and Bara-1), Amama-1 (219M–1829M) and Bara-1 (317M-1594M). Palynological and Paleontological analyses were carried out on 100 ditch cutting samples. The faunal and floral succession were of terrestrial and marine origin as described and logged. The well penetrated four stratigraphic units in Anambra Basin (the Nkporo, Mamu, Ajali and Nsukka) the wells yielded well preserved formanifera and palynormorphs. The well yielded 53 species of foram and 69 species of palynomorphs, with 12 genera Bara-1 (25 Species of foram and 101 species of palynormorphs). Amama-1permitted the recognition of 21 genera with 31 formainiferal assemblage zones, 32 pollen and 37 spores assemblage zones, and dinoflagellate cyst, biozonation, ranging from late Campanian – early Paleocene. Bara-1 yielded (60 pollen, 41 spore assemblage zone and 18 dinoflagellate cyst).The zones, in stratigraphically ascending order for the foraminifera and palynomorphs are as follows. Amama Biozone A-Globotruncanella havanensis zone: Late Campanian –Maastrichtian (695 – 1829m) Biozone B-Morozovella velascoensis zone: Early Paleocene(165–695m) Bara-1 Biozone A-Globotruncanella havanensis zone: Late Campanian(1512m) Biozone B-Bolivina afra, B. explicate zone: Maastrichtian (634–1204m) Biozone C - Indeterminate (305 – 634m) palynomorphs Amama-1 A.Ctenolophonidites costatus zone:Early Maastrichtian (1829m) B-Retidiporites miniporatus Zone: Late Maastrichtian (1274m) Constructipollenites ineffectus Zone: Early Paleocene(695m) Bara-1 Droseridites senonicus Zone: Late Campanian (994– 1600m) B. Ctenolophonidites costatus Zone: Early Maastrichtian (713–994m) C. Retidiporites miniporatus Zone: Late Maastrichtian (305 –713m) The paleo – environment of deposition were determined to range from non-marine to outer netritic. A detailed categorization of the palynormorphs into terrestrially derived palynormorphs and marine derived palynormorphs based on the distribution of three broad vegetational types; mangrove, fresh water swamps and hintherland communities were used to evaluate sea level fluctuations with respect to sediments deposited in the basins and linked with a particular depositional system tract. Amama-1 recorded 4 maximum flooding surface(MFS) at depth 165-1829, dated b/w 61ma-76ma and three sequence boundary(SB) at depth1048m - 1533m and 1581 dated b/w 634m - 1387m, dated 69.5ma - 82ma and four sequence boundary(SB) at 552m-876m, dated 68ma-77.5ma respectively. The application of ecostratigraphic description is characterised by the prominent expansion of the hinterland component consisting of the Mangrove to Lowland Rainforest and Afromontane – Savannah vegetation.Keywords: formanifera, palynomorphs. Campanian, Maastritchian, Ecostratigraphic, Anambra
Procedia PDF Downloads 18657 pH and Thermo-Sensitive Nanogels for Anti-Cancer Therapy
Authors: V. Naga Sravan Kumar Varma, H. G. Shivakumar
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The aim of the study was to develop dual sensitive poly (N-isopropylacrylamide-co-acrylic acid) (PNA) nanogels(NGs) and studying its applications for Anti-Cancer therapy. NGs were fabricated by free radical polymerization using different amount of N-isopropylacrylamide and acrylic acid. A study for polymer composition over the effect on LCST in different pH was evaluated by measuring the absorbance at 500nm using UV spectrophotometer. Further selected NG’s were evaluated for change in hydrodynamic diameters in response to pH and temperature. NGs which could sharply respond to low pH value of cancer cells at body temperature were loaded with Fluorouracil (5-FU) using equilibrium swelling method and studied for drug release behaviour in different pH. A significant influence of NGs polymer composition over pH dependent LCST was observed. NGs which were spherical with an average particle size of 268nm at room temperature, shrinked forming an irregular shape when heated above to their respective LCST. 5FU loaded NGs did not intervene any difference in pH depended LCST behaviour of NGs. The in vitro drug release of NGs exhibited a pH and thermo-dependent control release. The cytoxicity study of blank carrier to MCF7 cell line showed no cytotoxicity. The results indicated that PNA NGs could be used as a potential drug carrier for anti-cancer therapy.Keywords: pH and thermo-sensitive, nanogels, P(NIPAM-co-AAc), anti-cancer, 5-FU
Procedia PDF Downloads 350656 Refinement of Existing Benzthiazole lead Targeting Lysine Aminotransferase in Dormant Stage of Mycobacterium tuberculosis
Authors: R. Reshma srilakshmi, S. Shalini, P. Yogeeswari, D. Sriram
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Lysine aminotransferase is a crucial enzyme for dormancy in M. tuberculosis. It is involved in persistence and antibiotic resistance. In present work, we attempted to develop benzthiazole derivatives as lysine aminotransferase inhibitors. In our attempts, we also unexpectedly arrived at an interesting compound 21 (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid which even though has moderate activity against persistent phase of mycobacterium, it has significant potency against active phase. In the entire series compound 22 (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)isophthalic acid emerged as potent molecule with LAT IC50 of 2.62 µM. It has a significant log reduction of 2.9 and 2.3 fold against nutrient starved and biofilm forming mycobacteria. It was found to be inactive in MABA assay and M.marinum induced zebra fish model. It is also devoid of cytotoxicity. Compound 22 was also found to possess bactericidal effect which is independent of concentration and time. It was found to be effective in combination with Rifampicin in 3D granuloma model. The results are very encouraging as the hit molecule shows activity against active as well as persistent forms of tuberculosis. The identified hit needs further more pharmacokinetic and dynamic screening for development as new drug candidate.Keywords: benzothiazole, latent tuberculosis, LAT, nutrient starvation
Procedia PDF Downloads 330655 Effect of Chemical Modification of Functional Groups on Copper(II) Biosorption by Brown Marine Macroalgae Ascophyllum nodosum
Authors: Luciana P. Mazur, Tatiana A. Pozdniakova, Rui A. R. Boaventura, Vitor J. P. Vilar
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The principal mechanism of metal ions sequestration by brown algae involves the formation of complexes between the metal ion and functional groups present on the cell wall of the biological material. To understand the role of functional groups on copper(II) uptake by Ascophyllum nodosum, some functional groups were chemically modified. The esterification of carboxylic groups was carried out by suspending the biomass in a methanol/HCl solution under stirring for 48 h and the blocking of the sulfonic groups was performed by repeating the same procedure for 4 cycles of 48 h. The methylation of amines was conducted by suspending the biomass in a formaldehyde/formic acid solution under shaking for 6 h and the chemical modification of sulfhydryl groups on the biomass surface was achieved using dithiodipyridine for 1 h. Equilibrium sorption studies for Cu2+ using the raw and esterified algae were performed at pH 2.0 and 4.0. The experiments were performed using an initial copper concentration of 300 mg/L and algae dose of 1.0 g/L. After reaching the equilibrium, the metal in solution was quantified by atomic absorption spectrometry. The biological material was analyzed by Fourier Transform Infrared Spectroscopy and Potentiometric Titration techniques for functional groups identification and quantification, respectively. The results using unmodified algae showed that the maximum copper uptake capacity at pH 4.0 and 2.0 was 1.17 and 0.52 mmol/g, respectively. At acidic pH values most carboxyl groups are protonated and copper sorption suffered a significant reduction of 56%. Blocking the carboxylic, sulfonic, amines and sulfhydryl functional groups, copper uptake decreased by 24/26%, 69/81%, 1/23% and 40/27% at pH 2.0/4.0, respectively, when compared to the unmodified biomass. It was possible to conclude that the carboxylic and sulfonic groups are the main functional groups responsible for copper binding (>80%). This result is supported by the fact that the adsorption capacity is directly related to the presence of carboxylic groups of the alginate polymer, and the second most abundant acidic functional group in brown algae is the sulfonic acid of fucoidan that contributes, to a lower extent, to heavy metal binding, particularly at low pH.Keywords: biosorption, brown marine macroalgae, copper, ion-exchange
Procedia PDF Downloads 326654 Examining Litter Distributions in Lethbridge, Alberta, Canada, Using Citizen Science and GIS Methods: OpenLitterMap App and Story Maps
Authors: Tali Neta
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Humans’ impact on the environment has been incredibly brutal, with enormous plastic- and other pollutants (e.g., cigarette buds, paper cups, tires) worldwide. On land, litter costs taxpayers a fortune. Most of the litter pollution comes from the land, yet it is one of the greatest hazards to marine environments. Due to spatial and temporal limitations, previous litter data covered very small areas. Currently, smartphones can be used to obtain information on various pollutants (through citizen science), and they can greatly assist in acknowledging and mitigating the environmental impact of litter. Litter app data, such as the Litterati, are available for study through a global map only; these data are not available for download, and it is not clear whether irrelevant hashtags have been eliminated. Instagram and Twitter open-source geospatial data are available for download; however, these are considered inaccurate, computationally challenging, and impossible to quantify. Therefore, the resulting data are of poor quality. Other downloadable geospatial data (e.g., Marine Debris Tracker8 and Clean Swell10) are focused on marine- rather than terrestrial litter. Therefore, accurate terrestrial geospatial documentation of litter distribution is needed to improve environmental awareness. The current research employed citizen science to examine litter distribution in Lethbridge, Alberta, Canada, using the OpenLitterMap (OLM) app. The OLM app is an application used to track litter worldwide, and it can mark litter locations through photo georeferencing, which can be presented through GIS-designed maps. The OLM app provides open-source data that can be downloaded. It also offers information on various litter types and “hot-spots” areas where litter accumulates. In this study, Lethbridge College students collected litter data with the OLM app. The students produced GIS Story Maps (interactive web GIS illustrations) and presented these to school children to improve awareness of litter's impact on environmental health. Preliminary results indicate that towards the Lethbridge Coulees’ (valleys) East edges, the amount of litter significantly increased due to shrubs’ presence, that acted as litter catches. As wind generally travels from west to east in Lethbridge, litter in West-Lethbridge often finds its way down in the east part of the coulees. The students’ documented various litter types, while the majority (75%) included plastic and paper food packaging. The students also found metal wires, broken glass, plastic bottles, golf balls, and tires. Presentations of the Story Maps to school children had a significant impact, as the children voluntarily collected litter during school recess, and they were looking into solutions to reduce litter. Further litter distribution documentation through Citizen Science is needed to improve public awareness. Additionally, future research will be focused on Drone imagery of highly concentrated litter areas. Finally, a time series analysis of litter distribution will help us determine whether public education through Citizen Science and Story Maps can assist in reducing litter and reaching a cleaner and healthier environment.Keywords: citizen science, litter pollution, Open Litter Map, GIS Story Map
Procedia PDF Downloads 79653 Nanobiomaterials: Revolutionizing Drug Delivery and Tissue Engineering for Advanced Therapeutic Applications
Authors: Mohammad Hamed Asosheh
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The development of nanobiomaterials has opened new avenues in the field of biomedical engineering, offering unparalleled possibilities for advanced therapeutic applications. This study explores the synthesis and characterization of a distinct class of nanobiomaterials designed to enhance drug delivery systems and support tissue engineering. By integrating biodegradable polymers with bioactive nanoparticles, we have engineered a multifunctional platform that ensures controlled drug release, targeted delivery, and improved biocompatibility. Our findings demonstrate that these nanobiomaterials not only exhibit excellent mechanical properties but also promote cell proliferation and differentiation, making them ideal candidates for regenerative medicine. Furthermore, in vitro and in vivo assessments reveal that the engineered materials significantly reduce cytotoxicity while enhancing the therapeutic efficacy of encapsulated drugs. This research presents a promising approach to addressing current challenges in drug delivery and tissue regeneration, with the potential to revolutionize the treatment of chronic diseases and injury repair. Future work will focus on optimizing the material composition for specific clinical applications and conducting large-scale studies to evaluate long-term safety and effectiveness.Keywords: nanobiomaterials, drug delivery systems, therapeutic efficacy, bioactive nanoparticles
Procedia PDF Downloads 28652 Isolation and Characterization of Anti-melanoma (Skin Cancer) Compounds from Corchorus olitorius .L
Authors: Peramachi Sathiyamoorthy, Jacop Gopas, Avi Golan Goldhirsh
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Corchorus olitorius is a leafy vegetable and an industrial crop. The herb has antioxidant, anti inflammatory, and anti-cancer properties. To assay the pharmaceutical properties, aqueous extracts of leaves and seeds from C. olitorius were tested against drug resistant melanoma cell line. The test showed LC50 of the extract was 0.08µg/ml. Aqueous seed extract exhibited higher melanoma inhibiting activity than leaf extract. Dialysis of seed extract showed that the active compound is less than 12 KDa. The compound with <3 KDa MW separated by microconcentration of seed extract showed 70.5 % inhibition of melanoma cell growth. Among the two fractions obtained by Gel filtration with G10 column, the first fraction at 1:2000 dilutions exhibited 100% inhibition of melanoma growth. The compound with Rf value 0.86 (MA4) isolated by TLC separation showed about 98% cytotoxicity against melanoma at 1: 1000 dilutions. Furthermore, HPLC separation of MA4 compound with Superdex 75 column resulted in 4 compounds. Out of 4, one compound showed melanoma inhibition. The active compound is identified by reagent methods as Strophanthidin. Further toxicological and clinical studies will lead to the development of a potential drug to treat drug resistant melanoma.Keywords: corchorus olitorius, melanoma, drug development, strophanthidin
Procedia PDF Downloads 129651 Pisolite Type Azurite/Malachite Ore in Sandstones at the Base of the Miocene in Northern Sardinia: The Authigenic Hypothesis
Authors: S. Fadda, M. Fiori, C. Matzuzzi
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Mineralized formations in the bottom sediments of a Miocene transgression have been discovered in Sardinia. The mineral assemblage consists of copper sulphides and oxidates suggesting fluctuations of redox conditions in neutral to high-pH restricted shallow-water coastal basins. Azurite/malachite has been observed as authigenic and occurs as loose spheroidal crystalline particles associated with the transitional-littoral horizon forming the bottom of the marine transgression. Many field observations are consistent with a supergenic circulation of metals involving terrestrial groundwater-seawater mixing. Both clastic materials and metals come from Tertiary volcanic edifices while the main precipitating anions, carbonates, and sulphides species are of both continental and marine origin. Formation of Cu carbonates as a supergene secondary 'oxide' assemblage, does not agree with field evidences, petrographic observations along with textural evidences in the host-rock types. Samples were collected along the sedimentary sequence for different analyses: the majority of elements were determined by X-ray fluorescence and plasma-atomic emission spectroscopy. Mineral identification was obtained by X-ray diffractometry and scanning electron microprobe. Thin sections of the samples were examined in microscopy while porosity measurements were made using a mercury intrusion porosimeter. Cu-carbonates deposited at a temperature below 100 C° which is consistent with the clay minerals in the matrix of the host rock dominated by illite and montmorillonite. Azurite nodules grew during the early diagenetic stage through reaction of cupriferous solutions with CO₂ imported from the overlying groundwater and circulating through the sandstones during shallow burial. Decomposition of organic matter in the bottom anoxic waters released additional carbon dioxide to pore fluids for azurite stability. In this manner localized reducing environments were also generated in which Cu was fixed as Cu-sulphide and sulphosalts. Microscopic examinations of textural features of azurite nodules give evidence of primary malachite/azurite deposition rather than supergene oxidation in place of primary sulfides. Photomicrographs show nuclei of azurite and malachite surrounded by newly formed microcrystalline carbonates which constitute the matrix. The typical pleochroism of crystals can be observed also when this mineral fills microscopic fissures or cracks. Sedimentological evidence of transgression and regression indicates that the pore water would have been a variable mixture of marine water and groundwaters with a possible meteoric component in an alternatively exposed and subaqueous environment owing to water-level fluctuation. Salinity data of the pore fluids, assessed at random intervals along the mineralised strata confirmed the values between about 7000 and 30,000 ppm measured in coeval sediments at the base of Miocene falling in the range of a more or less diluted sea water. This suggests a variation in mean pore-fluids pH between 5.5 and 8.5, compatible with the oxidized and reduced mineral paragenesis described in this work. The results of stable isotopes studies reflect the marine transgressive-regressive cyclicity of events and are compatibile with carbon derivation from sea water. During the last oxidative stage of diagenesis, under surface conditions of higher activity of H₂O and O₂, CO₂ partial pressure decreased, and malachite becomes the stable Cu mineral. The potential for these small but high grade deposits does exist.Keywords: sedimentary, Cu-carbonates, authigenic, tertiary, Sardinia
Procedia PDF Downloads 131650 Using MALDI-TOF MS to Detect Environmental Microplastics (Polyethylene, Polyethylene Terephthalate, and Polystyrene) within a Simulated Tissue Sample
Authors: Kara J. Coffman-Rea, Karen E. Samonds
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Microplastic pollution is an urgent global threat to our planet and human health. Microplastic particles have been detected within our food, water, and atmosphere, and found within the human stool, placenta, and lung tissue. However, most spectrometric microplastic detection methods require chemical digestion which can alter or destroy microplastic particles and makes it impossible to acquire information about their in-situ distribution. MALDI TOF MS (Matrix-assisted laser desorption ionization-time of flight mass spectrometry) is an analytical method using a soft ionization technique that can be used for polymer analysis. This method provides a valuable opportunity to both acquire information regarding the in-situ distribution of microplastics and also minimizes the destructive element of chemical digestion. In addition, MALDI TOF MS allows for expanded analysis of the microplastics including detection of specific additives that may be present within them. MALDI TOF MS is particularly sensitive to sample preparation and has not yet been used to analyze environmental microplastics within their specific location (e.g., biological tissues, sediment, water). In this study, microplastics were created using polyethylene gloves, polystyrene micro-foam, and polyethylene terephthalate cable sleeving. Plastics were frozen using liquid nitrogen and ground to obtain small fragments. An artificial tissue was created using a cellulose sponge as scaffolding coated with a MaxGel Extracellular Matrix to simulate human lung tissue. Optimal preparation techniques (e.g., matrix, cationization reagent, solvent, mixing ratio, laser intensity) were first established for each specific polymer type. The artificial tissue sample was subsequently spiked with microplastics, and specific polymers were detected using MALDI-TOF-MS. This study presents a novel method for the detection of environmental polyethylene, polyethylene terephthalate, and polystyrene microplastics within a complex sample. Results of this study provide an effective method that can be used in future microplastics research and can aid in determining the potential threats to environmental and human health that they pose.Keywords: environmental plastic pollution, MALDI-TOF MS, microplastics, polymer identification
Procedia PDF Downloads 256649 Inflammatory Alleviation on Microglia Cells by an Apoptotic Mimicry
Authors: Yi-Feng Kao, Huey-Jine Chai, Chin-I Chang, Yi-Chen Chen, June-Ru Chen
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Microglia is a macrophage that resides in brain, and overactive microglia may result in brain neuron damage or inflammation. In this study, the phospholipids was extracted from squid skin and manufactured into a liposome (SQ liposome) to mimic apoptotic body. We then evaluated anti-inflammatory effects of SQ liposome on mouse microglial cell line (BV-2) by lipopolysaccharide (LPS) induction. First, the major phospholipid constituents in the squid skin extract were including 46.2% of phosphatidylcholine, 18.4% of phosphatidylethanolamine, 7.7% of phosphatidylserine, 3.5% of phosphatidylinositol, 4.9% of Lysophosphatidylcholine and 19.3% of other phospholipids by HPLC-UV analysis. The contents of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in the squid skin extract were 11.8 and 28.7%, respectively. The microscopic images showed that microglia cells can engulf apoptotic cells or SQ-liposome. In cell based studies, there was no cytotoxicity to BV-2 as the concentration of SQ-liposome was less than 2.5 mg/mL. The LPS induced pro-inflammatory cytokines, including tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6), were significant suppressed (P < 0.05) by pretreated 0.03~2.5mg/ml SQ liposome. Oppositely, the anti-inflammatory cytokines transforming growth factor-beta (TGF-β) and interleukin-10 (IL-10) secretion were enhanced (P < 0.05). The results suggested that SQ-liposome possess anti-inflammatory properties on BV-2 and may be a good strategy for against neuro-inflammatory disease.Keywords: apoptotic mimicry, neuroinflammation, microglia, squid processing by-products
Procedia PDF Downloads 482648 Cyclic NGR Peptide Anchored Block Co-Polymeric Nanoparticles as Dual Targeting Drug Delivery System for Solid Tumor Therapy
Authors: Madhu Gupta, G. P. Agrawa, Suresh P. Vyas
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Certain tumor cells overexpress a membrane-spanning molecule aminopeptidase N (CD13) isoform, which is the receptor for peptides containing the NGR motif. NGR-modified Docetaxel (DTX)-loaded PEG-b-PLGA polymeric nanoparticles (cNGR-DNB-NPs) were developed and evaluated for their in vitro potential in HT-1080 cell line. The cNGR-DNB-NPs containing particles were about 148 nm in diameter with spherical shape and high encapsulation efficiency. Cellular uptake was confirmed both qualitatively and quantitatively by Confocal Laser Scanning Microscopy (CLSM) and flow cytometry. Both quantitatively and qualitatively results confirmed the NGR conjugated nanoparticles revealed the higher uptake of nanoparticles by CD13-overexpressed tumor cells. Free NGR inhibited the cellular uptake of cNGR-DNB-NPs, revealing the mechanism of receptor mediated endocytosis. In vitro cytotoxicity studies demonstrated that cNGR-DNB-NPs, formulation was more cytotoxic than unconjugated one, which were consistent well with the observation of cellular uptake. Hence, the selective delivery of cNGR-DNB-NPs formulation in CD13-overexpressing tumors represents a potential approach for the design of nanocarrier-based dual targeted delivery systems for targeting the tumor cells and vasculature.Keywords: solid Tumor, docetaxel, targeting, NGR ligand
Procedia PDF Downloads 482647 Development of Nanostructrued Hydrogel for Spatial and Temporal Controlled Release of Active Compounds
Authors: Shaker Alsharif, Xavier Banquy
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Controlled drug delivery technology represents one of the most rapidly advancing areas of science in which chemists and chemical engineers are contributing to human health care. Such delivery systems provide numerous advantages compared to conventional dosage forms including improved efficacy, and improved patient compliance and convenience. Such systems often use synthetic polymers as carriers for the drugs. As a result, treatments that would not otherwise be possible are now in conventional use. The role of bilayered vesicles as efficient carriers for drugs, vaccines, diagnostic agents and other bioactive agents have led to a rapid advancement in the liposomal drug delivery system. Moreover, the site avoidance and site-specific drug targeting therapy could be achieved by formulating a liposomal product, so as to reduce the cytotoxicity of many potent therapeutic agents. Our project focuses on developing and building hydrogel with nanoinclusion of liposomes loaded with active compounds such as proteins and growth factors able to release them in a controlled fashion. In order to achieve that, we synthesize several liposomes of two different phospholipids concentrations encapsulating model drug. Then, formulating hydrogel with specific mechanical properties embedding the liposomes to manage the release of active compound.Keywords: controlled release, hydrogel, liposomes, active compounds
Procedia PDF Downloads 447646 An Alternative Nano Design Strategy by Neutralized AMPS and Soy Bean Lecithin to Form Nanoparticles
Authors: Esra Cansever Mutlu, Muge Sennaroglu Bostan, Fatemeh Bahadori, Ebru Toksoy Oner, Mehmet S. Eroglu
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Paclitaxel is used in treatment of different cancer types mainly breast, ovarian, lung and Kaposi’s sarcoma. It is poorly soluble in water; therefore, currently used formulations tremendously show side-effects and high toxicity. Encapsulation of the drug in a nano drug carrier which causes both reducing side effects and increasing drug activity is a desired new approach for the nano-medicine to target the site of cancer. In this study, synthesis of a novel nano paclitaxel formulation made of a new amphiphilic monomer was followed by the investigation of its pharmacological properties. UV radical polymerization was carried out by using the monomer Lecithin-2-Acrylamido-2-methylpropane (L-AMPS) and the drug-spacer, to obtain sterically high stabilized, biocompatible and biodegradable phospholipid nanoparticles, in which the drug paclitaxel (Pxl) was encapsulated (NanoPxl). Particles showed high drug loading capacity (68%) and also hydrodynamic size less than 200 nm with slight negative surface charge. The drug release profile was obtained and in vitro cytotoxicity test was performed on MCF-7 cell line. Consequently, these data indicated that paclitaxel loaded Lecithin-AMPS/PCL-MAC nanoparticles can be considered as a new, safe and effective nanocarrier for the treatment of breast cancer.Keywords: paclitaxel, nanoparticle, drug delivery, L-AMPS
Procedia PDF Downloads 320645 Biosynthesis of Selenium Oxide Nanoparticles by Streptomyces bikiniensis and Its Cytotoxicity as Antitumor Agents against Hepatocellular and Breast Cells Carcinoma
Authors: Maged Syed Ahamd, Manal Mohamed Yasser, Essam Sholkamy
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In this paper, we reported that selenium (Se) nanoparticles were firstly biosynthesized with a simple and eco-friendly biological method. Their shape, size, FTIR (Fourier Transform Infrared spectroscopy), UV–vis spectra, TEM (Transmission Electron Microscopy) images and EDS (Energy Dispersive Spectroscopy) pattern have been analyzed. TEM analyses of the samples obtained at different stages indicated that the formation of these Se nanostructures was governed by an incubation time (12- 24- 48 hours). The Se nanoparticles were initially generated and then would transform into crystal seeds for the subsequent growth of nanowires; however obtaining stable Se nanowire with a diameter of about 15-100 nm. EDS shows that Se nanoparticles are entirely pure. The IR spectra showed the peaks at 550 cm-1, 1635 cm-1, 1994 cm-1 and 3430 cm-1 correspond to the presence of Se-O bending and stretching vibrations. The concentrations of Se-NPs (0, 1, 2, 5 µg/ml) did not give significantly effect on both two cell lines while the highest concentrations (10- 100 µg/ml gave significantly effects on them. The lethal dose (ID50%) of Se-NPs on Hep2 G and MCF-7 cells was obtained at 75.96 and 61.86 µg/ml, respectively. Results showed that Se nanoparticles as anticancer agent against MCF-7 cells were more effective than Hep2 G cells. Our results suggest that Se-NPs may be a candidate for further evaluation as a chemotherapeutic agent for breast and liver cancers.Keywords: selenium nanoparticle, Streptomyces bikiniensis, nanowires, chemotherapeutic agent
Procedia PDF Downloads 444644 Derivation of Bathymetry from High-Resolution Satellite Images: Comparison of Empirical Methods through Geographical Error Analysis
Authors: Anusha P. Wijesundara, Dulap I. Rathnayake, Nihal D. Perera
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Bathymetric information is fundamental importance to coastal and marine planning and management, nautical navigation, and scientific studies of marine environments. Satellite-derived bathymetry data provide detailed information in areas where conventional sounding data is lacking and conventional surveys are inaccessible. The two empirical approaches of log-linear bathymetric inversion model and non-linear bathymetric inversion model are applied for deriving bathymetry from high-resolution multispectral satellite imagery. This study compares these two approaches by means of geographical error analysis for the site Kankesanturai using WorldView-2 satellite imagery. Based on the Levenberg-Marquardt method calibrated the parameters of non-linear inversion model and the multiple-linear regression model was applied to calibrate the log-linear inversion model. In order to calibrate both models, Single Beam Echo Sounding (SBES) data in this study area were used as reference points. Residuals were calculated as the difference between the derived depth values and the validation echo sounder bathymetry data and the geographical distribution of model residuals was mapped. The spatial autocorrelation was calculated by comparing the performance of the bathymetric models and the results showing the geographic errors for both models. A spatial error model was constructed from the initial bathymetry estimates and the estimates of autocorrelation. This spatial error model is used to generate more reliable estimates of bathymetry by quantifying autocorrelation of model error and incorporating this into an improved regression model. Log-linear model (R²=0.846) performs better than the non- linear model (R²=0.692). Finally, the spatial error models improved bathymetric estimates derived from linear and non-linear models up to R²=0.854 and R²=0.704 respectively. The Root Mean Square Error (RMSE) was calculated for all reference points in various depth ranges. The magnitude of the prediction error increases with depth for both the log-linear and the non-linear inversion models. Overall RMSE for log-linear and the non-linear inversion models were ±1.532 m and ±2.089 m, respectively.Keywords: log-linear model, multi spectral, residuals, spatial error model
Procedia PDF Downloads 297643 Maximizing Giant Prawn Resource Utilization in Banjar Regency, Indonesia: A CPUE and MSY Analysis
Authors: Ahmadi, Iriansyah, Raihana Yahman
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The giant freshwater prawn (Macrobrachium rosenbergii de Man, 1879) is a valuable species for fisheries and aquaculture, especially in Southeast Asia, including Indonesia due to their high market demand and potential for export. The growing demand for prawns is straining the sustainability of the Banjar Regency fishery. To ensure the long-term sustainability and economic viability of the prawn fishing in this region, it is imperative to implement evidence-based management practices. This requires comprehensive data on the Catch per Unit Effort (CPUE), Maximum Sustainable Yield (MSY) and the current rate of prawn resource exploitation. it analyzed five years of prawn catch data (2019-2023) obtained from South Kalimantan Marine and Fisheries Services. Fishing gears (e.g. hook & line and cast net) were first standardized with Fishing Power Index, and then calculated effort and MSY. The intercept (a) and the slope (b) values of regression curve were used to estimate the catch-maximum sustainable yield (CMSY) and optimal fishing effort (Fopt) levels within the framework of the Surplus Production Model. The estimated rates of resource utilization were then compared to the criteria of The National Commission of Marine Fish Stock Assessment. The findings showed that the CPUE value peaked in 2019 at 33.48 kg/trip, while the lowest value observed in 2022 at 5.12 kg/trip. The CMSY value was estimated to be 17,396 kg/year, corresponding to the Fopt level of 1,636 trips/year. The highest utilization rate was 56.90% recorded in 2020, while the lowest rate was observed in 2021 at 46.16%. The annual utilization rates were classified as “medium”, suggesting that increasing fishing effort by 45% could potentially maximize prawn catches at an optimum level. These findings provide a baseline for sustainable fisheries management in the region.Keywords: giant prawns, CPUE, fishing power index, sustainable potential, utilization rate
Procedia PDF Downloads 16642 Microfacies Analysis and Paleoenvironmental Trends of the Paleocene Farrud and Mabruk Reservoirs, Concession 11, West Sirte Basin, Libya
Authors: Nisreen Agha
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Investigation of representative core samples under the petrological microscope reveals common petrographic and mineralogical characteristics with distinct faunal assemblages, allowing establishing of the microfacies associations and deducing the paleoenvironmental trends of the Paleocene Farrud and Mabruk rock units. Recognition of the early and post-diagenetic processes, particularly dolomitization and micritization, as well as dissolution and precipitation of spary drusy calcite as a new morphism process affecting the reservoir rocks, is established. The microfacies trends detected from the investigation of 46 core samples from Farrud member (Lower Paleocene) representing six wells; QQQ1-11, GG1-11, LLL1-11, RRR1-11, RRR40-11, and RRR45-11 indicate that the deposition was started within the realm of shallow supratidal and intertidal subenvironments followed by deeper environments of the shelf bays with maximum sea level during inner shelf environment where fossiliferous bioclastic packstone dominated. The microfacies associations determined in 8 core samples from two wells LLL1and RRR40 representing Mabruk Member (Upper Paleocene), indicate paleoenvironmental trends marked by sea level fluctuations accompanied with a relatively marine shelf bay conditions intervened with short-lived shallow intertidal and supratidal warm coastal sedimentation. As a result, dolostone, evaporitic dismicrites, and gypsiferous dolostone of supratidal characters were deposited. They reflect rapid oscillation of the sea level marked by drop land-ward shift of the sea shore deposition prevailed by supratidal gypsiferous dolostone and numerous ferruginous materials as clouds straining many parts of dolomite and surrounded the micritized fossils. This situation ends the deposition of the Farrud Member in most of the studied wells. On the other hand, the facies in the northern part of the Concession -11 field indicates deposition in a deeper marine setting than in the southern facies.Keywords: Farrud and Mabruk members, paleocene, microfacies associations, diagenesis, sea level oscillation, depositional environments
Procedia PDF Downloads 76641 Performance Assessment of Horizontal Axis Tidal Turbine with Variable Length Blades
Authors: Farhana Arzu, Roslan Hashim
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Renewable energy is the only alternative sources of energy to meet the current energy demand, healthy environment and future growth which is considered essential for essential sustainable development. Marine renewable energy is one of the major means to meet this demand. Turbines (both horizontal and vertical) play a vital role for extraction of tidal energy. The influence of swept area on the performance improvement of tidal turbine is a vital factor to study for the reduction of relatively high power generation cost in marine industry. This study concentrates on performance investigation of variable length blade tidal turbine concept that has already been proved as an efficient way to improve energy extraction in the wind industry. The concept of variable blade length utilizes the idea of increasing swept area through the turbine blade extension when the tidal stream velocity falls below the rated condition to maximize energy capture while blade retracts above rated condition. A three bladed horizontal axis variable length blade horizontal axis tidal turbine was modelled by modifying a standard fixed length blade turbine. Classical blade element momentum theory based numerical investigation has been carried out using QBlade software to predict performance. The results obtained from QBlade were compared with the available published results and found very good agreement. Three major performance parameters (i.e., thrust, moment, and power coefficients) and power output for different blade extensions were studied and compared with a standard fixed bladed baseline turbine at certain operational conditions. Substantial improvement in performance coefficient is observed with the increase in swept area of the turbine rotor. Power generation is found to increase in great extent when operating at below rated tidal stream velocity reducing the associated cost per unit electric power generation.Keywords: variable length blade, performance, tidal turbine, power generation
Procedia PDF Downloads 276640 Effluent from Royal LERD Wastewater Treatment Systems to Furnish Nutrients for Phytoplankton to Generate the Abundance of Hard Clam (Meretrix spp.) on Muddy Beach
Authors: O. Phewnil, S. Khowhit, W. Inkapatanakul, A. Boutson, K. Chunkao, O. Chueawong, T. Pattamapitoon, N. Chanwong, C. Nimpee
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The King’s Royally Initiated Laem Phak Bia Environmental Research and Development Project (“the Royal LERD Project”) is located in Laem Phak Bia Sub-District, Ban Laem District, Phetchaburi Province, Thailand. Phetchaburi municipal wastewater was treated with a simple technology by using aquatic plants, constructed wetland, oxidation ponds through a nature-by-nature process. The effluent from the Royal LERD Project was discharged into Laem Phak Bia muddy beach. The soil sediment samples were collected from two zones (200 and 600 meters from the coast of the beach), and tested for cation-exchange capacity (CEC), pH and organic matter and soil particles content. The marine water samples were also collected from the beach in wet and dry seasons and analyzed for its quality and compositions, including but not limited to, biochemical oxygen demand (BOD), dissolved oxygen (DO), suspended solids (SS), nutrients, heavy metals (As, Cd, Cr, Hg, and Pb), and phytoplankton at high and low tides. The soil texture was sandy loam with high concentration of calcium and magnesium which showed a property of base (pH 8). The marine water was qualified with the standard limits of coastal water quality. A dominant species was Coscinodiscus sp. It was found approximately 70.46% of total phytoplankton species in Meretrix casta gastrointestinal tract. The concentration of the heavy metals (As, Cd, Cr, Hg, Ni and Pb) in the tissues and water content of two species of hard clams indicated that heavy metals in Meretrix casta were higher than those in Meretrix meretrix. However, the heavy metals in both species were under the standard limits and safe for consumption. It can be concluded that nutrients in effluent from the wastewater treatment systems play important role in promoting the growth of phytoplankton and generating abundance of hard clams on muddy beach.Keywords: wastewater, phytoplankton, hard clam (Meretrix spp.), muddy beach
Procedia PDF Downloads 307639 Adaptive CFAR Analysis for Non-Gaussian Distribution
Authors: Bouchemha Amel, Chachoui Takieddine, H. Maalem
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Automatic detection of targets in a modern communication system RADAR is based primarily on the concept of adaptive CFAR detector. To have an effective detection, we must minimize the influence of disturbances due to the clutter. The detection algorithm adapts the CFAR detection threshold which is proportional to the average power of the clutter, maintaining a constant probability of false alarm. In this article, we analyze the performance of two variants of adaptive algorithms CA-CFAR and OS-CFAR and we compare the thresholds of these detectors in the marine environment (no-Gaussian) with a Weibull distribution.Keywords: CFAR, threshold, clutter, distribution, Weibull, detection
Procedia PDF Downloads 588638 Using GIS for Assessment and Modelling of Oil Spill Risk at Vulnerable Coastal Resources: Of Misratah Coast, Libya
Authors: Abduladim Maitieg
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The oil manufacture is one of the main productive activities in Libya and has a massive infrastructure, including offshore drilling and exploration and wide oil export platform sites that located in coastal area. There is a threat to marine and coastal area of oil spills is greatest in those sites with a high spills comes from urban and industry, parallel to that, monitoring oil spills and risk emergency strategy is weakness, An approach for estimating a coastal resources vulnerability to oil spills is presented based on abundance, environmental and Scio-economic importance, distance to oil spill resources and oil risk likelihood. As many as 10 coastal resources were selected for oil spill assessment at the coast. This study aims to evaluate, determine and establish vulnerable coastal resource maps and estimating the rate of oil spill comes for different oil spill resources in Misratah marine environment. In the study area there are two type of oil spill resources, major oil resources come from offshore oil industries which are 96 km from the Coast and Loading/Uploading oil platform. However, the miner oil resources come from urban sewage pipes and fish ports. In order to analyse the collected database, the Geographic information system software has been used to identify oil spill location, to map oil tracks in front of study area, and developing seasonal vulnerable costal resources maps. This work shows that there is a differential distribution of the degree of vulnerability to oil spills along the coastline, with values ranging from high vulnerability and low vulnerability, and highlights the link between oil spill movement and coastal resources vulnerability. The results of assessment found most of costal freshwater spring sites are highly vulnerable to oil spill due to their location on the intertidal zone and their close to proximity to oil spills recourses such as Zreag coast. Furthermore, the Saltmarsh coastline is highly vulnerable to oil spill risk due to characterisation as it contains a nesting area of sea turtles and feeding places for migratory birds and the . Oil will reach the coast in winter season according to oil spill movement. Coastal tourist beaches in the north coast are considered as highly vulnerable to oil spill due to location and closeness to oil spill resources.Keywords: coastal recourses vulnerability, oil spill trajectory, gnome software, Misratah coast- Libya, GIS
Procedia PDF Downloads 314637 Construction and Cross-Linking of Polyelectrolyte Multilayers Based on Polysaccharides as Antifouling Coatings
Authors: Wenfa Yu, Thuva Gnanasampanthan, John Finlay, Jessica Clarke, Charlotte Anderson, Tony Clare, Axel Rosenhahn
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Marine biofouling is a worldwide problem at vast economic and ecological costs. Historically it was combated with toxic coatings such as tributyltin. As those coatings being banned nowadays, finding environmental friendly antifouling solution has become an urgent topic. In this study antifouling coatings consisted of natural occurring polysaccharides hyaluronic acid (HA), alginic acid (AA), chitosan (Ch) and polyelectrolyte polyethylenimine (PEI) are constructed into polyelectrolyte multilayers (PEMs) in a Layer-by-Layer (LbL) method. LbL PEM construction is a straightforward way to assemble biomacromolecular coatings on surfaces. Advantages about PEM include ease of handling, highly diverse PEM composition, precise control over the thickness and so on. PEMs have been widely employed in medical application and there are numerous studies regarding their protein adsorption, elasticity and cell adhesive properties. With the adjustment of coating composition, termination layer charge, coating morphology and cross-linking method, it is possible to prepare low marine biofouling coatings with PEMs. In this study, using spin coating technology, PEM construction was achieved at smooth multilayers with roughness as low as 2nm rms and highly reproducible thickness around 50nm. To obtain stability in sea water, the multilayers were covalently cross-linked either thermally or chemically. The cross-linking method affected surface energy, which was reflected in water contact angle, thermal cross-linking led to hydrophobic surfaces and chemical cross-linking generated hydrophilic surfaces. The coatings were then evaluated regarding its protein resistance and biological species resistance. While the hydrophobic thermally cross-linked PEM had low resistance towards proteins, the resistance of chemically cross-linked PEM strongly depended on the PEM termination layer and the charge of the protein, opposite charge caused high adsorption and same charge low adsorption, indicating electrostatic interaction plays a crucial role in the protein adsorption processes. Ulva linza was chosen as the biological species for antifouling performance evaluation. Despite of the poor resistance towards protein adsorption, thermally cross-linked PEM showed good resistance against Ulva spores settlement, the chemically cross-linked multilayers showed poor resistance regardless of the termination layer. Marine species adhesion is a complex process, although it involves proteins as bioadhesives, protein resistance its own is not a fully indicator for its antifouling performance. The species will pre select the surface, responding to cues like surface energy, chemistry, or charge and so on. Thus making it difficult for one single factors to determine its antifouling performance. Preparing PEM coating is a comprehensive work involving choosing polyelectrolyte combination, determining termination layer and the method for cross-linking. These decisions will affect PEM properties such as surface energy, charge, which is crucial, since biofouling is a process responding to surface properties in a highly sensitive and dynamic way.Keywords: hyaluronic acid, polyelectrolyte multilayers, protein resistance, Ulva linza zoospores
Procedia PDF Downloads 164636 Assessment of Cytotoxic and Genotoxic Effect of Tartrazine in Both Male and Female Albino Rats
Authors: Alaa F. A. Bakr, Sherein S. Abdelgayed, Osama. S. EL-Tawil, Adel M. Bakeer
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Objective: This study was carried out to evaluate the cytotoxic and genotoxic effect of tartrazine in both male and female albino rats. Methodology: Forty adult male (20) and female (20) Sprague Dawley albino rats (120 - 150g) were obtained and distributed into four experimental groups; Group I; 10 untreated males, Group II; 10 untreated females, Group III; 10 treated males, and Group IV; 10 treated females. Body weight was recorded weekly, reduced glutathione (RGH), lipid peroxidation (SOD), and superoxide dismutase activity (MDA) in liver tissue were carried out, histopathological studies of brain, liver, and kidneys were performed, COMET assay was performed, all values were statistically analyzed. Results: Decrease in the activity of RGH and SOD in the treated groups were reported, but there was a more significant decrease in the female treated group. MDA was increased in treated groups with tartrazine, moreover, it was more significant in the female treated group. Multiple histological lesions were developed in brain, liver, and kidneys. COMET showed positive results. Conclusion: Our study concluded that Tartrazine has a cytotoxic and genotoxic effect on albino rats and it was more significant in females than males.Keywords: tartrazine, cytotoxicity, genotoxicity, histopathology, albino rats
Procedia PDF Downloads 153635 Trastuzumab Decorated Bioadhesive Nanoparticles for Targeted Breast Cancer Therapy
Authors: Kasi Viswanadh Matte, Abhisheh Kumar Mehata, M.S. Muthu
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Brest cancer, up-regulated with human epidermal growth factor receptor type-2 (HER-2) led to the concept of developing HER-2 targeted anticancer therapeutics. Docetaxel-loaded D-α-tocopherol polyethylene glycol succinate 1000 conjugated chitosan (TPGS-g-chitosan) nanoparticles were prepared with or without Trastuzumab decoration. The particle size and entrapment efficiency of conventional, non-targeted and targeted nanoparticles were found to be in the range of 126-186 nm and 74-78% respectively. In-vitro, MDA-MB-231 cells showed that docetaxel-loaded non-targeted and HER-2 receptor targeted TPGS-g-chitosan nanoparticles have enhanced the cellular uptake and cytotoxicity with a promising bioadhesion property, in comparison to conventional nanoparticles. The IC50 values of non-targeted and targeted nanoparticles from cytotoxic assay were found to be 43 and 223 folds higher than DocelTM. The in-vivo pharmacokinetic study showed 2.33, and 2.82-fold enhancement in relative bioavailability of docetaxel for non-targeted and HER-2 receptor targeted nanoparticles, respectively than DocelTM, and after i.v administration, non-targeted and targeted nanoparticle achieved 3.48 and 5.94 times prolonged half-life in comparison to DocelTM. The area under the curve (AUC), relative bioavailability (FR) and mean residence time (MRT) were found to be higher for non-targeted and targeted nanoparticles compared to DocelTM. Further, histopathology results of non-targeted and targeted nanoparticles showed less toxicity on vital organs such as lungs, liver, and kidney compared to DocelTM.Keywords: breast cancer, HER-2 receptor, targeted nanomedicine, chitosan, TPGS
Procedia PDF Downloads 240634 Titanium Nitride Nanoparticles for Biological Applications
Authors: Nicole Nazario Bayon, Prathima Prabhu Tumkur, Nithin Krisshna Gunasekaran, Krishnan Prabhakaran, Joseph C. Hall, Govindarajan T. Ramesh
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Titanium nitride (TiN) nanoparticles have sparked interest over the past decade due to their characteristics such as thermal stability, extreme hardness, low production cost, and similar optical properties to gold. In this study, TiN nanoparticles were synthesized via a thermal benzene route to obtain a black powder of nanoparticles. The final product was drop cast onto conductive carbon tape and sputter coated with gold/palladium at a thickness of 4 nm for characterization by field emission scanning electron microscopy (FE-SEM) with energy dispersive X-Ray spectroscopy (EDX) that revealed they were spherical. ImageJ software determined the average size of the TiN nanoparticles was 79 nm in diameter. EDX revealed the elements present in the sample and showed no impurities. Further characterization by X-ray diffraction (XRD) revealed characteristic peaks of cubic phase titanium nitride, and crystallite size was calculated to be 14 nm using the Debye-Scherrer method. Dynamic light scattering (DLS) analysis revealed the size and size distribution of the TiN nanoparticles, with average size being 154 nm. Zeta potential concluded the surface of the TiN nanoparticles is negatively charged. Biocompatibility studies using MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) assay showed TiN nanoparticles are not cytotoxic at low concentrations (2, 5, 10, 25, 50, 75 mcg/well), and cell viability began to decrease at a concentration of 100 mcg/well.Keywords: biocompatibility, characterization, cytotoxicity, nanoparticles, synthesis, titanium nitride
Procedia PDF Downloads 178633 Detection of Cytotoxicity of Green Synthesized Silver, Gold, and Silver/Gold Bimetallic on Baby Hamster Kidney-21 Cells Using MTT Assay
Authors: Naila Sher, Mushtaq Ahmed, Nadia Mushtaq, Rahmat Ali Khan
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In cancer therapy, nanoparticles (NPs) shall be applied possibly by inoculation in the veins of humans. This action will connect them with white (WBCs) and red blood cells (RBCs) in the bloodstream before they reach their main targeted cancer cells. However, possible effects of silver, gold, and silver/gold bimetallic NPs (Ag, Au, and Ag/Au BNPs) on baby hamster kidney-21 (BHK-21) cells were studied by MTT assay. Here, Ag, Au, and their Ag/Au BNPs (bimetallic nanoparticles) were synthesized by using Hippeastrum hybridum (HH) extract. These NPs were characterized by UV-visible spectroscopy, FT-IR, XRD, and EDX, and SEM analysis. XRD analysis conferring the crystal structure with an average size of 13.3, 10.72, and 8.34nm of Ag, Au, and Ag/Au BNPs, respectively. SEM showed that Ag, Au, and Ag/Au BNPs had irregular morphologies, with nano measures calculated sizes of 40, 30, and 20 nm respectively. EDX spectrometers confirmed the presence of elemental Ag signal of the AgNPs with 22.75%, Au signal of the AuNPs with 48.08%, Ag signal with 12%, and Au signal with 38.26% of the Ag/Au BNPs. The BHK-21cells were incubated in the existence of doxorubicin, plant extract, Ag, Au, and Ag/Au BNPs. The cytotoxic effects could be observed in a dose-dependent mode; doxorubicin and Ag/Au BNPs were more toxic than plant extract, Ag, and Au NPs. It is demonstrated that NPs interact with BHK-21cells and significantly reduce cell viability in a concentration-dependent manner. However, to reduce the potential threats of NPs further studies are recommended.Keywords: hippeastrum hybridum, nanoparticle, BHK-21cells
Procedia PDF Downloads 133632 A Novel Small-Molecule Inhibitor of Influenza a Virus Acts by Suppressing PA Endonuclease Activity of the Viral Polymerase
Authors: Shuafeng Yuan, Bojian Zheng
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The RNA-dependent RNA polymerase of influenza a virus comprises conserved and independently folded subdomains with defined functionalities. The N-terminal domain of the PA subunit (PAN) harbors the endonuclease function so that it can serve as a desired target for drug discovery. To identify a class of anti-influenza inhibitors that impedes PAN endonuclease activity, a screening approach that integrated the fluorescence resonance energy transfer based endonuclease inhibitor assay with the DNA gel-based endonuclease inhibitor assay was conducted, followed by the evaluation of antiviral efficacies and potential cytotoxicity of the primary hits in vitro and in vivo. A small-molecule compound ANA-0 was identified as a potent inhibitor against the replication of multiple subtypes of influenza A virus, including H1N1, H3N2, H5N1, H7N7, H7N9 and H9N2, in cell cultures. Combinational treatment of zanamivir and ANA-0 exerted synergistic anti-influenza effect in vitro. Intranasal administration of ANA-0 protected mice from lethal challenge and reduced lung viral loads in H1N1 virus infected BALB/c mice. Docking analyses predicted ANA-0 bound the endonuclease cavity of PAN by interacting with the metal-binding and catalytic residues. In summary, ANA-0 shows potential to be developed to novel anti-influenza agents.Keywords: anti-influenza, novel compound, inhibition of endonuclease, PA
Procedia PDF Downloads 245631 Design and Identification of Mycobacterium tuberculosis Glutamate Racemase (MurI) Inhibitors
Authors: Prasanthi Malapati, R. Reshma, Vijay Soni, Perumal Yogeeswari, Dharmarajan Sriram
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In the present study, we attempted to develop Mycobacterium tuberculosis (Mtb) inhibitors by exploring the pharmaceutically underexploited enzyme targets which are majorly involved in cell wall biosynthesis of mycobacteria. For this purpose, glutamate racemase (coded by MurI gene) was selected. This enzyme racemize L-glutamate to D-glutamate required for the construction of peptidoglycan in the bacterial cell wall synthesis process. Furthermore this enzyme is neither expressed nor its product, D-glutamate is normally found in mammals, and hence designing inhibitors against this enzyme will not affect the host system as well act as potential antitubercular drugs. A library of BITS in house compounds were screened against Mtb MurI enzyme. Based on docking score, interactions and synthetic feasibility one hit lead was identified. Further optimization of lead was attempted and its derivatives were synthesized. Forty eight derivatives of 2-phenylbenzo[d]oxazole and 2-phenylbenzo[d]thiazole were synthesized and evaluated for Mtb MurI inhibition study, in vitro activities against Mtb, cytotoxicity against RAW 264.7 cell line. Chemical derivatization of the lead resulted in compounds NR-1213 AND NR-1124 as the potent M. tuberculosis glutamate racemase inhibitors with IC50 of 4-5µM which are remarkable and were found to be non-cytotoxic. Molecular dynamics, dormant models and cardiotoxicity studies of the most active molecules are in process.Keywords: cell wall biosynthesis, dormancy, glutamate racemase, tuberculosis
Procedia PDF Downloads 269630 Punica granatum (Pomegranate) of a Libyan Variety Exhibits in vitro Anti-Inflammatory Potential
Authors: Lamees A. Ben Saad, Kah Hwi Kim, Chin Chew Quah, Mustafa Shahimi
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Background: Punica granatum (pomegranate) was used as a traditional medicine in different parts of the world. It has been used in the treatment of pain and inflammatory conditions such as peptic ulcer. The numerous risks associated with nonsteroidal anti-inflammatory drugs (NSAIDs) for the treatment of pain and inflammation give rise to using medicinal herbs as alternative therapies. This study aimed to evaluate the anti-inflammatory effect of the ethyl acetate pomegranate fraction (EtOAc) by determination of its inhibitory effects on lipopolysaccharide (LPS), stimulated nitric oxide (NO), prostaglandin E2 (PGE-2), interleukin-6 (IL-6) and cyclooxxgenase-2 (COX2) release from RAW264.7cells. Methods: The inhibitory effect of EtOAc was evaluated on (LPS) induced NO production, PGE2, and IL-6 quantified by immunoassay kit and prostaglandin E2 competitive ELISA kit. COX2 production is an in vitro indication of possible anti-inflammatory activity and was estimated by Western blotting. Results: EtOAc potentially inhibited LPS-induced nitric oxide, prostaglandin, and IL-6 production. With these findings, it was evident that the EtOAc could reduce the LPS-induced cyclooxygenase-2 (COX-2) at the protein level in a dose-dependent manner as determined by Western blotting. Conclusion: The results emphasize potential therapeutic applications of Punica granatum in the treatment of inflammation.Keywords: inflammation, Punica granatum, cytotoxicity, cytokines
Procedia PDF Downloads 660629 Chemical Composition of Essential Oil and in vitro Antibacterial and Anticancer Activity of the Hydroalcolic Extract from Coronilla varia
Authors: A. A. Dehpour, B. Eslami, S. Rezaie, S. F. Hashemian, F. Shafie, M. Kiaie
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The aims of study were investigation on chemical composition essential oil and the effect of extract of Coronilla varia on antimicrobial and cytotoxicity activity. The essential oils of Coronilla varia is obtained by hydrodistillation and analyzed by (GC/MS) for determining their chemical composition and identification of their components. Antibacterial activity of plant extract was determined by disc diffusion method. The effect of hydroalcolic extracts from Cornilla varia investigated on MCF7 cancer cell line by MTT assay. The major components were Caryophyllene Oxide (60.19%), Alphacadinol (4.13%) and Homoadantaneca Robexylic Acid (3.31%). The extracts from Coronilla varia had interesting activity against Proteus mirabilis in the concentration of 700 µg/disc and did not show any activity against Staphylococus aureus, Bacillus subtillis, Klebsiella pneumonia and Entrobacter cloacae. The positive control, Ampicillin, Chloramphenicol and Cenphalothin had shown zone of inhibition resistant all bacteria. Corohilla varia ethanol extract could inhibit the proliferation of MCF7 cell line in RPMI 1640 medium. IC50 5(mg/ml) was the optimum concentration of extract from Coronilla varia inhibition of cell line growth. The MCF7 cancer cell line and Proteus mirabilis were more sensitive to Coronilla varia ethanol extract.Keywords: Coronilla varia, essential oil, antibacterial, anticancer, hela cell line
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