Search results for: peptide inhibitor

Authors: Farzaneh Ziaee, Mohammad Ziaee

Abstract:

N-acetyl-L-cysteine (NAC) is a well-known mucolytic agent, and recently its efficacy has been examined for the prevention and remediation of several diseases such as lung infections caused by Coronavirus. Also, it is administrated as the main antidote in paracetamol overdose and is effective for the treatment of idiopathic pulmonary fibrosis (IPF), chronic obstructive pulmonary disease (COPD). This medicine is used as an antioxidant to prevent diabetic kidney disease (nephropathy). In this study, a method for the acylation of amino acids is employed to manufacture this drug in a height yield. Regarding this patented path, NAC can be made in a single batch step at ambient pressure and temperature. Moreover, this study offers a technique to make peptide bonds which is of interest for pharmaceutical and medicinal industries. The separation process was undertaken using appropriate solvents to achieve an excellent purification level. The synthesized drug was characterized via proton nuclear magnetic resonance (1H NMR), high-performance liquid chromatography (HPLC), Fourier transform infrared spectroscopy (FT-IR), elemental analysis, and melting point.

Keywords: N-acetylcysteine, synthesis, mucolytic medication, lung anti-inflammatory, COVID-19, antioxidant, pharmaceutical supplement, characterization

Procedia PDF Downloads 165

Authors: S. A. M. Sabrina, Gouget Lammel, Anne Chantal, Chazalviel, Jean Noël, Ozanam François, Etcheberry Arnaud, Tighlit Fatma Zohra, B. Samia, Gabouze Noureddine

Abstract:

The elaboration and characterization of hybrid nano materials give rise to considerable interest due to the new properties that arising. They are considered as an important category of new materials having innovative characteristics by combining the specific intrinsic properties of inorganic compounds (semiconductors) with the grafted organic species. This open the way to improved properties and spectacular applications in various and important fields, especially in the environment. In this work, nano materials based-semiconductors were elaborated by chemical route. The obtained surfaces were grafted with organic functional groups. The functionalization process was optimized in order to confer to the hybrid nano material a good stability as well as the right properties required for the subsequent applications. Different characterization techniques were used to investigate the resulting nano structures, such as SEM, UV-Visible, FTIR, Contact angle and electro chemical measurements. Finally, applications were envisaged in environmental area. The elaborated nano structures were tested for the detection and the elimination of pollutants.

Keywords: hybrid materials, porous silicon, peptide, metal detection

Procedia PDF Downloads 470

Authors: Ji-Seok Hong, Hee-Jang Moon, Hong-Gye Sung

Abstract:

The details of flow structures and the coupling mechanism between vortex shedding and acoustic excitation in a solid rocket motor with two inhibitors have been investigated using 3D Large Eddy Simulation (LES) and Proper Orthogonal Decomposition (POD) analysis. The oscillation frequencies and vortex shedding periods from two inhibitors compare reasonably well with the experimental data and numerical result. A total of four different locations of the rear inhibitor has been numerically tested to characterize the coupling relation of vortex shedding frequency and acoustic mode. The major source of triggering pressure oscillation in the combustor is the resonance with the acoustic longitudinal half mode. It was observed that the counter-rotating vortices in the nozzle flow produce roll torque.

Keywords: large eddy simulation, proper orthogonal decomposition, SRM instability, flow-acoustic coupling

Procedia PDF Downloads 537

Authors: Maryam Zafar, Sajida Rasheed, Imran Hashmi

Abstract:

Water as an environmental reservoir is reported to act as a habitat and transmission route to microaerophilic bacteria such as Heliobacter pylori. It has been studied that in biofilms are the predominant dwellings for the bacteria to grow in water and protective reservoir for numerous pathogens by protecting them against harsh conditions, such as shear stress, low carbon concentration and less than optimal temperature. In this study, influence of these and many other parameters was studied on H. pylori in stagnant and moving water biofilms both in surface and underground aquatic reservoirs. H. pylori were recovered from pipe of different materials such as Polyvinyl Chloride, Polypropylene and Galvanized iron pipe cross sections from an urban water distribution network. Biofilm swabbed from inner cross section was examined by molecular biology methods coupled with gene sequencing and H. pylori 16S rRNA peptide nucleic acid probe showing positive results for H. pylori presence. Studies showed that pipe material affect growth of biofilm which in turn provide additional survival mechanism for pathogens like H. pylori causing public health concerns.

Keywords: biofilm, gene sequencing, heliobacter pylori, pipe materials

Procedia PDF Downloads 331

Authors: Ahmed Malki

Abstract:

Breast cancer has been identified as the most lethal form of cancer today. In our study, we designed and screened 16 steviosides derivatives for their cytotoxic activities in MCF-7human breast cancer cells and normal MCF-12a cells. Our data indicated that steviosides derivatives 9 and 15 decreased cell proliferation and induced apoptosis in MCF-7 breast cancer cells more thannormal breast cells epithelial cells. Flow cytometric analysis showed that both steviosides, derivatives 9 and 15 arrested the MCF-7 cells in G1 phase, which is further confirmed by the increased expression level of p21. Moreover, both steviosides derivatives increased caspase-9 activity, and the induction of apoptosis was significantly reduced after treating cells with caspase-9 inhibitor LEHD-CHO. Both steviosides derivatives increased Caspase 3 activities and induced Parp-1 cleavage in H1299 cells. Based on previous results, we have identified two novel steviosides derivatives which provoked apoptosis in breast cancer cells by arresting cells in G1 phase and increasing caspase-9 and caspase-3 activities which merits further development and investigations.

Keywords: steviosides, breast cancer, p53, cell cycle

Procedia PDF Downloads 94

Authors: Mohsina Akhter

Abstract:

Cancer has become a wide spread disease around the globe and takes many lives every year. Different treatments are being practiced but all have potential side effects with somewhat less specificity towards target sites. Pseudomonas aeruginosa is known to secrete a protein azurin with special anti-cancer function. It has unique cell penetrating peptide comprising of 18 amino acids that have ability to enter cancer cells specifically. Reported function of Azurin is to stabilize p53 inside the tumor cells and induces apoptosis through Bax mediated cytochrome c release from mitochondria. At laboratory scale, we have made recombinant azurin through cloning rpTZ57R/T-azu vector into E.coli strain DH-5α and subcloning rpET28-azu vector into E.coli BL21-CodonPlus (DE3). High expression was ensured with IPTG induction at different concentrations then optimized high expression level at 1mM concentration of IPTG for 5 hours. Purification has been done by using Ni+2 affinity chromatography. We have concluded that azurin can be a remarkable improvement in cancer therapeutics if it produces on a large scale. Azurin does not enter into the normal cells so it will prove a safe and secure treatment for patients and prevent them from hazardous anomalies.

Keywords: azurin, pseudomonas aeruginosa, cancer, therapeutics

Procedia PDF Downloads 281

Authors: Jung-Feng Hsieh, Chu Ze Chen

Abstract:

Curcumin is the main active compound of turmeric that can inhibit the activities of α-glucosidase and xanthine oxidase (XO). α-Glucosidase and XO inhibitors are widely used to treat patients with diabetes mellitus and gout, respectively; therefore, the objective of this research was to evaluate the inhibitory activities of curcumin and its analogs against α-glucosidase and XO. Our results demonstrated that CM-F had the strongest antioxidant activity with a half-maximal effective concentration (EC50) of 9.39 ± 0.16 μM, which was superior to vitamin E (EC50=17.03 ± 0.09 μM). CM-F also exhibited potent inhibitory activity against XO with an IC50 value of 6.14 ± 0.38 μM and enzyme kinetic results revealed competitive inhibition of XO. We also found that CM-1 and CM-2 inhibited α-glucosidase with IC50 values of 21.06 ± 0.92 μM and 5.95 ± 0.09 μM, respectively, and kinetic studies indicated that both CM-1 and CM-2 are mixed competitive inhibitors of α-glucosidase. Furthermore, docking simulation identified five hydrogen bonds between XO and CM-F; however, only one and two hydrogen bonds are involved in CM-1 and CM-2 binding to α-glucosidase, respectively. Accordingly, curcumin and its analogs have the potential to be used in the treatment of patients with diabetes mellitus and gout.

Keywords: curcumin, α-glucosidase, inhibitor, xanthine oxidase

Procedia PDF Downloads 178

Authors: Ghazala Yaqub, Zubi Sadiq, Almas Hamid, Saira Iqbal

Abstract:

This paper is the very first report of three dual action hybrids synthesized by covalent linkage of carbazole based novel antibacterial compounds with efflux pump inhibitors i.e., indole acetic acid/gallic acid. Novel carbazole based antibacterial compounds were prepared first and then these were covalently linked with efflux pump inhibitors which leads to the successful formation of hybrids. All prepared compounds were evaluated for their bacterial cell killing capability against Escherichia coli, Staphylococcus aureus, Pasteurella multocida and Bacillus subtilis. Compound were effective against all tested bacterial strains at different concentrations. But when these compounds were linked with efflux pump inhibitors they showed dramatic enhancement in their bacterial cell killing potential and minimum inhibitory concentration of all hybrids ranges from 7.250 µg/mL to 0.0283 µg/mL.

Keywords: antimicrobial assay, carbazole, dual action hybrids, efflux pump inhibitors

Procedia PDF Downloads 2073

Authors: Khaled Khleifat, Muayyad Abboud, Ahmad Almustafa

Abstract:

The effect of metabolic inhibitor/uncoupler(s) (CCCP and NaN3) and sulfhydryl reagents (dithiothreitol, 2 mercaptoethanol glutathione) on cadmium uptake was investigated in Enterobacter aerogenes strains. They include a transformed strain bearing the Vitreoscillahemoglobin gene, vgb as well as control strains that lack this transformed gene. The vgb-harboring strains showed better uptake of cadmium than vgb-lacking strains. Under low aeration, there was 2 fold enhancement of Cd+2 uptake in vgb-harboring strains compared with 1.6-fold enhancement under high aeration. The CCCP caused 36, 40 and 58% inhibition in cadmium uptake of parental, pUC9 harboring and VHb expressing cells, respectively. Similarly, the sodium azide exerted 44, 38 and 55% inhibition in Cd+2 uptake of parental, pUC9 harboring and VHb expressing cells, respectively. Less extensive inhibition of Cd+2 uptake in the range of 11 to 39% was observed with sulfhydryl reagents.

Keywords: bacterial hemoglobin, VHb, Cd uptake, biosorption

Procedia PDF Downloads 294

Authors: Friday A. Ogori, Ojotu M. Eke, Oneh J. Abu, Abraham T. Girgih

Abstract:

B.aeqygtiaca del (Balanites aegyptiaca del) seed protein concentrate (APC) was hydrolyzed using different enzymes such as pepsin+pancreatin (PP), Alcalase (Alca), and Flavourzyme (Flav). The Alca has higher yield (100%) when compared to PP (83.23%) and Flav (62.90%). The hydrophobic amino acid and Sulphur containing amino acid (40.19%, 7.04%) in PP hydrolysate were higher compared to Alcalase (38.92%, 6.69%), Flavourenzyme (37.43%,6.35%), and APC (39.97%, 6.95%) samples. The PP has stronger DPPH, Hydroxyl radical quenching, Ferric reducing activity, and linoleic acid peroxidation activity, followed by the protein concentrate (APC) and Alcalase (Alca), while Flavourenzyme (Flav) derived hydrolysate was least in scavenging and inhibiting radical peroxidation properties. Flavourenzyme derived hydrolysate had stronger Ferric reducing antioxidant potential and metal chelating property. The result showed that the Alcalase hydrolysate has promising peptide yield, and PP hydrolysate had excellent amino acid residues and good in-vitro antioxidant potentials and could be a preferred ingredients in the nutraceutical and functional food emerging industries.

Keywords: balanites aegyptiaca del, protein concentrate, protein hydrolysates, enzymatic hydrolysis, antioxidants

Procedia PDF Downloads 47

Authors: Nisrine Benzbiria, Mohammed Azzi, Mustapha Zertoubi

Abstract:

2XXX series of aluminum alloys are widely employed in several applications, such as beverages, automotive, and aerospace industries. However, they are particularly prone to localized corrosion, such as pitting, often induced by a difference in corrosion potential measured for intermetallic phases and pure metal. The galvanic cells comprising Al–Cu– Mn–Fe intermetallic phases control cathodically the dissolution rate as oxygen reduction reaction kinetics are privileged on Al–Cu–Mn–Fe particles. Hence, understanding the properties of cathode sites and the processes involved must be carried out. Our interest is to outline the cathodic behavior of AA2024-T3 in sodium sulfate solution using electrochemical techniques. Oxygen reduction reaction (ORR) was investigated in the mixed charge transfer and mass transport regime using the Koutecky-Levich approach. An environmentally benign inhibitor was considered to slow the ORR on the Cu-rich cathodic phases. The surface morphology of the electrodes was investigated with SEM/EDS and AFM. The obtained results were discussed accordingly.

Keywords: AA2024-T3, neutral medium, ORR kinetics, Koutecky-Levich, DFT

Procedia PDF Downloads 23

Authors: Shiva Emami, Jenny Persson, Bengt Johansson Lindbom

Abstract:

Group A streptococcus (GAS) is a prevalent human pathogen, causing a wide range of infections and diseases. One of the most well-known virulence factors in GAS is M protein, a surface protein that facilitates bacterial invasion. In this study, we used a recombinant GAS strain (GAS-2W) expressing M protein containing a hyper immunogenic peptide (2W). Mice were immunized three times with heat-killed-GAS subcutaneously at three weeks intervals. Three weeks post last immunization, mice were challenged intraperitoneally with a lethal dose of live GAS. In order to investigate the impact of IFN-ƴ and antibodies in protection against GAS infection, we used a mouse model knock-out for IFN-ƴ (IFN-ƴ KO). We observed immunization with GAS-2W strain can increase protection against GAS infection in mice compared with the original GAS strain. Higher levels of antibodies against M1 protein were measured in GAS-2W-immunized mice. There was also a significant increase in IgG2c response in mice immunized with GAS2W. By using IFN-ƴ KO mice, we showed that not a high level of total IgG, but IgG2c was correlated with protection through the i.p challenge. It also emphasizes the importance of IFN-ƴ cytokine to combat GAS by isotype switching to IgG2c (which is opsonic for phagocytosis). Our data indicate the crucial role of IFN-ƴ in the protective immune response that, together with IgG2c, can induce protection against GAS.

Keywords: Group A streptococcus, IgG2c, IFN-γ, protection

Procedia PDF Downloads 64

Authors: Rafayel Azizyan, Valeri Arakelyan, Aram Gevorgyan, Varduhi Balayan, Emil Gevorgyan

Abstract:

Currently, mathematical and computer modeling are widely used in different biological studies to predict or assess behavior of such complex systems as biological ones. This study deals with mathematical and computer modeling of bi-substrate enzymatic reactions, which play an important role in different biochemical pathways. The main objective of this study is to represent the results from in silico investigation of bi-substrate enzymatic reactions in the presence of uncompetitive inhibitors, as well as to describe in details the inhibition effects. Four models of uncompetitive inhibition were designed using different software packages. Particularly, uncompetitive inhibitor to the first [ES1] and the second ([ES1S2]; [FS2]) enzyme-substrate complexes have been studied. The simulation, using the same kinetic parameters for all models allowed investigating the behavior of reactions as well as determined some interesting aspects concerning influence of different cases of uncompetitive inhibition. Besides that shown, that uncompetitive inhibitors exhibit specific selectivity depending on mechanism of bi-substrate enzymatic reaction.

Keywords: mathematical modeling, bi-substrate enzymatic reactions, reversible inhibition

Procedia PDF Downloads 320

Authors: C. R. Stein; K. Skeff Neto, K. L. C. Miranda, P. P. C. Sartoratto, M. E. Xavier, Z. G. M. Lacava, S. M. De Freita, P. C. Morais

Abstract:

In this study, static magnetic birefringence (SMB) and transmission electron microscopy (TEM) were used to investigate the self-assembling of maghemite nanoparticles suspended as biocompatible magnetic fluid (BMF) while incubated or not with the Black Eyed–Pea Trypsin Chymotripsin Inhibitor–BTCI protein. The stock samples herein studied are dextran coated maghemite nanoparticles (average core diameter of 7.1 nm, diameter dispersion of 0.26, and containing 4.6×1016 particle/mL) and the dextran coated maghemite nanoparticles associated with the BTCI protein. Several samples were prepared by diluting the stock samples with deionized water while following their colloidal stability. The diluted samples were investigated using SMB measurements to assess the average sizes of the self-assembled and suspended mesoscopic structures whereas the TEM micrographs provide the morphology of the as-suspended units. The SMB data were analyzed using a model that includes the particle-particle interaction within the mean field model picture.

Keywords: biocompatible magnetic fluid, maghemite nanoparticles, self-assembling

Procedia PDF Downloads 460

Authors: Tanushree Jaitly, Shailendra Gupta, Leila Taher, Gerold Schuler, Julio Vera

Abstract:

Genomics-based personalized medicine is a promising approach to fight aggressive tumors based on patient's specific tumor mutation and expression profiles. A remarkable case is, dendritic cell-based immunotherapy, in which tumor epitopes targeting patient's specific mutations are used to design a vaccine that helps in stimulating cytotoxic T cell mediated anticancer immunity. Here we present a computational pipeline for epitope-based personalized cancer vaccines using patient-specific haplotype and cancer mutation profiles. In the workflow proposed, we analyze Whole Exome Sequencing and RNA Sequencing patient data to detect patient-specific mutations and their expression level. Epitopes including the tumor mutations are computationally predicted using patient's haplotype and filtered based on their expression level, binding affinity, and immunogenicity. We calculate binding energy for each filtered major histocompatibility complex (MHC)-peptide complex using docking studies, and use this feature to select good epitope candidates further.

Keywords: cancer immunotherapy, epitope prediction, NGS data, personalized medicine

Procedia PDF Downloads 228

Authors: M. L. Ibrahim, A. Abdulhamid

Abstract:

A surface active molecule synthesized by a rhizobacterial strain Bacillus lentus isolated from Cajanus cajan was investigated. The bioemulsifier was extracted, purified and partially characterized using standard methods. Surface properties of the bioemulsifier were determined by studying the emulsification index, solubility test and stability studies. Partial purification of the bioemulsifier was carried out using FT-IR analysis, Silica-gel column chromatography and thin layer chromatography. GC-MS analysis was carried out to detect the composition and mass of the lipids and esters. The isolate showed an emulsifying activity of 57% and surface activity of 36mm. The stability studies revealed that the bioemulsifier had better stability at temperature of 70oC, 8% pH and 8% NaCl concentration. FT-IR indicated the bioemulsifier to contain peptide and aliphatic chain, TLC revealed the compound to be ninhydrin positive and Column chromatography showed the presence of three amino acids namely; glutamine, valine and cysteine. GC-MS indicated the lipid moiety to contain aliphatic chain ranging from C9-C16 and two major peaks of 1,2-benzenedicarboxylic acid diethyl octyl ester. Therefore, surface active agent from Bacillus lentus can be used effectively in a wide range of applications such as in MEOR and in the biosynthesis of plasticizers for industrial uses.

Keywords: Bacillus lentus, bioemulsifiers, phthalic acid ester, Rhizosphere

Procedia PDF Downloads 387

Authors: W. P. Hu, J. V. Kumar, Jeffrey J. P. Tsai

Abstract:

The inhibition of SH2 domain regulated protein-protein interactions is an attractive target for developing an effective chemotherapeutic approach in the treatment of disease. Molecular simulation is a useful tool for developing new drugs and for studying molecular recognition. In this study, we searched potential drug compounds for the inhibition of SH2 domain by performing structural similarity search in PubChem Compound Database. A total of 37 compounds were screened from the database, and then we used the LibDock docking program to evaluate the inhibition effect. The best three compounds (AP22408, CID 71463546 and CID 9917321) were chosen for MD simulations after the LibDock docking. Our results show that the compound CID 9917321 can produce a more stable protein-ligand complex compared to other two currently known inhibitors of Src SH2 domain. The compound CID 9917321 may be useful for the inhibition of SH2 domain based on these computational results. Subsequently experiments are needed to verify the effect of compound CID 9917321 on the SH2 domain in the future studies.

Keywords: nonpeptide inhibitor, Src SH2 domain, LibDock, molecular dynamics simulation

Procedia PDF Downloads 242

Authors: Ryeong-Hyeon Kim, Ah-Reum Lee, Seong-Soo Roh, Gyo-Nam Kim

Abstract:

Appropriate regulation of melanogenesis is important for the management of skin pigmentation-related disease. Although several beneficial effects of fisetin (3,7,3’,4’-tetrahydroxyflavone) have been reported, the precise role and molecular mechanisms of fisetin in skin health both remain unclear. Here, we induced melanogenesis of HRM2 mice (n=7/group) by UVB irradiation for 20 days. UVB-induced HRM2 mice showed that the significantly increased melanin accumulation, however, fisetin treatment (25mg and 50mg/kg of body weight) dose-dependently and significantly inhibits UVB-induced melanogenesis. In line with this, fisetin treatment effectively down-regulated m RNA and expression levels of tyrosinase, TRP2, and MITF. In addition, our inhibitor assay revealed the down-regulated melanogenic marker genes by fisetin treatment were mediated with connective tissue growth factor (CCN2)/TGF-β signaling pathway. Useful information is provided for development of functional foods using fisetin for skin health.

Keywords: connective tissue growth factor, fisetin, melanogenesis, skin, TGF-beta

Procedia PDF Downloads 214

Authors: Hai Chi, Ibrahim Mehmeti, Kirill Ovchinnikov, Hegle Holo, Ingolf F. Nes, Dzung B. Diep

Abstract:

By using a panel of multiple indicator strains of different bacterial species and genera, we screened a large collection of bacterial isolates (over 1800 isolates) derived from raw milk, for bacteriocin producers with broad inhibition spectra (BIS). Fourteen isolates with BIS were identified, and by 16S rDNA sequencing they were found to belong to Lactococcus garvieae (10 isolates) and Enterococcus feacalis (4 isolates). Further analysis of the ten L. garvieae isolates revealed that they were very similar, if not identical, to each other in metabolic and genetic terms: they had the same fermentation profile on different types of sugars, repetitive sequence-based PCR (rep-PCR) DNA pattern as well as they all had the same inhibition profile towards over 50 isolates of different species. The bacteriocin activity from one of the L. garvieae isolates was assessed further. The bacteriocin which was termed garvicin KS, was found to be heatstable and proteinase-labile and its inhibition spectrum contained many distantly related genera of Firmicutes, comprising most lactic acid bacteria (LAB) as well as problematic species of Bacillus, Listeria, Streptococcus and Staphylococcus and their antibiotic resistant derivatives (e.g. VRE, MRSA). Taken together, the results indicate that this is a potent bacteriocin from L. garvieae and that its very broad inhibition spectrum can be a very useful property for use in food preservation as well as in infection treatments caused by gram-positive pathogens and their antibiotic-derivatives.

Keywords: bacteriocin, lactic acid bacteria, Lactococcus garvieae, antibiotics resistance

Procedia PDF Downloads 212

Authors: Rizwan H. Khan, Saima Nusrat

Abstract:

Despite the fact that amyloid associated neurodegenerative diseases and non-neuropathic systemic amyloidosis have allured the research endeavors, as no curative drugs have been proclaimed up till now except for symptomatic cure. Therapeutic compounds which can diminish or disaggregate such toxic oligomers and fibrillar species have been examined and more are on its way. In the present study, we had reported an extensive biophysical, microscopic and computational study, revealing that L-3, 4-dihydroxyphenylalanine (L-Dopa) possess undeniable potency to inhibit heat induced human lysozyme (HL) amyloid fibrillation and also retain the fibril disaggregating potential. L-Dopa interferes in the amyloid fibrillogenesis process by interacting hydrophobically and also by forming hydrogen bonds with the amino acid residues found in amyloid fibril forming prone region of HL as elucidated by molecular docking results. L-Dopa also disaggregates the mature amyloid fibrils into some unorganised species. Thus, L-Dopa and related compounds can work as a promising inhibitor for the therapeutic advancement prospective against systemic amyloidosis.

Keywords: amyloids, disaggregation, human lysozyme, molecular docking

Procedia PDF Downloads 300

Authors: Madhu Gupta, G. P. Agrawa, Suresh P. Vyas

Abstract:

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 459

Authors: Genaro Bolívar, Manuel Mas, Maria Tortolero, Jorge Salazar

Abstract:

Due to the extensive use of water injection for oil displacement and pressure maintenance in oil fields, many reservoirs experience the problem of scale deposition when injection water starts to break through. In most cases the scaled-up wells are caused by the formation of sulfate and carbonate scales of calcium and strontium. Due to their relative hardness and low solubility, there are limited processes available for their removal and preventive measures such as the “squeeze” inhibitor treatment have to be taken. It is, therefore, important to gain a proper understanding of the kinetics of scale formation and its detrimental effects on formation damage under both inhibited and uninhibited conditions. Recently, the production of chitosan was started in our country and in the PDVSA-Intevep laboratories was synthesized and evaluated the properties of carboxymethyl chitosan (CMQ) as chelating agent of Ca2 + ions in water injection. In this regard, the characterization of the biopolymer by 13C - NMR, FTIR, TGA, and TM0374-2007 standard laboratory test has demonstrated the ability to remove up to 70% calcium ions in solution and shows a behavior that approaches that of commercial products.

Keywords: carboxymethyl chitosan, scale, calcium carbonate scale deposition, water injection

Procedia PDF Downloads 412

Authors: Abdelaziz Messis, Azzeddine Bettache, Nawel Boucherba, Said Benallaoua, Mouloud Kecha

Abstract:

Actinobacteria are of special biotechnological interest since they are known to produce chemically diverse compounds with a wide range of biological activity. This distinct clade of Gram-positve bacteria include some of the key antibiotic producers and are also sources of several bioactive compounds, established commercially a newly filamentous bacteria was recovered from Tikjda forest soil (Algeria) for its high antifungal activity against various pathogenic and phytopathogenic fungi. The nucleotide sequence of the 16S rRNA gene (1454 pb) of Streptomyces sp. TKJ2 exhibited close similarity (99 %) with other Streptomyces16S rRNA genes. Antifungal metabolite production of Streptomyces sp TKJ2 was evaluated using six different fermentation media. The extracellular products contained potent antifungal agents. Antifungal protein produced by Streptomyces sp. TKJ2 on PCA medium has been purified by ammonium sulfate precipitation, SPE column chromatography and high-performance liquid chromatography in a reverse-phase column. The UV chromatograms of the active fractions obtained at 214 nm by NanoLC-ESI-MS/MS have different molecular weights. The F20 Peptidic fraction obtained from culture filtrat of Streptomyces sp. TKJ2 precipitated at 30% of ammonium sulfate was selected for analysis by infusion ESI-MS which yielded a singly charged ion mass of 437.17 Da.

Keywords: actinobacteria, antifungal protein, chromatography, Streptomyces

Procedia PDF Downloads 353

Authors: Weijie Gu, Sergio Martinez, Hoai Nguyen, Hongtao Xu, Piet Herdewijn, Steven De Jonghe, Kalyan Das

Abstract:

Nucleotide analogs are used for treating viral infections such as HIV, hepatitis B, hepatitis C, influenza, and SARS-CoV-2. To become polymerase substrates, a nucleotide analog must be phosphorylated by cellular kinases, which are rate-limiting. The goal of this study is to develop dNTP/NTP analogs directly from nucleotides. Tenofovir (TFV) analogs were synthesized by conjugating with natural or unnatural amino acids. It demonstrates that some conjugates act as dNTP analogs, and HIV-1 reverse transcriptase (RT) catalytically incorporates the TFV part as the chain terminator. X-ray structures in complex with HIV-1 RT/dsDNA showed binding of the conjugates at the polymerase active site, however, in different modes in the presence of Mg²⁺ vs. Mn²⁺ ions. The adaptability of the compounds is seemingly essential for catalytic incorporation of TFV by RT. 4d with a carboxyl sidechain demonstrated the highest incorporation. 4e showed weak incorporation and rather behaved as a dNTP-competitive inhibitor. This result advocates the feasibility of designing NTP/dNTP analogs by chemical substitutions to nucleotide analogs.

Keywords: dNTP analogs, nucleotide analogs, polymerase, tenofovir, X-ray structure

Procedia PDF Downloads 124

Authors: Rajesh P.P., Md. Tabish Noori, Makarand M. Ghangrekar

Abstract:

Methanogenic substrate loss is reported to be a major bottleneck in microbial fuel cell which significantly reduces the power production capacity and coulombic efficiency (CE) of microbial fuel cell (MFC). Nitroethane is found to be a potent inhibitor of hydrogenotrophic methanogens in rumen fermentation process. Influence of nitroethane pre-treated sewage sludge inoculum on suppressing the methanogenic activity and enhancing the electrogenesis in MFC was evaluated. MFC inoculated with nitroethane pre-treated anodic inoculum demonstrated a maximum operating voltage of 541 mV, with coulombic efficiency and sustainable volumetric power density of 39.85 % and 14.63 W/m3 respectively. Linear sweep voltammetry indicated a higher electron discharge on the anode surface due to enhancement of electrogenic activity while suppressing methanogenic activity. A 63 % reduction in specific methanogenic activity was observed in anaerobic sludge pre-treated with nitroethane; emphasizing significance of this pretreatment for suppressing methanogenesis and its utility for enhancing electricity generation in MFC.

Keywords: coulombic efficiency, methanogenesis inhibition, microbial fuel cell, nitroethane

Procedia PDF Downloads 290

Authors: Kasim Sakran Abass

Abstract:

This main aim of this study was to confirm and extend our current knowledge about the effects of dilutions on esterases activities in the blood for birds with respect to protecting the enzyme from organophosphate inhibition. There were significantly higher esterases activities in dilution 1:10 in all blood samples from quail, duck, and chick compared to other dilutions (1:5, 1:15, 1:20, and 1:25). Furthermore, our results also pointed to the importance of estimating different dilutions effects prior to using in birds as biomarker tools of environmental exposure. Concentration–inhibition curves were determined for the inhibitor in the presence of dilutions 1:5, 1:10 plus 1:15 (to stimulate carboxylesterase). Point estimates (concentrations calculated to produce 20, 50, and 80% inhibition) were compared across conditions and served as a measure of esterase-mediated detoxification. Among the thiol esters (dilution 1:5) was observed to have the highest specificity constant (kcat/Km), and the Km and kcat values were 176 μM and 16,765 s−1, respectively for S-phenyl thioacetate ester, while detected in (dilution 1:15) the lowest specificity constant (kcat/Km), and the Km and kcat values were 943 μM and 1154 s−1, respectively for acetylthiocholine iodide ester.

Keywords: esterase, animal, dilution, pesticides

Procedia PDF Downloads 500

Authors: K. N. Kipreou, E. Efthmiadou, G. Kordas

Abstract:

Biofouling represents one of the most crucial problems in the present maritime industries when its control still challenges the researchers all over the world. The present work is referred to the synthesis and characterization CeMo and Cu2O nanocontainers by using a wide range of techniques including scanning electron microscopy (SEM), X-ray diffraction (XRD) and thermogravimetric analysis (TGA) for marine applications. The above nanosystems will be loaded with active monomers and corrosion rendering healing ability to marine paints. The objective of this project is their ability for self-healing, self-polishing and finally for anti-corrosion activity. One of the driving forces for the exploration of CeMo, is the unique anticorrosive behavior, which will be confirmed by the electrochemistry methodology. It has be highlighted that the nanocontainers of Cu2O with the appropriate antibacterial inhibitor will improve the hydrophobicity and the morphology of the coating surfaces reducing the water friction. In summary, both novel nanoc will increase the lifetime of the paints releasing the antifouling agent in a control manner.

Keywords: marinepaints, nanocontainer, antifouling, anticorrosion, copper, electrochemistry, coating, biofouling, inhibitors, copper oxide, coating, SEM

Procedia PDF Downloads 310

Authors: Khalid Ahmed Eldwaib

Abstract:

In this study, Al-Mg alloy 5052 was used as the testing material. Corrosion fatigue life was studied for the alloy in 3.5% NaCl (pH=1, 3, 5, 7, 9, and 11), and 3.5% NaCl (pH=1) with inhibitors. The compound inhibitors were composed mainly of phosphate (PO4³-), adding a certain proportion of other nontoxic inhibitors so as to select alternatives to environmentally hazardous chromate (Cr2O7²-). The inhibitors were sodium dichromate Na2Cr2O7, sodium phosphate Na3PO4, sodium molybdate Na2MoO4, and sodium citrate Na3C6H5O7. The total amount of inhibiting pigments was at different concentrations (250,500,750, and 1000 ppm) in the solutions. Corrosion fatigue behavior was studied by using plane-bending corrosion fatigue machine with stress ratio R=0.5 and under the constant frequency of 13.3 Hz. Results show that in 3.5% NaCl the highest fatigue life (number of cycles to failure Nf) is obtained at pH=5 where the oxide film on aluminum has very low solubility, and the lowest number of cycles is obtained at pH=1, where the media is too aggressive (extremely acidic). When the concentration of inhibitor increases the cycles to failure increase. The surface morphology and fracture section of the specimens had been characterized through scanning electron microscope (SEM).

Keywords: Al-Mg alloy 5052, corrosion, fatigue, inhibitors

Procedia PDF Downloads 428

Authors: Venoos Iman, Suzita Mohd Noor, Syam Mohan, Mohamad Ibrahim Noordin

Abstract:

Girinimbine, a carbazole alkaloid was isolated from the stem bark and root of Murraya koenigii and its structure and purity was identified by HPLC and LC-MS. Here we report that Girinimbine strongly inhibit angiogenesis activity both in vitro and in vivo. MTT result showed that girinimbine inhibits cell proliferation of the HUVECS cell line in vitro. Result of endothelial cell invasion, migration, tube formation and wound healing assays also demonstrated significant time and does dependent inhibition by girinimbine. Moreover, girinibine mediates its anti-angiogenic activity through up- and down-regulation of angiogenic and anti-aniogenic proteins. Furthermore, anti-angiogenic potential of girinimbine was evidenced in vivo on zebrafish model. Girinimbine inhibited neo-vessels formation in zebrafish embryos during 24 hours exposure time. Together, these results demonstrated for the first time that girinimbine could effectively suppress angiogenesis and strongly suggest that it might be a novel angiogenesis inhibitor.

Keywords: anti-angiogenic, carbazole alkaloid, girinimbine, zebrafish

Procedia PDF Downloads 355

Authors: Olufunke O. Ezekiel, Adenike O. Ogunshe, Omotola F. Olagunju, Arinola O. Falola

Abstract:

Studies were conducted on fermentation of tamarind seed for production of food condiment. Fermentation followed the conventional traditional method of fermented locust bean (iru) production and was carried out over a period of three days (72 hours). Samples were withdrawn and analysed for proximate composition, pH, titratable acidity, tannin content, phytic acid content and trypsin inhibitor activity using standard methods. Effects of fermentation on proximate composition, anti-nutritional factors and sensory properties of the seed were evaluated. All data were analysed using ANOVA and means separated using Duncan multiple range test. Microbiological analysis to identify and characterize the microflora responsible for the fermentation of the seed was also carried out. Fermentation had significant effect on the proximate composition on the fermented seeds. As fermentation progressed, there was significant reduction in the anti-nutrient contents. Organisms isolated from the fermenting tamarind seeds were identified as non-pathogenic and common with fermented legumes.

Keywords: condiment, fermentation, legume, tamarind seed

Procedia PDF Downloads 312