Search results for: heterocycles based anticancer agents

Authors: Mathew Tran, Deepa Patel, Breann Prophete, Irandokht Khaki Najafabadi

Abstract:

Status epilepticus is a neurological disorder requiring emergent control with medical therapy. Based on guideline recommendations for adults with status epilepticus, the first-line treatment is to start a benzodiazepine, as they are quick at seizure control. The second step is to initiate a non-benzodiazepine anti-epileptic drug to prevent refractory seizures. Studies show that the anti-epileptic drugs are approximately equivalent in status epilepticus control once a benzodiazepine has been given. This review provides a brief overview of the management of status epilepticus based on evidence from the literature and evidence-based guidelines.

Keywords: neurological disorder, seizure, status epilepticus, benzo diazepines, antiepileptic agents

Procedia PDF Downloads 83

Authors: Marcel Verwey, Anna M. Joubert, Elsie M. Nolte, Wolfgang Dohle, Barry V. L. Potter, Anne E. Theron

Abstract:

A tetrahydroisoquinolinone (THIQ) core can be used to mimic the A,B-ring of colchicine site-binding microtubule disruptors such as 2-methoxyestradiol in the design of anti-cancer agents. Steroidomimeric microtubule disruptors were synthesized by introducing C'2 and C'3 of the steroidal A-ring to C'6 and C'7 of the THIQ core and by introducing a decorated hydrogen bond acceptor motif projecting from the steroidal D-ring to N'2. For this in vitro study, four non-steroidal THIQ-based analogues were investigated and comparative studies were done between the non-sulphamoylated compound STX 3450 and the sulphamoylated compounds STX 2895, STX 3329 and STX 3451. The objective of this study was to investigate the modes of cell death induced by these four THIQ-based analogues in A549 lung carcinoma epithelial cells and metastatic breast adenocarcinoma MDA-MB-231 cells. Cytotoxicity studies to determine the half maximal growth inhibitory concentrations were done using spectrophotometric quantification via crystal violet staining and lactate dehydrogenase (LDH) assays. Microtubule integrity and morphologic changes of exposed cells were investigated using polarization-optical transmitted light differential interference contrast microscopy, transmission electron microscopy and confocal microscopy. Flow cytometric quantification was used to determine apoptosis induction and the effect that THIQ-based analogues have on cell cycle progression. Signal transduction pathways were elucidated by quantification of the mitochondrial membrane integrity, cytochrome c release and caspase 3, -6 and -8 activation. Induction of autophagic cell death by the THIQ-based analogues was investigated by morphological assessment of fluorescent monodansylcadaverine (MDC) staining of acidic vacuoles and by quantifying aggresome formation via flow cytometry. Results revealed that these non-steroidal microtubule disrupting analogues inhibited 50% of cell growth at nanomolar concentrations. Immunofluorescence microscopy indicated microtubule depolarization and the resultant mitotic arrest was further confirmed through cell cycle analysis. Apoptosis induction via the intrinsic pathway was observed due to depolarization of the mitochondrial membrane, induction of cytochrome c release as well as, caspase 3 activation. Potential involvement of programmed cell death type II was observed due to the presence of acidic vacuoles and aggresome formation. Necrotic cell death did not contribute significantly, indicated by stable LDH levels. This in vitro study revealed the induction of the intrinsic apoptotic pathway as well as possible involvement of autophagy after exposure to these THIQ-based analogues in both MDA-MB-231- and A549 cells. Further investigation of this series of anticancer drugs still needs to be conducted to elucidate the temporal, mechanistic and functional crosstalk mechanisms between the two observed programmed cell deaths pathways.

Keywords: apoptosis, autophagy, cancer, microtubule disruptor

Procedia PDF Downloads 221

Authors: Vasudha Devi, Arul Amuthan, K. Narayanan, Praveen KS, Venkata Rao J

Abstract:

Background: Siddha Medicine is one of the Indian traditional medical systems, in which the cancer disease is mentioned as 'putrunoi' which literally means the disease of growth like termite mound. There are number of formulations available for the treatment of cancer disease. Neeradi muthu vallathymezugu (NMV) and thamira kattu chendooram (TKC) are two drugs commonly prescribed by Siddha physicians. These drugs have been clinically reported to be safe and effective when given orally. Though these formulations are in practice for centuries, no efforts have been made to standardize them and explore their anti-cancer potential systematically. Objective: To compare the cytotoxic activity of NMV and TKC with doxorubicin using cancer cell lines. Materials and methods: For this study, ethanol extract of NMV was taken, whereas TKC was used as such. In vitro cytotoxic activity was evaluated by sulphorhodamine (SRB) assay against human hepatic cancer cells (HepG2), human breast cancer cells (MCF-7) and human cervical cancer cells [KeLa]. Doxorubicin was used as the standard. The SRB assay is based on the ability of cellular proteins to bind with sulphorhodamine-B. The number of live cells in drug treated cell lines directly affects the color formation in the assay, which is estimated calorimetrically by measuring the absorbance at 540 nm to calculate the cytotoxicity (inhibitory concentration - IC50 value) of the drug. Results: The IC50values of NMV, TKC and doxorubicin against HepG2 were 3.08 µg/ml, 20.21 µg/ml and 1.21µg/ml respectively. In MCF-7, it was 11.75 µg/ml, 17.67 µg/ml and 2.8µg/ml. In HeLa, the values were 24.76 µg/ml, 73.35 µg/ml and 1.12µg/ml. Conclusions: The study proves the possible anti-cancer potential of these two formulations. Compared to TKC, NMV showed good cytotoxic effect even at low dose. Human hepatic cancer cells responded well even at very low dose, when compared to other cancer cells. Though, cytotoxic potential of these compounds was found to be less compared to doxorubicin, the isolated lead compound may have the potential to be used as an anticancer drug clinically.

Keywords: Neeradi muthu vallathymezugu (Hydnocarpus laurifolia), thamira kattu chendooram, cytotoxicity, in-vitro, Siddha Medicine

Procedia PDF Downloads 424

Authors: Parastou Kharazmi

Abstract:

Degradation of building materials particularly pipelines causes environmental damage during renovation or replacement and is a time consuming and costly process. Rehabilitation by polymer composites is a solution for renovation of degraded pipeline in heritage buildings and other structures which are less costly, faster and causes less damage to the environment; however, it is still not clear for how long these materials can perform as expected in the field and working condition. To study their service life, two types of composites based on Epoxy and Polyester resins have been evaluated by accelerated exposure and field exposure. The primary degradation agent used in accelerated exposure has been cycling temperature with half of the tests performed in presence of water. Thin films of materials used in accelerated testing were prepared in laboratory by using the same amount of material as well as technique of multi-layers application used in majority of the field installations. Extreme intensity levels of degradation agents have been used only to evaluate materials properties and as also mentioned in ISO 15686, are not directly correlated with degradation mechanisms that would be experienced in service. In the field exposure study, the focus has been to identify possible failure modes, causes, and effects. In field exposure, it has been observed that there are other degradation agents present which can be investigated further such as presence of contaminants and rust before application which prevents formation of a uniform layer of polymer or incompatibility between dissimilar materials. This part of the study also highlighted the importance of application’s quality of the materials in the field for providing the expected performance and service life. Results from extended accelerated exposure and field exposure can help in choosing inspection techniques, establishing the primary degradation agents and can be used for ageing exposure programs with clarifying relationship between different exposure periods and sites.

Keywords: building, renovation, service life, pipelines

Procedia PDF Downloads 170

Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

Abstract:

Triazoles are basic five-membered ring heterocycles with an unsaturated, six-delocalized electron ring system. Since the dawn of click chemistry, triazoles have represented a functional heterocyclic core that has been the foundation of medicinal chemistry. The compounds with 1,2,3-triazole rings can be used in several fields, including medicine, organic synthesis, polymer chemistry, fluorescent imaging, horticulture, and industries, to name a few. Besides that, they found it to have health applications in the prevention and reduction of the risk of diseases, such as anti-cancer, antimicrobial, antiviral, and anti-inflammatory properties. Here, we present the synthesis of twelve 1,2,3-triazolyl chalcone derivatives (4a–l), which were produced in high yields by coupling substituted aldehydes and triazolyl acetophenone (3a–d) in ethanol. The title products were characterized by physicochemical, infrared, nuclear magnetic resonance, and mass spectral methods. The in vitro tests were used to evaluate the antioxidant and antimicrobial activity of each of the prepared molecules. The preliminary assessment and 2,2-diphenyl-1-picrylhydrazyl activity of the title compounds showed significantly higher antibacterial activity and moderate-to-good antifungal and antioxidant activities compared to their standards. This work presents the synthesis of triazolyl chalcone derivatives and their biological activity. Based on the findings, these compounds could be used as lead compounds in antimicrobial and antioxidant research in the future.

Keywords: antibacterial activity, antifungal activity, antioxidant activity, chalcone, 1, 2, 3-triazole

Procedia PDF Downloads 84

Authors: Houcine Ammar

Abstract:

Chromenederivatives are an important class of heterocycles that are found in a wide range of natural products. Chromenes are commonly used as cosmetics, food additives, and possibly biodegradable agrochemicals. Recently, the synthesis of chromene derivatives has drawn more attention due to their pharmacological and biological applications. In the present work, we are interested in the synthesis and characterization of chromeno [2,3-b] pyridin-4-yl) formimidate, carried out in 4 steps: (i) the synthesis of 3-cyanoiminocoumarins is realized first by Knœvenagel reaction by reacting malonitrile with variously substituted o-phenolic benzaldehydes. In order to undergo reduction by sodium tetraborohydride NaBH4 to lead to new 2-amino-3-cyano-4H-chromenes, these compounds were easily transformed by the action of malonitrile leading to 2,4-diamino-5H-chromeno [2,3-b] pyridine-3-carbonitrile under microwave activation. For the final step, the action of triethylorthoformate on 2,4-diamino-5H-chromeno [2,3-b] pyridine-3-carbonitrile leads to new chromeno [2,3-b] pyridinheterocycles. -4-yl) formimidate. The synthesized compounds have been characterized by different spectroscopic techniques 1 H-NMR, 13 C-NMR, and IRTF.

Keywords: chromene, microwave, knovenagel condensation, chromeno [2, 3-b] pyridine

Procedia PDF Downloads 63

Authors: Sangil Han, In Su Kim

Abstract:

Transition-metal-catalyzed C–H bond activation and its subsequent functionalization has been one of the most attractive topics in organic synthesis because of its remarkable potential for atom economy and environmental sustainability. In this addition, a variety of C(sp2)–H functionalization has been developed under metal catalysis in the past decade. Recently, much attention has been moved towards the C(sp3)–H functionalization events, which continue to be a challenging issue. In this area, directing group assisted sp3 C–H functionalization has been explored by use of amides, carboxylic acids, oximes, N-heterocycles, and etc. In particular, 8-methylquinolines have been found as good substrates for sp3 C–H functionalization due to its ability to form cyclometalated complexes. Succinimides have been recognized as privileged structural cores found in a number of bioactive natural products, pharmaceuticals, and functional materials. Furthermore, the reduced derivatives such as pyrrolidines and γ-lactams have been also found in a large number of pharmaceutical relevant molecules, thus making them one of the most important and promising compounds. We herein describe the first C(sp3)–H activation of 8-methylquinolines and subsequent functionalization with maleimides to afford various succinimide derivatives.

Keywords: C(sp3)–H activation, 8-methylquinolines, maleimides, succinimides

Procedia PDF Downloads 198

Authors: N. D. Iswarya, M. A. Maluk Mohamed, N. Vijaya

Abstract:

Grid is infrastructure that allows the deployment of distributed data in large size from multiple locations to reach a common goal. Scheduling data intensive applications becomes challenging as the size of data sets are very huge in size. Only two solutions exist in order to tackle this challenging issue. First, computation which requires huge data sets to be processed can be transferred to the data site. Second, the required data sets can be transferred to the computation site. In the former scenario, the computation cannot be transferred since the servers are storage/data servers with little or no computational capability. Hence, the second scenario can be considered for further exploration. During scheduling, transferring huge data sets from one site to another site requires more network bandwidth. In order to mitigate this issue, this work focuses on incorporating cognitive science in scheduling. Cognitive Science is the study of human brain and its related activities. Current researches are mainly focused on to incorporate cognitive science in various computational modeling techniques. In this work, the problem solving approach of human brain is studied and incorporated during the data intensive scheduling in grid environments. Here, a cognitive engine is designed and deployed in various grid sites. The intelligent agents present in CE will help in analyzing the request and creating the knowledge base. Depending upon the link capacity, decision will be taken whether to transfer data sets or to partition the data sets. Prediction of next request is made by the agents to serve the requesting site with data sets in advance. This will reduce the data availability time and data transfer time. Replica catalog and Meta data catalog created by the agents assist in decision making process.

Keywords: data grid, grid workflow scheduling, cognitive artificial intelligence

Procedia PDF Downloads 368

Authors: Senthil Rajan Dharmalingam, Shamala Nadaraju, Srinivasan Ramamurthy

Abstract:

Doxorubicin is the most widely used anticancer drugs in chemotherapy treatment. However, problems related to the development of multidrug resistance (MDR) and acute cardiotoxicity have led researchers to investigate alternative forms of administering doxorubicin for cancer therapy. Several methods have been attempted to overcome MDR, including the co-administration of a chemosensitizer inhibiting the efflux caused by ATP binding cassette transporters with anticancer drugs, and the bypass of the efflux mechanism. Co encapsulation of doxorubicin (Dox) and cyclosporine A (CSA) into poly (DL-lactide-co-glycolide) nanoparticles was emulsification-solvent evaporation method using polyvinyl alcohol as emulsion stabilizers. The Dox-CSA loaded nanoparticles were evaluated for particle size, zeta potential and PDI by light scattering analysis and thermal characterizations by differential scanning calorimetry (DSC). Loading efficiency (LE %) and in-vitro dissolution samples were evaluated by developed and validated HPLC method. The optimum particle size obtained is 298.6.8±39.4 nm and polydispersity index (PDI) is 0.098±0.092. Zeta potential is found to be -29.9±4.23. Optimum pH to increase Dox LE% was found 7.1 which gave 42.5% and 58.9% increase of LE% for pH 6.6 and pH 8.6 compared respectively. LE% achieved for Dox is 0.07±0.01 % and CSA is 0.09±0.03%. Increased volume of PVA and weight of PLGA shows increase in size of nanoparticles. DSC thermograms showed shift in the melting peak for the nanoparticles compared to Dox and CSA indicating encapsulation of drugs. In conclusion, these preliminary studies showed the feasibility of PLGA nanoparticles to entrap Dox and CSA and require future in-vivo studies to be performed to establish its potential.

Keywords: doxorubicin, cyclosporine, PLGA, nanoparticles

Procedia PDF Downloads 435

Authors: D. J. Kalita

Abstract:

Cancer is one of the prime causes of early death worldwide. Mutation of the gene involve in DNA repair and damage, like BRCA2 (Breast cancer gene two) genes, can be detected efficiently by PCR-RFLP to early breast cancer diagnosis and adopt the suitable method of treatment. Host Defense Peptide can be used as blueprint for the design and synthesis of novel anticancer drugs to avoid the side effect of conventional chemotherapy and chemo resistance. The change at nucleotide position 392 of a -› c in the cancer sample of dog mammary tumour at BRCA2 (exon 7) gene lead the creation of a new restriction site for SsiI restriction enzyme. This SNP may be a marker for detection of canine mammary tumour. Support vector machine (SVM) algorithm was used to design and predict the anticancer peptide from the mature functional peptide. MTT assay of MCF-7 cell line after 48 hours of post treatment showed an increase in the number of rounded cells when compared with untreated control cells. The ability of the synthesized peptide to induce apoptosis in MCF-7 cells was further investigated by staining the cells with the fluorescent dye Hoechst stain solution, which allows the evaluation of the nuclear morphology. Numerous cells with dense, pyknotic nuclei (the brighter fluorescence) were observed in treated but not in control MCF-7 cells when viewed using an inverted phase-contrast microscope. Thus, PCR-RFLP is one of the attractive approach for early diagnosis, and synthetic cationic peptide can be used for the treatment of canine mammary tumour.

Keywords: cancer, cationic peptide, host defense peptides, Breast cancer genes

Procedia PDF Downloads 60

Authors: Demet Yavuz

Abstract:

Freeze-thaw cycles are one of the greatest threats to concrete durability. Lately, protection against this threat excites scientists’ attention. Air-entraining admixtures have been widely used to produce freeze-thaw resistant at concretes. The use of air-entraining agents (AEAs) enhances not only freeze-thaw endurance but also the properties of fresh concrete such as segregation, bleeding and flow ability. This paper examines the effects of air-entraining on compressive strength of concrete. Air-entraining is used between 0.05% and 0.4% by weight of cement. One control and four fiber reinforced concrete mixes are prepared and three specimens are tested for each mix. It is concluded from the test results that when air entraining is increased the compressive strength of concrete reduces for all mixes with AEAs.

Keywords: concrete, air-entraining, compressive strength, mechanical properties

Procedia PDF Downloads 244

Authors: Yasemin Seki, Aysun Akşit

Abstract:

The goal of this research is to modify the surface characterization of jute yarns with different chemical agents to improve the compatibility with a non-polar polymer, polypropylene, when used as reinforcement. A literature review provided no knowledge on surface treatment of jute fibers with sodium perborate trihydrate. This study also aims to compare the efficiency of sodium perborate trihydrate on jute fiber treatment with other commonly used chemical agents. Accordingly, jute yarns were treated with 0.02% potassium dichromate (PD), potassium permanganate (PM) and sodium perborate trihydrate (SP) aqueous solutions in order to enhance interfacial compatibility with polypropylene in this study. The effect of treatments on surface topography, surface chemistry and interfacial shear strength of jute yarns with polypropylene were investigated. XPS results revealed that surface treatments enhanced surface hydrophobicity by increasing C/O ratios of fiber surface. Surface roughness values increased with the treatments. The highest interfacial adhesion with polypropylene was achieved after SP treatment by providing the highest surface roughness values and hydrophobic character of jute fiber.

Keywords: jute, chemical modification, sodium perborate, polypropylene

Procedia PDF Downloads 482

Authors: Funmilola O. Omoya, Abdul O. Momoh

Abstract:

Malaria constitutes one of the major health problems in Nigeria. One of the reasons attributed for the upsurge was the development of resistance of Plasmodium falciparum and the emergence of multi-resistant strains of the parasite to anti-malaria drugs. A continued search for other effective, safe and cheap plant-based anti-malaria agents thus becomes imperative in the face of these difficulties. The objective of this study is therefore to evaluate the in vivo anti-malarial efficacy of ethanolic extracts of Chromolaena odorata and Androgaphis paniculata leaves. The two plants were evaluated for their anti-malaria efficacy in vivo in a 4-day curative test assay against Plasmodium berghei strain in mice. The group treated with 500mg/ml dose of ethanolic extract of A. paniculata plant showed parasite suppression with increase in Packed Cell Volume (PCV) value except day 3 which showed a slight decrease in PCV value. During the 4-day curative test, an increase in the PCV values, weight measurement and zero count of Plasmodium berghei parasite values was recorded after day 3 of drug administration. These results obtained in group treated with A. paniculata extract showed anti-malarial efficacy with higher mortality rate in parasitaemia count when compared with Chromolaena odorata group. These results justify the use of ethanolic extracts of A. paniculata plant as medicinal herb used in folklore medicine in the treatment of malaria.

Keywords: anti-malaria, curative, plant-based anti-malaria agents, biology

Procedia PDF Downloads 264

Authors: Yeseul Park

Abstract:

Biopolymers produced by organisms highly contribute to the production of metal sulfides, both in extracellular and intracellular biomineralization. We discovered a new type of intracellular biomineral composed of copper sulfide in the periplasm of a sulfate-reducing bacterium. We suggest that the structural features of biomineral composed of 1-2 nm subgrains are based on biopolymer-based capping agents and an organic compartment. We further compare with other types of metal sulfide biominerals.

Keywords: biomineralization, copper sulfide, metal sulfide, biopolymer, capping agent

Procedia PDF Downloads 83

Authors: Debasmita Mukhopadhyay, Manika Pal Bhadra

Abstract:

MiRNAs contribute to oncogenesis either as tumor suppressors or oncogenes. Hence, discovery of miRNA-based therapeutics are imperative to ameliorate cancer. Modulation of miRNA maturation is accomplished via several therapeutic agents, including small molecules and oligonucleotides. Due to the attractive pharmacokinetic properties of small molecules over oligonucleotides, we set to identify small molecule inhibitors of a metastasis-inducing microRNA. Cytotoxicity profile of aza-flavanone C1 was analyzed in a panel of breast cancer cells employing the NCI-60 screen protocols. Flow cytometry, immunofluorescence and western blotting of apoptotic or EMT markers were performed to analyze the effect of C1. A dual luciferase assay unequivocally suggested that C1 repressed endogenous miR-10b in MDA-MB-231 cells. A derivative of aza-flavanone C1 is shown as a strong inhibitor miR-10b. Blockade of miR-10b by C1 resulted in decreased expression of miR-10b targets in an aggressive breast cancer cell line model, MDA-MB-231. Abrogation of TWIST1, an EMT-inducing transcription factor also contributed to C1 mediated apoptosis. Moreover C1 exhibited a specific and selective down-regulation of miR-10b and did not function as a general inhibitor of miRNA biogenesis or other oncomiRs of breast carcinoma. Aza-flavanone congener C1 functions as a potent inhibitor of the metastasis-inducing microRNA, miR-10b. Our present study provides evidence for targeting metastasis-inducing microRNA, miR-10b with a derivative of Aza-flavanone. Better pharmacokinetic properties of small molecules place them as attractive agents compared to nucleic acids based therapies to target miRNA. Further work, in generating analogues based on aza-flavanone moieties will significantly improve the affinity of the small molecules to bind miR-10b. Finally, it is imperative to develop small molecules as novel miRNA-therapeutics in the fight against cancer.

Keywords: breast cancer, microRNA, metastasis, EMT

Procedia PDF Downloads 517

Authors: Mehrnaz Mostafavi

Abstract:

Nanoliposomes, minute lipid-based vesicles at the nano-scale, show promise in the realm of photothermal therapy (PTT). This study presents an extensive overview of nanoliposomes in PTT, exploring their distinct attributes and the significant progress in this therapeutic methodology. The research delves into the fundamental traits of nanoliposomes, emphasizing their adaptability, compatibility with biological systems, and their capacity to encapsulate diverse therapeutic substances. Specifically, it examines the integration of light-absorbing materials, like gold nanoparticles or organic dyes, into nanoliposomal formulations, enabling their efficacy as proficient agents for photothermal treatment Additionally, this paper elucidates the mechanisms involved in nanoliposome-mediated PTT, highlighting their capability to convert light energy into localized heat, facilitating the precise targeting of diseased cells or tissues. This precise regulation of light absorption and heat generation by nanoliposomes presents a non-invasive and precisely focused therapeutic approach, particularly in conditions like cancer. The study explores advancements in nanoliposomal formulations aimed at optimizing PTT outcomes. These advancements include strategies for improved stability, enhanced drug loading, and the targeted delivery of therapeutic agents to specific cells or tissues. Furthermore, the paper discusses multifunctional nanoliposomal systems, integrating imaging components or targeting elements for real-time monitoring and improved accuracy in PTT. Moreover, the review highlights recent preclinical and clinical trials showcasing the effectiveness and safety of nanoliposome-based PTT across various disease models. It also addresses challenges in clinical implementation, such as scalability, regulatory considerations, and long-term safety assessments. In conclusion, this paper underscores the substantial potential of nanoliposomes in advancing PTT as a promising therapeutic approach. Their distinctive characteristics, combined with their precise ability to convert light into heat, offer a tailored and efficient method for treating targeted diseases. The encouraging outcomes from preclinical studies pave the way for further exploration and potential clinical applications of nanoliposome-based PTT.

Keywords: nanoliposomes, photothermal therapy, light absorption, heat conversion, therapeutic agents, targeted delivery, cancer therapy

Procedia PDF Downloads 52

Authors: Hoda Sabry Othman, Randa Helmy Swellem, Galal Abd El-Moein Nawwar

Abstract:

N-cyanoacetyl glycine is a reactive polyfunctional precursor for synthesis of new difficult accessible compounds including pyridones, thiazolopyridine and others. The key step of this protocol is the formation of different ylidines which underwent Michael addition with carbon nucleophiles affording various heterocyclic compounds. Selected compounds underwent pharmacological evaluation, in vitro against two cell lines; breast cell line (MCF-7),and liver cell line(HEPG2). Compounds 14, 15a and 16 showed IC50 values 8.93, 8.18 and 8.03 (µ/ml) respectively for breast cell line (MCF-7), while the standard drug (Tamoxifen) revealed IC50 8.31. With respect to the liver cell line (HEPG2), compounds 14 and 15a revealed IC50 18.4 and 13.6(µ/ml) respectively while the IC50 of the standard drug(5-Flurouracil) is 25(µ/ml). The antimicrobial activity was also screened and revealed that oxime 7 and ylidine 9f showed a broad-spectrum activity.

Keywords: antitumor, cyanoacetyl glycine, heterocycles, pyridones

Procedia PDF Downloads 301

Authors: Soheir Mohamed Fathey

Abstract:

Biofilms are complex biological communities which are hard to be eliminated by conventional antibiotic administration and implemented in eighty percent of humans infections. Green remedies have been used for centuries and have shown obvious effects in hindering and combating microbial biofilm infections. Nowadays, there has been a growth in the number of researches on the anti-biofilm performance of natural agents such as plant essential oil (EOs) and propolis. In this study, we investigated the antibiofilm performance of various natural agents, including four essential oils (EOs), cinnamon (Cinnamomum cassia), tea tree (Melaleuca alternifolia), and clove (Syzygium aromaticum), as well as propolis versus the biofilm of both Gram-positive pathogenic bacterium Staphylococcus aureus and Gram-negative pathogenic bacterium Pseudomonas aeruginosa which are major human and animal pathogens rendering a high risk due to their biofilm development ability. The antibiofilm activity of the tested agents was evaluated by crystal violet staining assay and detected by scanning electron and fluorescent microscopy. Antibiofilm performance declared a potent effect of the tested products versus the tested bacterial biofilms.

Keywords: biofilm, essential oils, electron microscopy, fluorescent

Procedia PDF Downloads 63

Authors: Yani Shi, Jiaqi Yan

Abstract:

A new product is important for companies to extend consumers and manifest competitiveness. New product often involves new features that consumers might not be familiar with while it may also have a competitive advantage to attract consumers compared to established products. However, although most online retailers employ recommendation agents (RA) to influence consumers’ product choice decision, recommended new products are not accepted and chosen as expected. We argue that it might also be caused by providing a new product recommendation in the wrong way at the wrong time. This study seeks to discuss how new product evaluations sourced from third parties could be employed in RAs as evidence of the superiority for the new product and how the new product recommendation could be provided to a consumer at the right time so that it can be accepted and finally chosen during the consumer’s decision-making process. A 2*2 controlled laboratory experiment was conducted to understand the selection of new product recommendation sources and recommendation timing. Human subjects were randomly assigned to one of the four treatments to minimize the effects of individual differences on the results. Participants were told to make purchase choices from our product categories. We find that a new product recommended right after a similar existing product and with the source of the expert review will be more likely to be accepted. Based on this study, both theoretical and practical contributions are provided regarding new product recommendation.

Keywords: new product recommendation, recommendation timing, recommendation source, recommendation agents

Procedia PDF Downloads 128

Authors: Grzegorz Swiderski, Agata Jablonska-Trypuc, Natalia Popow, Renata Swislocka, Wlodzimierz Lewandowski

Abstract:

Doxorubicin belongs to the group of anthracycline antitumor antibiotics. Because of the wide spectrum of actions, it is one of the most widely used anthracycline antibiotics, including the treatment of breast, ovary, bladder, lung cancers as well as neuroblastoma, lymphoma, leukemia and myeloid leukemia. Antitumor activity of doxorubicin is based on the same mechanisms as for most anthracyclines. Like the metal ions affect the nucleic acids on many biological processes, so the environment of the metal chelates of antibiotics can have a significant effect on the pharmacological properties of drugs. Complexation of anthracyclines with metal ions may contribute to the production of less toxic compounds. In the framework of this study, the composition of complexes obtained in aqueous solutions of doxorubicin with metal ions (Cu2+ and Zn2+). Complexation was analyzed by spectrophotometric titration in aqueous solution at pH 7.0. The pH was adjusted with 0.02M Tris-HCl buffer. The composition of the complexes found was Cu: doxorubicin (1: 2) and a Zn: doxorubicin (1: 1). The effect of Dox, Dox-Cu and Dox-Zn was examined in MCF-7 breast cancer cell line, which were obtained from American Type Culture Collection (ATCC). The compounds were added to the cultured cells for a final concentration in the range of 0,01µM to 0,5µM. The number of MCF-7 cells with division into living and dead, was determined by direct counts of cells with the use of trypan blue dye using LUNA Logos Biosystems cell counter. ApoTox-Glo Triplex Assay (Promega, Madison, Wisconsin, USA) was used according to the manufacturer’s instructions to measure the MCF-7 cells’ viability, cytotoxicity and apoptosis. We observed a decrease in cells proliferation in a dose-dependent manner. An increase in cytotoxicity and decrease in viability in the ApoTox Triplex assay was also showed for all tested compounds. Apoptosis, showed as caspase 3/7 activation, was observed only in Dox treatment. In Dox-Zn and Dox-Cu caspase 3/7 activation was not observed. This work was financially supported by National Science Centre, Poland, under the research project number 2014/13/B/NZ7/02 352.

Keywords: anticancer properties, anthracycline antibiotic, doxorubicine, metal complexes

Procedia PDF Downloads 251

Authors: Shradha S. Binani, Pravin S. Bodke, Ravi V. Joat

Abstract:

An efficient method has been described for the synthesis of 6-(substituted aryl)-4-(2'- hydroxy-5'-chlorophenyl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antibacterial and antifungal agents. The diketones of title compounds were synthesized in four steps and subsequently these diketones were further reacted with thiourea in the presence of DMF, which led to the formation of dihydropyrimidine derivatives 5 (a-f). Compounds 5 (a-f) were screened for their in vitro antibacterial and antifungal activity by agar well method. Compounds 5b, 5c, 5e, and 5f were exhibited significant antimicrobial potential against tested strains at 50ug/ml and 100ug/ml concentrations. Six novel dihydropyrimidine analogues have been synthesized, characterized and found to be promising antibacterial and antifungal agents.

Keywords: diketones, dihyropyrimidine, antimicrobial activity, thiol group

Procedia PDF Downloads 403

Authors: Anita Vidacs, Csaba Vagvolgyi, Judit Krisch

Abstract:

The attachment of microorganisms to different surfaces and the development of biofilms can lead to outbreaks of food-borne diseases and economic losses due to perished food. In food processing environments, bacterial communities are generally formed by mixed cultures of different species. Plants are sources of several antimicrobial substances that may be potential candidates for the development of new disinfectants. We aimed to investigate cinnamon (Cinnamomum zeylanicum), marjoram (Origanum majorana), and thyme (Thymus vulgaris). Essential oils and their major components (cinnamaldehyde, terpinene-4-ol, and thymol) on four-species biofilms of E. coli, L. monocytogenes, P. putida, and S. aureus. Experiments had three parts: (i) determination of minimum bactericide concentration and the killing time with microdilution methods; (ii) elimination of the four-species 24– and 168-hours old biofilm from stainless steel, polypropylene, tile and wood surfaces; and (iii) comparing the disinfectant effect with industrial used per-acetic based sanitizer (HC-DPE). E. coli and P. putida were more resistant to investigated essential oils and their main components in biofilm, than L. monocytogenes and S. aureus. These Gram-negative bacteria were detected on the surfaces, where the natural based disinfectant had not total biofilm elimination effect. Most promoted solutions were the cinnamon essential oil and the terpinene-4-ol that could eradicate the biofilm from stainless steel, polypropylene and even from tile, too. They have a better disinfectant effect than HC-DPE. These natural agents can be used as alternative solutions in the battle against bacterial biofilms.

Keywords: biofilm, essential oils, surfaces, terpinene-4-ol

Procedia PDF Downloads 74

Authors: Ibrahim A. Aref, Tarek El-Mihoub, Khadiga Ben Musa

Abstract:

This paper presents Carrier Sense Multiple Access (CSMA) communication model based on SoC design methodology. Such model can be used to support the modelling of the complex wireless communication systems, therefore use of such communication model is an important technique in the construction of high performance communication. SystemC has been chosen because it provides a homogeneous design flow for complex designs (i.e. SoC and IP based design). We use a swarm system to validate CSMA designed model and to show how advantages of incorporating communication early in the design process. The wireless communication created through the modeling of CSMA protocol that can be used to achieve communication between all the agents and to coordinate access to the shared medium (channel).

Keywords: systemC, modelling, simulation, CSMA

Procedia PDF Downloads 392

Authors: Ankit Nagar, Dinesh Kumar Nauriyal, S. P. Singh

Abstract:

This paper examines farmers' perceptions of the efficacy of extension services in equipping them with the necessary information and skills required to maximise agricultural productivity. It is based on primary data collected through an interview schedule in India's Western Uttar Pradesh region. It uses descriptive statistics, factor analysis, and MANOVA to determine the typical farmer's view of an extension worker's technical prowess and behavioural traits, as well as the key factors associated with farmers' perception and the demographic characteristics that affect farmer's perception variations. The vast majority of farmers appear to consider extension personnel's efficiency and accessibility unfavourably. Farmers feel that extension personnel are well-trained notwithstanding their disagreements on the viability of their technical advice. Small and marginal farmers view the effectiveness, objectivity, and cooperativeness of extension agents less favourably than large farmers. This study proposes strategies such as routine follow-ups, practical demonstrations, and regular extension professional training camps as part of a holistic plan to increase farmer trust in the agricultural extension system. In addition, it proposes ensuring their accountability.

Keywords: agriculture extension, farmers’ perception, extension agents, factor analysis

Procedia PDF Downloads 83

Authors: Kheireddine El-Boubbou

Abstract:

Drug delivery to target human acute myeloid leukemia (AML) using a nanoparticulate chemotherapeutic formulation that can deliver drugs selectively to AML cancer is hugely needed. In this work, we report the development of a nanoformulation made of polymeric-stabilized multifunctional magnetic iron oxide nanoparticles (PMNP) loaded with the anticancer drug Doxorubicin (Dox) as a promising drug carrier to treat AML. Dox@PMNP conjugates simultaneously exhibited high drug content, maximized fluorescence, and excellent release properties. Nanoparticulate uptake and cell death following addition of Dox@PMNPs were then evaluated in different types of human AML target cells, as well as on normal human cells. While the unloaded MNPs were not toxic to any of the cells, Dox@PMNPs were found to be highly toxic to the different AML cell lines, albeit at different inhibitory concentrations (IC₅₀ values), but showed very little toxicity towards the normal cells. In comparison, free Dox showed significant potency concurrently to all the cell lines, suggesting huge potentials for the use of Dox@PMNPs as selective AML anticancer cargos. Live confocal imaging, fluorescence and electron microscopy confirmed that Dox is indeed delivered to the nucleus in relatively short periods of time, causing apoptotic cell death. Importantly, this targeted payload may potentially enhance the effectiveness of the drug in AML patients and may further allow physicians to image leukemic cells exposed to Dox@PMNPs using MRI.

Keywords: magnetic nanoparticles, drug delivery, acute myeloid leukemia, iron oxide, cancer nanotherapy

Procedia PDF Downloads 204

Authors: E. Mosiniewicz-Szablewska, P. Suchocki, P. C. Morais

Abstract:

Despite the significant progress in cancer treatment, there is a need to search for new therapeutic methods in order to minimize side effects. Chemotherapy, the main current method of treating cancer, is non-selective and has a number of limitations. Toxicity to healthy cells is undoubtedly the biggest problem limiting the use of many anticancer drugs. The problem of how to kill cancer without harming a patient can be solved by using organic selenium (IV) compounds. Organic selenium (IV) compounds are a new class of materials showing a strong anticancer activity. They are first organic compounds containing selenium at the +4 oxidation level and therefore they eliminate the multidrug-resistance for all tumor cell lines tested so far. These materials are capable of selectively killing cancer cells without damaging the healthy ones. They are obtained by the incorporation of selenous acid (H2SeO3) into molecules of fatty acids of sunflower oil and therefore, they are inexpensive to manufacture. Attaching these compounds to magnetic carriers enables their precise delivery directly to the tumor area and the simultaneous application of the magnetic hyperthermia, thus creating a huge opportunity to effectively get rid of the tumor without any side effects. Polylactic-co-glicolic acid (PLGA) nanocapsules loaded with maghemite (-Fe2O3) nanoparticles and organic selenium (IV) compounds are successfully prepared by nanoprecipitation method. In vitro antitumor activity of the nanocapsules were evidenced using murine melanoma (B16-F10), oral squamos carcinoma (OSCC) and murine (4T1) and human (MCF-7) breast lines. Further exposure of these cells to an alternating magnetic field increased the antitumor effect of nanocapsules. Moreover, the nanocapsules presented antitumor effect while not affecting normal cells. Magnetic properties of the nanocapsules were investigated by means of dc magnetization, ac susceptibility and electron spin resonance (ESR) measurements. The nanocapsules presented a typical superparamagnetic behavior around room temperature manifested itself by the split between zero field-cooled/field-cooled (ZFC/FC) magnetization curves and the absence of hysteresis on the field-dependent magnetization curve above the blocking temperature. Moreover, the blocking temperature decreased with increasing applied magnetic field. The superparamagnetic character of the nanocapsules was also confirmed by the occurrence of a maximum in temperature dependences of both real ′(T) and imaginary ′′ (T) components of the ac magnetic susceptibility, which shifted towards higher temperatures with increasing frequency. Additionally, upon decreasing the temperature the ESR signal shifted to lower fields and gradually broadened following closely the predictions for the ESR of superparamagnetoc nanoparticles. The observed superparamagnetic properties of nanocapsules enable their simple manipulation by means of magnetic field gradient, after introduction into the blood stream, which is a necessary condition for their use as magnetic drug carriers. The observed anticancer and superparamgnetic properties show that the magnetic nanocapsules loaded with organic selenium (IV) compounds should be considered as an effective material system for magnetic drug delivery and magnetohyperthermia inductor in antitumor therapy.

Keywords: cancer treatment, magnetic drug delivery system, nanomaterials, nanotechnology

Procedia PDF Downloads 176

Authors: Raquel Camprubí

Abstract:

Cultural tourism has been postulated as relevant motivation for tourist over the world during the last decades. In this context, museums are the main attraction for cultural tourists who are seeking to connect with the history and culture of the visited place. From the point of view of an urban destination, museums and other cultural resources are essential to have a strong tourist supply at the destination, in order to be capable of catching attention and interest of cultural tourists. In particular, museums’ challenge is to be prepared to offer the best experience to their visitors without to forget their mission-based mainly on protection of its collection and other social goals. Thus, museums individually want to be competitive and have good positioning to achieve their strategic goals. The life cycle of the destination and the level of maturity of its tourism product influence the need of tourism agents to cooperate and collaborate among them, in order to rejuvenate their product and become more competitive as a destination. Additionally, prior studies have considered an approach of different models of a public and private partnership, and collaborative and cooperative relations developed among the agents of a tourism destination. However, there are no studies that pay special attention to museums and the strategic alliances developed to obtain mutual benefits. Considering this background, the purpose of this study is to analyze in what extent museums of a given urban destination have established strategic links and relations among them, in order to improve their competitive position at both individual and destination level. In order to achieve the aim of this study, the city of Girona (Spain) and the museums located in this city are taken as a case study. Data collection was conducted using in-depth interviews, in order to collect all the qualitative data related to nature, strengthen and purpose of the relational ties established among the museums of the city or other relevant tourism agents of the city. To conduct data analysis, a Social Network Analysis (SNA) approach was taken using UCINET software. Position of the agents in the network and structure of the network was analyzed, and qualitative data from interviews were used to interpret SNA results. Finding reveals the existence of strong ties among some of the museums of the city, particularly to create and promote joint products. Nevertheless, there were detected outsiders who have an individual strategy, without collaboration and cooperation with other museums or agents of the city. Results also show that some relational ties have an institutional origin, while others are the result of a long process of cooperation with common projects. Conclusions put in evidence that collaboration and cooperation of museums had been positive to increase the attractiveness of the museum and the city as a cultural destination. Future research and managerial implications are also mentioned.

Keywords: cultural tourism, competitiveness, museums, Social Network analysis

Procedia PDF Downloads 92

Authors: Khadse Saurabh, Talele Gokul, Surana Sanjay

Abstract:

In an endeavor to find a new class of anti-inflammatory agents, a series of novel benzamides (ab1-ab16) were synthesized by utilizing some arylideneoxazolones (az1-az4) having 2-acetyloxyphenyl substitution on their second position. Structures of these synthesized compounds were confirmed by IR, 1H-NMR, 13C NMR, and HRMS. Among the tested benzamide compounds 3ab1, 3ab2, 3ab11, and 3ab16 showed promising anti-inflammatory activity with lessened propensity to cause gastro-intestinal hypermotility and ulceration when compared with standard Indomethacin. Virtual screening was performed by docking the designed compounds into the ATP binding site of COX-2 receptor to predict if these compounds have analogous binding mode to the COX-2 inhibitor.

Keywords: benzamides, anti-inflammatory, gastro-intestinal hypermotility, ulcerogenic activity, docking

Procedia PDF Downloads 411

Authors: Fatima Doganc, Hakan Goker

Abstract:

Benzimidazole moiety is an important pharmacophore and privileged structure for the medicinal chemists, since it exhibits various important biological activities. Some clinically used drugs have benzimidazole moiety, such as omeprazole, astemizole, albendazole and domperidone. 2-(4-tert-Butylphenyl)benzimidazole, is a PGC-1α transcriptional regulator shown to have beneficial effects in diabetic mice. We planned to modify the structure of this compound for developing new antidiabetic drug candidates. Hence, a series of guanidino or amidino, benzo/pyrido/pyrimidino-imidazole derivatives were freshly prepared. Mass, 1H-NMR, 13C-NMR, 2D-NMR spectroscopy techniques were used for the new derivatives to clarify their structures and their purity was controlled through the elemental analysis. Antidiabetic activity studies of the synthesized compounds are under the investigation.

Keywords: antidiabetic agents, benzimidazole, imidazopyridine, imidazopyrimidine

Procedia PDF Downloads 320

Authors: Shaker Alsharif, Xavier Banquy

Abstract:

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 418