Search results for: biological and pharmacological activity
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 7970

Search results for: biological and pharmacological activity

7670 Preparation and Biological Evaluation of 186/188Re-Chitosan for Radiosynovectomy

Authors: N. Ahmadi, H. Yousefnia, A. Bahrami-Samani

Abstract:

Chitosan is a natural and biodegradable polysaccharide with special characteristic for application in intracavital therapy. 166Ho-chitosan has been reported for the treatment of hepatocellular carcinoma and RSV with promising results. The aim of this study was to prepare 186/188Re-chitosan for radiosynovectomy purposes and investigate the probability of its leakage from the knee joint. 186/188Re was produced by neutron irradiation of the natural rhenium in a research reactor. Chemical processing was performed to obtain (186/188Re)-NaReO4- according to the IAEA manual. A stock solution of chitosan was prepared by dissolving in 1 % acetic acid aqueous solution (10 mg/mL). 1.5 mL of this stock solution was added to the vial containing the activity and the mixture was stirred for 5 min in the room temperature. The radiochemical purity of the complex was checked by the ITLC method, showing the purity of higher than 98%. Distribution of the radiolabeled complex was determined after intra-articular injection into the knees of rats. Excellent retention was observed in the joint with approximately no activity in the other organs.

Keywords: chitosan, leakage, radiosynovectomy, rhenium

Procedia PDF Downloads 317
7669 Synthesis and Biological Evaluation of Pyridine Derivatives as Antimicrobial Agents

Authors: Dagim Ali Hussen, Adnan A. Bekhit, Ariaya Hymete

Abstract:

In this study, several pyridine derivatives were synthesized and evaluated for their in vitro antimicrobial activity against gram-positive bacteria (S. aureus and B. Cereus), gram-negative bacteria (P. aeruginosa and E. coli) and fungus (C. albican and A niger). The intermediate chalcone derivative 2a,b was synthesized by condensation of pyrazole aldehydes 1a,b with acetophenone in alcoholic KOH. Cyclization of 2a,b with ethyl cyanoacetate ad ammonium acetate resulted in pyridine carbonitrile derivatives 3a,b. Furthermore, condensation of pyridine-4-carboxaldeyhe with different amino-derivatives gave rise to pyridine derivatives 5a,b, 6a,b. The oxadiazole derivative 7a was prepared by cyclization of 6a with acetic anhydride. Characterization of the synthesized compound was performed using IR, 1H NMR, 13C NMR spectra and elemental microanalyses. The antimicrobial results revealed that compounds 5a, 6b and 7a exhibited half fold antibacterial activity compared to ampicillin, against B. cereus. On the other hand, compound 3b showed an equivalent activity compared to miconazole against candida albican (CANDAL 03) and to clotrimazole against the clinical isolate candida albican 6647. Moreover, this compound 3b was further tested for its acute toxicity profile. The results showed that oral LD50 is more that 300 mg/kg and parentral LD50 is more than 100 mg/kg. Compound 3b is a good candidate for antifungal agent with good toxicity profile, and deserves more chemical derivatization and clinical study.

Keywords: antifungal, antimicrobial, Candida albican, pyridine

Procedia PDF Downloads 481
7668 Walnut (Juglans Regia) Extracts: Investigation of Antioxidant Effect, Total Phenols and Tyrosinase Inhibitory Activity

Authors: N. Saki, S. Nalbantoglu, M. Akin, G. Arabaci

Abstract:

Walnut has a great range of phenolic profile and it is used in Asia and Africa for treatment of many diseases and cancer. Phenolic compounds play a number of crucial roles in complex metabolism of plants and of also fruit trees. Consumption of certain phenolics in the food is considered beneficial for human nutrition. Phenolic compounds known as anti-radical inactivators with their high antioxidant activities and these activities play an important role in inhibition of multi-metal corrosion. Many common corrosion inhibitors that are still in use today are health hazards. Therefore, there is still an increased attention directed towards the development of environmentally compatible, nonpolluting corrosion inhibitors. The present study reports the total phenols content, antioxidant potentials and tyrosinase inhibitory activity of the walnut (Juglans regia L.) produced in Turkey. The anti-tyrosinase activity was investigated for walnut at 2 h extraction time and all extracts exhibited tyrosinase activity. The results of this study suggested that walnut can be used as an excellent, easily accessible source of natural antioxidant.

Keywords: antioxidant activity, Juglans Regia, total phenols, tyrosinase activity

Procedia PDF Downloads 281
7667 Synthesis and Antiproliferative Activity of 5-Phenyl-N3-(4-fluorophenyl)-4H-1,2,4-triazole-3,4-diamine Derivatives

Authors: L. Mallesha, P. Mallu, B. Veeresh

Abstract:

In the present study, 2, 6-diflurobenzohydrazide and 4-fluorophenylisothiocyanate were used as the starting materials to synthesize 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3, 4-diamine. Further, compound 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3,4-diamine reacted with fluoro substituted benzaldehydes to yield a series of Schiff bases. All the final compounds were characterized using IR, 1H NMR, 13C NMR, MS and elemental analyses. New compounds were evaluated for their antiproliferative effect using the MTT assay method against four human cancer cell lines (K562, COLO-205, MDA-MB231, and IMR-32) for the time period of 24 h. Among the series, few compounds showed good activity on all cell lines, whereas the other compounds in the series exhibited moderate activity.

Keywords: Schiff bases, MTT assay, antiproliferative activity, human cancer cell lines, 1, 2, 4-triazoles

Procedia PDF Downloads 345
7666 Differentiation of Drug Stereoisomers by Their Stereostructure-Selective Membrane Interactions as One of Pharmacological Mechanisms

Authors: Maki Mizogami, Hironori Tsuchiya, Yoshiroh Hayabuchi, Kenji Shigemi

Abstract:

Since drugs exhibit significant structure-dependent differences in activity and toxicity, their differentiation based on the mechanism of action should have implications for comparative drug efficacy and safety. We aimed to differentiate drug stereoisomers by their stereostructure-selective membrane interactions underlying pharmacological and toxicological effects. Biomimetic lipid bilayer membranes were prepared with phospholipids and sterols (either cholesterol or epicholesterol) to mimic the lipid compositions of neuronal and cardiomyocyte membranes and to provide these membranes with the chirality. The membrane preparations were treated with different classes of stereoisomers at clinically- and pharmacologically-relevant concentrations (25-200 μM), followed by measuring fluorescence polarization to determine the membrane interactivity of drugs to change the physicochemical property of membranes. All the tested drugs acted on lipid bilayers to increase or decrease the membrane fluidity. Drug stereoisomers could not be differentiated when interacting with the membranes consisting of phospholipids alone. However, they stereostructure-selectively interacted with neuro-mimetic and cardio-mimetic membranes containing 40 mol% cholesterol ((3β)-cholest-5-en-3-ol) to show the relative potencies being local anesthetic R(+)-bupivacaine > rac-bupivacaine > S(‒)-bupivacaine, α2-adrenergic agonistic D-medetomidine > rac-medetomidine > L-medetomidine, β-adrenergic antagonistic R(+)-propranolol > rac-propranolol > S(–)-propranolol, NMDA receptor antagonistic S(+)-ketamine > rac-ketamine, analgesic monoterpenoid (+)-menthol > (‒)-menthol, non-steroidal anti-inflammatory S(+)-ibuprofen > rac-ibuprofen > R(‒)-ibuprofen, and bioactive flavonoid (+)-epicatechin > (‒)-epicatechin. All of the order of membrane interactivity were correlated to those of beneficial and adverse effects of the tested stereoisomers. In contrast, the membranes prepared with epicholesterol ((3α)-chotest-5-en-3-ol), an epimeric form of cholesterol, reversed the rank order of membrane interactivity to be S(‒)-enantiomeric > racemic > R(+)-enantiomeric bupivacaine, L-enantiomeric > racemic > D-enantiomeric medetomidine, S(–)-enantiomeric > racemic > R(+)-enantiomeric propranolol, racemic > S(+)-enantiomeric ketamine, (‒)-enantiomeric > (+)-enantiomeric menthol, R(‒)-enantiomeric > racemic > S(+)-enantiomeric ibuprofen, and (‒)-enantiomeric > (+)-enantiomeric epicatechin. The opposite configuration allows drug molecules to interact with chiral sterol membranes enantiomer-selectively. From the comparative results, it is speculated that a 3β-hydroxyl group in cholesterol is responsible for the enantioselective interactions of drugs. In conclusion, the differentiation of drug stereoisomers by their stereostructure-selective membrane interactions would be useful for designing and predicting drugs with higher activity and/or lower toxicity.

Keywords: chiral membrane, differentiation, drug stereoisomer, enantioselective membrane interaction

Procedia PDF Downloads 201
7665 Analysis of Cardiac Health Using Chaotic Theory

Authors: Chandra Mukherjee

Abstract:

The prevalent knowledge of the biological systems is based on the standard scientific perception of natural equilibrium, determination and predictability. Recently, a rethinking of concepts was presented and a new scientific perspective emerged that involves complexity theory with deterministic chaos theory, nonlinear dynamics and theory of fractals. The unpredictability of the chaotic processes probably would change our understanding of diseases and their management. The mathematical definition of chaos is defined by deterministic behavior with irregular patterns that obey mathematical equations which are critically dependent on initial conditions. The chaos theory is the branch of sciences with an interest in nonlinear dynamics, fractals, bifurcations, periodic oscillations and complexity. Recently, the biomedical interest for this scientific field made these mathematical concepts available to medical researchers and practitioners. Any biological network system is considered to have a nominal state, which is recognized as a homeostatic state. In reality, the different physiological systems are not under normal conditions in a stable state of homeostatic balance, but they are in a dynamically stable state with a chaotic behavior and complexity. Biological systems like heart rhythm and brain electrical activity are dynamical systems that can be classified as chaotic systems with sensitive dependence on initial conditions. In biological systems, the state of a disease is characterized by a loss of the complexity and chaotic behavior, and by the presence of pathological periodicity and regulatory behavior. The failure or the collapse of nonlinear dynamics is an indication of disease rather than a characteristic of health.

Keywords: HRV, HRVI, LF, HF, DII

Procedia PDF Downloads 399
7664 Phytochemical Profiles and Antioxidant Activity of Selected Indigenous Vegetables in Northern Mindanao, Philippines

Authors: Renee P. Baang, Romeo M. del Rosario, Nenita D. Palmes

Abstract:

The crude methanol extracts of five indigenous vegetables namely, Amarathus tricolor, Basella rubra L, Chochurus olitorius L., Ipomea batatas, and Momordica chuchinensis L., were examined for their phytochemical profile and antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The values for DPPH radical scavenging activity ranged from 7.6-89.53% with B. rubra and I. batatas having the lowest and highest values, respectively. The total flavonoid content of all five indigenous vegetables ranged from 74.65-277.3 mg quercetin equivalent per gram of dried vegetable material while the total phenolic content ranged from 1.93-6.15 mg gallic acid equivalent per gram dried material. Phytochemical screening revealed the presence of steroids, flavonoids, saponins, tannins, carbohydrates and reducing sugars, which may also be associated with the antioxidant activity shown by these indigenous vegetables.

Keywords: antioxidant, DPPH radical scavenging activity, Philippine İndigenous vegetables, phytochemical screening

Procedia PDF Downloads 314
7663 Validity of Clinical Disease Activity Index (CDAI) to Evaluate the Disease Activity of Rheumatoid Arthritis Patients in Sri Lanka: A Prospective Follow up Study Based on Newly Diagnosed Patients

Authors: Keerthie Dissanayake, Chandrika Jayasinghe, Priyani Wanigasekara, Jayampathy Dissanayake, Ajith Sominanda

Abstract:

The routine use of Disease Activity Score-28 (DAS28) to assess the disease activity in rheumatoid arthritis (RA) is limited due to its dependency on laboratory investigations and the complex calculations involved. In contrast, the clinical disease activity index (CDAI) is simple to calculate, which makes the "treat to target" strategy for the management of RA more practical. We aimed to assess the validity of CDAI compared to DAS28 in RA patients in Sri Lanka. A total of 103 newly diagnosed RA patients were recruited, and their disease activity was calculated using DAS 28 and CDAI during the first visit to the clinic (0 months) and re-assessed at 4 and 9 months of the follow-up visits. The validity of the CDAI, compared to DAS 28, was evaluated. Patients had a female preponderance (6:1) and a short symptom duration (mean = 6.33 months). The construct validity of CDAI, as assessed by Cronbach's α test, was 0.868. Convergent validity was assessed by correlation and Kappa statistics. Strong positive correlations were observed between CDAI and DAS 28 at the baseline (0 months), 4, and 9 months of evaluation (Spearman's r = 0.9357, 0.9354, 0.9106, respectively). Moderate-good inter-rater agreements between the DAS-28 and CDAI were observed (Weighted kappa of 0.660, 0.519, and 0.741 at 0, 4, and 9 months respectively). Discriminant validity, as assessed by ROC curves at 0, 4th, and 9th months of the evaluation, showed the area under the curve (AUC) of 0.958, 0.985, and 0.914, respectively. The suggested cut-off points for different CDAI disease activity categories according to ROC curves were ≤ 2 (Remission), >2 to ≤ 5 (low), >5 to ≤ 18 (moderate), > 18 (high). These findings indicate that the CDAI has good concordance with DAS 28 in assessing the disease activity in RA patients in this study sample.

Keywords: rheumatoid arthritis, CDAI, disease activity, Sri Lanka, validation

Procedia PDF Downloads 125
7662 Anti-inflammatory and Antioxidant Activity of Heliotropium indicum Linn. Used for Cancer Patients Treatment

Authors: Jitpisute Chunthorng-Orn, Thana Juckmeta, Onmanee Prajuabjinda, Arunporn Itharat

Abstract:

Inflammation and oxidative stress work together to produce symptoms in cancer patients. The whole part of it is used as a preparation to treat cancer patients in Khampramong temple which has been a place of treatment and palliative care for cancer patients since 2005. Thus, the objective of this study was to investigate anti-inflammatory and antioxidant activities of Heliotropium indicum extracts. Dried plant materials were extracted in a similar manner to those practiced by the Khampramong Temple i.e. maceration in 95% ethanol and boiling in water. For anti-inflammation activity, both extracts were tested for suppression of nitric oxide (NO) production in LPS-induced RAW 264.7 cells. They were also tested for antioxidant activity by DPPH radical scavenging assay. This study found that the ethanolic extract of Heliotropium indicum exhibited higher inhibitory activity of NO release than Indomethacin as a positive control (IC50 value of 24.17±2.12 and 34.67±6.23 μg/mL, respectively). For DPPH radical scavenging assay, the ethanolic extract also exhibited antioxidant activity but less than BHT as a antioxidant compound (EC50 values = 28.91±4.26 and 13.08±0.29 μg/mL, respectively). In contrast, its water extract had no inhibitory activity on NO release (IC50 > 100 μg/mL) and no inhibitory activity on DPPH radicals (EC50 values > 100 μg/mL). The results showed correlation between anti-inflammation and antioxidant activity and these results also support using this plant to treat cancer patients.

Keywords: Heliotropium indicum, RAW 264.7, DPPH, Khampramong Temple

Procedia PDF Downloads 514
7661 The Influence of Ligands Molecular Structure on the Antibacterial Activity of Some Metal Complexes

Authors: Sanja O. Podunavac-Kuzmanović, Lidija R. Jevrić, Strahinja Z. Kovačević

Abstract:

In last decade, metal-organic complexes have captured intensive attention because of their wide range of biological activities such as antibacterial, antifungal, anticancerous, antimicrobial and antiHIV. Therefore, it is of great importance for the development of coordination chemistry to explore the assembly of functional organic ligands with metal ion and to investigate the relationship between the structure and property. In view of our studies, we reasoned that benzimidazoles complexed to metal ions could act as a potent antibacterial agents. Thus, we have bioassayed the inhibitory potency of benzimidazoles and their metal salts (Co or Ni) against Gram negative bacteria Escherichia coli. In order to validate our in vitro study, we performed in silico studies using molecular docking software’s. The investigated compounds and their metal complexes (Co, Ni) showed good antibacterial activity against Escherichia coli. In silico docking studies of the synthesized compounds suggested that complexed benzimidazoles have a greater binding affinity and enhanced antibacterial activity in comparison with noncomplexed ligands. In view of their enhanced inhibitory properties we propose that the studied complexes can be used as potential pharmaceuticals. This study is financially supported by COST action CM1306 and the project No. 114-451-347/2015-02, financially supported by the Provincial Secretariat for Science and Technological Development of Vojvodina.

Keywords: benzimidazoles, complexes, antibacterial, Escherichia coli, metal

Procedia PDF Downloads 291
7660 Radiological Assessment of Fish Samples Due to Natural Radionuclides in River Yobe, North Eastern Nigeria

Authors: H. T. Abba, Abbas Baba Kura

Abstract:

Assessment of natural radioactivity of some fish samples in river Yobe was conducted, using gamma spectroscopy method with NaI(TI) detector. Radioactivity is phenomenon that leads to production of radiations, whereas radiation is known to trigger or induce cancer. The fish were analyzed to estimate the radioactivity (activity) concentrations due to natural radionuclides (Radium 222(226Ra), Thorium 232 (232Th) and Potassium 40 (40K)). The obtained result show that the activity concentration for (226Ra), in all the fish samples collected ranges from 15.23±2.45 BqKg-1 to 67.39±2.13 BqKg-1 with an average value of 34.13±1.34 BqKg-1. That of 232Th, ranges from 42.66±0.81 BqKg-1 to 201.18±3.82 BqKg-1, and the average value stands at 96.01±3.82 BqKg-1. The activity concentration for 40K, ranges between 243.3±1.56 BqKg-1 to 618.2±2.81 BqKg-1 and the average is 413.92±1.7 BqKg-1. This study indicated that average daily intake due to natural activity from the fish is valued at 0.913 Bq/day, 2.577Bq/day and 11.088 Bq/day for 226Ra, 232Th and 40K respectively. This shows that the activity concentration values for fish, shows a promising result with most of the fish activity concentrations been within the acceptable limits. However locations (F02, F07 and F12) fish, became outliers with significant values of 112.53μSvy-1, 121.11μSvy-1 and 114.32μSvy-1 effective Dose. This could be attributed to variation in geological formations within the river as while as the feeding habits of these fish. The work shows that consumers of fish from River Yobe have no risk of radioactivity ingestion, even though no amount of radiation is assumed to be totally safe.

Keywords: radiation, radio-activity, dose, radionuclides, river Yobe

Procedia PDF Downloads 290
7659 Isolation and Characterization of Actinophages Infecting Streptomyces scabies in Egypt

Authors: D. Zahran, M. AlKhazindar, M. Khalil, E. T. A. Sayed

Abstract:

Streptomyces scabies is a pathogenic actinomycete that infects potato crop causing severe production losses. Actinophages affect the composition and diversity of the bacterial population, thereby, can be used as a biological control. Samples of actinomycetes and phages were collected from different cultivated soils including farms of Faculty of Science, Faculty of Agriculture and different locations in Giza, Egypt. Actinomycetes were identified by using biochemical, morphological tests and molecular studies using 16S rRNA sequencing. Two specific phages (E1 and E2) against Streptomyces scabies and other hosts were isolated. Phages were identified using dilution end point (DEP), longevity in vitro (LIV), thermal inactivation point (TIP), host range and electron microscopy. PhageE1 was characterized by 10-8 (DEP),180 days(LIV), 95°C(TIP), narrow host range and electron microscopy showed ahead (59.9 nm) and neck (10.4nm). On the other hand phageE2 had 10-20 (DEP),180 days(LIV), 90°C(TIP), and the size of head was (67.2 nm) and tail (114nm). Antiviral activity was also studied using different chemicals (NaCL, KCL, CaCL2, BaCL2, CoCL2, AgNO3, ALCL3and HgCL2) with different concentrations and different plant extracts with different concentrations (star anise, tea, tillia, peppermint, ginger, cumin, chamomile, turmeric cinnamon, marjoram and black cumin). Both Phage E1and phage E2 were vulnerable to (cumin, ginger, chamomile, guavas leaves and star anise) but resistant to (Tillie, marjoram, fennelflower seeds, peppermint, and cinnamon).

Keywords: potato scab, actinophages, biological control, electron microscopy, TIP, DEP, LIV, antiviral activity

Procedia PDF Downloads 415
7658 The Influence of Physical Activity and Health Literacy on Depression Level of First and Second Turkish Generation Living in Germany

Authors: Ceren Akyüz, Ingo Froboese

Abstract:

Health literacy has gained importance with the further spread of the coronavirus disease (COVID-19) worldwide and has been associated with health status in various chronic diseases. Many studies indicate that mental health can be improved by low- or moderate-intensity activity, and several studies have been proposed to explain the relationship between physical activity and mental health. The aim of the present study is to investigate the levels of physical activity, health literacy, and depression in first- and- second generation Turkish people in Germany. The research consists of 434 participants (255 females, 179 males; age 38.09 ± 13.73). 40.8 % of participants are married, and 59.2 % of participants are single. Education levels are mostly at university level (54.8 %), and graduate level is 18.9 %. While 24.9 % of the participants are second generation, 75.1 % of participants are first generation. All analyses were stratified on gender, marital status, education, generation and income status, and five age categories: 18–30, 31–40, 41–50, 51–60, and 61–79, which were defined to account for age-specific trends while maintaining sufficient cell size for statistical analysis. A correlation of depression with physical activity and health literacy levels between first- and- second generation Turks in Germany was evaluated in order to find out whether there are significant differences between the two populations and demographic variables (gender, marital status, education, generation, income status) with carrying out questionnaires which are European Health Literacy Survey Questionnaire (HLS-EU-Q47), International Physical Activity Questionnaire ( IPAQ) and the Patient Health Questionnaire-9 (PHQ-9).

Keywords: health literacy, turks in germany, migrants, depression, physical activity

Procedia PDF Downloads 57
7657 Chemical Composition, Antioxidant and Antimicrobial Activities of the Essential Oils of Different Pinus Species from Kosovo

Authors: Fatbardhë Kurti, Giangiacomo Beretta, Behxhet Mustafa, Fabrizio Gelmini, Avni Hajdari

Abstract:

Chemical profile, antioxidant and antimicrobial activity of total and fractionated essential oils (EOs) (F1 – hexane, F2 – hexane/diethyl ether, F3 – diethyl ether) derived from five Pinus species (Pinus heldreichii, P. peuce, P. mugo, Pinus nigra, P. sylvestris), were investigated. The hydrodistilled EOs and their chromatographic fractions (direct solid phase extraction, SPE) were analysed by GC-MS and 112 compounds separated and identified. The main constituents were α-pinene, β-pinene, D-limonene, β-caryophyllene, germacrene D, bornyl acetate and 3-carene. The antioxidant activities of total EOs were lower than those of the corresponding fractions, with F2 the strongest in all cases. EOs and fractions showed different degrees of antibacterial efficacy against different microbial pathogens (moderately strong antimicrobial activity against C. albicans and C. krusei ,while low or no activity against E. faecalis and E. coli strains). The detected inhibition zones and MICs for the EOs and fractions were in the range of 14 -35 mm and 0.125 - 1% (v/v), respectively. The components responsible for the antioxidant and antimicrobial activity were oxygenated monoterpenes and sesquiterpenes recovered in the polar EO fractions. These activities seem to be regulated by reciprocal interactions among the different subclasses of phytochemical species present in the EOs.

Keywords: antagonism, antioxidant activity, antibacterial activity, essential oil, fractions, GC-MS, pinus

Procedia PDF Downloads 207
7656 Study on the Relationship between the Emission Property of Barium-Tungsten Cathode and Micro-Area Activity

Authors: Zhen Qin, Yufei Peng, Jianbei Li, Jidong Long

Abstract:

In order to study the activity of the coated aluminate barium-tungsten cathodes during activation, aging, poisoning and long-term use. Through a set of hot-cathode micro-area emission uniformity study device, we tested the micro-area emission performance of the cathode under different conditions. The change of activity of cathode micro-area was obtained. The influence of micro-area activity on the performance of the cathode was explained by the ageing model of barium-tungsten cathode. This helps to improve the design and process of the cathode and can point the way in finding the factors that affect life in the cathode operation.

Keywords: barium-tungsten cathode, ageing model, micro-area emission, emission uniformity

Procedia PDF Downloads 388
7655 Biological Evaluation and Molecular Modeling Study of Thiosemicarbazide Derivatives as Bacterial Type IIA Topoisomerases Inhibitors

Authors: Paweł Stączek, Tomasz Plech, Aleksandra Strzelczyk, Katarzyna Dzitko, Monika Wujec, Edyta Kuśmierz, Piotr Paneth, Agata Paneth

Abstract:

In this contribution, we will describe the inhibitory potency of nine thiosemicarbazide derivatives against bacterial type IIA topoisomerases, their antibacterial profile, and molecular modeling evaluation. We have found that one of the tested compounds, 4-benzoyl-1-(2-methyl-furan-3-ylcarbonyl) thiosemicarbazide, remarkably inhibits the activity of S. aureus DNA gyrase with the IC50 below 5 μM. Besides, this compound displays antibacterial activity on Staphylococcus spp. and E. faecalis at non-cytotoxic concentrations in mammalian cells, with minimal inhibitory concentrations (MICs) values at 25 μg/mL. Based on the enzymatic and molecular modeling studies we propose two factors, i.e. geometry of molecule and hydrophobic/hydrophilic balance as important molecular properties for developing thiosemicarbazide derivatives as potent Staphylococcus aureus DNA gyrase inhibitors.

Keywords: bioactivity, drug design, topoisomerase, molecular modeling

Procedia PDF Downloads 539
7654 The Formation of Motivational Sphere for Learning Activity under Conditions of Change of One of Its Leading Components

Authors: M. Rodionov, Z. Dedovets

Abstract:

This article discusses ways to implement a differentiated approach to developing academic motivation for mathematical studies which relies on defining the primary structural characteristics of motivation. The following characteristics are considered: features of realization of cognitive activity, meaning-making characteristics, level of generalization and consistency of knowledge acquired by personal experience. The assessment of the present level of individual student understanding of each component of academic motivation is the basis for defining the relevant educational strategy for its further development.

Keywords: learning activity, mathematics, motivation, student

Procedia PDF Downloads 398
7653 Leisure, Domestic or Professional Activities so as to Prevent Cognitive Decline: Results FreLE Longitudinal Study

Authors: Caroline Dupre, David Hupin, Christ Goumou, Francois Belan, Frederic Roche, Thomas Celarier, Bienvenu Bongue

Abstract:

Background: Previous cohorts have been notably criticized for not studying the different type of physical activity and not investigating household activities. The objective of this work was to analyse the relationship between physical activity and cognitive decline in older people living in the community. Impact of type of physical activity on the results has been realised. Methods: The study used data from the longitudinal and observational study , FrèLE (FRagility: Longitudinal Study of Expressions). The collected data included: socio-demographic variables, lifestyle, and health status (frailty, comorbidities, cognitive status, depression). Cognitive decline was assessed by using: Mini-Mental State Examination (MMSE) and Montreal Cognitive Assessment (MoCA). Physical activity was assessed by the Physical Activity Scale for the Elderly (PASE). This tool is structured in three sections: the leisure activity, domestic activity, and professional activity. Logistic regressions and proportional hazards regression models (Cox) were used to estimate the risk of cognitive disorders. Results: At baseline, the prevalence of cognitive disorders was 6.9% according to MMSE. In total, 1167 participants without cognitive disorders were included in the analysis. The mean age was 77.4 years, and 52.1% of the participants were women. After a 2 years long follow-up, we found cognitive disorders on 53 participants (4.5%). Physical activity at baseline is lower in older adults for whom cognitive decline was observed after two years of follow-up. Subclass analyses showed that leisure and domestic activities were associated with cognitive decline, but not professional activities. Conclusions: Analysis showed a relationship between cognitive disorders and type of physical activity. The current study will be completed by the MoCA for mild cognitive impairment. These findings compared to other ongoing studies, will contribute to the debate on the beneficial effects of physical activity on cognition.

Keywords: aging, cognitive function, physical activity, mixed models

Procedia PDF Downloads 106
7652 Optimised Path Recommendation for a Real Time Process

Authors: Likewin Thomas, M. V. Manoj Kumar, B. Annappa

Abstract:

Traditional execution process follows the path of execution drawn by the process analyst without observing the behaviour of resource and other real-time constraints. Identifying process model, predicting the behaviour of resource and recommending the optimal path of execution for a real time process is challenging. The proposed AlfyMiner: αyM iner gives a new dimension in process execution with the novel techniques Process Model Analyser: PMAMiner and Resource behaviour Analyser: RBAMiner for recommending the probable path of execution. PMAMiner discovers next probable activity for currently executing activity in an online process using variant matching technique to identify the set of next probable activity, among which the next probable activity is discovered using decision tree model. RBAMiner identifies the resource suitable for performing the discovered next probable activity and observe the behaviour based on; load and performance using polynomial regression model, and waiting time using queueing theory. Based on the observed behaviour αyM iner recommend the probable path of execution with; next probable activity and the best suitable resource for performing it. Experiments were conducted on process logs of CoSeLoG Project1 and 72% of accuracy is obtained in identifying and recommending next probable activity and the efficiency of resource performance was optimised by 59% by decreasing their load.

Keywords: cross-organization process mining, process behaviour, path of execution, polynomial regression model

Procedia PDF Downloads 312
7651 Critical Activity Effect on Project Duration in Precedence Diagram Method

Authors: Salman Ali Nisar, Koshi Suzuki

Abstract:

Precedence Diagram Method (PDM) with its additional relationships i.e., start-to-start, finish-to-finish, and start-to-finish, between activities provides more flexible schedule than traditional Critical Path Method (CPM). But, changing the duration of critical activities in PDM network will have anomalous effect on critical path. Researchers have proposed some classification of critical activity effects. In this paper, we do further study on classifications of critical activity effect and provide more information in detailed. Furthermore, we determine the maximum amount of time for each class of critical activity effect by which the project managers can control the dynamic feature (shortening/lengthening) of critical activities and project duration more efficiently.

Keywords: construction project management, critical path method, project scheduling, precedence diagram method

Procedia PDF Downloads 486
7650 Smartphone-Based Human Activity Recognition by Machine Learning Methods

Authors: Yanting Cao, Kazumitsu Nawata

Abstract:

As smartphones upgrading, their software and hardware are getting smarter, so the smartphone-based human activity recognition will be described as more refined, complex, and detailed. In this context, we analyzed a set of experimental data obtained by observing and measuring 30 volunteers with six activities of daily living (ADL). Due to the large sample size, especially a 561-feature vector with time and frequency domain variables, cleaning these intractable features and training a proper model becomes extremely challenging. After a series of feature selection and parameters adjustment, a well-performed SVM classifier has been trained.

Keywords: smart sensors, human activity recognition, artificial intelligence, SVM

Procedia PDF Downloads 124
7649 Implementing Activity-Based Costing in Architectural Aluminum Projects: Case Study and Lessons Learned

Authors: Amer Momani, Tarek Al-Hawari, Abdallah Alakayleh

Abstract:

This study explains how to construct an actionable activity-based costing and management system to accurately track and account the total costs of architectural aluminum projects. Two ABC models were proposed to accomplish this purpose. First, the learning and development model was introduced to examine how to apply an ABC model in an architectural aluminum firm for the first time and to be familiar with ABC concepts. Second, an actual ABC model was built on the basis of the results of the previous model to accurately trace the actual costs incurred on each project in a year, and to be able to provide a quote with the best trade-off between competitiveness and profitability. The validity of the proposed model was verified on a local architectural aluminum company.

Keywords: activity-based costing, activity-based management, construction, architectural aluminum

Procedia PDF Downloads 67
7648 Synthesis of 3,4-Dihydro-1H-Quinoxalin-2-Ones and 1H‑Quinolin-2-Ones and Evaluation of Their Anti-Bacterial Activity

Authors: Ali Amiri, Arash Esfandiari, Elham Zarenezhad

Abstract:

We report here an efficient and rapid method for the preparation of 3,4-dihydro-1H-quinoxalin-2-ones and 1H‑quinolin-2-ones that involves grinding of o-, m-, or p‑phenylenediamine and three dialkyl acetylenedicarboxylates using a pestle and mortar. This solvent-free approach requires only a few minutes of reaction time. This type of reaction is expected to be the most economical method since neither catalyst nor solvent is used. Finally, all synthesised compounds were screened for antimicrobial activity against two Gram-positive bacteria (Pseudomonas aeruginosa PTCC 1077, Escherichia coli PTCC1330) and two Gram-negative bacteria (Staphylococcus aureus PTCC 1133, Bacillus cereus PTCC 1015) and their activity. Compared with gentamycin and ampicillin as reference drugs for Gram-negative and Gram-positive bacteria, respectively. The minimum inhibitory concentration (MIC) of the synthesised compounds and reference drugs were determined by the microdilution method. Good antibacterial activity was observed for 3,4-dihydro-1H-quinoxalin-2-ones against all species of Gram-positive and Gram-negative bacteria, and1H‑quinolin-2-ones showed good antibacterial activity against two Gram-positive bacteria.

Keywords: quinolin, quinoxalin, anti-bacterial activity, minimum inhibitory concentration (MIC)

Procedia PDF Downloads 317
7647 Determination of Antimicrobial Effect and Essential Oil Composition Salvia verticillata L. Subsp. amasiaca

Authors: Tanju Teker, Yener Tekeli̇, Esra Karpuz

Abstract:

Salvia species are known as medicinal plant and often used in public. The antimicrobial effects and essential oil composition of Salvia verticillata L. subsp. amasiaca were determined. The antimicrobial activity is determined by using disk diffusion method against two Gram-positive bacteria, two Gram-negative bacteria and one kind of yeast and essential oil composition was determined by GC - MS. As a result of antimicrobial analysis while sample has shown very strong antimicrobial activity against Staphylococcus aureus, moderately effective against Pseudomonas aeruginosa and low effective against Enterococcus faecalis, it has not shown antimicrobial activity against Escherichia coli and C. albicans. Trans-caryophyllene (% 35.07), germacrene-d (% 10.98) and caryopyllene oxide (% 5.81) are the main components of essential oil composition.

Keywords: salvia, medicinal plant, antimicrobial activity, essential oil

Procedia PDF Downloads 430
7646 Investigating the Use of Seaweed Extracts as Biopesticides

Authors: Emma O’ Keeffe, Helen Hughes, Peter McLoughlin, Shiau Pin Tan, Nick McCarthy

Abstract:

Biosecurity is emerging as one of the most important issues facing the agricultural and forestry community. This is as a result of increased invasion from new pests and diseases with the main protocol for dealing with these species being the use of synthetic pesticides. However, these chemicals have been shown to exhibit negative effects on the environment. Seaweeds represent a vast untapped resource of bio-molecules with a broad range of biological activities including pesticidal. This project investigated both the antifungal and antibacterial activity of seaweed species against two problematic root rot fungi, Armillaria mellea and Heterobasidion annosum and ten quarantine bacterial plant pathogens including Xanthomonas arboricola, Xanthomonas fragariae, and Erwinia amylovora. Four seaweed species were harvested from the South-East coast of Ireland including brown, red and green varieties. The powdered seaweeds were extracted using four different solvents by liquid extraction. The poisoned food technique was employed to establish the antifungal efficacy, and the standard disc diffusion assay was used to assess the antibacterial properties of the seaweed extracts. It was found that extracts of the green seaweed exhibited antifungal activity against H. annosum, with approximately 50% inhibition compared to the negative control. The protectant activities of the active extracts were evaluated on disks of Picea sitchensis, a plant species sensitive to infection from H. annosum and compared to the standard chemical control product urea. The crude extracts exhibited very similar activity to the 10% and 20% w/v concentrations of urea, demonstrating the ability of seaweed extracts to compete with commercially available products. Antibacterial activity was exhibited by a number of seaweed extracts with the red seaweed illustrating the strongest activity, with a zone of inhibition of 15.83 ± 0.41 mm exhibited against X. arboricola whilst the positive control (10 μg/disk of chloramphenicol) had a zone of 26.5 ± 0.71 mm. These results highlight the potential application of seaweed extracts in the forestry and agricultural industries for use as biopesticides. Further work is now required to identify the bioactive molecules that are responsible for this antifungal and antibacterial activity in the seaweed extracts, including toxicity studies to ensure the extracts are non-toxic to plants and humans.

Keywords: antibacterial, antifungal, biopesticides, seaweeds

Procedia PDF Downloads 144
7645 Effect of a GABA/5-HTP Mixture on Behavioral Changes and Biomodulation in an Invertebrate Model

Authors: Kyungae Jo, Eun Young Kim, Byungsoo Shin, Kwang Soon Shin, Hyung Joo Suh

Abstract:

Gamma-aminobutyric acid (GABA) and 5-hydroxytryptophan (5-HTP) are amino acids of digested nutrients or food ingredients and these can possibly be utilized as non-pharmacologic treatment for sleep disorder. We previously investigated the GABA/5-HTP mixture is the principal concept of sleep-promoting and activity-repressing management in nervous system of D. melanogaster. Two experiments in this study were designed to evaluate sleep-promoting effect of GABA/5-HTP mixture, to clarify the possible ratio of sleep-promoting action in the Drosophila invertebrate model system. Behavioral assays were applied to investigate distance traveled, velocity, movement, mobility, turn angle, angular velocity and meander of two amino acids and GABA/5-HTP mixture with caffeine treated flies. In addition, differentially expressed gene (DEG) analyses from next generation sequencing (NGS) were applied to investigate the signaling pathway and functional interaction network of GABA/5-HTP mixture administration. GABA/5-HTP mixture resulted in significant differences between groups related to behavior (p < 0.01) and significantly induced locomotor activity in the awake model (p < 0.05). As a result of the sequencing, the molecular function of various genes has relationship with motor activity and biological regulation. These results showed that GABA/5-HTP mixture administration significantly involved the inhibition of motor behavior. In this regard, we successfully demonstrated that using a GABA/5-HTP mixture modulates locomotor activity to a greater extent than single administration of each amino acid, and that this modulation occurs via the neuronal system, neurotransmitter release cycle and transmission across chemical synapses.

Keywords: sleep, γ-aminobutyric acid, 5-hydroxytryptophan, Drosophila melanogaster

Procedia PDF Downloads 291
7644 Impact of Education on Levels of Physical Activity and Depression in Taiwanese Vegetarians and Omnivores

Authors: Ya-Lin Chang, Chia Chen Chang, Yu-Ru Liang, Joyce Chen, You-Kang Chang, Tina Chiu

Abstract:

Physical activity and mental health status are important for health. The purpose of this study was to examine levels of physical activities and depression in Taiwanese vegetarians (VEG) and omnivores (OMNI). Sixty-three vegetarians (20 males) and 56 omnivores (23 males) with an average age of 51 years were recruited for a food frequency validation study at Taipei Tzu Chi Hospital from July to September in 2016. Participants filled out a validated Chinese version international physical activity questionnaire-short-form (IPAQ), Beck Depression Inventory-II-Chinese version (BDI), food frequency questionnaire (FFQ) and a questionnaire on demographics and medical history upon recruitment. Total BDI scores were calculated for depression and the metabolic equivalent of task (MET) was calculated for physical activity levels. Mann-Whitney U tests and Chi-square test were used to compare demographics, physical activity levels and depression scores. VEG and OMNI did not differ significantly on MET (1441.9 ± 3387.3 vs. 1605.8 ± 2486.1. p=0.2652, respectively). VEG scored slightly lower on BDI compared to OMNI without statistical significance (5.6 ± 5.7 vs. 7.4 ± 6.3. p=0.06). In addition, we found that regardless of diet practice, those who held a college degree and above scored better on MET (1788.1 ± 2532.6 vs. 1215.5 ± 3425.5. p=0.0014) and BDI (5.2 ± 5.1 vs. 7.8 ± 6.7. p=0.03). In this cross-sectional study, Taiwanese vegetarians and omnivores scored comparatively on physical activity levels and depression. However, education is a significant determinant of physical activity and depression.

Keywords: BDI, diet, education, physical activity

Procedia PDF Downloads 363
7643 Methyltrioctylammonium Chloride as a Separation Solvent for Binary Mixtures: Evaluation Based on Experimental Activity Coefficients

Authors: B. Kabane, G. G. Redhi

Abstract:

An ammonium based ionic liquid (methyltrioctylammonium chloride) [N8 8 8 1] [Cl] was investigated as an extraction potential solvent for volatile organic solvents (in this regard, solutes), which includes alkenes, alkanes, ketones, alkynes, aromatic hydrocarbons, tetrahydrofuran (THF), alcohols, thiophene, water and acetonitrile based on the experimental activity coefficients at infinite THF measurements were conducted by the use of gas-liquid chromatography at four different temperatures (313.15 to 343.15) K. Experimental data of activity coefficients obtained across the examined temperatures were used in order to calculate the physicochemical properties at infinite dilution such as partial molar excess enthalpy, Gibbs free energy and entropy term. Capacity and selectivity data for selected petrochemical extraction problems (heptane/thiophene, heptane/benzene, cyclohaxane/cyclohexene, hexane/toluene, hexane/hexene) were computed from activity coefficients data and compared to the literature values with other ionic liquids. Evaluation of activity coefficients at infinite dilution expands the knowledge and provides a good understanding related to the interactions between the ionic liquid and the investigated compounds.

Keywords: separation, activity coefficients, methyltrioctylammonium chloride, ionic liquid, capacity

Procedia PDF Downloads 122
7642 In vitro Antifungal Activity of Methanolic Extracts of Eight Various Cultivar of Persian Punica granatum L. against Candida Species

Authors: Shahindokht Bassiri-Jahromi, Mohammad Reza Pourshafie, Farzad Katiraee, Mannan Hajimahmoodi, Ehsan Mostafavi, Malihe Talebi

Abstract:

Objective: Resistance of Candida species to antifungal agents has potentially serious implications for management of infections. Candida species are now fourth common organisms isolated from hospitalized patients. It is important to increase effective therapy. In the past decade, numerous reports of treatment failures were reported. Prevention and control of these infections will require new antimicrobial agents. Plant-derived antifungal have always been a source of novel therapeutics. The aim of this study was to investigate the antifungal effect of methanolic extract of pomegranate peel and pulp against Candida species. Material and Methods: Eight cultivars of Punica granatum L. were collected from Saveh Agricultural Investigation Center in Iran. Both pomegranate pulp and peel were dried and powdered separately. The dried powders were extracted by using a soxhlet extractor. The antifungal effect of methanolic extract of pomegranate peel and pulp were determined in vitro by minimum inhibitory concentration (MIC) against five standard species of (ATCC 10231), C. parapsilosis (ATCC 22019), C. tropicalis (ATCC 750), C. glabrata (PTCC 5297), and C. kroseii (PTCC 5295). Results: Maximum inhibitions of antifungal effect were attributed to peel extract pomegranate cultivar and Candida species. The most potential antifungal inhibition among 8 different cultivars observed by sour malas, sour white peel, and sour summer extracts respectively, against five Candida strains. The antifungal activity of pulp extracts against Candida species was approximately negative. Conclusion: The use of Punica granatum peel extract has been shown to possess antifungal activities. The phytochemistry and pharmacological actions of Punica granatum peel components suggest a wide range of clinical applications for the treatment and prevention of candidiasis.

Keywords: antifungal activity, Candida species, Punica granatum L., pharmacognosy

Procedia PDF Downloads 454
7641 The Effect of Biochar, Inoculated Biochar and Compost Biological Component of the Soil

Authors: Helena Dvořáčková, Mikajlo Irina, Záhora Jaroslav, Elbl Jakub

Abstract:

Biochar can be produced from the waste matter and its application has been associated with returning of carbon in large amounts into the soil. The impacts of this material on physical and chemical properties of soil have been described. The biggest part of the research work is dedicated to the hypothesis of this material’s toxic effects on the soil life regarding its effect on the soil biological component. At present, it has been worked on methods which could eliminate these undesirable properties of biochar. One of the possibilities is to mix biochar with organic material, such as compost, or focusing on the natural processes acceleration in the soil. In the experiment has been used as the addition of compost as well as the elimination of toxic substances by promoting microbial activity in aerated water environment. Biochar was aerated for 7 days in a container with a volume of 20 l. This way modified biochar had six times higher biomass production and reduce mineral nitrogen leaching. Better results have been achieved by mixing biochar with compost.

Keywords: leaching of nitrogen, soil, biochar, compost

Procedia PDF Downloads 303