Search results for: antiviral drugs
384 Attempts for the Synthesis of Indol-Ring Fluorinated Tryptophan Derivatives to Enhance the Activity of Antimicrobial Peptides
Authors: Anita K. Kovacs, Peter Hegyes, Zsolt Bozso, Gabor Toth
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Fluorination has been used extensively by the pharmaceutical industry as a strategy to improve the pharmacokinetics of drugs due to its effectiveness in increasing the potency of antimicrobial peptides (AMPs). Multiple-fluorinated indole-ring-containing tryptophan derivatives have the potential of having better antimicrobial activity than the widely used mono-fluorinated indole-ring containing tryptophan derivatives, but they are not available commercially. Therefore, our goal is to synthesize multiple-fluorinated indole-ring containing tryptophan derivatives to incorporate them into AMPs to enhance their antimicrobial activity. During our work, we are trying several methods (classical organic synthesis, enzymic synthesis, and solid phase peptide synthesis) for the synthesis of the said compounds, with mixed results. With classical organic synthesis (four different routes), we did not get the desired results. The reaction of serin with substituted indole in the presence of acetic anhydride led to racemic tryptophane; with the reaction of protected serin with indole in the presence of nickel complex was unsuccessful; the reaction of serin containing protected dipeptide with disuccinimidyl carbonate we achieved a tryptophane containing dipeptide, its chiral purity is being examined; the reaction of alcohol with substituted indole in the presence of copper complex was successful, but it was only a test reaction, we could not reproduce the same result with serine. The undergoing tryptophan-synthase method has shown some potential, but our work has not been finished yet. The successful synthesis of the desired multiple-fluorinated indole-ring-containing tryptophan will be followed by solid phase peptide synthesis in order to incorporate it into AMPs to enhance their antimicrobial activity. The successful completion of these phases will mean the possibility of manufacturing new, effective AMPs.Keywords: halogenation, fluorination, tryptophan, enhancement of antimicrobial activity
Procedia PDF Downloads 93383 A Handheld Light Meter Device for Methamphetamine Detection in Oral Fluid
Authors: Anindita Sen
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Oral fluid is a promising diagnostic matrix for drugs of abuse compared to urine and serum. Detection of methamphetamine in oral fluid would pave way for the easy evaluation of impairment in drivers during roadside drug testing as well as ensure safe working environments by facilitating evaluation of impairment in employees at workplaces. A membrane-based point-of-care (POC) friendly pre-treatment technique has been developed which aided elimination of interferences caused by salivary proteins and facilitated the demonstration of methamphetamine detection in saliva using a gold nanoparticle based colorimetric aptasensor platform. It was found that the colorimetric response in saliva was always suppressed owing to the matrix effects. By navigating the challenging interfering issues in saliva, we were successfully able to detect methamphetamine at nanomolar levels in saliva offering immense promise for the translation of these platforms for on-site diagnostic systems. This subsequently motivated the development of a handheld portable light meter device that can reliably transduce the aptasensors colorimetric response into absorbance, facilitating quantitative detection of analyte concentrations on-site. This is crucial due to the prevalent unreliability and sensitivity problems of the conventional drug testing kits. The fabricated light meter device response was validated against a standard UV-Vis spectrometer to confirm reliability. The portable and cost-effective handheld detector device features sensitivity comparable to the well-established UV-Vis benchtop instrument and the easy-to-use device could potentially serve as a prototype for a commercial device in the future.Keywords: aptasensors, colorimetric gold nanoparticle assay, point-of-care, oral fluid
Procedia PDF Downloads 39382 Protective Impact of Some Natural Extracts Against Acute Hepatotoxicity in Wistar Rats: DNA Protecting, Antioxidant and Anti-Inflammatory Effects
Authors: Yara Mohamed Taha, Mohamed Ali El Desouky, Heba Kamal Abdel Hakim, Maha Hanafy Mahmoud
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Hepatotoxicity due to drugs and toxic chemicals constitutes a crucial health problem nowadays. Medicinal plants are widely used recently for protecting against many liver disorders and inflammatory conditions. This study aims to evaluate hepatoprotective impact of green tea extract (GTE), rosemary extract (RE) and rosmarinic acid (RA) against hepatotoxins; ferric nitrilotriacetate (Fe-NTA) and diethylnitrosamine (DEN) in rats. Five groups of male Wistar rats were included; one control negative, while the other groups were treated intraperitoneally with DEN as 160 mg.kg-1 b.w. on 15th day and Fe-NTA as 5 mg.kg-1 b.w. on 33rd day. One of them was control positive. The other three groups were pre-administered with daily protective oral doses of either 200 mg.kg-1 b.w. of RE or 1 g.kg- 1 b.w. of GTE or 50 mg.kg-1 b.w. of RA two weeks prior to DEN exposure and continued till the end of the experimental period. The obtained data revealed a highly significant increase of MDA, 8-OHdG, DNA damage percent, a significant depletion of GSH and elevated Gr-1 protein expression in hepatocytes with liver tissue histopathological changes of rats exposed to DEN+Fe-NTA. Pre-administration of protective doses of RE, GTE and RA to DEN+Fe-NTA treated rats could normalize the altered biochemical, histopathological and immunohistochemical parameters. In conclusion, RE, GTE and RA showed a hepatoprotective effect against liver toxicity induced by DEN+Fe-NTA, with the best antioxidant and anti-inflammatory impact were for RA and GTE. Therefore, the current study declared that rosemary, green tea and products enriched with rosmarinic acid should be involved daily in diet of people who are exposed to chemicals and environmental toxins to protect themselves from hepatotoxicity.Keywords: hepatotoxicity, diethylnitrosamine and ferric nitrilotriacetate, rosemary extract (RE), green tea extract (GTE), rosmarinic acid (RA)
Procedia PDF Downloads 85381 Effectively Improving Cognition, Behavior, and Attitude of Diabetes Inpatients through Nutritional Education
Authors: Han Chih Feng, Yi-Cheng Hou, Jing-Huei Wu
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Diabetes is a chronic disease. Nutrition knowledge and skills enable individuals with type 2 diabetes to optimize metabolic self-management and quality of life. This research studies the effect of nutritional education on diabetes inpatients in terms of their cognition, behavior, and attitude. The participants are inpatients diagnosed with diabetes at Taipei Tzu Chi Hospital. A total of 103 participants, 58 male, and 45 females, enrolled in the research between January 2018 and July 2018. The research evaluates cognition, behavior, and attitude level before and after nutritional education conducted by dietitians. The result shows significant improvement in actual consumption (2.5 ± 1.4 vs 3.8 ± 0.7; p<.001), diet control motivation (2.7 ± 0.8 vs 3.4 ± 0.6; p<.001), correct nutrition concept (1.2± 0.4 vs 2.4 ± 0.5; p<.001), learning willingness (2.7± 0.9 vs 3.4 ± 0.6; p<.001), cognitive behaviors (1.4 ± 0.5 vs 2.9 ± 0.7; p<.001). AC sugar (278.5 ± 321.5 vs 152.2 ± 49.1; p<.001) and HbA1C (10.3 ± 2.6 vs 8.6 ± 1.9; p<.001) are significant improvement after nutritional education. After nutritional education, participants oral hypoglycemic agents increased from 16 (9.2%) to 33 (19.0%), insulin decreased from 75 (43.1%) to 68 (39.1%), and hypoglycemic drugs combined with insulin decreased from 83 (47.7%) to 73 (42.0%).Further analysis shows that female inpatients have significant improvement in diet control motivation (3.91 ± 0.85 vs 4.44 ± 0.59; p<0.000), correct nutrition concept (3.24± 0.48 vs 4.47± 0.51; p<0.000), learning willingness (3.89 ± 0.86 vs 4.44 ± 0.59; p<0.000) and cognitive behaviors (2.42 ± 0.58 vs 4.02 ± 0.69; p<0.000); male inpatients have significant improvement in actual food intake (4.41± 0.92 vs 3.97 ± 0.42; p<0.000), diet control motivation (3.62 ± 0.86 vs 4.29 ± 0.62; p<0.000), correct nutrition concept (3.26 ± 0.44 vs 4.36 ± 0.49; p<0.000), learning willingness (3.72± 0.93 vs 4.33± 0.63; p<0.000) and cognitive behaviors (2.45± 0.54 vs 4.03± 0.77; p<0.000). In conclusion, nutritional education proves effective, regardless of gender, in improving an inpatient’s cognition, behavior, and attitude toward diabetes self-management.Keywords: diabetes, nutrition education, actual consumption, diet control motivation, nutrition concept, learning willingness, cognitive behaviors
Procedia PDF Downloads 80380 Value of Unilateral Spinal Anaesthesia For Hip Fracture Surgery In The Elderly (75 Cases)
Authors: Fedili Benamar, Beloulou Mohamed Lamine, Ouahes Hassane, Ghattas Samir
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Background and aims: While in Western countries, unilateral spinal anesthesia has been widely practiced for a long time, it remains little known in the local anesthesia community, and has not been the object of many studies. However, it is a simple, practical and effective technique. Our objective was to evaluate this practice in emergency anesthesia management in frail patients and to compare it with conventional spinal anesthesia. Methods: This is a prospective, observational, comparative study between hypobaric unilateral and conventional spinal anaesthesia for hip fracture surgery carried out in the operating room of the university military hospital of Staoueli. The work was spread over of 12-month period from 2019 to 2020. The parameters analyzed were hemodynamic variations, vasopressor use, block efficiency, postoperative adverse events, and postoperative morphine consumption. Results: -75 cases (mean age 72±14 years) -Group1= 41 patients (54.6%) divided into (ASA1=14.6% ASA2=60.98% ASA3=24.39%) single shoot spinal anaesthesia -Group2= 34 patients (45.3%) divided into (ASA1=2.9%, ASA2=26.4% ASA3=61.7%, ASA4=8.8%) unilateral hypobaric spinal anesthesia. -Hemodynamic variations were more severe in group 1 (51% hypotension) compared to 30% in group 2 RR=1.69 and odds ratio=2.4 -these variations were more marked in the ASA3 subgroup (group 1=70% hypotension versus group 2=30%) with an RR=2.33 and an odds ratio=5.44 -39% of group 1 required vasoactive drugs (15mg +/- 11) versus 32% of group 2 (8mg+/- 6.49) - no difference in the use of morphine in post-op. Conclusions: Within the limits of the population studied, this work demonstrates the clinical value of unilateral spinal anesthesia in ortho-trauma surgery in the frail patient.Keywords: spinal anaesthesia, vasopressor, morphine, hypobaric unilateral spinal anesthesia, ropivacaine, hip surgery, eldery, hemodynamic
Procedia PDF Downloads 63379 The Social Psychology of Illegal Game Room Addiction in the Historic Chinatown District of Honolulu, Hawaii: Illegal Compulsive Gambling, Chinese-Polynesian Organized Crime Syndicates, Police Corruption, and Loan Sharking Rings
Authors: Gordon James Knowles
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Historically the Chinatown district in Sandwich Islands has been plagued with the traditional vice crimes of illegal drugs, gambling, and prostitution since the early 1800s. However, a new form of psychologically addictive arcade style table gambling machines has become the dominant form of illegal revenue made in Honolulu, Hawaii. This study attempts to document the drive, desire, or will to play and wager with arcade style video gaming and understand the role of illegal game rooms in facilitating pathological gambling addiction. Indicators of police corruption by Chinese organized crime syndicates related to protection rackets, bribery, and pay-offs were revealed. Information fusion from a police science and sociological intelligence perspective indicates insurgent warfare is being waged on the streets of Honolulu by the People’s Republic of China. This state-sponsored communist terrorism in the Hawaiian Islands used “contactless” irregular warfare entailing: (1) the deployment of psychologically addictive gambling machines, (2) the distribution of the physically addictive fentanyl drug as a lethal chemical weapon, and (3) psychological warfare by circulating pro-China anti-American propaganda newspapers targeted at the small island populace.Keywords: Chinese and Polynesian organized crime, china daily newspaper, electronic arcade style table games, gaming technology addiction, illegal compulsive gambling, and police intelligence
Procedia PDF Downloads 61378 Prevalence of Diabetes Mellitus Among Human Immune Deficiency Virus-Positive Patients Under Anti-retroviral Attending in Rwanda, a Case Study of University Teaching Hospital of Butare
Authors: Venuste Kayinamura, V. Iyamuremye, A. Ngirabakunzi
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Anti-retroviral therapy (ART) for HIV patient can cause a deficiency in glucose metabolism by promoting insulin resistance, glucose intolerance, and diabetes, diabetes mellitus keep increasing among HIV-infected patients worldwide but there is limited data on levels of blood glucose and its relationship with antiretroviral drugs (ARVs) and HIV-infection worldwide, particularly in Rwanda. A convenient sampling strategy was used in this study and it involved 323 HIV patients (n=323). Patients who are HIV positive under ARVs were involved in this study. The patient’s blood glucose was analyzed using an automated machine or glucometer (COBAS C 311). Data were analyzed using Microsoft Excel and SPSS V. 20.0 and presented in percentages. The highest diabetes mellitus prevalence was 93.33 % in people aged >40 years while the lowest diabetes mellitus prevalence was 6.67% in people aged between 21-and 40 years. The P-value was (0.021). Thus, there is a significant association between age and diabetes occurrence. The highest diabetes mellitus prevalence was 28.2% in patients under ART treatment for more than 10 years, 16.7% were <5years while 20% of patients were on ART treatment between 5-10 years. The P-value here is (0.03), thus the incidence of diabetes is associated with long-term ART use in HIV-infected patients. This study assessed the prevalence of diabetes among HIV-infected patients under ARVs attending the University Teaching Hospital of Butare (CHUB), it shows that the prevalence of diabetes is high in HIV-infected patients under ARTs. This study found no significant relationship between gender and diabetes mellitus growth. Therefore, regular assessment of diabetes mellitus especially among HIV-infected patients under ARVs is highly recommended to control other health issues caused by diabetes mellitus.Keywords: anti-retroviral, diabetes mellitus, antiretroviral therapy, human immune deficiency virus
Procedia PDF Downloads 103377 Cas9-Assisted Direct Cloning and Refactoring of a Silent Biosynthetic Gene Cluster
Authors: Peng Hou
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Natural products produced from marine bacteria serve as an immense reservoir for anti-infective drugs and therapeutic agents. Nowadays, heterologous expression of gene clusters of interests has been widely adopted as an effective strategy for natural product discovery. Briefly, the heterologous expression flowchart would be: biosynthetic gene cluster identification, pathway construction and expression, and product detection. However, gene cluster capture using traditional Transformation-associated recombination (TAR) protocol is low-efficient (0.5% positive colony rate). To make things worse, most of these putative new natural products are only predicted by bioinformatics analysis such as antiSMASH, and their corresponding natural products biosynthetic pathways are either not expressed or expressed at very low levels under laboratory conditions. Those setbacks have inspired us to focus on seeking new technologies to efficiently edit and refractor of biosynthetic gene clusters. Recently, two cutting-edge techniques have attracted our attention - the CRISPR-Cas9 and Gibson Assembly. By now, we have tried to pretreat Brevibacillus laterosporus strain genomic DNA with CRISPR-Cas9 nucleases that specifically generated breaks near the gene cluster of interest. This trial resulted in an increase in the efficiency of gene cluster capture (9%). Moreover, using Gibson Assembly by adding/deleting certain operon and tailoring enzymes regardless of end compatibility, the silent construct (~80kb) has been successfully refactored into an active one, yielded a series of analogs expected. With the appearances of the novel molecular tools, we are confident to believe that development of a high throughput mature pipeline for DNA assembly, transformation, product isolation and identification would no longer be a daydream for marine natural product discovery.Keywords: biosynthesis, CRISPR-Cas9, DNA assembly, refactor, TAR cloning
Procedia PDF Downloads 269376 Design, Synthesis and Pharmacological Investigation of Novel 2-Phenazinamine Derivatives as a Mutant BCR-ABL (T315I) Inhibitor
Authors: Gajanan M. Sonwane
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Nowadays, the entire pharmaceutical industry is facing the challenge of increasing efficiency and innovation. The major hurdles are the growing cost of research and development and a concurrent stagnating number of new chemical entities (NCEs). Hence, the challenge is to select the most druggable targets and to search the equivalent drug-like compounds, which also possess specific pharmacokinetic and toxicological properties that allow them to be developed as drugs. The present research work includes the studies of developing new anticancer heterocycles by using molecular modeling techniques. The heterocycles synthesized through such methodology are much effective as various physicochemical parameters have been already studied and the structure has been optimized for its best fit in the receptor. Hence, on the basis of the literature survey and considering the need to develop newer anticancer agents, new phenazinamine derivatives were designed by subjecting the nucleus to molecular modeling, viz., GQSAR analysis and docking studies. Simultaneously, these designed derivatives were subjected to in silico prediction of biological activity through PASS studies and then in silico toxicity risk assessment studies. In PASS studies, it was found that all the derivatives exhibited a good spectrum of biological activities confirming its anticancer potential. The toxicity risk assessment studies revealed that all the derivatives obey Lipinski’s rule. Amongst these series, compounds 4c, 5b and 6c were found to possess logP and drug-likeness values comparable with the standard Imatinib (used for anticancer activity studies) and also with the standard drug methotrexate (used for antimitotic activity studies). One of the most notable mutations is the threonine to isoleucine mutation at codon 315 (T315I), which is known to be resistant to all currently available TKI. Enzyme assay planned for confirmation of target selective activity.Keywords: drug design, tyrosine kinases, anticancer, Phenazinamine
Procedia PDF Downloads 107375 Protective Effect of Diosgenin against Silica-Induced Tuberculosis in Rat Model
Authors: Williams A. Adu, Cynthia A. Danquah, Paul P. S. Ossei, Selase Ativui, Michael Ofori, James Asenso, George Owusu
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Background Silicosis is an occupational disease of the lung that is caused by chronic exposure to silica dust. There is a higher frequency of co-existence of silicosis with tuberculosis (TB), ultimately resulting in lung fibrosis and respiratory failure. Chronic intake of synthetic drugs has resulted in undesirable side effects. Diosgenin is a steroidal saponin that has been shown to exert a therapeutic effect on lung injury. Therefore, we investigated the ability of diosgenin to reduce the susceptibility of silica-induced TB in rats. Method Silicosis was induced by intratracheal instillation of 50 mg/kg crystalline silica in Sprague Dawley rats. Different doses of diosgenin (1, 10, and 100 mg/kg), Mycobacterium smegmatis and saline were administered for 30 days. Afterwards, 5 of the rats from each group were sacrificed, and the 5 remaining rats in each group, except the control, received Mycobacterium smegmatis. Treatment of diosgenin continued until the 50th day, and the rats were sacrificed at the end of the experiment. The result was analysed using a one-way analysis of variance (ANOVA) with a Graph-pad prism Result At a half-maximal inhibition concentration of 48.27 µM, diosgenin inhibited the growth of Mycobacterium smegmatis. There was a marked decline in the levels of immune cell infiltration and cytokines production. Lactate dehydrogenase and total protein levels were significantly reduced compared to control. There was an increase in the survival rate of the treatment group compared to the control. Conclusion Diosgenin ameliorated silica-induced pulmonary tuberculosis by declining the levels of inflammatory and pro-inflammatory cytokines and, in effect, significantly reduced the susceptibility of rats to pulmonary TB.Keywords: silicosis, tuberculosis, diosgenin, fibrosis, crystalline silica
Procedia PDF Downloads 54374 Study of a Cross-Flow Membrane to a Kidney Encapsulation Engineering Structures for Immunosuppression Filter
Authors: Sihyun Chae, Ryoto Arai, Waldo Concepcion, Paula Popescu
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The kidneys perform an important role in the human hormones that regulate the blood pressure, produce an active form of vitamin D and control the production of red blood cells. Kidney disease can cause health problems, such as heart disease. Also, increase the chance of having a stroke or heart attack. There are mainly to types of treatments for kidney disease, dialysis, and kidney transplant. For a better quality of life, the kidney transplant is desirable. However, kidney transplant can cause antibody reaction and patients’ body would be attacked by immune system of their own. For solving that issue, patients with transplanted kidney always take immunosuppressive drugs which can hurt kidney as side effects. Patients willing to do a kidney transplant have a waiting time of 3.6 years in average searching to find an appropriate kidney, considering there are almost 96,380 patients waiting for kidney transplant. There is a promising method to solve these issues: bioartificial kidney. Our membrane is specially designed with unique perforations capable to filter the blood cells separating the white blood cells from red blood cells. White blood cells will not pass through the encapsulated kidney preventing the immune system to attack the new organ and eliminating the need of a matching donor. It is possible to construct life-time long encapsulation without needing pumps or a power supply on the cell’s separation method preventing futures surgeries due the Cross-Channel Flow inside the device. This technology allows the possibility to use an animal kidney, prevent cancer cells to spread through the body, arm and leg transplants in the future. This project aims to improve the quality of life of patients with kidney disease.Keywords: kidney encapsulation, immunosuppression filter, leukocyte filter, leukocyte
Procedia PDF Downloads 194373 Fabrication and Characterization of Folic Acid-Grafted-Thiomer Enveloped Liposomes for Enhanced Oral Bioavailability of Docetaxel
Authors: Farhan Sohail, Gul Shahnaz Irshad Hussain, Shoaib Sarwar, Ibrahim Javed, Zajif Hussain, Akhtar Nadhman
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The present study was aimed to develop a hybrid nanocarrier (NC) system with enhanced membrane permeability, bioavailability and targeted delivery of Docetaxel (DTX) in breast cancer. Hybrid NC’s based on folic acid (FA) grafted thiolated chitosan (TCS) enveloped liposomes were prepared with DTX and evaluated in-vitro and in-vivo for their enhanced permeability and bioavailability. Physicochemical characterization of NC’s including particle size, morphology, zeta potential, FTIR, DSC, PXRD, encapsulation efficiency and drug release from NC’s was determined in vitro. Permeation enhancement and p-gp inhibition were performed through everted sac method on freshly excised rat intestine which indicated that permeation was enhanced 5 times as compared to pure DTX and the hybrid NC’s were strongly able to inhibit the p-gp activity as well. In-vitro cytotoxicity and tumor targeting was done using MDA-MB-231 cell line. The stability study of the formulations performed for 3 months showed the improved stability of FA-TCS enveloped liposomes in terms of its particles size, zeta potential and encapsulation efficiency as compared to TCS NP’s and liposomes. The pharmacokinetic study was performed in vivo using rabbits. The oral bioavailability and AUC0-96 was increased 10.07 folds with hybrid NC’s as compared to positive control. Half-life (t1/2) was increased 4 times (58.76 hrs) as compared to positive control (17.72 hrs). Conclusively, it is suggested that FA-TCS enveloped liposomes have strong potential to enhance permeability and bioavailability of hydrophobic drugs after oral administration and tumor targeting.Keywords: docetaxel, coated liposome, permeation enhancement, oral bioavailability
Procedia PDF Downloads 403372 Examining How Youth Use Mobile Devices for Health Information: Preliminary Findings of a Survey Study with High School Students in Croatia
Authors: Sung Un Kim, Ivana Martinović, Snježana Stanarević Katavić
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As more and more youth use mobile devices, such as tablets and smartphones, for information seeking in their everyday lives, the purpose of this study is to understand the behaviors of youth seeking health information on mobile devices. The specific objective of this study is to examine 1) for what health issues youth use mobile devices, 2) for what reasons youth use mobile devices to obtain health information, 3) in what ways youth use mobile devices for health information, and 4) the features of health applications that youth find useful. The researchers devised a questionnaire for this study. Four hundred eight students from two high schools, located in Osijek, Croatia, participated by answering the questionnaire (281 girls and 127 boys). The collected data were analyzed using descriptive statistics and content analysis. The results show that among all participants, about 85 percent (n = 344) reported having used mobile devices for health information. The most frequent health topic for which they had been using mobile devices is physical activity (n = 273), followed by eating issues and nutrition (n = 224), mental health (n = 160), sexual health (n = 157), alcohol, drugs, and tobacco (n = 125), safety (n = 96) and particular diseases (n = 62). They use mobile devices to obtain health information due to the ease of use (n = 342), the ease of sharing health information (n = 281), portability (n = 215), timeliness (n = 162), and the ease of tracking/recording/monitoring health status (n = 147). Of those who have used mobile devices for health information, three-quarters (n = 261) use mobile devices to search health information, while 32.8% (n =113) use applications and 31.7% (n =109) browse information. Those who have used applications for health information (n = 113) consider the alert feature (n=107) as the most useful, followed by the tracking/recording/monitoring feature (n =92), the customized information feature (n = 86), the video feature (n = 58), and the sharing feature (n =39). It is notable that although health applications have been actively developed and studied, a majority of the participants search for or browse information on mobile devices, instead of using applications. The researchers will discuss reasons that some of them did not use mobile devices to obtain health information, students’ concerns about using health applications, and features that they wish to have in health applications.Keywords: Croatia, health information, information seeking behaviors, mobile devices, youth
Procedia PDF Downloads 390371 Antibacterial Activity of Calendula officinalis Extract Loaded Chitosan Nanoparticles
Authors: Sanjay Singh, Swati Jaiswal, Prashant Mishra
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Nanoparticle based formulations of drug delivery systems have shown their potential in improving the performance of existing drugs and have opened avenues for new therapies. Calendula extract is a low cost, wide spectrum bioactive material that has been used for a long term therapy of various infections. Aim: The aim of this study was to develop Calendula officinalis extract based nanoformulations and to study the antibacterial activity of either Calendula extract loaded chitosan nanoparticles or Calendula extract coated silver nanoparticles for increased bioavailability and their long term effect. Methods: Chitosan nanoparticles were prepared by the process of ionotropic gelation, based on interaction between the negative groups of tri polyphosphate (TPP) and positively charged amino groups of chitosan. The size of the Calendula extract-loaded chitosan particles was determined using dynamic light scattering and scanning electron microscopy. Antibacterial activities of these formulations were determined based on minimum inhibitory concentration and time kill studies. In addition, silver nanoparticles were also synthesized in the presence of Calendula extract and characterized by UV visible spectrum, DLS and XRD. Experiments were conducted on 96-plates against two Gram-positive bacteria; Staphylococcus aureus and Bacillus subtilis two Gram-negative bacteria; Escherichia coli and Pseudomonas aeruginosa. Results: Results demonstrated time dependent antibacterial activity against different microbes studied. Both Calendula extract and Calendula extract loaded chitosan nanoparticles have shown good antimicrobial activity against both Gram positive and Gram negative bacteria. Conclusion: Calendula extract loaded chitosan nanoparticles and calendula extract coated silver nanoparticles are potential antibacterial for their long term antibacterial effects.Keywords: antibacterial, Calendula extract, chitosan nanoparticles, silver nanoparticles
Procedia PDF Downloads 335370 Entry Inhibitors Are Less Effective at Preventing Cell-Associated HIV-2 Infection than HIV-1
Authors: A. R. Diniz, P. Borrego, I. Bártolo, N. Taveira
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Cell-to-cell transmission plays a critical role in the spread of HIV-1 infection in vitro and in vivo. Inhibition of HIV-1 cell-associated infection by antiretroviral drugs and neutralizing antibodies (NAbs) is more difficult compared to cell-free infection. Limited data exists on cell-associated infection by HIV-2 and its inhibition. In this work, we determined the ability of entry inhibitors to inhibit HIV-1 and HIV-2 cell-to cell fusion as a proxy to cell-associated infection. We developed a method in which Hela-CD4-cells are first transfected with a Tat expressing plasmid (pcDNA3.1+/Tat101) and infected with recombinant vaccinia viruses expressing either the HIV-1 (vPE16: from isolate HTLV-IIIB, clone BH8, X4 tropism) or HIV-2 (vSC50: from HIV-2SBL/ISY, R5 and X4 tropism) envelope glycoproteins (M.O.I.=1 PFU/cell).These cells are added to TZM-bl cells. When cell-to-cell fusion (syncytia) occurs the Tat protein diffuses to the TZM-bl cells activating the expression of a reporter gene (luciferase). We tested several entry inhibitors including the fusion inhibitors T1249, T20 and P3, the CCR5 antagonists MVC and TAK-779, the CXCR4 antagonist AMD3100 and several HIV-2 neutralizing antibodies (Nabs). All compounds inhibited HIV-1 and HIV-2 cell fusion albeit to different levels. Maximum percentage of HIV-2 inhibition (MPI) was higher for fusion inhibitors (T1249- 99.8%; P3- 95%, T20-90%) followed by co-receptor antagonists (MVC- 63%; TAK-779- 55%; AMD3100- 45%). NAbs from HIV-2 infected patients did not prevent cell fusion up to the tested concentration of 4μg/ml. As for HIV-1, MPI reached 100% with TAK-779 and T1249. For the other antivirals, MPIs were: P3-79%; T20-75%; AMD3100-61%; MVC-65%.These results are consistent with published data. Maraviroc had the lowest IC50 both for HIV-2 and HIV-1 (IC50 HIV-2= 0.06 μM; HIV-1=0.0076μM). Highest IC50 were observed with T20 for HIV-2 (3.86μM) and with TAK-779 for HIV-1 (12.64μM). Overall, our results show that entry inhibitors in clinical use are less effective at preventing Env mediated cell-to-cell-fusion in HIV-2 than in HIV-1 which suggests that cell-associated HIV-2 infection will be more difficult to inhibit compared to HIV-1. The method described here will be useful to screen for new HIV entry inhibitors.Keywords: cell-to-cell fusion, entry inhibitors, HIV, NAbs, vaccinia virus
Procedia PDF Downloads 300369 Antimutagenic Activity of a Protein, Lectin Fraction from Urtica Dioica L.
Authors: Nijole Savickiene, Antonella Di Sotto, Gabriela Mazzanti, Rasa Starselskyte, Silvia Di Giacomo, Annabella Vitalone
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Plant lectins are non-enzymic and non-immune origin proteins that specifically recognize and bind to various sugar structures and possess the activity to agglutinate cells and/or precipitate polysaccharides and glycoconjugates. The emerging evidences showed that plant lectins contribute not only to tumour cell recognition but also to cell adhesion and localization, to signal transduction, to mitogenic cytotoxicity and apoptosis. Among chitin-binding lectins, the Urtica dioica agglutinin (UDA), which is a complex of different isoforms, has been poorly studied for its biological activity. In this context and according to the increasing interest for lectins as novel antitumor drugs, present paper aimed at evaluating the potential antimutagenic activity of a lectin-like glycoprotein-enriched fraction from aerial part of Urtica dioica L. Aim: to evaluate the potential chemopreventive properties of a protein - lectin fraction from the aerial part of Urtica dioica. Materials and methods: Protein – lectin fraction has been tested for the antimutagenic activity in bacteria (50–800 mg/plate; Ames test by the preincubation method) and for the cytotoxicity on human hepatoma HepG2 cells (0.06–2 mg/mL; 24 and 48 h incubation). Results: Protein – lectin fraction from stinging nettle was not cytotoxic on HepG2 cells up to 2 mg/mL; conversely, it exhibited a strong antimutagenic activity against the mutagen 2-aminoanthracene (2AA) in all strains tested (maximum inhibition of 56.78 and 61% in TA98, TA100, and WP2uvrA strains, respectively, at 800 mg/plate). Discussion and conclusions: Protein – lectin fraction from Urtica dioica L. possesses antimutagenic and radical scavenging properties. Being 2AA a pro-carcinogenic agent, we hypothesize that the antimutagenicity of it can be due to the inhibition of CYP450-isoenzymes, involved in the mutagen bioactivation.Keywords: lectins, antimutagenicity, chemoprevention, Urtica dioica
Procedia PDF Downloads 414368 Systolic Blood Pressure and Its Determinants: Study in a Population Attending Pharmacies in a Portuguese Coastal City
Authors: M. J. Reis Lima, J. Oliveira, M. Brito, C. Lemos, A. Mascarenhas, E. Teixeira Lemos
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Hypertension is a common condition causing cardio and cerebrovascular complications. Portugal has one of the highest mortality rates from stroke and a high prevalence of hypertension. Systolic blood pressure (SBP) is an important risk factor for cardiovascular events (myocardial infarction and stroke) and premature mortality, particularly in the elderly population. The present study aims to estimate the prevalence of hypertension in a Portuguese population living in a coastal city and to identify some of its determinants (namely gender, age, the body mass index and physical activity frequency). A total of 91 adults who attended three pharmacies of a coastal city in the center of Portugal, between May and August of 2013 were evaluated. Attendants who reported to have diabetes or taking antihypertensive drugs in the 2 previous weeks were excluded from the study. Sociodemographic factors, BMI, habits of exercise and BP were assessed. Hypertension was defined as blood pressure ≥140/90 mmHg. The majority of the studied population was constituted by women (75.8%), with a mean age of 54.2±1.6 years old, married or living in civil union and that had completed secondary school or had higher education (40%). They presented a mean BMI of 26.2±4.76 Kg/m2. and were sedentary. The mean BP was 127.0±17.77mmHg- 74.69 ± 9.53. In this population, we found 4.3% of people with hypertension and 16.1% with normal high blood pressure. Men exhibit a tendency to present higher systolic blood pressure values than women. Of all the factors considered, SBP values also tended to be higher with age and higher BMI values. Despite the fact that the mean values of SBP did not present values higher than 140 mmHg we must be concerned because the studied population is undiagnosed for hypertension. Our study even with some limitations might be a prelude to the upcoming research about the underlying factors responsible for the occurrence of SBP.Keywords: hypertension, age, exercise, obesity and gender
Procedia PDF Downloads 535367 Phytochemical Screening, Antioxidant and Antibacterial Activity of Annona cherimola Mill
Authors: Arun Jyothi Bheemagani, Chakrapani Pullagummi, Anupalli Roja Rani
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Exploration of the chemical constituents of the plants and pharmacological screening may provide us the basis for the development of novel agents. Plants have provided us some of the very important life saving drugs used in the modern medicine. The aim of our work was to screen the phytochemical constituents and antimicrobial and antioxidant activities of methanol extract of leaves of Annona cherimola Mill plant from Tirumala forest, Tirupathi. It was originally called Chirimuya by the Inca people who lived where it was growing in the Andes of South America, is an edible fruit-bearing species of the genus Annona from the family Annonaceae. Annona cherimola Mill is a multipurpose tree with edible fruits and is one of the sources of the medicinal products. The antibacterial activity was measured by agar well diffusion method; the diameter of the zone of bacterial growth inhibition was measured after incubation of plates. The inhibitory effect was studied against the pathogenic bacteria (Klebsiella pneumonia, Bacillus subtilis, Staphylococcus aureus and Escherichia coli (E. coli). Antioxidant assays were also performed for the same extracts by spectrophotometric methods using known standard antioxidants as reference. The studied plant extracts were found to be very effective against the pathogenic microorganisms tested. The methanolic extract of Annona cherimola Mill from showed maximum activity against Escherichia coli and Staphylococcus aureus and the least concentration required showing the activity was 0.5mg/ml. Phytochemical screening of the plants revealed the presence of flavonoids, alkaloids, steroids and carbohydrates. Good presence of antioxidants was also found in the methanolic extracts.Keywords: annona cherimola, phytochemicals, antioxidant and antibacterial activity, methanol extract
Procedia PDF Downloads 442366 Oral Betahistine Versus Intravenous Diazepam in Acute Peripheral Vertigo: A Randomized, Double-Blind Controlled Trial
Authors: Saeed Abbasi, Davood Farsi, Soudabeh Shafiee Ardestani, Neda Valizadeh
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Objectives: Peripheral vertigo is a common complaint of patients who are visited in emergency departments. In our study, we wanted to evaluate the effect of betahistine as an oral drug vs. intravenous diazepam for the treatment of acute peripheral vertigo. We also wanted to see the possibility of substitution of parenteral drug with an oral one with fewer side effects. Materials and Methods: In this randomized, double-blind study, 101 patients were enrolled in the study. The patients were divided in two groups in a double-blind randomized manner. Group A took oral placebo and 10 mg of intravenous diazepam. Group B received 8mg of oral betahistine and intravenous placebo. Patients’ symptoms and signs (Vertigo severity, Nausea, Vomiting, Nistagmus and Gate) were evaluated after 0, 2, 4, 6 hours by emergency physicians and data were collected by a questionnaire. Results: In both groups, there was significant improvement in vertigo (betahistine group P=0.02 and Diazepam group P=0.03). Analysis showed more improvement in vertigo severity after 4 hours of treatment in betahistine group comparing to diazepam group (P=0.02). Nausea and vomiting were significantly lower in patients receiving diazepam after 2 and 6 hours (P=0.02 & P=0.03).No statistically significant differences were found between the groups in nistagmus, equilibrium & vertigo duration. Conclusion: The results of this randomized trial showed that both drugs had acceptable therapeutic effects in peripheral vertigo, although betahistine was significantly more efficacious after 4 hours of drug intake. As for higher nausea and vomiting in betahistine group, physician should consider these side effects before drug prescription.Keywords: acute peripheral vertigo, betahistine, diazepam, emergency department
Procedia PDF Downloads 376365 Quantitative Detection of the Conformational Transitions between Open and Closed Forms of Cytochrome P450 Oxidoreductase (CYPOR) at the Membrane Surface in Different Functional States
Authors: Sara Arafeh, Kovriguine Evguine
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Cytochromes P450 are enzymes that require a supply of electrons to catalyze the synthesis of steroid hormones, fatty acids, and prostaglandin hormone. Cytochrome P450 Oxidoreductase (CYPOR), a membrane bound enzyme, provides these electrons in its open conformation. CYPOR has two cytosolic domains (FAD domain and FMN domain) and an N-terminal in the membrane. In its open conformation, electrons flow from NADPH, FAD, and finally to FMN where cytochrome P450 picks up these electrons. In the closed conformation, cytochrome P450 does not bind to the FMN domain to take the electrons. It was found that when the cytosolic domains are isolated, CYPOR could not bind to cytochrome P450. This suggested that the membrane environment is important for CYPOR function. This project takes the initiative to better understand the dynamics of CYPOR in its full length. Here, we determine the distance between specific sites in the FAD and FMN binding domains in CYPOR by Forster Resonance Energy Transfer (FRET) and Ultrafast TA spectroscopy with and without NADPH. The approach to determine these distances will rely on labeling these sites with red and infrared fluorophores. Mimic membrane attachment is done by inserting CYPOR in lipid nanodiscs. By determining the distances between the donor-acceptor sites in these domains, we can observe the open/closed conformations upon reducing CYPOR in the presence and absence of cytochrome P450. Such study is important to better understand CYPOR mechanism of action in various endosomal membranes including hepatic CYPOR which is vital in plasma cholesterol homeostasis. By investigating the conformational cycles of CYPOR, we can synthesize drugs that would be more efficient in affecting the steroid hormonal levels and metabolism of toxins catalyzed by Cytochrome P450.Keywords: conformational cycle of CYPOR, cytochrome P450, cytochrome P450 oxidoreductase, FAD domain, FMN domain, FRET, Ultrafast TA Spectroscopy
Procedia PDF Downloads 266364 The Effect of Undernutrition on Sputum Culture Conversion and Treatment Outcomes among People with Multidrug-Resistant Tuberculosis: A Systematic Review and Meta-Analysis
Authors: Fasil Wagnew, Kerri Viney, Kefyalew Addis Alene, Matthew Kelly, Darren Gray
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Background: Undernutrition is a risk factor for tuberculosis (TB), including poor treatment outcomes. However, evidence regarding the effect of undernutrition on TB treatment outcomes is not well understood. We aimed to evaluate the effect of undernutrition on sputum culture conversion and treatment outcomes among people with multi-drug resistance (MDR)-TB. Methods: We searched for publications in the Medline, Embase, Scopus, and Web of Science databases without restrictions on geography or year of publication. We conducted a random-effect meta-analysis to estimate the effects of undernutrition on sputum culture conversion and treatment outcomes. Two reviewers independently assessed the study eligibility, extracted the necessary information, and assessed the risk of bias. Depending on the nature of the data, odds ratio (OR) and hazard ratio (HR) with 95% confidence intervals (CIs) were used to summarize the effect estimates. Potential publication bias was checked using funnel plots and Egger’s tests. Results: Of 2358 records screened, 59 studies comprising a total of 31,254 people with MDR-TB were included. Undernutrition was significantly associated with a lower sputum culture conversion rate (HR 0·7, 95% CI 0·6–0·9, I2=67·1%) and a higher rate of mortality (OR 2·9, 95%CI 2·1–3·8, I2=23·7%) and unfavourable treatment outcomes (OR 1·8, 95%CI 1·5–2·0, I2=72·7%). There was no statistically significant publication bias in the included studies. Three studies were low, forty-two studies were moderate, and fourteen studies were high quality. Interpretations: Undernutrition was significantly associated with unfavourable treatment outcomes, including mortality and lower sputum culture conversion among people with MDR-TB. These findings have implications for supporting targeted nutritional interventions alongside standardised second-line TB drugs.Keywords: undernutrition, MDR-TB, sputum culture conversion, treatment outcomes, meta-analysis
Procedia PDF Downloads 142363 Egg Yolk Peptide Stimulated Osteogenic Gene Expression
Authors: Hye Kyung Kim, Myung-Gyou Kim, Kang-Hyun Leem
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Postmenopausal osteoporosis is characterized by low bone density which leads to increased bone fragility and greater susceptibility to fracture. Current treatments for osteoporosis are dominated by drugs that inhibit bone resorption although they also suppress bone formation that may contribute to pathogenesis of osteonecrosis. To restore the extensive bone loss, there is a great need for anabolic treatments that induce osteoblasts to build new bone. Pre-osteoblastic cells produce proteins of the extra-cellular matrix, including type I collagen at first, and then to successively produce alkaline phosphatase (ALP) and osteocalcin during differentiation to osteoblasts. Finally, osteoblasts deposit calcium. Present study investigated the effects of egg yolk peptide (EYP) on osteogenic activities and bone matrix gene expressions in human osteoblastic MG-63 cells. The effects of EYP on cell proliferation, alkaline phosphatase (ALP) activity, collagen synthesis, and mineralization were measured. The expression of osteogenic genes including COL1A1 (collagen, type I, alpha 1), ALP, BGLAP (osteocalcin), and SPP1 (secreted phosphoprotein 1, osteopontin) were measured by quantitative realtime PCR. EYP dose-dependently increased MG-63 cell proliferation, ALP activity, collagen synthesis, and calcium deposition. Furthermore, COL1A1, ALP, and SPP1 gene expressions were increased by EYP treatment. Present study suggested that EYP treatment enhanced osteogenic activities and increased bone matrix osteogenicgenes. These results could provide a mechanistic explanation for the bone-strengthening effects of EYP.Keywords: egg yolk peptide, osteoblastic MG-63 cells, alkaline phosphatase, collagen synthesis, osteogenic genes, COL1A1, osteocalcin, osteopontin
Procedia PDF Downloads 379362 Maternal Health Care Utilization and Its Effect on Pregnancy Outcome in Nepal
Authors: Adrita Banerjee, Ajeet Kumar Singh
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Antenatal care (ANC) from a skilled provider is important to monitor the pregnancy and reduce the risk of morbidity for mother and baby during pregnancy and delivery. The quality of antenatal care can be monitored through the content of services received and the kind of information mothers are given during their visit. Objective: The paper tries to examine the association between ANC check-ups and size/ birth weight. It also focuses on investigating the relationship between utilization of recommended prenatal care for mothers and its effect on infant survival in Nepal. Data and methods: This paper uses data from Nepal demographic Health Survey 2011. To understand the relationship bi-variate statistical analysis and logistic regressions has been done. Maternal health care utilization include ANC check-ups i.e. the type of ante-natal care providers, the number and timing of the visit. The various components of the check-ups include intake of iron tablets/syrups, intestinal parasitic drugs, etc. Results: The results show that women who had no antenatal care visits about 40% had small sized babies at the time of birth compared to women to had at least 3 ANC check up. Women who had at least 3 check-ups 17% of the babies have a small size. It has also been found that about 50 % of the women prefer ANC check-ups during pregnancies which have resulted in lowering the infant mortality by about 40% during 1996-2011. Conclusion: Ante natal care check is care and monitoring of the pregnant woman and her foetus throughout pregnancy. ANC checks have an effect on the infant health and child survival. A woman who had at least three check-ups the possibilities of adverse effect on infant health and infant survival was significantly lower. The findings argue for a more enhanced focus on ANC check-ups for improving the maternal and child health in Nepal.Keywords: maternal, health, pregnancy, outcome
Procedia PDF Downloads 231361 The Gastroprotective Potential of Clematis Flammula Leaf Extracts
Authors: Dina Atmani-Kilani, Farah Yous, Djebbar Atmani
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The etiology of peptic ulcer is closely related to stress, excessive consumption of nonsteroidal anti-inflammatory drugs, or ethanol. Clematis flammula (Ranunculaceae) is a medicinal plant widely used by rural populations to treat inflammatory disorders. This study was designed to assess the gastroprotective potential of C. flammula extracts. Gastric ulcer was induced by stress, indomethacin, HCl / ethanol, and absolute ethanol on NMRI-type mice. The antioxidant potency of the ethanolic extract of Clematis flammula (EECF) was evaluated on catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx) activities. Glutathione (GSH) and malonaldehyde (MDA) levels were also quantified. The anti-inflammatory potential was evaluated through the effect of EECF on myeloperoxidase activity (MPO) and vascular permeability. Complementary tests concerning the quantification of mucus levels, gastric motility, inhibition of ATPase H+/K+activity, as well as a histopathological study were also undertaken to explore the mechanism of action of the EECF. The EECF exhibited a significant (p <0.001) and optimal (100 mg/kg) gastroprotective effect by elevating SOD, CAT, and GSH levels, thereby minimizing the production of MDA and lowering the activity of MPO and vascular permeability. EECF also increased the rate of mucus production, decreased gastric motility, and completely suppressed the H+/K+ ATPase activity. Histopathological study confirmed the effectiveness of the extract in the prevention of peptic ulcer. The results obtained in this study demonstrated the gastro-protective effect of EECF via acidic antioxidant, anti-inflammatory, cytoprotective and anti-secretory mechanisms, which may justify its use as a substitute in peptic ulcer treatment.Keywords: clematis flammula, superoxide dismutase, myeloperoxidase, ATPase, pump
Procedia PDF Downloads 194360 A Machine Learning-Based Model to Screen Antituberculosis Compound Targeted against LprG Lipoprotein of Mycobacterium tuberculosis
Authors: Syed Asif Hassan, Syed Atif Hassan
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Multidrug-resistant Tuberculosis (MDR-TB) is an infection caused by the resistant strains of Mycobacterium tuberculosis that do not respond either to isoniazid or rifampicin, which are the most important anti-TB drugs. The increase in the occurrence of a drug-resistance strain of MTB calls for an intensive search of novel target-based therapeutics. In this context LprG (Rv1411c) a lipoprotein from MTB plays a pivotal role in the immune evasion of Mtb leading to survival and propagation of the bacterium within the host cell. Therefore, a machine learning method will be developed for generating a computational model that could predict for a potential anti LprG activity of the novel antituberculosis compound. The present study will utilize dataset from PubChem database maintained by National Center for Biotechnology Information (NCBI). The dataset involves compounds screened against MTB were categorized as active and inactive based upon PubChem activity score. PowerMV, a molecular descriptor generator, and visualization tool will be used to generate the 2D molecular descriptors for the actives and inactive compounds present in the dataset. The 2D molecular descriptors generated from PowerMV will be used as features. We feed these features into three different classifiers, namely, random forest, a deep neural network, and a recurring neural network, to build separate predictive models and choosing the best performing model based on the accuracy of predicting novel antituberculosis compound with an anti LprG activity. Additionally, the efficacy of predicted active compounds will be screened using SMARTS filter to choose molecule with drug-like features.Keywords: antituberculosis drug, classifier, machine learning, molecular descriptors, prediction
Procedia PDF Downloads 381359 Survival and Retention of the Probiotic Properties of Bacillus sp. Strains under Marine Stress Starvation Conditions and Their Potential Use as a Probiotic for Aquaculture Objectives
Authors: Abdelkarim Mahdhi, Fdhila Kais, Faouzi Lamari, Zeineb Hmila, Fathi Kamoun, Maria Ángeles Esteban, Amina Bakhrouf
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Aquaculture is the world’s fastest growing food-production sector. However, one of the most serious problems regarding the culture of marine fishes is the mortality associated with pathogenic bacteria that occurs in the critical phases of larval development. Conventional approaches, such as the use of antimicrobial drugs to control diseases, have had limited success in the prevention or cure of aquatic diseases. Promising alternatives to antibiotics are probiotics, which are food supplements consisting of live microorganisms that benefit the host organism. In the search for more effective and environmentally friendly treatments with probionts against pathogenic species in shrimp larval culture, the probiotic properties of Bacillus strains isolated from Artemia culture such as antibacterial activity, adhesion, pathogenicity, toxicity and the effect of marine stress on viability and survival were investigated, as well as the changes occurring in their properties. Analyses showed that these bacteria corresponded to the genus Bacillus sp. Antagonism and adherence assays revealed that these strains have an inhibitory effect against pathogenic bacteria in vitro and in vivo conditions and are fairly adherent. Challenge tests performed with Artemia larvae provided evidence that the tested Bacillus strains were neither pathogenic nor toxic to the host. The tested strains maintained their viability and their probiotic properties during the period of study. The results suggest that the tested strains have suffered changes allowing them to survive in seawater in the absence of nutrients and outside their natural host, identifying them as potential probiotic candidates for Artemia culture.Keywords: bacillus, probiotic, cell viability, stress response
Procedia PDF Downloads 377358 Antioxidant and Cytotoxic Effects of Different Extracts of Fruit Peels Against Three Cancer Cell Lines
Authors: Emad A. Shalaby
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Cancer is a disease that causes abnormal cell proliferation and invades nearby tissues. Lung cancer is the second most frequent cancer worldwide. Natural anti-cancer drugs have been developed with low side effects and toxicity. Citrus peels and extracts have been demonstrated to have significant pharmacological and physiological effects as a result of the high concentration of phenolic compounds found in citrus fruits, particularly peels. Tangerine peels can serve as an effective source of bioactive substances such as phenolics, flavonoids, and catechins, which have antioxidant, antibacterial, anticancer, and anti-inflammatory properties. Consequently, this work aims to determine the anticancer activity of ethanol extract of Tangerine peels against the A549 cell line and identify the phenolic compound profile (19 compounds) by using HPLC. Anticancer and antioxidant potentials of the extract were evaluated by MTT assay and TLC- TLC-bioautography sprayed with DPPH reagent, respectively. The obtained results revealed that tangerine peel extract showed significant activity against the A549 cell line with IC50 of 97.66 μg/mL. HPLC analysis proved that the highest concentration is naringenin 464.05 mg/g. More studies indicate that naringenin has significant anticancer potential on A549 cancer cells. The results showed that naringenin binds t0 EGFR protein in A549 with high binding affinity and thus may reduce lung cancer cell migration and enhance the apoptosis of cancer cells. From the obtained results it could be concluded that tangerine peel extract is an effective anti-cancer agent that may potentially serve as a natural therapeutic option for lung cancer treatment.Keywords: tangerine peel, A549 cell line, anticancer, naringenin, HPLC analysis, naringenin, TLC bioautography
Procedia PDF Downloads 54357 The Effects on Abomasal Emtying Rate of Erythromycin and Bethanechol in Healthy, Premature and Diarrheic Calves
Authors: Sebnem Canikli Engin, Mutlu Sevinc, Hasan Guzelbektes
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In this study, we aim to define the effects of erythromycin and bethanechol which are prokinetic agents, on the value of abomasal discharge in healthy, diarrhea and premature calves. In the work, 5 healty calves, 12 diarrheaic calves and 12 premature calves, amounting to a total of 29 calves. In healty calves work; the same 5 calves were used for controlled, erythromycin and bethanechol studies (there was a 48-hour waiting period between each work). In diarrheic calves work; 12 diarrheic calves were used during the study (4 of them for control group, 4 of them bethanechol group and last 4 calves erythromycin group). In premature calves works; 12 premature calves were used during the study (4 of them for control group, 4 of them bethanechol group and last 4 calves erythromycin group). 10 mg/kg IM dose of erythromycin were applied to each erythromycin group, 0,07 mg/kg IM dose of bethanechol were applied on bethanechol group. No drugs were applied to the control group and substitution milk was given to all calves. 50 mg/kg acetominophen and 25 gram/L glucose have been added into the substitution milk to evaluate the speed of gastrointestinal motility with the test results of absorptions of acetominophen and glucose. The blood samples have been taken before substitution milk application and 30, 60, 90, 120, 180, 240 and 300 minutes after substitution milk application. Respiratory rates and number of heartbeats were also recorded during the test time. No changes were observed in the number of heartbeats, respiratory rates and general conditions for all groups after drug application. It is observed that, the feces of some calves became slightly watery and viscous and premature calves generaly defecated after 180 minutes. When Cmax, Tmax and AUC values of acetaminophen and glucose are compared with control group’s after applying erythromycin on the calves in the premature group, we obtain higher Cmax (P<0,05), shorter Tmax and greather AUC (P>0,05) values. In conclusion, according to clinical and laboratory findings, it may be stated that the application of 10 mg/kg doze of erythromycin IM has provided faster abomazal emptying in premature calves.Keywords: abomazal emptying, bethanechol, calf, erythromycin
Procedia PDF Downloads 327356 Assessment of Maternal Satisfaction Regarding Quality of Care during Labor
Authors: Farida Habib, Haya Alfozan, Eman Miligi, Najla Alotaibi
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Background: Women’s satisfaction with maternity services, especially care during labor and birth, has become highly significant to healthcare providers, administrators, and policymakers. Purpose: The aims of this study were to assess maternal satisfaction regarding the quality of care during labor and to compare the level of maternal satisfaction between women who delivered by physicians and those delivered by midwives. Methodology: A descriptive, cross-sectional, correlational design was used. A convenient sample of 180 low-risk cases of immediate postpartum women who delivered at King Abdul-Aziz medical city was recruited. Women whose babies were diagnosed with serious health problems were excluded from the study. Data were collected using a self-administered questionnaire. The validity and reliability of the questionnaire were ensured. The questionnaire included three parts, namely: demographics data, medical history, and obstetrical history, and the last part is the satisfaction assessment tool. Ethical confederations were ensured. Maternal satisfaction during labor was classified in terms of health care, health workers' communication, and the environment. Results: Regarding health care, women were highly satisfied with care received from nurse (M = 4.21 + 0.88), medical care received (M = 4.17 + 0.79), and comfort techniques (M = 4.04 + 0.91). Regarding health workers' communication, women were highly satisfied with the provider to treat with dignity and respect (M = 4.03 + 0.91) and orientation to the toilet, bathroom, washing area (M = 4.00 + 0.93). Regarding the environment, women were highly satisfied with the experience of their baby's birth (M = 4.18 + 0.98) and supplies with drugs and supplies (M = 4.09 + 0.97). There was no statistically significant difference in maternal satisfaction between women who delivered by physicians and those delivered by midwives. Conclusion: Women were generally satisfied with their labor and delivery experience. There was no difference in maternal satisfaction on the labor process between women who delivered by physicians and those delivered by midwives.Keywords: maternity, satisfaction, labor, delivery
Procedia PDF Downloads 176355 Spironolactone in Psoriatic Arthritis: Safety, Efficacy and Effect on Disease Activity
Authors: Ashit Syngle, Inderjit Verma, Pawan Krishan
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Therapeutic approaches used previously relied on disease-modifying antirheumatic drugs (DMARDs) that had only partial clinical benefit and were associated with significant toxicity. Spironolactone, an oral aldosterone antagonist, suppresses inflammatory mediators. Clinical efficacy of spironolactone compared with placebo in patients with active psoriatic arthritis despite treatment with prior traditional DMARDs. In the 24-week, placebo-controlled study patients (n=31) were randomized to placebo and spironolactone (2 m/kg/day). Patients on background concurrent DMARDs continued stable doses (methotrexate, leflunomide, and/or sulfasalazine). Primary outcome measures were the assessment of disease activity measures i.e. 28-joint disease activity score (DAS28) and diseases activity in psoriatic arthritis (DAPSA) at week 24. The key secondary endpoint was change from baseline in Health Assessment Questionnaire–Disability Index (HAQ-DI) at week 24. Additional efficacy outcome measures at week 24 included improvements in the markers of inflammation (ESR and CRP) and pro-inflammatory cytokines TNF-α, IL-6 and IL-1. At week 24, spironolactone significantly reduced disease activity measure DAS-28 (p<0.001) and DAPSA (p=0.001) compared with placebo. Significant improvements in key secondary measures HAQ-DI (disability index) were evident with spironolactone (p=0.02) versus placebo. After week 24, there was significant reduction in pro-inflammatory cytokines level TNF-α, IL-6 (p<0.01) as compared with placebo group. However, there was no significant improvement in IL-1 in both treatment and placebo groups. There were minor side effects which did not mandate stopping of spironolactone. No change in any biochemical profile was noted after spironolactone treatment. Spironolactone was effective in the treatment of PsA, improving disease activity, physical function and suppressing the level of pro-inflammatory cytokines. Spironolactone demonstrated an acceptable safety profile and was well tolerated.Keywords: spironolactone, inflammation, inflammatory cytokine, psoriatic arthritis
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