bluuebunny/crossref_metadata_2025 huggingface dataset:
DIFFERENCES IN THE POTENTIAL MUTAGENICITY OF RESIN-, SILICONE-, AND BIOCERAMIC-BASED SEALERS ON LYMPHOCYTES: A PROTEIN EXPRESSION ANALYSIS
Authors: SURYADARMA SANI , . KAMIZAR , SUPRASTIWI ENDANG , MEIDYAWATI RATNA , FITRI MAIDA
Published: April 2019

Objective: The objective of this study was to compare the potential mutagenicity of resin-, silicone-, and bioceramic-based sealers on proteinexpression in human lymphocytes. There has been limited research on resin-, silicone-, and bioceramic-based sealers effects on protein expressionin lymphocytes.Methods: Nine samples of each sealer were incubated in 2 mL human blood for 1, 3, and 7 days. Then, the isolated lymphocytes are observed forprotein separation by electrophoresis method. Profile of protein bands observed and data were analyzed statistically by Kruskal–Wallis and post hocMann–Whitney.Results: Although no statistically significant differences in protein bands were observed among the resin-, silicone-, and bioceramic-based sealers(p=0.111), there was a statistically significant difference between the resin- and silicone-based sealers on the 1st day (p=0.046) and 3rd day (p=0.046)and between the silicone- and bioceramic-based sealers on the 1st day (p=0.046). Thus, the present study shows that there were differences in thepotential mutagenicity on the 1st day; resin was potentially more mutagenic followed by bioceramic and silicone. On the 3rd and 7th days, bioceramicwas potentially more mutagenic followed by resin and silicone.Conclusion: The manuscript describes the study in detail and concludes that resin was potentially more mutagenic followed by bioceramic- andsilicone-based sealers.
ANTIOXIDATIVE ACTIVITY OF ALPHA-MANGOSTIN IN ACETALDEHYDE-INDUCED HEPATIC STELLATE CELLS: AN IN VITRO STUDY
Authors: LESTARI NOVRIANTIKA , PRATAMA SAMUEL , GOTAMA KELVIN THEANDRO , SOETIKNO VIVIAN , LOUISA MELVA
Published: April 2019

Objective: Alcohol accumulation in the liver can cause pathological disorders such as liver fibrosis that can develop into hepatocellular carcinoma,one of the main causes of mortality associated with liver disease. The previous studies have shown that a plant compound, alpha-mangostin, has anantioxidant effect in the inhibition of pancreatic tumor growth in vitro. This study aimed to analyze the antioxidative properties of alpha-mangostin inacetaldehyde-induced liver fibrosis in vitro.Methods: Immortalized hepatic stellate cells (HSCs), of the LX-2 cell line, were incubated with acetaldehyde in the presence or absence of alphamangostin(10 and 20 μM). The cells were then counted and lysed, and LX-2 cell viability was determined with the trypan blue exclusion method. Themalondialdehyde levels, superoxide dismutase activity, and glutathione (GSH) levels were also determined using the cell lysates.Results: Acetaldehyde treatment resulted in a significant increase in HSC cell viability and decreased the production of GSH. Alpha-mangostintreatment resulted in reduced cell viability of the HSCs and prevention of the loss of intracellular GSH.Conclusion: Alpha-mangostin reduced acetaldehyde-induced cell proliferation, and this was affected at least in part by its antioxidative properties
THE EFFECT OF CURCUMIN ON THE PROLIFERATION AND EXTRACELLULAR MATRIX PRODUCTION IN ETHANOL-INDUCED HEPATIC STELLATE CELLS
Authors: RAHMANIAH RAHMANIAH , LOUISA MELVA , WARDHANI BANTARI WK , SOETIKNO VIVIAN
Published: April 2019

Objectives: In various liver disease models, including those for alcoholic liver diseases, curcumin, a polyphenolic compound derived fromCurcuma longa, is known to have an hepatoprotective effect. However, the mechanism of action underlying its effects on alcohol-induced hepaticfibrosis remains unknown. We aimed to investigate the mechanisms of action underlying the effects of curcumin, mainly involving the transforminggrowth factor (TGF)-β/Smad pathway.Methods: Hepatic stellate cells (HSCs), LX2, were incubated with 50 mM ethanol with or without curcumin (1 and 10 μM). Viable HSCs were countedusing a LUNATM automated cell counter, whereas the expressions of TGF-β, Smad3, tissue inhibitor of metalloproteinases-1 (TIMP-1), and type 1collagen mRNA were measured using quantitative reverse transcriptase polymerase chain reactions.Results: Curcumin significantly suppressed ethanol-induced HSCs proliferation. The antiproliferative effect of curcumin appeared to be dosedependent. In addition, the mRNA expressions of TGF-β, Smad3, TIMP-1, and type 1 collagen decreased in the cells treated with curcumin.Conclusion: Curcumin seems to attenuate ethanol-induced HSCs proliferation through the suppression of TGF-β and appears to reduce the productionof extracellular matrix as shown by the decreased expression of type 1 collagen.
ANTIBACTERIAL EFFECTIVENESS OF 2% CHITOSAN AND 2% CHLORHEXIDINE AGAINST ENTEROCOCCUS FAECALIS IN BIOFILM (LABORATORY EXPERIMENT)
Authors: SIMANJUNTAK PRISCILLA ARLYTA , DJAUHARIE NILAKESUMA , NURSASONGKO BAMBANG
Published: April 2019

Objective: Enterococcus faecalis can form biofilms and has a major role in the etiology of persistent lesions after root canal. We analyzed the efficacyof chitosan and chlorhexidine against E. faecalis in biofilms.Methods: Polymerase chain reaction was used to analyze E. faecalis DNA that survived and lived after immersing the biofilm in an antibacterialsolution.Results: A statistically significant difference was noted in living E. faecalis between chitosan and control and between 2% chlorhexidine and controlgroups (p≤0.05). No significant difference was noted between chitosan and chlorhexidine groups (p>0.05).Conclusions: Antibacterial effectivity of chitosan is equal to that of chlorhexidine against E. faecalis in biofilm.
EFFECT OF TRIPLE ANTIBIOTIC PASTE, CALCIUM HYDROXIDE, LEDERMIX® ON VIABILITY OF PULP MESENCHYMAL STEM CELLS
Authors: PRASANTI EMIRIA DITA , MARGONO ANGGRAINI , DJAUHARIE NILAKESUMA
Published: April 2019

Objective: The goal of regenerative endodontic therapy is biological healing of the pulp tissue. It involves the disinfection of the canals with irrigantsand medicaments. The medicaments that are currently used for this purpose are a triple antibiotic paste (TAP), calcium hydroxide (Ca[OH]2), andLedermix®, a paste containing demeclocycline and triamcinolone. Therefore, the purpose of this study was to evaluate the effects of TAP, Ca(OH)2, andLedermix® on the viability of dental pulp stem cells (DPSC).Methods: Primary cultures of DPSC were obtained from immature third molars. Immunofluorescence assay using STRO-1 marker was performedto confirm the mesenchymal nature of the DPSC. The cells were exposed to TAP, Ca(OH)2, and Ledermix® at concentrations of 0.1 and 1 mg/mL. Cellviability was analyzed using the MTT assay.Results: Significant differences in viability were noted between the cells exposed to the medicaments and those in the control group (p<0.05).Conclusions: All three medicaments decreased the viability of DPSC, with the Ledermix® paste demonstrating the highest toxic effect.
GARLIC EXTRACT EFFICACY AGAINST THE VIABILITY OF ENTEROCOCCUS FAECALIS (IN VITRO)
Authors: OCTAVIA ANDRIANI , BUDIARDJO SARWORINI BAGIO , INDIARTI IKE SITI , FAUZIAH EVA , SUHARSINI MARGARETHA , SUTADI HERIANDI , RIZAL MOCHAMAD FAHLEVI
Published: April 2019

Objective: Enterococcus faecalis, Gram-positive facultative anaerobe capable of invading the dentinal tubules, is resistant to several irrigating solutionsand intracanal medications. Motivated by the antibacterial effect exhibited by garlic extract against a wide variety of Gram-positive and Gram-negativebacteria, as well as anaerobic bacteria such as Lactobacillus and E. faecalis, we aimed in this study to analyze the efficacy of garlic extract against theviability of E. faecalis from clinical isolates of nonvital primary root canals.Methods: We used MTT assay to determine the viability of E. faecalis after exposure to increasing concentrations of garlic extract (10%, 25%, 50%,and 100%) and chlorhexidine (CHX) 2% as a positive control.Results: We performed the analysis using the Kruskal–Wallis test and the post hoc test for multiple comparisons at a 0.05 significance level. At allconcentrations, garlic extracts decreased the viability of E. faecalis. We found no significant differences between the viability values for 25%, 50%,and 100% garlic extracts (p>0.05); however, they were significantly different from the 10% extract and CHX 2% (p<0.05), both with a lower viabilityvalues.Conclusion: Our results showed that garlic extract was effective in decreasing the viability of E. faecalis.
EFFICACY OF DISINFECTANTS AGAINST GRAM-POSITIVE BACTERIA FOUND ON THERMOPLASTIC RETAINERS
Authors: ISMAH NADA , PURWANEGARA MIESJE K , RAHMAWATI TUTI
Published: April 2019

Objective: The present study aimed to compare the efficacy of two disinfectants against Gram-positive bacteria, particularly Streptococcus mutans,for use as a disinfectant for dental retainers.Methods: In total, 35 thermoplastic retainers in this study were categorized into three immersion groups: control group; mouthwash group, usingchlorhexidine 0.1%; and denture cleanser tablet group. The retainers were worn for 15 days, and Gram-positive bacteria were enumerated before andafter the retainers were immersed.Results: We found a significant difference in bacterial numbers between the two disinfectant groups and the non-disinfectant or control group. Bothdisinfectant groups had decreased numbers of Gram-positive bacteria.Conclusions: Disinfectant use is effective in decreasing the load of Gram-positive bacteria on thermoplastic retainers.
IN SILICO STUDY OF SIRT1 ACTIVATORS USING A MOLECULAR DYNAMIC APPROACH
Authors: AZMINAH AZMINAH , RADJI MAKSUM , MUN’IM ABDUL , SYAHDI REZI RIADHI , YANUAR ARRY
Published: April 2019

Objective: The importance of SIRT1 activator’s role in antidiabetic and anti-aging therapies is widely demonstrated. Drug discovery and developmentare time consuming. Drug design can be performed in silico using molecular dynamic approaches to accelerate and facilitate identification of the bestcompound candidates and their physicochemical characteristics and hit-to-lead selection.Methods: In silico study of SIRT1 activator for complexes using of Protein Data Bank (PDB) IDs 4ZZI, 4ZZJ 4ZZH, and 5BTR and 4TO ligand. Ligand–receptor interactions and bond energies were determined using molecular docking with the AutoDock4Zn program. Then, the complex with thebest bond energy was identified using a simulation of the molecular dynamics (50 ns) using the Amber program, and values for root mean squaredeviation, root mean square fluctuation, and bond energy were determined using the Molecular Mechanic–Poisson Boltzmann (Generalized Born)surface area (MM-PB[GB]SA) calculation.Results: Interaction analysis between activator ligand (4TO) and the SIRT1 receptor (PDB IDs 4ZZJ and 5BTR) revealed the ligand’s selectivity forhydrophobic interaction at Leu206, Ile223, Ile227, and hydrophilic interaction at Asn226, Glu230. Hydrogen bond interactions between Glu230 and Arg234(allosteric region) with Arg446, Val459, His473, and Asp475 (catalytic region) brought them close to the bounding substrate area. Bond energy valuesobtained using the MM-GB(PB)SA calculation showed 4TO interaction with 4ZZJ (MMGBSA ΔG, −31.4729–−26.6756; MMPBSA ΔG, −32.6292–−28.486].The bond energy value of the 4TO interaction with 5BTR showed MMGBSA ΔG = −40.6255–−30.0653 and MMPBSA ΔG = −34.6713–−25.9951.Conclusions: These findings provide important information on the target interaction of the bonds to the more selective SIRT1 activator useful fordrug discovery and development.
ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITY OF SYNTHESIZED MANNICH BASE DERIVATIVES OF (2E,6E)-2-[(4-HYDROXY-3-METHOXYPHENYL)METHYLIDENE]-6-(PHENYL METHYLIDENE)CYCLOHEXAN-1-ONE
Authors: HAYUN HAYUN , MAGGADANI BAITHA PALANGGATAN , KURNIA ARINI , HANIFAH AULIA , YULIANDI MEIDI , FITRIYANI IDA , HADRIANTI SEPTIANI PUTRI
Published: April 2019

Objective: To further understand this compound, we synthesized and evaluated the antioxidant and anti-inflammatory activity of a series of itsMannich base derivatives.Methods: We synthesized the compounds via the previously reported Mannich reaction method. Their structures were elucidated by Fouriertransforminfrared,1H-NMR,13C-NMR, and high-resolution mass spectra. The derivatives’ anti-inflammatory and antioxidant activities were testedusing the inhibition of protein denaturation method and the 2,2-diphenyl-2-picrylhydrazyl free radical scavenging assay.Results: The IC50 values for the anti-inflammatory activity of the 2,6-dimethylmorpholine, pyrrolidine, 1-methylpiperazine, and dimethylamineMannich base derivatives 2a–d were 10.67, 10.72, 37.75, and 1.93 μM, respectively; for (2E,6E)-2-({4-hydroxy-3-methoxyphenyl}methylidene)-6-(phenylmethylidene)cyclohexan-1-one (1), diclofenac sodium, and curcumin, the IC50 values were 56.29, 1.52, and 8.43 μM, respectively. The IC50values for the antioxidant activity of compounds 2a–2d were 229.62, 57.29, 280.43, and 219.22 μM, respectively; for compound 1, quercetin, andcurcumin, the IC50 values were 144.22, 27.28, and 26.45 μM, respectively.Conclusion: Substituting Mannich bases into (2E,6E)-2-[(4-hydroxy-3-methoxyphenyl) methylidene]-6-(phenylmethylidene)cyclohexan-1-oneenhanced its anti-inflammatory activity, but lowered its antioxidant activity. Compound 2d, (2E,6E)-2-({3-[(dimethylamino)methyl]-4-hydroxy-5-methoxyphenyl}methylidene)-6-(phenyl methylidene)cyclohexan-1-one, exhibited potent anti-inflammatory activity comparable to diclofenacsodium and four times higher than curcumin. However, further investigation of this compound’s mechanism of action and toxicity is warranted.
EFFECTS OF CENTELLA ASIATICA (L.) LEAF EXTRACT ON BONE CALCIUM AND PHOSPHATE LEVELS OF OVARIECTOMIZED RATS
Authors: BONG YULITA , SOEKANTO SRI ANGKY , IDRUS ERIK
Published: April 2019

Objective: This study aimed to evaluate the efficacy of Centella asiatica leaf extract in maintaining calcium and phosphate levels in the bone forpreventing osteoporosis in postmenopausal women.Methods: The obtained C. asiatica leaf extract was administered to ovariectomized rats at the doses of 60, 120, and 180 mg/kg body weight (BW)for 30 days. Subsequently, the rats were euthanized by ether overdose, and bone calcium and phosphate levels were determined by the wet ashingtechnique and spectrophotometry.Results: The results showed no significant differences in the bone calcium and phosphate levels among rats administered with different doses ofC. asiatica leaf extract.Conclusion: Our results indicate that C. asiatica leaf extract cannot be used as a source of phytoestrogens to maintain calcium and phosphate levelsin the bones.
EFFECTIVENESS OF TOOTHPASTE CONTAINING PROPOLIS, TEA TREE OIL, AND SODIUM MONOFLUOROPHOSPHATE AGAINST PLAQUE AND GINGIVITIS
Authors: SURIAMAH NELLY , LESSANG ROBERT , KEMAL YULIANTI
Published: April 2019

Objective: Natural ingredients such as propolis and tea tree oil are known to possess antibacterial and anti-inflammatory effects that areeffective against periodontal diseases. This study aimed to determine the effectiveness of toothpaste containing propolis, tea tree oil, and sodiummonofluorophosphate against dental plaque and gingivitis.Methods: A randomized clinical trial was conducted for 7 days with 20 subjects in test (using the experimental toothpaste) and control (usingtoothpaste without any natural ingredients) groups each. Measurements of plaque index (PI) and papillary bleeding index (PBI) scores wereperformed on days 0 and 7.Results: Significant decreases (p<0.05) in PI (0.53–0.27) and PBI (0.55–0.11) scores were noted in the test group but not in the control group.Conclusions: Brushing teeth with toothpaste containing propolis, tea tree oil, and sodium monofluorophosphate might be effective in reducing theaccumulation of dental plaque and the severity of gingival bleeding.
IN VITRO ANTIBACTERIAL EFFECT OF BREADFRUIT LEAF EXTRACT AGAINST STREPTOCOCCUS SANGUINIS ATCC 10556 BIOFILM
Authors: NADIA VAZA , UTAMI SRI , FARIDA RATNA
Published: April 2019

Objective: Evidence indicates that breadfruit leaf extract may have antibacterial properties. In terms of bacterial plaque, Streptococcus sanguinis isknown as an early agent of its formation. The purpose of this study was to analyze the antibacterial effects of breadfruit leaf extract on the growth ofS. sanguinis.Methods: S. sanguinis ATCC 10556 was cultured in 96-well plates and was incubated at 37°C for 20 h (the accumulation phase) or 24 h (the maturationphase). Then, breadfruit leaf extract was added at concentrations of 5, 10, 20, 40, 80, and 100%. The viability of S. sanguinis was evaluated using the3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay at a wavelength of 490 nm.Results: Our results demonstrated that the viability of S. sanguinis, after exposure to the breadfruit leaf extract at all concentrations, during theaccumulation and maturation phases was lower than the control group (p<0.05). In addition, the viability of S. sanguinis after exposure to the breadfruitleaf extract at concentrations of 20, 80, and 100% during the accumulation phase was lower than that observed during the maturation phase.Conclusion: Collectively, our novel findings should provide insight into the potential of breadfruit leaf extract to positively affect oral and dentalhealth.
EVALUATION OF MEDICATION COMPLIANCE IN PATIENTS WITH CONGESTIVE HEART FAILURE IN YEMEN
Authors: MOHAMMED AL-Z AL-ZAAZAAI ET AL ALI AHMED , AL-AMRANI MANSOUR A. , ALAKHALI KHALID , ALJABER NOURADDEN
Published: April 2019

Objective: Non-compliance with heart failure medication is related to the highest mortality, morbidity, and health-care costs. The objective of this study was to evaluate medication compliance with patients with congestive heart failure.

Methods:Inpatients of the cardiac care unit and medical ward of Republican Hospital, German Hospital, Revolutionary Hospital, and Chinese–Yemeni Friendship Hospital were recruited for this study. The study was conducted on patients that were diagnosed as having congestive heart failure and were receiving treatment. Questionnaires were distributed and personal interviews to evaluate the patients’ compliance was conducted to determine the reasons for their non-compliance in taking drugs.

Results: Of 86 patients, 44% (n = 38) reported compliance and 56% (n = 48) reported non-compliance. The distribution of the patients in terms of sex was as follows: among men, 41% (n = 24) were compliant and 59% (n = 35) were non-compliant; among women, 52% (n = 14) were compliant and 48% (n = 13) were non-compliant. In addition, smoking status was too significantly linked with non-compliance (P = 0.001). Furthermore, the status of chewing of khat tree leaves was also significantly associated with non-compliance (P = 0.007).

Conclusion: This study indicates that the reasons for non-compliance with medications among patients can be attributed to lack of education, chewing of khat tree leaves, lack of health insurance, and cigarette smoking. Therefore, healthcare professionals should create strategies to address these reasons in order to increase medication compliance with patients in heart failure.
DRUMSTICK MUCILAGE MICROSPHERES FOR CONTROLLED RELEASE OF LAMIVUDINE: DESIGN, OPTIMIZATION AND IN VITRO EVALUATION
Authors: Gada Santosh G , Y. ANANDKUMAR , SETTY C. MALLIKARJUN
Published: April 2019

Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage.

Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design.

Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism.

Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.
DEVELOPMENT AND VALIDATION OF SENSITIVE LC-ESI-MS/MS METHOD FOR THE SIMULTANEOUS ESTIMATION OF DAPAGLIFLOZIN AND SAXAGLIPTIN IN HUMAN PLASMA
Authors: Adluri Phanindra , Y Shravan Kumar
Published: April 2019

Objective: To develop and validate a sensitive liquid chromatography-electrospray ionization-tandem mass spectrometric (LC-ESI-MS/MS) technique for the quantification of dapagliflozin and saxagliptin in plasma by linagliptin as internal standard.

Methods: Chromatography was achieved on hypersil C18 (50 mmx4 mm) 5 µ analytical column with 0.1% formic acid and acetonitrile (25:75 V/V) as mobile phase at 0.7 ml/min flow rate. Dapagliflozin, saxagliptin, and linagliptin were detected at m/z 409.14/135.0, m/z 316.2/180.13 and m/z 472.54/456.21 respectively. Drugs and internal standard were extracted by LLE (liquid-liquid extraction).

Results: Developed technique was validated over 0.5-1500.0 ng/ml linear concentration range for dapagliflozin and 2.00-2000.0 ng/ml for saxagliptin. This method established with intra-batch and inter-batch precision within 2.44-8.12% and 1.25-7.14 % for dapagliflozin and 1.84-7.5 % and 1.02–6.00 % for saxagliptin. This method established with intra-batch and inter-batch accuracy for dapagliflozin within 98.86-103% and 96.98-102 % respectively and for saxagliptin within 98.05-109.06 % and 97.00-104.00 % respectively.

Conclusion: Both dapagliflozin and saxagliptin were stable during three freeze-thaw cycles, long term and bench-top stability studies. The developed method was useful for the routine analysis of dapagliflozin and saxagliptin simultaneously in plasma samples.
SIMPLE METHOD FOR OPTIMIZATION OF HEPARIN AND ENOXAPARIN DETECTION USING AGAROSE GEL ELECTROPHORESIS
Authors: Almeman Ahmad Abdulrahman
Published: April 2019

Objective: A simple gel electrophoresis method for low-molecular-weight heparins (LMWH) is required for use in a variety of laboratories to allow further identification and purification. This study aimed to optimize the detection of heparin and enoxaparin (low-molecular-weight heparin by gel electrophoresis.

Methods: Several gel electrophoresis conditions were tested to optimize the detection of enoxaparin by using a simple method with a modified Volpi’s approach. Multiple gel thicknesses, voltage settings, and enoxaparin concentrations were tested in the optimization procedure. Enoxaparin was purchased from a local supplier as pre-filled pharmaceutical injections. Highly purified 0.5% and 1.0% agarose gels were prepared and a series of enoxaparin concentrations was added to both gels for comparison and optimization. The 0.2% toluidine blue stain was prepared by the addition of 1 ml in an ethanol-water-acetic acid mixture (50:49:1; v/v/w). The staining process comprised two steps: first, toluidine blue was added for 30 min and destained overnight in the solvent mixture. Subsequently, the following morning, the second step was conducted, in which the gel was restained for 30 min with the same concentration of toluidine blue. We continued to stain the gel until the bands were visible.

Results: The gel electrophoresis results showed that clearest and sharpest bands were obtained using 65–75 mAh and 85 V settings. At 95 mAh, the bands were slightly washed out.

Conclusion: This study successfully facilitated the detection of enoxaparin, a LMWH, and heparin in the laboratory by using simple tools and techniques available in most laboratories.
3D QSAR AND DOCKING STUDY OF INDOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS
Authors: Chavan Rajashree , MORE HARINATH
Published: April 2019

Objective: Non-steroidal anti-inflammatory agents (NSAIDs) continue to be one of the most widely used groups of therapeutic agents. QSAR (quantitative structure-activity relationship) approach is a very useful and widespread technique for drug design. 3D QSAR facilitates evaluation of three-dimensional molecular fields around molecules and generates a relationship of these fields' values with the activity.

Methods: 3D QSAR study was performed on selected twenty-four compounds from synthesized indole derivatives using the stepwise variable selection k-nearest neighbor (kNN) molecular field analysis approach for indicating the contribution of the steric and electronic field for activity. The docking study was performed to further confirm the binding affinity of synthesized molecules (ligands) to COX-2 enzyme as well as to study binding nature.

Results: Statistically significant model was generated using VLife Molecular Design Suite 3.5 software with cross-validated correlation coefficient q2 of 0.9461 and high predictive correlation coefficient (Pred_r2) of 0.8782 indicating that the model is robust. The results of docking study suggest that the synthesized compounds have a comparable binding affinity with the COX-2 enzyme.

Conclusion: The present study may prove to be helpful in the development and optimization of existing indole derivatives as anti-inflammatory agents with selective COX-2 inhibition.
Campesinos a contracorriente. Estrategias organizativas, productivas y comerciales de la cooperativa indígena campesina Maya Vinic
Authors: López Barrios Cledi , Zamora Lomelí Carla , Cortina Villar Sergio , Pat Fernández Lucio
Published: April 2019

El objetivo de este artículo es examinar las estrategias organizativas, productivas y comerciales implementadas por la cooperativa Maya Vinic, para que la miel orgánica que produce permanezca en el esquema de comercio justo. El enfoque analítico empleado es la teoría de la acción colectiva orientada a la movilización de recursos, con información de entrevistas semiestructuradas y observación participante. Aquí se aportan elementos para comprender la dinámica de una organización de pequeños productores rurales para permanecer en el comercio justo, que les procura estabilidad y garantiza la vigencia de la actividad campesina. Los resultados muestran que, mediante la acción colectiva, la cooperativa ha podido fortalecer el capital social, recibir apoyo de organismos solidarios y asesores externos, generar economías de escala y lograr la capitalización. Se concluye que se requieren estrategias para arraigar a los jóvenes en sus comunidades, y mecanismos para adaptar la apicultura a las exigencias del mercado y a la precariedad de recursos de los miembros.
Relaciones cuantitativas estructura-actividad/propiedad en dos dimensiones empleando el programa R
Authors: Dominguez Dueñas Laura , Goode-Romero Guillermo , Aguayo-Ortiza Rodrigo
Published: April 2019

 

Las relaciones cuantitativas estructura-actividad (QSAR) y estructura-propiedad (QSPR) son modelos matemáticos aplicados a la predicción de actividades biológicas o propiedades de un grupo de compuestos. Estos modelos son generados y validados por análisis estadístico a partir de un grupo de moléculas con una actividad biológica o propiedad conocida. En este trabajo se explica la metodología general para realizar un análisis QSAR/QSPR utilizando el lenguaje de programación de R, analizando como caso de estudio la predicción del transporte a través de la barrera hematoencefálica.
Improvement of methods for determining power and energy characteristics of fibre-reinforced concrete crack resistance
Authors: Pukharenko Yuri V. , Zhavoronkov Mikhail I. , Panteleev Dmitry A.
Published: April 2019

Introduction. The actual problem of improving the methods of experimental studies of the properties of fibre-reinforced concrete obtained using various types of fibre is considered in the article. As a result of the analysis of the technical literature, some shortcomings of the existing test methods of one of the most important characteristics of fibre-reinforced concrete, crack resistance, were revealed. The aim of this study is to develop methods for determining the fibre-reinforced concrete crack resistance parameters. Materials and methods. The GOST 29167 standard is used as a basis for the development of a new method and device. Regulations of this standard pursue an aim of obtaining the most informative data about the material by plotting the dependences of test specimen deflections on the applied loads and determining with their assistance the power and energy parameters of the crack resistance. The test samples are presented by fibre-reinforced fine concrete beams made using steel wire fibre of circular cross-section and wave profile. Diagrams of the dependences of sample deflections on applied loads were plotted in the course of the tests for tension in bending. Calculations of power and energy parameters of crack resistance were conducted. Results. The device and method of testing the fibre-reinforced concrete crack resistance are developed and proved. A comparative analysis of the results of tests of steel fibre concrete samples is made. Conclusions. The proposed device and method allow researching influence of the fibre reinforcement parameters on fibre-reinforced concrete crack resistance parameters quickly and with minimal labour expenditures for preparation and tests. Increased adequacy of the obtained data promotes building up new trends in research and rapid introduction of fibre-reinforced concrete in the construction industry. As a result of the analysis of the obtained data, it is established that the proposed device and method can be recommended for research of the influence of fibrous reinforcement parameters on the obtained fibre-reinforced concrete properties and accumulation of statistical data for the development and improvement of normative and technical documents.
Features of operation of sewage pumping stations of heat and power stations in in conditions the Far North
Authors: Dement’eva Мarina Е. , Kurokhtin Аrtem А.
Published: April 2019

Introduction. The subject of the study is the study of technologies to ensure the reliability of sewage pumping stations (SPS), exploited in the Far North. One of the most important problems is the freezing of water in the SPS tanks, associated with the incorrect selection of the insulation of the SPS of new TPPs, as well as the deterioration of the insulation of the SPS under the influence of aggressive media on the old TPPs. As a solution, the article considers two main methods of internal heating: liquid and electric. Both methods were analyzed using the example of the Yakutsk State District Power Plant-2, where the disruption of the drainage system may lead to a station shutdown. Materials and methods. The purpose of the study was a comparative analysis and selection on the basis of a feasibility study of the most reliable method of heating the pumping unit of the Yakutsk State District Power Plant-2, exposed to low temperatures and, as a consequence, the freezing of wastewater in tanks. On the basis of field surveys and the processing of their results using mathematical statistics, the causes of the problem of water freezing in the SPS units at Yakutsk State District Power Plant-2 were studied and analyzed. Technological characteristics of the installed SPS were also analyzed, heat engineering calculations were performed, economic indicators were calculated, and further solutions to the problem under consideration were determined. Results. Analysis of the technical parameters and configuration of the SPS showed that the installed insulation and the heating system do not correspond to the territorial conditions in which this equipment is installed. To bring the SPS into working condition, two solutions for internal heating of tanks were developed and their comparative analysis was performed. Selected heating option with heating cable. This system has been successfully implemented and is operating normally. Conclusions. The results of the work can be used to repair thermal insulation and install a heating system for industrial pumping stations without using earthworks in the conditions of the Far North and on the territory of permafrost soils.
BONE MARROW LESIONS: DIAGNOSIS WITHOUT BIOPSY
Authors: Nazinkina Yu. V.
Published: April 2019

Routine spinal MRI can be used for bone marrow lesions detection. The most useful standard pulse sequence is T1- WI, which helps both in local and diffuse bone marrow diseases. Additional new pulse sequences, including chemical shift imaging and diffusion weighted imaging, can be used as solving-problem techniques.
MAGNETIC RESONANCE IMAGING FOR DIAGNOSTICS OF COMPRESSION MYELOPATHY IN PATIENTS WITH INFECTIOUS SPONDYLITIS
Authors: Makogonova M. E. , Trofimova T. N. , Mushkin A. Yu.
Published: April 2019

The clinical and neurological status and magnetic resonance imaging (MRI) of the spine were studied in successively examined 100 patients with suspected infectious spondylitis. The study design is a prospective monocentric cohort with a period of recruitment of the material in 2015–2017. Level of evidence — III. The prevalence of intramedullary changes in the form of gliosis/myeloischemia-edema in comparison with other variants of the detected changes was revealed; the presence of a higher degree of spinal sagittal stenosis (SCSs) and spinal cord kifosis (SCK) and also the average number of affected vertebrae in tuberculous spondylitis than in non-specific ones has been proven. In HIVpositive patients, higher values of the degree of maximum sagittal canal stenosis (SCSs) were observed than in HIVnegative ones. The statistical dependence between the severity of neurological disorders estimated by the Frankel scale with the etiology of the process and with specific variants of structural changes in the spinal cord has not been proven. Indicators of tactile and pain sensitivity were significantly higher in patients with intramedullary changes in the form of gliosis / myeloischemia-edema than in myelomalacia.
PERFUSION COMPUTED TOMOGRAPHY IN REFINEMENT NATURE AND FOCAL LUNG DISEASE
Authors: Lagкueva I. D. , Sergeev N. I. , Kotlyarov P. M. , Izmailov T. R. , Padalko V. V. , Solodkiy V. A.
Published: April 2019

Introduction:The study of the possibilities of perfusion computed tomography (PCT) in determining the nature of focal lung formations in the absence of morphological verification, doubtfulness of the data of native CT — the actual problem of thoracic radiology.The aim of the studywas to Refine the methodology and capabilities of PCT in determining the nature of formations of the lungs.Material and methods of research:The data of PCT of 29 patients with benign and malignant changes in the lungs on 128 slice computed tomography with data processing at the workstation were analyzed.Conclusion:Low-dose scanning Protocol for lung PCT allows to obtain reliable data on the angiogenesis of focal lung formations. Upon receipt of the perfusion map, the ROI is placed on the area of the highest blood flow. With sufficient PCT data on the nature and prevalence of lung disease from CT with contrast enhancement may refuse. Average PS, TTP are the main and leading factors in determining the nature of the lesion in the lungs. Qualitative and quantitative analysis of PCT data allows to speak reliably about the nature of foci in the lungs.
Formation of osseointegrating (bone integrating) surfaces on titanium by laser irradiation
Authors: Olsson Rickard , Powell John , Palmquist Anders , Brånemark Rickard , Frostevarg Jan , Kaplan Alexander F. H.
Published: April 2019

Pulsed lasers can be used to modify the surface of medical implants in order to accelerate bone growth (osseointegration). A surface covered in attached droplets with diameters between 1 and 20 μm is a beneficial surface for rapid osseointegration. This paper presents the results of an experimental program in which a broad range of laser parameters and different atmospheres were used to create different surface textures on titanium substrates, including the desired “attached droplet” topology. The resulting surfaces were analyzed by scanning electron microscopy and micro-computer tomography. The paper explains how different types of surfaces are created by the laser–material interaction under different conditions and focus characteristics. It is shown that optimization of the laser parameters results in a robust process, which produces a surface that is fundamentally different from those created by nonlaser methods.
Multimaterial bathless stereolithography using aerosol jet printing and UV laser based polymerization
Authors: Hohnholz Arndt , Obata Kotaro , Albrecht Daniel , Koch Jürgen , Hohenhoff Gerrit , Suttmann Oliver , Kaierle Stefan , Overmeyer Ludger
Published: April 2019

Conventional stereolithography uses a bath based system, in which a constant layer thickness is applied to realize 3D printing. This approach limits the fabrication of parts consisting of one material only. To overcome this issue, the authors developed a new approach for additive manufacturing using UV curing polymers. In a two step layer-by-layer process, first a liquid monomer film is applied using an Aerosol Jet. Two droplet generators allow the deposition of pure materials as well as various compositions of both materials. In this way, a discrete transition from one pure material to another one from one layer to another is possible. The Aerosol Jet is also able to atomize materials with viscosities greater than 1000 mPa s, allowing a wider range of materials compared to conventional stereolithography. After coating, a laser initiates the one photon polymerization reaction completing one cycle of the layer-by-layer fabrication. In this study, the penetration depth of the raw materials is investigated. In addition, the feasibility of hybrid stereolithography is shown in terms of solid freeform fabrication as well as the multimaterial approach in building direction.
Power and welding speed influence on bead quality for overlapped joint laser welding
Authors: dos Santos Paes Luiz Eduardo , Pereira Milton , de Souza Pinto Pereira Adriano , Enrique Niño Borhóquez Carlos , Lindolfo Weingaertner Walter
Published: April 2019

Laser welding has gained more and more industry acceptance due to narrow heat affected zone, low distortion levels, possibility of remote processing, and outstanding welding speeds when compared to traditional electric arc processes. Automotive industry requires a significant amount of overlapped joint welding, which usually is applied to the chassis assembling. Thus, as a mean to support laser users to optimize the welding process, this paper presents an approach through an experimental methodology followed by a phenomenological discussion about the quality of overlapped welded joints. Arguments are based on power and welding speed parameters variation and their related outcomes. This approach allows mapping of main defects such as porosity, undercut, and insufficient penetration, as well as identifying eventual preventive actions. A 10 kW IPG Photonics YLS 10000 fiber laser was used to weld 3 mm SAE 1008 steel sheets. The power ranged from 5 to 7 kW while the welding speed ranged from 2 to 5 m/min. High power levels at low welding speeds led to high temperature, resulting in an undercut issue, and low power levels at high welding speed led to insufficient penetration. Porosity was the most common defect. The best results, which did not show any type of discontinuity, were obtained at a laser power of 5 kW and a welding speed of 3 and 4 m/min.
Penerapan Model Paired Storytelling dalam Pembelajaran Bercerita
Authors: Hesti Resmi Suryaning
Published: April 2019

Penelitian ini bertujuan, mengetahui bagaimana penerapan model Paired Storytelling untuk meningkatkan motivasi belajar siswa kelas V SD Negeri  Kumendung Rembang, mengetahui kelebihan, kekurangan, kendala penerapan model Paired Storytelling pada siswa kelas V SD Negeri Kumendung Rembang. Penelitian ini merupakan penelitian kualitatif. Subjek penelitian diambil dari siswa kelas V sebanyak  30 orang. Teknik pengumpulan data menggunakan  Nonprobability Sampling. Data dalam penelitian ini diperoleh melalui observasi, dokumentasi, dan tes. Setting penelitian ini di SD Negeri Kumendung Rembang. Hasil penelitian menunjukkan bahwa, Penerapan model paired storrytelling dalam pembelajaran bercerita oleh kelompok 1 mendapat prosentase 80%, Kelompok 2 mendapat prosentase 65%, Kelompok 3 mendapat prosentase 75%, Kelompok 4 mendapat prosentase 80%. Kelompok 5 mendapat prosentase 70%, Kelompok 6 mendapat prosentase 75%, Kelompok 7 mendapat prosentase 75%, Kelompok 8 mendapat prosentase 55%, Kelompok 9 termasuk mendapat prosentase 80%, serta penerapan model paired storrytelling dalam pembelajaran bercerita oleh kelompok 10 mendapat prosentase 65%. Dengan demikian diatas dapat disimpulkan bahwa penerapan model paired storrytelling mampu meningkatkan motivasi belajar siswa kelas V SD Negeri  Kumendung Rembangpada kelas V SD Negeri Kumendung Rembang
Penerapan Model Pembelajaran Berbasis Masalah untuk Meningkatkan Hasil Belajar
Authors: Lutfita Sari Tria , Dewi Koeswanti Henny
Published: April 2019

Penelitian tindakan kelas ini dilakukan untuk meningkatkan hasil belajar Tema 6 Subtema 3 Pembelajaran 1 dan 2 dengan menerapkan model Pembelajaran Berbasis Masalah pada siswa kelas V yang terdiri dari 16 siswa. Meningkatkan hasil belajar Tema 6 Subtema 3 Pembelajaran 1 dan 2 dengan menerapkan model Pembelajaran Berbasis Masalah. Faktor-faktor yang menyebabkan peningkatan hasil belajar Tema 6 Subtema 3 Pembelajaran 1 dan 2 dengan penerapan model Pembelajaran Berbasis Masalah Siswa Kelas V SD N Kutowinangun 10 Salatiga. Subjek penelitian adalah  siswa kelas V dengan jumlah 16 siswa. Hasil penelitian adalah peningkatan hasil belajar sebelum tindakan dilakukan untuk siklus I dan siklus II. Hasil belajar pada pra siklus dengan persentase 31,25%, kemudian ada peningkatan di siklus I dengan persentase 43,75%. Selanjutnya hasil belajar siklus II meningkat dengan persentase 81,25%, dibuktikan dengan adanya penerapan model Pembelajaran Berbasis Masalah dapat meningkatkan hasil belajar Tematik Siswa Kelas V SD N Kutowinangun 10 Salatiga.
Upaya Meningkatkan Aktivitas dan Hasil Belajar Bahasa Indonesia Melalui Model Pembelajaran Group Investigation dengan Pendekatan Galery
Authors: Gede Mudana I Gusti Agung Made
Published: April 2019

Penelitian ini dilaksanakan di kelas X.9 SMAN 8 Denpasar dengan tujuan untuk meningkatkan aktivitas dan hasil belajar bahasa Indonesia dengan menggunakan metode pembelajaran Group Investigation melalui pendekatan galery. Menurut Slavin (1995) pembelajaran Group Investigation (GI) adalah pembelajaran yang dilakukan secara berkelompok, siswa dalam satu kelas dijadikan kelompok-kelompok kecil yang terdiri dari 4 sampai 5 orang untuk memahami konsep yang difasilitasi oleh guru. Galery adalah segala sesuatu yang diwujudkan secara visual yang diwujudkan dalam bentuk dua dimensi sebagai curahan perasaan atau fikiran (Hamalik, 1986). Jadi Galery yang dimaksud disini adalah hasil kerja kelompok yang dipajang secara visual dan kelompok lain memberikan input atau pendapat mengenai hasil karya kelompok. Penelitian  ini dirancang dalam dua siklus dengan masing-masing siklus terdiri atas tahap perencanaan, pelaksanaan, observasi, evaluasi serta analisis dan refleksi tindakan. Dalam penelitian ini diperoleh informasi bahwa aktivitas belajar siswa tergolong cukup aktif pada siklus I, menjadi tergolong sangat aktif pada siklus II.  Hasil belajar siswa tergolong  tuntas  yaitu dari  68,02  pada siklus I, menjadi  83,02 pada siklus II. Diharapkan kedepan, model pembelajaran ini bisa diterapkan dalam proses pembelajaran pada mata pelajaran yang lain sehingga apa yang menjadi tujuan pendidik yaitu meningkatkan kualitas pendidikan tercapai.
Peningkatan Kompotensi Guru Melalui Pelatihan Membuat RPP Kurikulum 2013 Edisi Revisi dengan Mengaktifkan MGMP Tingkat SMA/K di Kabupaten Bangli
Authors: Wandri I Nyoman
Published: April 2019

Tujuan dari penelitian untuk meningkatkan Kompotensi guru melalui  Pelatihan membuat RPP Kurikulum 2013 edisi revisi Tingkat SMA/K di Kabupaten Bangli. Penelitian ini adalah Penelitian Tindakan Sekolah (PTS) dengan menggunakan rancangan tiga siklus dan masing-masing siklus terdiri dari empat tahapan yaitu: perencanaan – tindakan – observasi – refleksi. Dalam mencapai data hasil penelitian dipergunakan teknik pengukuran berupa tes  supaya mendapatkan data kuantitatif. Lembar observasi dipergunakan agar mendapatkan data kualitatif. Kumpulan data dianalisis dengan menggunakan analisis deskriftif. Penelitian ini menggunakan subjek penelitian sebanyak 26 Guru Agama Hindu, pada MGMP tingkat SMA/K di Kabupaten Bangli dengan kreteria kurang sedang dan mampu. Hasil penelitian yang dilaksanakan dalam dua siklus yaitu siklus pertama dan siklus kedua diperoleh hasil sebagai berikut: Pertama; Pada akhir pelaksanaan siklus pertama dan kedua terdapat peningkatan rata-rata hasil kompotensi guru melalui Pelatihan membuat RPP Kurikulum 2013 dari hasil pelatihan sebelumnya  sebesar 76,00 menjadi 85,60 setelah dilaksanakan siklus III pada tingkat profesional guru mencapai nilai baik. Kedua; Ternyata peningkatan Kompotensi guru melalui Pelatihan membuat RPP Kurikulum 2013 dengan mengaktifkan MGMP tingkat SMA/K di  Kabupaten Bangli tahun 2018 menunjukan hasil yang sangat signifikan dari kondisi awal sebelum mendapat pelatihan dan bermanfaat sebagai pedoman mengajar.
Çocukluk dönemi mutluluk ve huzur anılarının bilişsel şemalar ve psikolojik semptomlarla ilişkisi
Authors: Yılmaz Hasan
Published: April 2019

Yapılan pek çok araştırma, çocukluk çağı yaşantıları ile ileriki yaşlarda bireylerin kendi kendini kontrol, uyum ve problem davranışları arasında ilişkiyi konu almıştır. Bu anlamda, erken yaşlara ilişkin anılar, yetişkin yaşamında gözlenen psikolojik sorunlar için bir veri bankası niteliği taşımaktadır. Bu araştırmanın amacı, çocukluk dönemi mutluluk ve huzur anıları ile uyumsuz bilişsel şemalar ve psikolojik semptomlar arasındaki ilişkiyi ortaya koymaktır, Hangi şema alanının-boyutunun ve hangi psikolojik semptomun, çocukluk dönemi mutluluk ve huzur anıları ile daha yüksek bir ilişki içerdiği belirlemenin yanında yordama gücünü ortaya koymak hedeflenmiştir. Araştırmada ilişkisel tarama yöntemi kullanılmıştır. Bu amaçla, çocukluk dönemi mutluluk ve huzur anıları ölçeği, şema ölçeği ve kısa semptom tarama envanteri 468 kişilik üniversite öğrenci grubuna uygulanmıştır. Araştırmanın sonunda, aşırı tetikte olma - ketlenme, zedelenmiş otonomi, kopukluk-reddedilme şema alanlarının, ÇDMHA’nın en güçlü ve anlamlı yordayıcıları olduğu saptanmıştır. Bunun yanında psikolojik semptomlardan olumsuz benlik, somatizasyon ve depresyon belirtileri ile ÇDMHA arasında negatif yönde anlamlı ve yüksek korelasyon gözlenmiştir. Beş semptom birlikte, ÇDMHA puanlarına ilişkin toplam varyansın %46’sını açıklamaktadır. Araştırma bulgularından ebeveynlik eğitim programlarının hazırlanması ve geliştirilmesinde ve okullardaki önleyici ve geliştirici rehberlik hizmetlerinin etkililiğinin artırılmasında yararlanılabileceği önerilmektedir.