bluuebunny/crossref_metadata_2025 huggingface dataset:
PENGEMBANGAN HIGHER ORDER THINKING MULTIPLE CHOICE TEST UNTUK MENGUKUR KETERAMPILAN BERPIKIR KRITIS IPA KELAS VII SMP/MTs
Authors: Hartini Hartini , Sukardjo Sukardjo
Published: February 2017

This study aims to: (1) develop higher order thinking multiple choice test (HOT-MCT) to measure the critical thinking skills of students of class VII IPA SMP/MTs, (2) determine the quality of the test theoretically, and (3) determine the quality of the test empirically. The procedure consists of seven-step, which adapted from 10 models of research and development steps Borg & Gall which includes: (1) the preliminary study, (2) planning , (3) development, (4) a small test group, (5) revision, (6) field trials, and (7) revision. The quality of the test theoretically validated by experts and science teachers. Empirically test the quality of trials conducted small groups and field trials. Analysis of the data using the parameters of the classical theory. This research resulted in about HOT-MCT with the following explanation: (1) a multiple choice question with four answer options consisting of 23 items was, (2) the test is valid theoretically valid, and (3)the test is valid emperically with reliability index α = 0.723.
Pengembangan perangkat pembelajaran model project based learning (PjBL) untuk meningkatkan keterampilan proses sains dan kreativitas
Authors: Kusumaningrum Sih , Djukri Djukri
Published: February 2017

Penelitian ini bertujuan untuk: (1) menghasilkan perangkat pembelajaran biologi dengan model PjBL yang layak digunakan dalam pembelajaran biologi; (2) menghasilkan perangkat pembelajaran biologi dengan model PjBL yang efektif untuk meningkatkan keterampilan proses sains dan kreativitas siswa kelas X SMAN 8 Yogyakarta; dan (3) membandingkan pembelajaran yang menggunakan perangkat pembelajaran model PjBL dengan pembelajaran yang menggunakan perangkat konvensio-nal dalam meningkatkan keterampilan proses sains dan kreativitas siswa. Metode penelitian diadaptasi dari Borg & Gall yang terdiri dari sembilan tahapan. Hasil penelitian pengembangan adalah: (1) perangkat pembelajaran biologi dengan model PjBL yang layak digunakan dalam pembelajaran biologi; (2) perangkat pembelajaran biologi dengan model PjBL yang efektif untuk untuk meningkatkan keterampilan proses sains dan kreativitas siswa pada aspek berpikir kreatif siswa kelas X SMAN 8 Yogyakarta; dan (3) tidak ada perbedaan antara pembelajaran yang menggunakan perangkat dengan model PjBL dengan pembelajaran perangkat konvensional dalam meningkatkan keterampilan proses sains dan kreativitas siswa.Kata Kunci: perangkat pembelajaran, model project based learning, keterampilan proses sains, kreativitas Developing a Learning Kit with Project Based Learning Model (PjBL) to Improve Scientific Process Skills and Creativity AbstractThe aims of this research are to: (1) produce an appropriate biology learning kit with PjBL model for learning activities; (2) produce an effective biology learning kit with PjBL model that can be used to improve scientific process skills and creativity; and (3) investigate the difference between the biology learning kit with PjBL model and conventional learning kit in improving scientific process skills and creativity. This research method was adapted from Borg & Gall which consisted of nine steps. The results of this research are: (1) an appropriate biology learning kit with PjBL model which consists of syllabus, lesson plans, student’s worksheet, and authentic assessment based on validation result of expert judgments and biology teachers, and also field test result; (2) an effective biology learning kit with PjBL model that can be used to improve scientific process skills and creativity especially on creative thinking aspect; and (3) there is no difference between PjBL model and conventional learning kit in improving students’ scientific process skills and creativity.Keywords: learning kit, project based learning model, scientific process skills,creativity
Un estudio experimental sobre la influencia de la música en la coreografía: movimiento y espacio
Authors: Meschini Fabrizio , Payri Blas
Published: February 2017

En este estudio experimental investigamos la relación entre música y danza a partir de cuatrofragmentos musicales compuestos por Pep Llopis para espectáculos de danza. Participan dos coreógrafos profesionales ajenos a los espectáculos en cuestión y sin información sobre el origen o la intención de los fragmentos musicales. Los coreógrafos trabajan de manera aislada y sin compartir información. Primero, cada coreógrafo hace una escucha previa de cada fragmento, y verbaliza las evocaciones sugeridas (imágenes, sensaciones, etc.) y los movimientos y desplazamientos visualizados. Se le encarga concebir una coreografía improvisada que, en una sesión posterior, se graba en vídeo. Se procede a un análisis cualitativo detallado sobre el vídeo, con la ayuda de una segunda entrevista a los coreógrafos. Se realiza un análisis cuantitativo del espacio y de los elementos técnicos: espacio ocupado, direcciones y mirada,tipos de desplazamientos/dinámicas, recorridos/trayectorias, alturas/niveles, peso, ritmo y energía corporal. Los resultados muestran una influencia estadísticamente muy significativa de la música en los elementos coreográficos (altura, peso, forma corporal, ocupación espacial, recorridos, pasos) independientemente de las evocaciones internas de cada coreógrafo. También destaca una influencia en la posición/dirección respecto al público y dirección dela mirada.
Armonía como cifrado en la audición musical
Authors: Tanco Matías
Published: February 2017

El cifrado de números romanos es el tipo de escritura más utilizado en los ámbitos académicos para el análisis armónico de obras musicales. En este trabajo indagamos el uso del cifrado armónico que los estudiantes de música realizan en actividades de audición musical. En el estudio, los participantes transcribieron el preludio de una suite barroca para cello, en donde la melodía compuesta presentaba tonos sucesivos (no simultáneos) en una textura de conducción de voces. Durante la realización de la tarea los alumnos realizaron producciones sonoras con la voz y/o un instrumento para tocar y escribir las reducciones armónicas en un pentagrama, a partir de las cuales finalmente cifraron los acordes. Los resultados del estudio presentan diferentes respuestas para los grados armónicos que fueron cifrados entre los límites de las armonías de tónica y dominante de la primera frase del preludio. La discusión de los resultados obtenidos vincula a la audición musical que se produce en la interacción del alumno con la grabación y la producción de reducciones armónicas para la interpretación del movimiento de las voces, involucrando aspectos performáticos que se integran al análisis, la teoría musical y la notación de la armonía como cifrado.
Цукровий діабет, індукований екзогенним введенням глюкокортикостероїдів
Authors: Nykytiuk L.A.
Published: February 2017

В лекції розглядаються питання діагностики та лікування стероїдіндукованого цукрового діабету.
Порушення мозкового кровообігу в жінок з надмірною масою тіла та ожирінням
Authors: Glugovska S.V.
Published: February 2017

Цереброваскулярні захворювання — одні з найбільш дезадаптуючих розладів людського організму. При цьому в жіночій популяції порівняно з чоловічою порушення мозкового кровообігу виникають істотно пізніше. Інсульти у жінок характеризуються більш високою частотою традиційних чинників ризику, таких як артеріальна гіпертензія, миготлива аритмія, а також наявністю специфічних чинників (використання пероральних контрацептивів і періоди вагітності). Крім того, у жінок порівняно з чоловіками більша частка тяжких інсультів, вища частота ускладнень і випадків тяжкої інвалідизації після інсульту. У формуванні статевих відмінностей при цереброваскулярній патології беруть участь як гормональні механізми, так і інші чинники, не пов’язані з впливом репродуктивних гормонів. Розуміння цих закономірностей важливе для розробки стратифікованих підходів до надання допомоги жінкам із цереброваскулярними захворюваннями.
Оцінка сумарного серцево-судинного ризику у пацієнтів із гіпертонічною хворобою і порушенням толерантності до глюкози
Authors: Cherniavska I.V.
Published: February 2017

Мета. Своєчасне виявлення хворих категорії високого ризику розвитку серцево-судинних захворювань, для яких більш раннє втручання для корекції кардіоваскулярного ризику буде максимально ефективним. Матеріали і методи. Обстежено 70 пацієнтів із гіпертонічною хворобою ІІ ст. та порушенням толерантності до глюкози (ПТГ) і високим серцево-судинним ризиком згідно з Фремінгемськими критеріями віком від 30 до 55 років. Проводили порівняльний аналіз оцінки серцево-судинного ризику за двома шкалами — SCORE і PROCAM. Результати. При порівнянні результатів оцінки серцево-судинного ризику за SCORE і PROCAM у процентному відношенні кількість чоловіків з високим серцево-судинним ризиком вища на 52,3 % порівняно з жінками за шкалою SCORE, а за шкалою PROCAM — більша лише на 2,3 %. На відміну від жінок у чоловіків суттєвої різниці в оцінці серцево-судинного ризику за двома шкалами не виявлено. Відповідно до отриманих результатів кількість жінок із високим серцево-судинним ризиком у процентному відношенні за шкалою PROCAM на 50 % вища порівняно зі шкалою SCORE. Висновки. Найбільший вплив на рівень сумарного серцево-судинного ризику пацієнтів із гіпертонічною хворобою ІІ ст. та ПТГ мають вік пацієнта, рівень систолічного артеріального тиску, куріння, порушення ліпідного та вуглеводного обміну. Проводячи оцінку сумарного серцево-судинного ризику, не варто обмежуватись лише визначенням тих факторів, що враховує шкала SCORE, доцільно оцінювати фактори ризику і за шкалою PROCAM, особливо у жінок.
Залежність результативності лікування безпліддя в жінок, хворих на ендометріоз, від стану імуногенетичної регуляції
Authors: Koval H.D. , Chopyak V.V. , Yuzko O.M.
Published: February 2017

Мета роботи: оптимізувати підходи до комплексного лікування безпліддя в жінок, хворих на ендометріоз, шляхом розробки моделі прогнозування ефективності терапії на підставі аналізу динаміки змін імунних показників. Матеріали та методи. У статті наведено результати дослідження впливу імунних факторів на результативність лікування безпліддя з використанням стандартних підходів і допоміжних репродуктивних технологій у 65 жінок, хворих на ендометріоз, асоційований із безпліддям. Результати. Клінічна ефективність лікування безпліддя в жінок, хворих на ендометріоз, найбільше залежить від ступеня змін експресії мРНК T-bet, GATA-3, Foxp3, TLR2, TLR4, рівнів IL-2 та IL-4. Результативність консервативних підходів обернено пропорційна ступеню змін експресії TLR2 та Foxp3 у тканині ендометрія та рівню IL-2 у сироватці крові (інформативність — 2,66; 1,81; 1,33 відповідно), а результативність використання допоміжних репродуктивних технологій обернено пропорційна ступеню змін експресії T-bet/GATA-3, GATA-3 у тканині ендометрія та рівню IL-4 у сироватці крові (інформативність — 2,23; 2,12; 1,26 відповідно). Дані результати дають змогу персоніфікувати підходи та підвищити ефективність лікування безпліддя у хворих на ендометріоз. Висновки. Для оптимізації лікування безпліддя в жінок, хворих на ендометріоз, доцільно застосовувати розроблену модель прогнозування результатів лікування з урахуванням впливу імунних чинників. У жінок із сумою більше ніж 5,56 бала за результатами прогнозування оптимальним є консервативне лікування безпліддя, а жінок із сумою менше ніж 5,56 бала слід направляти на лікування з використанням допоміжних репродуктивних технологій.
SYNTHESIS, MOLECULAR DOCKING AND ANTI-PROLIFERATIVE ACTIVITY OF NEW SERIES OF 1-METHYLSULPHONYL-3-INDOLYL HETEROCYCLES
Authors: Abo-salem Heba M. , Ahmed Khadiga M. , Hallouty Salwa El- , El-sawy Eslam R. , Mandour Adel H.
Published: February 2017

Objective: The present work aimed to synthesize a new series of 1-methylsulphonyl-3-indolyl heterocycles and study their cytotoxic activity. In addition, we attempted to explore the mode of the interaction of anti-proliferative compounds with the active site of carbonic anhydrase IX (CA IX) theoretically via molecular docking study.

Methods: Novel series of pyrazole, pyrimidine and triazole derivatives bearing 1-methylsulphonyl-1H-indole were prepared via a series of hetero cyclization reactions utilizing 3-(1-methylsulphonyl-1H-indol-3-yl)-1-(substituted phenyl)-1H-pyrazole-4-carboxaldehydes 3a-d and 3-chloro-3-(1-methylsulphonyl-1H-indol-3-yl)propenal (6) and evaluating their anti-proliferative activity. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, NMR and mass spectral data. In addition, molecular docking study of the most promising antiproliferative compounds against the active site of carbonic anhydrase IX (PDB ID: 4BCW) theoretically is discussed.

Results: Compounds 5c, 7 and 12 revealed potent anti-proliferative effects against A-549 cancer cell line with IC50 of 44.3, 17.2 and 38.7 µmol/l, respectively compared to the reference drug doxorubicin (IC50 of 48.8 µmol/l). While compound 5c was found to be highly active with IC50 of 5.66 µmol/l against HCT-116 cancer cell line than doxorubicin (IC50 of 65.00 µmol/l).

Conclusion: Further work is recommended to confirm the inhibition of CA IX in a specific bioassay.
GENDER SPECIFIC VARIATION OF TWO PHENOLIC GLYCOSIDES (POPULIN AND SALICIN) IN POPULUS CILIATA AND IDENTIFICATION OF A NEW COMPOUND (CINNAMOYL-SALICIN)
Authors: Kumari Amita , Upadhyay Navneet K. , Khosla Prem K.
Published: February 2017

Objective: To observe gender specific seasonal variation of two phenolic glycosides (PG’s) (populin and salicin) in Populus ciliata male and female trees.

Methods: Plant material (bark) was collected from male and female trees throughout the year. The content of salicin and populin was measured using HPLC. Because of the lack of populin in the market, the standard compound was synthesized in the laboratory from salicin following standard procedure. Confirmation and characterization of synthesized populin were done using 1H NMR and 13C NMR. TLC and LC-MS of methanolic extract were performed to observe the presence of populin and salicin in the plant bark.

Results: TLC showed the presence of populin and salicin in crude plant extract at Rf value 0.84 and 0.52, respectively. The results of monthly variation showed a consistent pattern of two PG’s for both the sexes. However, salicin content was observed highest compared to populin content. Whereas female trees were observed with low content of PG’s compared to male trees. The maximum content of salicin and populin was observed in the flowering season. LC-MS of bark methanolic extract confirmed the presence of a significantly larger peak, which was identified as a cinnamoyl-salicin peak at 463.

Conclusion: The study confirms the highest content of PG’s in the flowering season. Additionally, LC-MS study concluded a new compound cinnamoyl-salicin (M+at 463) which is reported first time to the best of author’s knowledge. It seems that it could be the denaturation product of 2'-O-cinnamoyl salicortin and can be further explored for biological applications.
IS RENAL IMPAIRMENT CONCEALED IN ELDERLY DIABETICS????
Authors: Shastry Rajeshwari , M. R. Prabha Adhikari , M. Shashidhar Kotian
Published: February 2017

Objective: To compare and evaluate the renal profile of elderly and younger diabetics.

Methods: This cross sectional study was conducted in a tertiary care teaching hospital. Patients with type-2-diabetes were grouped into elderly (age≥60years) and younger diabetics. Patients’ demographics, duration of diabetes and serum creatinine were recorded. Cockcroft-Gault formula was used to calculate creatinine clearance (Clcr). Statistical analysis was done using Students’‘t’ test and Pearson’s correlation. Regression analysis to adjust for covariables was done wherever required.

Results: A total of 477 diabetics were included (elderly n=320, young n=157). Body mass index (BMI) was significantly lower (p=0.003) and duration of diabetes was significantly longer (p=0.001) among elderly. Significant difference was noted in serum creatinine (1.06±0.32 vs 0.95±0.29 mg/dl; p=0.0002) and Clcr (57.82±17.41 vs 88.07±24.60 ml/min; p=0.001) between elderly and younger diabetics. Only 4.7% of elderly, whereas 47.8% of young had normal Clcr. Clcr showed a negative correlation with age in elderly (r=-0.389, p<0.001) and young (r=-0.396, p<0.001) and positive correlation with BMI in elderly (r=0.401, p<0.001) and young(r=0.337, p<0.001). Regression analysis of Clcr in elderly and young showed a positive correlation for BMI and inverse relationship for age and duration of diabetes mellitus.

Conclusion: Almost 95% of the elderly and 50% of younger diabetics had impaired creatinine clearance. Renal impairment was concealed in most of them since mean serum creatinine was 1 mg/dl. Indian elderly diabetics should be considered renally impaired and drugs for all conditions need adjustment for creatinine clearance.
HEPATOPROTECTIVE EVALUATION OF EPALTES DIVARICATA (L.) CASS. WHOLE PLANT EXTRACTS AGAINST PARACETAMOL-INDUCED HEPATOTOXICITY IN RATS
Authors: Amala K. , Ilavarasan R. , Arunadevi R. , Amerjothy S.
Published: February 2017

Objective: The plant of Epaltes divaricata (L.) Cass. Traditionally used for jaundice. The present work aimed to investigate the hepatoprotective activity of alcohol and aqueous extract of the whole plant against paracetamol-induced hepatotoxicity in rats to substantiate its traditional use.

Methods: The alcohol and aqueous (200 and 400 mg/kg) extract of Epaltes divaricata prepared by cold maceration were administered orally to the animals with hepatotoxicity induced by paracetamol (1000 mg/kg). Silymarine (40 mg/k) was given as reference standard. Hepatoprotective activity was assessed by estimating marker enzymes and by histopathological studies.

Results: Both alcohol and aqueous (200 and 400 mg/kg) extract treatment significantly restored the paracetamol-induced elevations in levels of serum enzymes aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphate (ALP) and total bilirubin in a dose-dependent manner. Histopathological examination revealed that the treatment attenuated the paracetamol-induced damage to the liver. The hepatoprotective effect of both extracts was comparable to that of the standard hepatoprotective agent, silymarin.

Conclusion: The alcohol and aqueous extract of E. divaricata exhibited hepatoprotective effect against paracetamol-induced liver damage in rats. This study also validated their traditional medicinal use in jaundice.
DETERMINATION OF 10-GINGEROL IN INDIAN GINGER BY VALIDATED HPTLC METHOD OF SAMPLES COLLECTED ACROSS SUBCONTINENT OF INDIA
Authors: Ashraf Kamran , Shah Syed Adnan Ali , Mujeeb Mohd
Published: February 2017

Objective: A simple, sensitive, precise, and accurate stability indicating HPTLC (high-performance thin-layer chromatography) method for analysis of 10-gingerol in ginger has been developed and validated as perICH guidelines.

Methods: The separation was achieved on TLC (thin layer chromatography) aluminum plates pre-coated with silica gel 60F254 using n-hexane: ethyl acetate 55:45 (%, v/v) as a mobile phase. Densitometric analysis was performed at 569 nm.

Results: This system was found to have a compact spot of 10-gingerol at RF value of 0.57±0.03. For the proposed procedure, linearity (r2 = 0.998±0.02), limit of detection (18ng/spot), limit of quantification (42 ng/spot), recovery (ranging from 98.35%–100.68%), were found to be satisfactory.

Conclusion: Statistical analysis reveals that the content of 10-gingerol in different geographical region varied significantly. The highest and lowest concentration of 10-gingerol in ginger was found to be present in a sample of Patna, Lucknow and Surat respectively which inferred that the variety of ginger found in Patna, Lucknow are much superior to other regions of India.
BRINE SHRIMP LETHALITY BIOASSAY OF ABRUS PRECATORIUS (LINN) LEAVES AND ROOT EXTRACT
Authors: Y. Wakawa H. , R. Prof D. , A. Fasihuddin B.
Published: February 2017

Objective: The present study was conducted to test for in vivo Brine Shrimp Lethality Assay (BSLA) of Abrus precarious leaves and root extracts after successive maceration in four solvents (n-hexane, dichloromethane (DCM) ethyl acetate and methanol) and correlate cytotoxicity results with known pharmacological activities of the plant.

Methods: Cytotoxicity was evaluated in terms of LC50 (lethality concentration), 10 nauplii were added into three replicates of each concentration of the plant extracts, and after 24 h the surviving brine shrimp larvae were counted, and LC50 was assessed.

Results: Potent cytotoxicity was found for both the leaves and root extracts of Abrus precatorius, results showed a concentration dependent increment in mortality rate of the brine shrimp nauplii and the n-hexane and dichloromethane fractions of the root and leaves extracts were more potent against the brine shrimp with LC50 values of 7.870 ppm and 19.135 ppm (µg/ml) respectively, whereas methanol fractions of both the extracts exhibited low potent activity with LC50 values 61.575 ppm and 226.053 ppm (µg/ml) in root and leaves respectively.

Conclusion: The result indicated bioactive components are present in this plant that could be accounted for its pharmacological effects.
HYPOGLYCEMIC EFFECT OF OLIVE MILL WASTEWATER IN MICE INVOLVES THE SGLT-1 TRANSPORTER
Authors: Oularbi Nassima Senani , Mati Farida Moulti , Letteron Philippe , Ducroc Robert , Benna Jamel El , Marie Jean Claude
Published: February 2017

Objective: Olive mill wastewater (OMWW) is a by-product of olive oil production and contains biologically active compounds. The aim of this study was to investigate the effect of OMWW on intestinal glucose absorption in mice, a target for treating diabetes.

Methods: The effect oral administration of OMWW on mice glycemia was evaluated by oral glucose tolerance tests (OGTT), and mice jejunal mucosal strips were mounted in Ussing chambers to evaluate the activity of sodium-dependent glucose transporter (SGLT-1). Western blot analysis was performed to study SGLT-1 and protein kinase C (PKC) at the brush border membranes (BBM) of mice jejunal mucosa.

Results: We found that the raised glycemia in mice in response to oral glucose administration (OGTT) was decreased in presence of OMWW, being highly effective at 4 g/kg of body weight. Further, OMWW inhibited glucose induced short-circuit current (Isc) in mice jejunal, which is a marker of SGLT-1 activity. The effect was rapid, with maximal inhibition of 80 % versus control. Also, OMWW induced a strong decrease of SGLT-1 protein (60%) as well as PKC (30%), a key effector protein in BBM of mice jejunal mucosa in response to glucose.

Conclusion: Our results suggest that OMWW may be beneficial for diabetes through its novel hypoglycemic effect by acting on the PKC-SGLT-1 axis.
DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE
Authors: B. Preethi G. , Kunal Prashanth
Published: February 2017

Objective: The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.

Methods: Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and in vitro release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.

Results: It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics.

Conclusion: It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, in vitro drug release and stability.
COMPARATIVE ANALYSIS OF POTENTIALITY OF ESCULIN AND HINOKITOL (Β-THUJAPLICIN) AS ANTI-PARKINSONISM DRUGS: A PILOT IN SILICO STUDY
Authors: Varier Krishnapriya Madhu , Thangarajan Sumathi , Chinnasamy Arulvasu , Balakrishnan Gopalsamy , Paulose Renjith
Published: February 2017

Objective: Parkinson’s disease (PD) is a leading cause of mental disability and death worldwide. Even though there are many advances in drug development against PD, a potent low dosage drug with fewer side effects are still in its nursery. This is a pioneer in silico attempt to test the anti-PD actions of esculin and hinokitol to act novel drugs.

Methods: In this study, using Auto dock tools 4.2, esculin and hinokitol (β-Thujaplicin) were predicted for its inhibitory actions with Alpha-Synuclein (AS) Apo site, Dopamine D3 Receptor (D3R), Glycogen Synthase Kinase-3 Beta (GSK3β), Mono Oxidase B (MAO-B), Parkin and Tyrosine 3-Hydroxylase (TH) with levodopa standard. The reliability of the 3D predicted model of these proteins were analysed using RAMPAGE. Further, the blood-brain barrier (BBB) crossing ability of the natural compounds were analysed using cbligand. The In silico ADME (Absorption, Distribution, Metabolism, Excretion) properties of esculin and hinokitol were compared with that of levodopa using molinspiration and admetSAR @ LMMD software.

Results: The predictions were that hinokitol, being blood-brain barrier positive (BBB+) with fewer side effects could be a potent anti-PD drug than esculin as it proved to be blood-brain barrier negative (BBB-). Hinokitol was predicted to be good inhibitors of AS, MAO-B and Parkin.

Conclusion: The study revealed that hinokitol could be a potent anti-PD drug, being BBB+. Hinokitol was additionally predicted as a good inhibitor of AS, MAO-B and Parkin than levodopa standard.

 
REVIEW ON PHORBOL ESTER DEGRADATION OF JATROPHA SEED CAKE FOR ITS USE AS ANIMAL FEED
Authors: Ahluwalia Shilpi , Bidlan Rajkumar , Sharma Jai Gopal , Singh Pushpendra
Published: February 2017

Jatropha curcas is an oil-seed plant with good adaptability to grow in unfavourable conditions like infertile soil with scanty rainfall. It had been exploited for the extraction of oil for bio-diesel. The compressed seed cake, after the oil extraction, is a rich source of protein with certain toxic and anti-nutritional factors. The major toxins in the seed cake are phorbol esters and trypsin inhibitors that lead to various health problems if ingested. Even though the application of the various extracts carries a lot of beneficial advantages, yet the toxicity in oil and the compressed cake does not allow the by-products and the oil to be used elsewhere. Various physicochemical and biological methods have been described for the detoxification of Jatropha seed cake and oil of which the chemical extraction with methanol and ethanol have shown promising results in reducing the toxin contents by 97-100% while UV-irradiation reduced the phorbol esters completely. Submerged fermentation by Bacillus sp. achieved complete detoxification of phorbol esters within a week. A new strain was found to degrade the phorbol esters to phorbol, myristic acid and acetic acid within 12 h of incubation in submerged fermentation process. The detoxified products, in future, can be used as animal feed and food supplement to help utilize the by-products as a healthy diet.
IN VITRO ANTHELMINTIC AND ANTI-AMYLASE PROPERTIES OF GARCINIA PEDUNCULATA ROXB. ETHANOLIC EXTRACT
Authors: Sarmah Pinky , Kobing Nako , Gogoi Jyotchna , Dutta Ananta Madhab
Published: February 2017

Objective: The present study aims to investigate in vitro anthelmintic and anti-amylase properties of the ethanolic fruit extract of Garcinia pedunculata.

Methods: For the study, mature fruits of G. pedunculata were collected from local markets during April-May. Fleshy pericarps of fruits were chopped into small pieces, dried and extracted by using a Soxhlet apparatus. Ethanol extract of G. pedunculata was used for evaluation of in vitro anthelmintic and anti-amylase activities. In vitro anthelmintic activity was evaluated in animal models, Pheretima posthuma, an earthworm species. In vitro anti-amylase activity was evaluated by using zymographic, achromic point analysis (Starch-Iodine method) and spectrophotometric method [Di Nitro Salicylic acid (DNS)–Maltose method].

Results: Ethanolic extract of G. pedunculata showed anthelmintic activity at a concentration of 75 mg/ml, paralysis and death timing was reported at 0.62±0.26 min and 1.42±0.07 min, respectively. The reference standard (Albendazole) showed paralysis time: 2.13±0.28 min and death time: 5.12±0.29 min. In the anti-amylase study, a zymographic density analysis of G. pedunculata showed significant variation in band intensity as compared to Starch–Iodine achromic point analysis and DNS–Maltose method. A concentration of 1.5 mg/ml of extract showed inhibition of amylase: 67.65±1.53 % as compared to other concentrations and control sets.
Conclusion: It could be concluded that ethanolic extract of G. pedunculatahas biological properties which could be utilised in medicine by characterising its bioactive components.
 
FLASH DISSOLVING SUBLINGUAL ALMOTRIPTAN MALATE LYOTABS FOR MANAGEMENT OF MIGRAINE
Authors: Kassem Abeer Ahmed , Labib Gihan Salah
Published: February 2017

Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs.

Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR).

Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients.

Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
DESIGN AND SYNTHESIS OF 4-SUBSTITUTED QUINAZOLINE DERIVATIVES FOR THEIR ANTICONVULSANT AND CNS DEPRESSANT ACTIVITIES
Authors: Dash Biswajit , Dash Suvakanta , Laloo Damiki
Published: February 2017

Objective: The present work is designed to synthesise some isomeric new series of Quinazoline-4-one/4-thione derivatives, based on the pharmacophoric model of central nervous system (CNS) activity by structural modifications retaining the essential structural features for the activity and evaluated for their anticonvulsant and CNS depressant properties.

Methods: A series of 7-chloro-3-[substituted (amino/phenylamino)]-2-phenyl quinazolin-4 (3H)-one/thione derivatives and 1-(7-chloro-4-oxo/-2-phenylquinazoline-3 (4H-yl)) substituted urea derivatives were prepared. The reaction scheme proceeds through the intermediate 7-chloro-2-phenyl-4H-benzo[d] [1, 3] oxazin-4-one. The structures of the newly synthesised compounds were characterized from infrared (IR), 1H nuclear magnetic resonance (NMR) and mass spectra (m/z) and elemental analysis. The anti-convulsant and CNS depressant activity were investigated by maximum electroshock (MES) seizure test and porsolt’s behavioural despair test (forced swimming) respectively. The rota-rod test was performed to assess any probable changes in motor coordination induced by the test compounds.

Results: The physicochemical and spectroscopic data clearly confirmed the synthesis of quinazoline derivatives with a common skeleton. The synthesised compounds were evaluated for their anticonvulsant and CNS depressant properties. Among them, six compounds (IIc, IIg, IIj, IIIc, IIIg, IIIj) exhibited a good activity profile in CNS depressant activity. Five compounds (IIc, IIg, IIj, IIIg, IIIh) showed protection against MES-induced seizures.

Conclusion: The Quinazoline derivatives obtained from this research work indicates that the methyl/methoxy group in phenyl ring, amine and thiourea substitution at 3rd position of quinazoline derivatives are essential for CNS depressant activity as well as anticonvulsant activity. Compounds IIc, IIg, IIj, IIIc, IIIg, IIIj, and IIIh were found to be a potent compound which may be effective as a potential source for the development of CNS depressant and anti-convulsant drugs with lesser side effects
MIMOSA PUDICA EXERTS NEUROPROTECTION AGAINST MPP+INDUCED NEUROTOXICITY IN SHSY5Y CELL LINES-AN IN VITRO MODEL OF ANTI-PARKINSONISM
Authors: V. Mahadevan M. , S. Ramaswamy R. , V. Banumathi
Published: February 2017

Objective: Parkinson’s disease (PD) is one of the of a neurodegenerative disorder, It’s decreased the dopaminergic neurones, tyrosine hydroxylase (TH) and increased the α-synuclein protein level. This study was conducted to investigate the neuroprotective effect of Mimosa pudica have the abilities to improve TH and DAT proteins expression against MPP+ induced neurotoxicity, in in vitro model of Parkinson’s disease using SH-SY5Y human neuroblastoma cell lines.

Methods: Mimosa pudica were pre-treated with various concentration for cell viability assay. Vehicle alone or Mimosa pudica (300µg) for 24 h, and then were co-treated with 1000µM MPP+ for 15 min in the continued presence of vehicle or Mimosa pudica. After treatment, cells were collected for protein expression.

Results: Cell viability assay confers the inhibitory concentration cell death of Mimosa pudica. MPP+significantly down-regulated the protein expression of TH (p<0.01) and DAT (p<0.05). Mimosa pudica decreased the expression of α synuclein (p<0.01) in MPP+ intoxicated cell lines.

Conclusion: The present study showed that Mimosa pudica exerts neuroprotection by suppressing α synuclein and the dopaminergic neurdegeneration. Mimosa pudica may be due to quecertin which might be acted via the anti-oxidant mechanism. The above finding suggests that Mimosa pudica may act as a potential target in the management of PD.

 
A PROSPECTIVE STUDY OF THE PATTERN OF USE OF ANTIMICROBIAL AGENTS IN SURGICAL PROPHYLAXIS IN A TERTIARY CARE CENTRE
Authors: Brethis C. S. , Thamizharasan S. , Sridevi S. A. , Kalaiselvi B. , Singh M. Balaji , Vijaykumar K.
Published: February 2017

Objective: To evaluate the most common class of antimicrobial agents used in surgical prophylaxis. To evaluate the timing, dosage, route and duration of use of antimicrobial agents in surgical prophylaxis.

Methods: The study subjects were 214 patients who underwent general surgical procedures at Vinayaka Missions Kirupananda Variyar Medical College from July 2013 to June 2014. The use of antimicrobial agents was noted from the first dose of antibiotic given before the induction of anaesthesia. After surgery was completed the duration of antibiotic in the post-operative ward was noted.

Results: Majority of the patients were males of age group 50-60 y and the most common surgical procedure was hernioplasty. Combination therapy with two antimicrobial agents was more preferred regimen 126 (58.9%). Among the antimicrobial agent's cefotaxime 114 (24.8%) was the most commonly prescribed drug and it was followed by metronidazole 121 (21.9%). ceftriaxone 60 (13.1%) was the third most commonly prescribed antimicrobial agent. The mean duration of prescription of antimicrobial agents in the present study was 4.78 d and the mean cost of drug treatment was 787.54 rupees. The cost-effective regimen was that of aminoglycosides and imidazole.

Conclusion: The choice of antimicrobial agent was based on the local prevalence pattern of microorganisms. The intravenous administration of antibiotic prophylaxis immediately before or after the induction of anaesthesia is the most reliable method for ensuring effective serum concentration at the time of surgery. The antimicrobial agent chosen must cover all the most likely contaminating organisms.
CYTOTOXIC EFFECT OF CRUDE EXTRACT AND FRACTION FROM CALOTROPIS GIGANTEA LEAVES ON HUMAN COLON CANCER WIDR CELL LINES
Authors: Mutiah Roihatul , . Sukardiman , Widyawaruyanti Aty
Published: February 2017

Objectives: This paper sought to understand and determine the cytotoxic’s effects of crude extract and its fraction from Calotropis gigantea leaves on human colon cancer WiDr cell lines.

Methods: The ethanolic extract was fractionated gradually with certain substances to yield four fractions. The substances were dichloromethane, ethyl acetate, and butanol. The four fractions resulted in dichloromethane fraction, ethyl acetate fraction, butanol fraction, and a water fraction. These fractions were then investigated for their cytotoxic effects on WiDr cells. The cell viability was assessed using MTT colorimetric assay.

Results: The result indicated that the cytotoxic effects of the ethanolic extract (IC5048.5 μg/ml), ethyl acetate fraction (IC5041.79 μg/ml), and dichloromethane fraction (IC5040.57μg/ml) produced a much more potent effect than the butanol fraction (IC50 737.74 μg/ml) and water fraction (IC508493 μg/ml).

Conclusion: The ethanolic extract, ethyl acetate fraction and dichloromethane fraction exhibited a potent cytotoxic effect on human colon cancer WiDr cell line. The crude extract and fractions are potential to be developed as an anticancer agent in colon cancer therapy.
ANTIBACTERIAL EFFECTIVENESS OF SELECTED MOROCCAN ESSENTIAL OILS AGAINST THE HIGHLY VIRULENT JP2 CLONE OF AGGREGATIBACTER ACTINOMYCETEMCOMITANS
Authors: Lakhdar Leila , Farah Abdellah , Lahlou Idriss , Rida Sana , Bouziane Amal , Ennibi Oumkeltoum
Published: February 2017

Objective: Aggregatibacter actinomycetemcomitans (Aa) serotype b JP2 clone is a highly virulent strain, considered as a major etiologic agent in aggressive periodontitis in patients of African descent, such as Moroccan adolescents. Antibiotics have been and continue to be the only effective treatment of periodontal infections caused by this periodontal bacterium. However, today there is enough scientific evidence on the existence of an increased resistance of oral bacteria to antibiotics. Therefore, the search for new natural agents, that are safe and effective, such "essential oils," has become a necessity. The present study was conducted to evaluate the in vitro antibacterial activities of three selected essential oils from Moroccan aromatic medicinal plants (Origanum compactum, Thymus vulgaris and Cymbopogon martinii) against clinical Moroccan isolate of Aa JP2 strain.

Methods: Antibacterial activity of essential oils was investigated using agar well diffusion method, then measured using broth microdilution method.

Results: All the selected essential oils exhibited significant antibacterial activity on the highly pathogenic JP2 strain of Aa. Essential oil of Origanum compactum was found to be the most effective with a minimum inhibitory concentration (MIC) value of 0.03% (v/v) and a minimum bactericidal concentration value (MBC) of 0.07%.

Conclusion: The present findings indicate the possibility of exploiting these essential oils as potential antimicrobial agents in treatment of aggressive periodontitis associated to this pathogen.
EVALUATION OF THE ANTICONVULSANT EFFECT OF AQUEOUS EXTRACT OF CENTELLA ASIATICA IN ALBINO MICE
Authors: Deka Dipjyoti , Chakravarty Pinaki , Purkayastha Ayan
Published: February 2017

Objective: To evaluate the antiepileptic activity of aqueous extract of Centella asciatica in maximal electroshock (MES) and pentylenetetrazole (PTZ) induced convulsions.

Methods: The anticonvulsant activity of leaves of Centella asciatica (200 mg/kg and 400 mg/kg) in mice was assessed using MES and PTZ induced seizure models. Abolition of tonic hind limb extension (MES and PTZ) and increase in seizure latency (PTZ) when compared to control group, were taken as a measure of protection. Statistical analysis was done using one-way ANOVA followed by Tukey-Kramer multiple comparisons test. The test was considered to be significant at p<0.05.

Results: The aqueous extract of Centella asiatica at a dose of 200 mg/kg has abolished tonic hind limb extension in 1 out of 6 animals in MES while there was no anticonvulsant action in PTZ convulsions. At a dose of 400 mg/kg body weight, the aqueous extract of Centella asiatica has shown a significant anticonvulsant effect against both MES and PTZ convulsions, where it has abolished tonic hind limb extension in 4 mice in MES method and in all 6 mices in PTZ method.

Conclusion: The aqueous extract of Centella asiatica showed efficacy in both MES and PTZ convulsions in mice at a dose of 400 mg/kg. Since the clinical correlates of MES seizures are tonic-clonic convulsions and correlates of PTZ seizures are absence seizures, the aqueous extract of Centella asiatica is likely to be useful in the treatment of tonic-clonic and absence seizures.
IMPROVING ANTIBIOTIC PRESCRIBING PATTERN AND ASSESSMENT OF CO-MORBIDITIES ASSOCIATED WITH RESPIRATORY TRACT INFECTIONS
Authors: K. Shyama , R. Prudence A.
Published: February 2017

Objective: The objective of this study was to describe the antibiotic prescribing pattern and co-morbidities associated with lower respiratory tract infections by means of cross-observational study.

Methods: A cross-sectional, open labelled and observational study was undertaken in a multi-speciality hospital for a period of 9 mo (November 2013-July2014). Lower respiratory tract infected patients who satisfied the selection criteria were included in the study. They were followed clinically and biochemically in the study.

Results: During the study period, most predominant antibiotics used were cephalosporin’s which constitute about 63 % (with 3rd generation being the highest). Hypertension was found to be the most frequent co-morbidity (43%). Route of administration for most of the patients was parenteral followed by tablets and a very few on capsules. A few were changed from parenteral to oral when they met with the clinical criteria’s for switching over therapy.

Conclusion: This study describes the antibiotic prescribing pattern and co-morbidities associated with lower respiratory tract infected patients.
COMPARATIVE STUDY ON THE BENEFICIAL EFFECTS OF TELMISARTAN AND OTHER ANTIHYPERTENSIVE AGENTS IN STROKE PATIENTS
Authors: Jose Anju , Wilson Deepthi , George Mintu , Thomas Reshma K. , Justin A.
Published: February 2017

Objective: To compare the beneficial effects of telmisartan with other anti-hypertensive agents during stroke with respect to improvement from neurological dysfunction.

Methods: A prospective observational study was performed on 98 eligible study participants. The blood pressure, National Institute of Health Stroke Scale (NIHSS) score and power of limbs were noted. The data were analysed using one-way Analysis Of Variance (ANOVA) followed by Dunnett’s Multiple Comparison Test.

Results: Among 150 randomised patients, 110 met the inclusion criteria, and 98 came for follow-up whose data was recorded. Telmisartan showed significant improvement in total NIHSS score compared to amlodipine (P ≤ 0.01) and mannitol (P ≤ 0.01). The mean reduction in SBP and DBP was significant with respect to telmisartan compared to amlodipine (P≤ 0.01). Telmisartan showed significant improvement of power in right upper limb (UL) compared to amlodipine (P ≤ 0.05) and mannitol (P ≤ 0.01). Improvement of power in right lower limb (LL) showed significance with respect to telmisartan compared to mannitol (P ≤ 0.05). Significant improvement of power in left LL was observed in telmisartan compared to mannitol (P ≤ 0.01).

Conclusion: Blood pressure reduction is an inevitable component of stroke treatment. Anti-hypertensive treatment seems to be highly efficacious in protecting patients against stroke and stroke recurrence, especially on long term basis. Thus, telmisartan provides a viable insight into the stroke prevention strategy and may be prudent to consider as a reasonable add-on therapy.
HAEMATOCOCCUS PLUVIALIS MODULATING EFFECT ON NEUROTRANSMITTERS, HORMONES AND OXIDATIVE DAMAGE-ASSOCIATED WITH ALZHEIMER´S DISEASE IN EXPERIMENTAL RAT´S MODEL
Authors: El-baz Farouk K. , Aly Hanan F. , Ali Gamila H.
Published: February 2017

Objective: This study was planned to assess the efficacy of Haematococcus pluvialis in the regression of Alzheimer’s disease (AD).

Methods: Fifty rats were divided into five groups. Positive control group orally received aluminium chloride in a dose 100 mg/kg to induce AD: AD induced rats were orally treated with H. pluvialis extract (150 mg/kg) and rivastigmine standard drug (4.6 mg/kg/day) for 30 d. Brain acetylcholine esterase (AchE), acetylcholine (Ach), dopamine (DA), adrenaline (A), noradrenaline (NA), oxidative stress biomarkers and superoxide dismutase (SOD) were determined. Further, adrenocorticotropic hormone (ACTH) and cortisol (CORT) levels were evaluated. Also, brain histopathological investigation was examined.

Results: AD induced rats recorded a significant increase in the brain AchE, concomitant with a significant decrease in Ach, DA, NA, A and SOD levels. While, a significant increase in NO and H2O2, CORT and ACTH was recorded. Moreover, brain histopathological investigation in AD rats showed the formation of amyloid plaques and necrosis of neurons. Treatment of AD induced rats with extract of H. pluvialis or standard drug resulted in an improvement in the most of the all studied biochemical parameters. Also, AD groups treated with extract or standard drug showed great improvement in the brain morphological structure with normalisation of cerebral cortex and hippocampus, though, necrosis of some cerebral neurones was detected.

Conclusion: This current study indicated that H. pluvialis extract and drug significantly ameliorates the neurotransmitters level, oxidative damage as well as pituitary function due to their anticholinesterase activity, antioxidant efficacy, beside the anti-inflammatory effect.