bluuebunny/crossref_metadata_2025 huggingface dataset:
HOW STAR WARS ILLUMINATES CONSTITUTIONAL LAW
Authors: Sunstein Cass R.
Published: February 2017

Human beings often see coherence and planned design when neither exists. This is so in movies, literature, history, economics, and psychoanalysis – and constitutional law. Contrary to the repeated claims of George Lucas, its principal author, the Star Wars series was hardly planned in advance; it involved a great deal of improvisation and surprise, even to Lucas himself. Serendipity and happenstance, sometimes in the forms of eruptions of new thinking, play a pervasive and overlooked role in the creative imagination, certainly in single authored works, and even more in multi-authored ones extending over time. Serendipity imposes serious demands on the search for coherence in art, literature, history, and law. That search leads many people (including Lucas) to misdescribe the nature of their own creativity and authorship. The misdescription appears to respond to a serious human need for sense-making and pattern-finding, but it is a significant obstacle to understanding and critical reflection. Whether Jedi or Sith, many authors of constitutional law are a lot like the author of Star Wars, disguising the essential nature of their own creative processes.
Зміни вмісту цитокінів у хворих на артеріальну гіпертензію з ожирінням залежно від тривалості захворювання
Authors: Kapustnik V.A. , Kostyuk I.F. , Shelest В.О. , J.O. Кovalyova
Published: February 2017

При артеріальній гіпертензії (АГ) з ожирінням мають значення інтерлейкіни‑2, 6, 10 і С-реактивний білок. Ці маркери запалення регулюють міжклітинні взаємодії, проліферацію мезангію і викликають низку змін на клітинному рівні, тим самим сприяючи запальним процесам. Мета дослідження: виявити особливості маркерів запалення у хворих на артеріальну гіпертензію з ожирінням залежно від тривалості захворювання. Матеріал і методи. Обстежено 52 хворих на АГ II стадії з ожирінням в трьох групах за тривалістю захворювання. У першу групу увійшли 19 хворих з тривалістю захворювання до п’яти років, в другу — 18 хворих з тривалістю захворювання 6–10 років і в третю — 15 пацієнтів з тривалістю захворювання понад 11 років. Активність сироваткових рівнів маркерів запалення визначали імуноферментним методом. Результати. При тривалості захворювання 6–10 років рівень ІЛ‑6 дещо підвищувався порівняно з першими 5 роками, а потім знижувався. Вміст ІЛ‑2 був підвищений в перші 5 років в 3,74 раза, а в подальшому знижувався у 3,15 раза і 3,04 раза відповідно порівняно з контролем. Рівні ІЛ‑10 і СРБ мали таку ж тенденцію, як і ІЛ‑6. Висновки. Встановлено, що хворим з артеріальною гіпертензією та ожирінням притаманне істотне підвищення рівня в крові інтерлейкіну‑2, 6 і 10 і С-реактивного білка (більше рівні прозапальних цитокінів, ніж протизапального). При подовженні тривалості захворювання запальний процес стає менш вираженим, що може свідчити про більш глибокі імунологічні порушення. Після стандартної терапії підвищені початкові концентрації цитокінів і С-реактивного білка в крові значно знижуються, але вірогідно не відрізняються від контролю, крім рівня інтерлейкіну‑2.
Defined Contribution Plan Participant’s Position after the Subprime Crisis
Authors: Morris Pamela D.
Published: February 2017

The growing number of Defined Contribution Plans available in the U.S. has presented many in the U.S. work force with investment decisions. Decisions many of these workers have not been faced with in the past. An analysis of the Survey of Consumer Finance data over the early portion of the sample period, 1992-2010 has shown that the annual average percentage of liquid retirement plan savings allocated to equity assets increased from 43.02% to 66.42%. In 2010, after the subprime crisis, the allocation to equity declined but remained high at 50.65%, even though the market in 2001 and 2008 changed the allocation for many participants. Researchers attempt to find the reason that retirement savings plan participants have chosen to take a riskier position over the years. After controlling for factors such as age and income classifications, this study finds the educational classification to be a significant factor in explaining the percentage that participants allocate to the relatively riskier assets.
A NEW STABILITY-INDICATING RP-HPLC METHOD FOR DETERMINATION OF CURCUMIN: AN APPLICATION TO NANOPARTICULATE FORMULATION
Authors: Panigrahi Suchitra , Hirlekar Rajashree
Published: February 2017

Objective: The present study was aimed to develop a rapid, accurate, linear, sensitive and stability-indicating high performance liquid chromatographic method for determination of curcumin and to implement the developed method for the estimation of curcumin in the nanoparticulate formulation.

Methods: Method development was performed using various solvent, buffer-solvent ratios, at different flow rates for better resolution and to decrease the run time. The developed method was validated in accordance with the international conference on harmonization (ICH) guidelines. The developed method was implemented to estimate the amount of curcumin in the curcumin-nanoparticulate formulation.

Results: The optimum chromatographic conditions with adequate resolution for curcumin (16.10 min) was achieved when the separation was carried using C18 column at ambient temperature with an isocratic elution mode of mobile phase composed of a degassed mixture of phosphate buffer pH 3 and acetonitrile (50:50 v/v) at 1.0 ml/min flow rate with a total run time of 20 min. The developed method was validated for system suitability, accuracy, precision, limit of detection (LOD), limit of quantitation (LOQ), linearity and range. The LOD and LOQ were found to be 0.018 and 0.056 μg/ml respectively, which indicates that the method was sensitive, and can detect and quantify at lower levels of curcumin. Linearity range was from 5-15 μg/ml for curcumin with regression coefficient 0.997 indicates that at this concentration range curcumin was highly linear. Percent assay of curcumin was found to be 98.7% and curcumin recovered was found to be 0.78 mg which are estimated by using the developed method.

Conclusion: The developed analytical method is simple, precise, and reproducible and thus can be used for stability-indicating analysis of curcumin in pharmaceutical formulations.
SESAMOL ANTAGONIZES ROTENONE-INDUCED CELL DEATH IN SH-SY5Y NEURONAL CELLS
Authors: D. Rohini , K. Vijayalakshmi
Published: February 2017

Objective: To investigate the neuroprotective effect of sesamol against rotenone-induced cell death in SH-SY5Y cells associated with Parkinsonism.

Methods: SH-SY5Y cells were maintained in Dulbecco’s modified Eagle’s medium. After differentiation, the cells were incubated with rotenone (20 μM) and sesamol at different concentrations (10-100 μM). Cell viability was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide assay. The reactive oxygen species, mitochondrial membrane potential and nuclear morphology were determined by dichlorofluorescein diacetate, rhodamine 123 and 4’, 6-diamidino-2-phenylindole, respectively. Thiobarbituric acid reactive substances, activities of catalase, superoxide dismutase, and glutathione peroxidase and glutathione level were determined by standard assays.

Results: Sesamol significantly increased the cell viability and decreased the rotenone-induced cell death in SH-SY5Y cells. Sesamol antagonized rotenone-induced reactive oxygen species generation, loss of mitochondrial membrane potential and nuclear damage. Sesamol also decreased thiobarbituric acid reactive substances level, increased the activities of catalase, superoxide dismutase, glutathione peroxidase and increased the level of glutathione in rotenone-induced cells.

Conclusion: The results obtained strongly indicate the promising neuroprotective role of sesamol against rotenone-induced death in SH-SY5Y cells.
THE BLOOD PRESSURE AND THERAPY EXPENDITURE CHANGE DUE TO HYPERTENSION COMORBIDITY: AN ANALYTICAL PROSPECTIVE STUDY IN SECONDARY CARE HOSPITALS IN JOGJAKARTA INDONESIA
Authors: Suhadi Rita , Thobari Jarir At , Irawan Bambang , Dwiprahasto Iwan
Published: February 2017

Objective: To measure the comorbid effect on blood pressure and therapy expenditure in 4 secondary care hospitals in Jogjakarta.

Methods: We conducted an 8-month prospective pharmacoeconomic study with hospital perspective. All hypertensive outpatients, with Askes-insurance whose beneficiaries were governmental employees, with at least 2 moly visits at the index date were included. The subjects with malignancy, hemodialysis, and less than 4 visits were excluded. The expenditure comprised the cost for cardiovascular medicine, doctor, physical/laboratory test, emergency visit, and physiotherapy. We analyzed the expenditure change and sensitivity analysis with Anova-test, whereas the proportion of subjects with good controlled blood pressure with the chi-square test.

Results: The eligible subjects (N=656) consisted of no comorbid (n=105), stroke (n=82), cardiovascular (n=209), diabetes mellitus/chronic kidney disease or DM/CKD (n=149), and combined comorbid (n=111) groups. The baseline blood pressure was similar to no comorbid (p>0.05), except for the diastolic blood pressure in a cardiovascular group. The stroke and cardiovascular groups had more subjects at mean systolic blood pressure lower than 140 mmHg with odds ratio (OR) 2.01 (CI95%:1.12-3.62) and 2.10 (CI95%:1.31-3.39) respectively than no comorbid group; but the mean blood pressure was not clinically different. The total therapy expenditure increased at 6.5% (p<0.61); 22.7% (p<0.03); 78.6% (p<0.01); 78.5% (p<0.01) per subject-visit for stroke, cardiovascular, DM/CKD, and combined-comorbid groups than no comorbid group respectively. Except for stroke group, the incremental expenditure was price-sensitive (p<0.05).

Conclusion: The total therapy expenditure but not blood pressure was likely to be influenced by hypertension comorbidity. We suggest that preventing hypertension comorbidity has the benefit to reduce total therapy expenditure.
IN SILICO PREDICTION OF DELETERIOUS AND NON-DELETERIOUS nsSNPs IN CFTR GENE VARIANTS
Authors: Murthy Vemulapati Bhadra , Chowdary Meghana , . Sucharitha
Published: February 2017

Objective: The major objective of the study was to carry out comparative bioinformatics analyses to identify different nsSNPs that were predicted to be deleterious or damaging to the structure and functions of CFTR protein causing cystic fibrosis.

Methods: The CFTR gene variants (nsSNPs) and their related protein sequences from Homo sapiens were subjected to computational analyses using the following bioinformatics tools (a) SIFT: a sequence-homology based prediction tool that can be used to distinguish between the intolerant from tolerant SNP changes. (b) PolyPhen2: a structure and sequence-based physical and comparison tool to study the impact of amino acid substitution on the structure and function of human proteins and (c) I-Mutant2: to predict the protein stability changes arising due to single point mutations.

Results: SIFT, PolyPhen2, and I-Mutant2 analyses indicated that 21 out of 108 nsSNPs were identified to be common that were strongly predicted to be deleterious and damaging for CTFR protein in cystic fibrosis conditions. Most of the substitutions in the CFTR protein contained the amino acids valine followed by cysteine and proline respectively. Homology modeling carried out to determine if any of these nsSNPs had a role in changing the conformation of CFTR protein drastically. Homology modeling of selected nsSNP variants indicated that these substitutions,however did not change the overall CFTR protein structure but predicted to cause severe damaging changes to the phenotypes of CFTR protein. Results indicated that multiple bioinformatics tools are needed to predictthe effect of substitutions and these prediction tools need to be analyzed more into detail and common determination factors are required to predict a nsSNP to be deleterious or damaging to the overall functioning of the CFTR protein.

Conclusion: Multiple bioinformatics tools are in fact the need of the hour to establish if a strong relationship between nsSNPs that could alter the protein stability and cause a deleterious or damaging phenotypic change to the individual with cystic fibrosis involving the CFTR protein.
SCREENING OF α-GLUCOSIDASE INHIBITORS FROM TERMINALIA CATAPPA L. FRUITS USING MOLECULAR DOCKING METHOD AND IN VITRO TEST
Authors: Sari Bina Lohita , Mun’im Abdul , Yanuar Arry , Riadhi Rezi
Published: February 2017

Objective: Terminalia catappa L. (T. catappa L.) fruit has inhibitory activity on α-glucosidase, therefore, can be a potential natural source for the treatment of type II diabetes mellitus. Inhibitory activity of ethanol fruit extract with IC50 3.02 µg/ml was the strongest inhibition when compared with 54 medicinal plants used as an antidiabetic agent in Indonesia. This project was aimed to find the active compound from T. catappa L. fruit using molecular docking, identification ethyl acetate subfraction using TLC and GC-MC, determine in vitro test on α-glucosidase inhibitory activity from ethyl acetate extract and subfraction.

Methods: Molecular docking using AutoDock 4.2 was performed to predict the binding modes of α-glucosidase enzyme from Saccharomyces cereviciae with 13 chemical constituents of T. catappa. α-Glucosidase enzyme was obtained from Protein Data Bank (PDB code: 3A4A). Acarbose, voglibose and miglitol were used as standards. Docking result determines the highest binding energy (ΔG) and inhibition constants (Ki) as an active compound. Visualization of amino acid residues around the active compound was identified with PyMOL and LigPlot. Screening of active compound was carried out by T. catappa L. fruit remaceration extraction use hexane and ethyl acetate. Ethyl acetate extract was separated on silica gel column chromatography using n-hexane, ethyl acetate and methanol sequentially based on polarity of each solvent. Identification of an active compound from ethyl acetate sub fractions using TLC and GC-MS method. The inhibitory activity of the active compound of α-glucosidase was determined with in vitro test using α-glucosidase enzyme.

Results: The highest binding energy and inhibition constant is β–sitosterol with ΔG-10.61 kcal/mol and Ki 0.02 µM. The ligand was situated around of 18 amino acid residues. Ethyl acetate subfractions A, B and C showed that subfraction B contains similar spot characteristic and Rf value (0.42) with β-Sitosterol standard. Identification with GC-MS gave β–sitosterol acetate and sitostenone. Redocking process of β–sitosterol acetate and sitostenone showed ΔG-11.14 kcal/mol and-9.79 kcal/mol with Ki 0.01 μM and 0.07 μM respectively. In vitro test of acarbose, ethyl acetate extract and subfraction B gave IC50 17.52; 192.51 and 296.28 µg/ml.

Conclusion: Three steroids that are β-sitosterol, β-sitosterol acetate and sitostenone were the active compounds responsible for α-glucosidase inhibitory activity of T. catappa L. fruit. According to the in vitro test, ethyl acetate extract has stronger α-glucosidase inhibitory activity than ethyl acetate subfraction B.
PRENATAL DEVELOPMENTAL TOXICITY EVALUATION OF FUROSTANOL SAPONIN GLYCOSIDE BASED STANDARDIZED FENUGREEK SEED EXTRACT DURING ORGANOGENESIS PERIOD OF PREGNANCY IN RATS
Authors: Deshpande Pallavi , Mohan Vishwaraman , Pore Mukul , Gumaste Shailesh , Thakurdesai Prasad
Published: February 2017

Objective: To evaluate prenatal safety of furostanol saponin glycoside based standardized fenugreek seed extract (Fenu-FG) on pregnant female Wistar rats on embryo–fetal development organogenesis period in accordance with OECD guideline (No. 414).

Methods: Fenu-FG was administered to pregnant rats by gavage at 250, 500, and 1000 mg/kg/day over the exposure period of gestational days 5–19. The vehicle control (VC) group was also maintained. All dams were subjected to a cesarean section on gestational day 20 and the fetuses were examined for external, visceral, and skeletal alterations.

Results: There was no significant difference found during maternal examination (body weights, food consumption, numbers of pregnant and non-pregnant female rats) or reproductive parameters (gravid uterus weights, litter size and weights, number of fetuses, sex ratio (male/female numbers of implantations and resorption, number of implantation per female, pre-and post-implantation loss (%), dead and live fetuses (%), numbers and weights of corpora lutea) in Fenu-FG-treated as compared to VC group. Furthermore, the few incidental and non-significant malformations were observed in Fenu-FG-treated as well as VC group during external, visceral or skeletal examinations.

Conclusion: The prenatal oral exposure of Fenu-FG during organogenesis period to pregnant female rats was devoid of maternal or developmental (fetotoxicity or teratogenicity) with "No Observed Adverse Effect Level” (NOAEL) greater than 1000 mg/kg.
INHIBITION OF LIPID ACCUMULATION IN 3T3-L1 ADIPOCYTES BY MORINDA CITRIFOLIA LINN. LEAF EXTRACTS AND COMMERCIAL HERBAL FORMULAS FOR WEIGHT CONTROL
Authors: Saraphanchotiwitthaya Aurasorn , Sripalakit Pattana
Published: February 2017

Objective: To determine the in vitro anti-obesity effects of Morinda citrifolia leaf extract and herbal formulas used for weight loss in Thailand on lipid accumulation in 3T3-L1 adipocytes.

Methods: Differentiated 3T3-L1 adipocytes were treated with 0.1, 0.5 and 1 mg/ml M. citrifolia leaf extract, three herbal formulas (JL-RU, JL-TH, CD-H) and 1, 5 and 10 mg/ml rutin, gallic acid and caffeine. Lipid accumulation determined by measuring Oil Red O staining and triglyceride content measured by a colorimetric method in adipocytes were assayed compared to the control. The effect of test samples on the viability of preadipocytes and differentiated adipocytes were investigated.

Results: Differentiated adipocytes treated with 1 mg/ml M. citrifolia extract moderately inhibited fat accumulation (45.12%) and highly reduced triglyceride content (85.09%). Among the three herbal formulas, JL-TH considerably inhibited fat accumulation (109.17%, 1 mg/ml) and decreased triglyceride content (95.00%, 1 mg/ml) in adipocytes; this was higher than that for CD-H and JL-RU, respectively. The viability of preadipocytes treated with CD-H at 1 mg/ml was slightly decreased while those treated with JL-TH at 0.05-1 mg/ml showed moderately decreased viability in a dose-response manner. For differentiated adipocytes, CD-H at 0.5-1 mg/ml moderately decreased cell viability while JL-TH at 0.05-1 mg/ml caused moderate to high reduction of cell viability in a dose-response relationship.

Conclusion: M. citrifolia extract and three herbal formulas had anti-obesity effects in 3T3-L1 adipocytes, as indicated by a significant reduction in lipid accumulation, triglyceride content, and cell viability. These findings suggest a potential therapeutic approach for the prevention and treatment of obesity.
DRUG-RELATED PROBLEMS IN CHRONIC KIDNEYS DISEASE PATIENTS IN AN INDONESIAN HOSPITAL: DO THE PROBLEMS REALLY MATTER?
Authors: Ramadaniati Hesty U. , Anggriani Yusi , Wowor Vonny M. , Rianti Alvina
Published: February 2017

Objective: To identify and evaluate drug-related problems (DRPs) in patients with chronic kidney disease (CKD).

Methods: A prospective observational three-month study was conducted in adult patients with CKD hospitalized in five general medical wards and one intensive cardiac care unit in a major teaching hospital in Indonesia. Principal researcher (pharmacist) identified the occurrence of DRPs through the direct patient interview, discussion with nurses and assessment of patients’ medication charts and medical records. The identified DRPs were validated by a senior pharmacist and classified using Pharmaceutical Care Network Europe/PCNE classification scheme for DRP V6.2. Descriptive analysis was applied for demographic data, drug utilization and DRP profiles.

Results: There were 105 patients who met the inclusion criteria and 80% of these patients had end-stage renal disease. A total of 2404 medication orders were reviewed and 1026 DRPs were identified. Potential DRPs accounted for around two-thirds of the cases. The rate of overall DRPs was 42.7 DRPs per 100 medication orders and each patient in the study experienced approximately ten DRPs during their hospitalization. Treatment effectiveness and adverse reaction domains contributed to the majority of DRPs primary domains for problems. Drugs for cardiovascular diseases and drugs for correcting electrolyte imbalance were most commonly implicated in DRP incidence.

Conclusion: This study uncovered higher rate of DRPs experienced by each patient compared to other CKD studies. There were variations of DRP types when comparing with similar studies. Pharmacists’ competencies to identify, prevent and resolve DRPs are vital measures to improve clinical outcomes in CKD patients.
XYLAZINE-KETAMINE ANAESTHESIA; COMPARATIVE STUDIES IN MALE AND FEMALE CANE RATS (THRYONOMYS SWINDERIANUS)
Authors: A Olatunji-akioye , N Ojiaka H , S Samuel E.
Published: February 2017

Objective: Domestication of the Cane rats is on-going globally and might replace the conventional rodents used in biomedical research in future. However, the paucity of information on adequate anaesthesia vis-a-vis xylazine-ketamine drug combination in the male and female Cane rats warranted this study.

Methods: Six adult Cane rats {1.8±0.7 kg body weights (bwt.)} assigned into group A (Female) and group B (Male) of three rats each was used for the study. Each animal was premedicated with atropine sulphate (0.05 mg/kg bwt), and later administered xylazine (10 mg/kg bwt) and ketamine (100 mg/kg bwt) intramuscularly. Meanwhile, anaesthetic characteristics and physiologic indices of anaesthesia were monitored.

Results: Results obtained showed that the physiologic indices; open eyelids, smooth induction and recovery, skeletal muscle relaxation and somatic analgesia were observed in all the animals, however, the anaesthetic indices; time to induction, time to standing, duration of analgesia and duration of recumbency showed marked sex variations. The mean values for the duration of analgesia and recumbency were significantly elevated (P<0.05) in group B as compared with group A. Similar trend was seen for time to standing, but, it was non-significant (P>005). However, time to induction mean value for group A was non-significantly increased (P>005) when compared with group B. The heart rate, respiratory rate and rectal temperature mean values decreased in both groups non-significantly (P>0.05).

Conclusion: Conclusively, the xylazine-ketamine combination produced anaesthesia in Cane rat and the combination is more tolerated in the male Cane rats than the female Cane rats.
VARIOUS FORMULATION VARIABLES EFFECTING FLOATATION BEHAVIOUR OF SINGLE UNIT GASTRORETENTIVE CAPSULES OF OFLOXACIN
Authors: Raza Syed Naiem , Khan Nisar Ahmad
Published: February 2017

Objective: Objective of the present study was to prepare simple single unit gastro-retentive capsules of ofloxacin with the aim to have the gastric retention of the system for longer periods of time (12h) and to study the effect of various polymers on floating behaviour of such single unit gastro-retentive capsules of ofloxacin.

Methods: The method used for the preparation of gastro-retentive capsules was a simple physical blending of various low-density hydrophilic polymers alone and in combination with hydrophobic polymers and filling into capsules. These capsules were then subjected to in vitro floatation and matrix integrity study in 0.1N HCl using static volume beaker method and the United States pharmacopoeia (USP) type II dissolution apparatus method at 100rpm.

Results: Two grades of hydroxypropyl methylcellulose (HPMC) K4M and K15M used were found suitable for the purpose. Results showed that increase in HPMC level increased colloidal gel barrier strength along with matrix integrity with consequently improved buoyancy. Lactose which was added as release rate modifier decreased matrix integrity and buoyancy. Eudragit a hydrophobic polymer was added so as to have intact, the buoyant formulation for 12 h with desired drug release characteristics. The addition of eudragit enhanced matrix integrity and floatation time to certain levels but higher levels showed negative results. Floatation time of more than 16 h was observed in the formulations containing 2:1 ratio of HPMC K15M and eudragit respectively. 32 factorial design was used to study the effect of various formulation variables on buoyancy and matrix integrity. Formulations containing zero level of HPMC were found buoyant for more than 12 h with all levels of eudragit S100 (i.e.,-1, 0,+1 level). It was also observed that matrix integrity consequently buoyancy increased with increase in eudragit with all levels of HPMC.

Conclusion: The study concludes that eudragit S100 a hydrophobic polymer increased floatation time of the formulated capsules with all the three levels of HPMC K15M, but at the same time eudragit level should not exceed HPMC, while lactose a release rate enhancer decreased matrix integrity/floatation time of the formulated capsules.
ENHANCEMENT OF LORNOXICAM SOLUBILITY BY INCLUSION COMPLEXATION WITH CYCLODEXTRIN: PREPARATION AND CHARACTERIZATION
Authors: El-menshawe Shahira Fawzy , Eissa Essam , Ali Adel A. , Abderhman Ahmed A.
Published: February 2017

Objective: Lornoxicam is a potent anti-inflammatory drug which has analgesic and antipyretic properties. It is water-insoluble powder. The inclusion complexes of lornoxicam (LOR) with β-cyclodextrin (βCD) and 2-hydroxypropyl-β-cyclodextrin (HPCD) were prepared and characterised in order to improve the solubility of the drug and enhance its bioavailability.

Methods: Complexes were prepared by physical mixing and freeze-drying in three different drug/polymer ratios (1:1, 1:2 and 3:2). The solid complexes were characterised through differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffraction, nuclear magnetic resonance (NMR) spectroscopy, and Fourier transformed infrared (FTIR) spectroscopy.

Results: The data showed that LOR may be complexed with cyclodextrin (CD) forming soluble complexes. The lyophilized 1:2 LOR/HPCD complex is the most soluble.

Conclusion: Solubility increases with lyophilization than with physical mixing and by the use of HPCD than βCD in complexation.
BIOCHEMICAL EFFECT OF A HIGH DOSE OF THAUMATIN IN WISTAR RATS
Authors: Khayata Warid , Kamri Ahmad , Alsaleh Rasha
Published: February 2017

Objective: The aim of this work was to investigate the capability of a high dose of thaumatin; a sweet tasting protein, of improving induced protein malnutrition in male Wistar rats.

Methods: For this study, 12 rats were divided into 2 groups and treated orally along with a high-carbohydrate, low-protein diet as follows: water group as a negative control, and thaumatin group at a dose of 464 mg/kg for 3 consecutive w. Blood samples were collected to analyse glucose, triglycerides, total cholesterol, and total protein, and body weight was measured. An oral glucose tolerance test (OGTT) was carried out at the end of the experiment.

Results: Despite the high amount of thaumatin used, only a slight increase in blood glucose occurred and was within the normal range, whereas serum triglycerides and cholesterol decreased significantly unlike control. Body weight had declined in both groups due to a low-protein diet, while total protein and glucose tolerance remained unchanged.
Conclusion: It is found that thaumatin is safe to consume by Wistar rats even at high doses. Besides that high-carbohydrate, low-protein diet caused falling of body weight, it had drawbacks of increased triglycerides and cholesterol levels which can be useful to create animal models of abnormal lipid metabolism without obesity. However, simultaneous ingestion of thaumatin with this diet had altered the outcomes to the best case. In future, it may be possible to use this combination for achieving healthy eating patterns without drug intervention that is needed for obese patients with various dysglycemia or dyslipidemia manifestations and people following regimes for weight reduction.
 
A COMPARATIVE STUDY ON THE EFFECT OF SOLVENTS ON THE PHYTOCHEMICAL PROFILE AND BIOLOGICAL POTENTIAL OF ORMOCARPUM COCHINCHINENSE AUCT. NON (LOUR.) MERRILL
Authors: Hepsibah A. Hannah , Jothi G. Jeya
Published: February 2017

Objective: Plants contain different classes of phytochemicals which have different levels of solubility in solvents, based on their polarity. Hence, this study aims to compare the effects of various solvents on the phytochemical profile and biological potential of Ormocarpum cochinchinense. The present study is the first to evaluate the antifungal activity of the plant.

Methods: The sequential extraction was carried out using two sets of solvent systems namely hexane, ethyl acetate, ethanol and chloroform, acetone, methanol. The extracts were subjected to standard phytochemical analysis, antimicrobial activity by disc diffusion method against eight bacteria and six fungi and antioxidant activity by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay.

Results: Varied range of phytochemicals was found in the extracts. Acetone extract was rich in phenolic compounds, whereas terpenoids were extracted only in methanol. Acetone extracts showed highest antibacterial activity with a maximum zone of 14.5 mm against Shigella flexineri whereas ethyl acetate extract showed the best antifungal activity with the highest zone of inhibition of 12 mm against Trichophyton menta agrophytes. Hexane and chloroform extracts did not show any antimicrobial activity. For DPPH assay, the ethanol extracts showed the highest percentage inhibition of 92.87%.

Conclusion: The present investigation on the plant O. cochinchinense has proved that the selection of solvent for extraction should be based on the target compounds and their bioactivity and concludes that acetone was the best for the extraction of antibacterial compounds and ethyl acetate for antifungal compounds whereas, ethanol was the best for extracting antioxidant compounds in O. cochinchinense.
DESIGN, SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW METFORMIN DERIVATIVES
Authors: Mahdi Monther F. , Arif Inam S. , Jubair Najwan K.
Published: February 2017

Objective: The purpose of this work was to enhance oral bioavailability of metformin by incorporation of different amino acid residues through the glycolic acid spacer.

Methods: Two series of metformin derivatives (V a-e) and (VI a-e) were synthesized by incorporation of five amino acids (glycine, alanine, phenylalanine, proline and GABA amino butyric acid) and their methyl esters respectively into metformin through glycolic acid spacer and preliminary evaluation for the antihyperglycemic activity was carried out using streptozotocin-induced diabetic rats model.

Results: In vivo anti-hyperglycemic activity of the final compounds (V a-e) and (VI a-e) showed that compounds (V b, V c, VI c and V e) produced higher percent of decrease in blood glucose level compared to metformin after 5 h of the treatment while compounds (VI b, VI c, V d, VI d, V e and VI e) showed profound effect after 24 h of the treatment. Although compounds (V a, VI a, V b and V c) showed a significant decrease in blood glucose level at 5 h but their effect diminished at 24 h. Compound (V e) showed higher anti-hyperglycemic effect than metformin and its effect continued up to 24 h.

Conclusion: From this study, it was concluded that incorporation of these amino acids or their methyl esters maintained or enhanced the antihyperglycemic effect of metformin. 
SUSTAINABILITY OF THE PROBIOTIC LACTOBACILLUS CASEI IN FORTIFIED INDIAN MILK CAKES UNDER DIFFERENT PRESERVATION CONDITIONS-EFFECTS OF CO-IMMOBILIZATION OF L. CASEI AND COMMERCIAL PREBIOTIC INULIN (CHICORY BASED) AND MILLET INULIN
Authors: Banerjee Debolina , Bag Puja , Chowdhury Ranjana , Bhattacharya Pinaki
Published: February 2017

Objective: The objective of the present article is to identify the most suitable Indian millet inulin for the growth of probiotic Lactobacillus casei and to evaluate the effects of the fortification vectors (probiotics and probiotic-prebiotic combination in immobilized conditions) and immobilization methods on the sustainability of L. casei in a fortified Indian sweet (milk cake) preserved under different conditions.

Methods: Inulin was extracted from pearl, finger and great millets. The concentrations of L. casei, grown on three millet inulins, were compared in 24 h batch culture. The L. casei and probiotic-prebiotic combinations namely L. casei-commercial inulin and L. casei-pearl millet inulin were immobilized using entrapment, external and internal microencapsulation methods. The Indian milk cake samples were fortified with the immobilized probiotic cells, co-immobilized probiotic-prebiotic combinations. The fortified samples were preserved at different conditions (temperature: 4 °C and-20 °C; Time: 1-4 w). The sustainability of L. casei in the preserved samples was determined using spread plate method and the cell concentrations were compared among all fortified samples.

Results: Pearl millet inulin is determined to be the most suitable millet inulin for the growth of L. casei. The synergistic combination of L. casei–pearl millet inulin, co-immobilized with internal gelation technique is the best fortification vector for the viability of L. casei in preserved food samples.

Conclusion: The L. casei, co-immobilized with pearl millet inulin through internal gelation technique, can be utilized as an effective fortification vector for the sustainability of probiotic cells in preserved Indian milk cakes and similar food samples.
RESVERATROL INCLUSION COMPLEX WITH β-CYCLODEXTRIN (RCD): CHARACTERIZATION AND EVALUATION OF TOXICITY IN WISTAR RATS
Authors: Nishihira V. S. K. , Mezzomo N. J. , Baldissera M. D. , Vaucher R. A. , Pinto C. G. , Pohl A. R. , Gomes P. , Junior L. F. Rodrigues , Frizzo C. P. , Bender C. R. , Fantinel L. , Fernandes L. S. , Giongo J. L. , Raffin R. P. , Rech V. C.
Published: February 2017

Objective: The aim of this study was to characterise the resveratrol inclusion complex with β-cyclodextrin (RCD) and evaluate their toxicity in wistar rats.

Methods: The RCD were prepared in ultra-turrax. For characterization of the RCD were used: Fourier transform infra-red Spectroscopy, Nuclear Magnetic Resonance (NMR), Differential Scanning Calorimetry (DSC) and X-ray powder diffraction. The RCD and others 4 treatments were performed by the chronic oral administration in 35 rats during 60 ds. After the treatments they were euthanized and the serum blood were collected to analyzed some hemogram and biochemical parameters including aspartyl aminotransferase (AST); alanine aminotransferase (AST); phosphatase alkaline (ALP); total bilirubin (TB); direct bilirubin (DB); total protein (TP); total cholesterol (TC), triacylglycerol (TAG), very low-density lipoprotein (VLDL), high-density lipoprotein (HDL), calcium, iron and phosphate using fully automated biochemistry analyzer.

Results: The characterization results indicated a successful formation of the RCD. All hematological parameters analysed were within the normal values in all the groups. Furthermore, the hemogram and biochemical parameters were significantly (P>0.05) similar to the control group.

Conclusion: The daily oral administration during 60 d of RCD are not harmful on blood parameters of Wistar rats. Thus, RCD can be used safely for treatment of some metabolic diseases.
FORMULATION, OPTIMIZATION, CHARACTERIZATION AND IN VIVO ANTI-ULCER ACTIVITY OF ESOMEPRAZOLE MAGNESIUM TRIHYDRATE GASTRORESISTANT MICROSPHERES
Authors: Sawant Krutika , Patel Mitali , Patel Jiten , Mundada Piyush
Published: February 2017

Objective: The objective of the present investigation was to prepare gastro-resistant microspheres of esomeprazole magnesium trihydrate (EMT) to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption.

Methods: EMT loaded gastro-resistant microspheres were prepared using hypromellose acetate succinate (HPMCAS) as the gastro-resistant polymer by ‘non-aqueous solvent evaporation’ technique. A 3-factor 3 level factorial design was used to optimise EMT: HPMCAS ratio, the concentration of Span 80 and stirring speed with respect to percent entrapment efficiency and particle size. Further characterization was carried out using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), In vitro release study and In vivo anti-ulcer activity.

Results: Fourier transform infrared (FTIR) study indicated compatibility between drug and polymer. DSC study revealed that the drug was molecularly dispersed in the polymer. The optimised batch showed 49.63±1.23% drug entrapment and 170.12±3.36 μm particle size. SEM study showed that microspheres were spherical in shape. In vitro drug release study showed only 4.28±1.23% drug release in simulated gastric media in 2 hr and 93.46±1.20% release in simulated intestinal media after 1 hr from the optimised batch.

Conclusion: Results of in vitro release studies indicated the gastro-resistant nature of the developed microspheres. In vivo anti-ulcer activity demonstrated that EMT loaded microspheres were able to significantly reduce ethanol-induced ulcer formation in rats’ stomach as compared to the aqueous solution of EMT. So it can be concluded that the developed gastro-resistant microspheres of EMT prevented drug release in the stomach which would lead to a significant improvement in its bioavailability through enhanced intestinal absorption
ROLE OF SUSPENDED PARTICULATE MATTER IN ANGIOGENESIS EMPLOYING CROWN GALL TUMOR ASSAY
Authors: Kaur Simerpreet , Katnoria Jatinder K.
Published: February 2017

Objective: Aim of the study was to screen the suspended particulate matter for their role in enhancing angiogenesis employing crown gall tumor assay.

Methods: Particulate matter (PM10) samples were collected, on glass fiber filter paper at the rate of 1.12–1.14 m3/min for 8 hr using high volume sampler, from six different sites of Amritsar city. Aqueous extracts of suspended particulate matter were prepared using a mechanical shaker for 24 hour and the filtrate was centrifuged and lyophilized.

Results: Maximum (34.67±1.764) tumors were induced by samples collected from Crystal chowk whereas tumor inducing ratio (TIR) was found to be comparably high for two sites viz., Crystal chowk and Bhandari bridge.

Conclusion: High tumor inducing ratio at the above-mentioned sites was correlated to high traffic emission from automobile exhaust. Crown gall tumor assay has been proved to be rapid, economical and reliable screening assay for angiogenesis agent.
THEEFFECT OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS ON CARDIOVASCULAR DISEASE RISK IN TYPE 2 DIABETES MELLITUS
Authors: Tolba Marwa K.a. , Khashab Khaled A. El , Said Amira S.a.
Published: February 2017

Objective: The aim of this study was is to investigate the proposed beneficial cardiovascular effects of a novel class of antidiabetic drugs named; dipeptidyl peptidase 4 inhibitors. In this study, we compared the effect of using add-on therapy of vildagliptin (dipeptidyl peptidase-4 inhibitor; DPP-4i) and gliclazide (sulphonylurea; SU) to that when using gliclazide monotherapy in patients with type 2 diabetes mellitus (T2DM) and acute coronary syndrome (ACS) on different cardiovascular outcomes.

Methods: A total of 60 patients diagnosed with T2DM, and ACS were randomly recruited into two treatment groups each of 30 patients to receive either gliclazide monotherapy (SU) or vildagliptin (DPP4i)+gliclazide (SU) add-on therapy, administered in a double-blind fashion. Outpatient visits were scheduled at 3, 6, and 12 mo where patient was reevaluated for cardiovascular (CV) outcomes and followed up for any arising cardiovascular complication.

Results: The vildagliptin (DPP4i) plus gliclazide (SU) add-on therapy group have significantly shown more improved glycemic control, lipid profile and ventricular performance compared to gliclazide (SU) monotherapy group with p values<0.05.

Conclusion: Vildagliptin as a DPP4i provides favourable cardiovascular effects beyond glucose control. Yet, its long-term safety and efficacy data still needs further investigations.
REVERSIBLE CONTRACEPTIVE POTENTIAL OF HARAD IN MALE ALBINO MICE
Authors: Gupta Prakash Chandra
Published: February 2017

Objective: Developing a male contraceptive of plant origin has always been of great interest among researchers. The aim of present investigation was to evaluate the contraceptive potential of Terminalia chebula R. (Harad) with respect to dose and reversibility in male albino mice.

Methods: Aqueous bark extract of Harad was administered orally at 100 (G III), 300 (G IV) and 500 (G V) mg/kg b.w. to males for 35 d, and the effect on histology of testis and accessory sex organs, enzymes 3ß-and 17ß-HSDs, SOD, catalase and LPO levels, sialic acid and fructose levels, sperm parameters, serum testosterone and fertility parameters was determined. Toxicological and recovery studies (G VI and VII) were also carried out.

Results: Harad-treated mice showed dose-related histological alterations in reproductive organs with reductions in weights, the height of germinal epithelium, germ cell number and diameter of stage VII tubules, along with adverse effect on biochemical and sperm parameters compared to controls. No alterations were noticed in SOD, catalase and LPO levels, though, mice in G V showed an increased LPO level. Libido was not affected, but fertility suppressed significantly in Harad-treated males (G VI) compared to controls. However, 42 d after treatment withdrawal, alterations in reproductive end points and fertility recovered to control levels. Body and organ weights, histo-architecture of vital organs, levels of ALT, AST and creatinine, and hematological parameters remained unchanged.

Conclusion: The results suggest that Harad causes dose-dependent reversible contraception in mice without any toxicity. 
EFFECTIVE MANAGEMENT OF HEMOLYTIC COMPLICATIONS BY TRADITIONALLY PREPARED KĀNTAM FORMULATIONS
Authors: Rajasekar Geetha Sudheer , Brindha P. , Ramanathan V.
Published: February 2017

Objective: Kāntam based formulations are unique herbo-metallic preparations, used in Siddha system of medicine (Indian traditional medicine) for managing various haematological complications. Their therapeutic doses were also well established in Siddha literature. In this work an attempt was made to understand the comparative effect of three different kāntam formulations in the management of hemolytic complications.

Methods: Hemolysis was induced in Wistar rats by intraperitoneal injection of acetylphenylhydrazine. Three different kāntam formulations (Kāntac centūram1 (K1), Kāntac centūram2 (K2) and Kāntap paṟpam (K3) were administered with proper controls at their therapeutic doses (20.0 mg/day) for a period of 20 d. Cage side observations, hematological, biochemical and histopathological analysis were performed to understand the effect of the formulations.

Results: Cage-side observations revealed that only K1 is effective in curing oral ulcers formed during hemolysis. Haematological analysis revealed the effect of K1 and K3 in regulating reticulocyte maturation and effect of K1, K2 and K3 in the removal of extracellular haemoglobin. Histopathological analysis revealed the effect of K1 in regulating stress erythropoiesis and effect of K1, K2 and K3 in regulating kupffer cells in the liver. Overall, the kāntam formulations demonstrate an appreciable relevance (in managing hemolytic conditions) within the contemporary pharmacological parlance.

Conclusion: Our study demonstrated the effective role of Kāntam formulations in the treatment of hemolytic complications by promoting reticulocyte maturation, removing extracellular haemoglobin, regulating stress erythropoiesis in the spleen, regulating kupffer cells in the liver and preventing oral ulcers. However, all the three formulations did not show all the activities and differ in efficacy profile.
IN VITRO AND IN SILICO ANTIMICROBIAL STUDY OF STANNANE OF PYRIDOXAL 5-PHOSPHATE
Authors: Aniyery Rohit Babu , Gupta Anita , Singh Prashant , . Sanju
Published: February 2017

Objective: The main objective of this research work is to synthesize a novel stannane of pyridoxal 5-phosphateand to study its antibacterial property.

Methods: Conventional method was used to synthesize the stannane of pyridoxal 5-phosphateand its characterization was carried using UV-visible and 1H NMR. The antibacterial study was carried against, Staphylococcus aureus (gram positive) and Escherichia coli 1610(gram negative) using well diffusion method. In silico antimicrobial was carried out using computational software iGemDock v2.1 tool.(Graphical Drug Design system for Docking, Screening, and Post-analysis), computational docking was carried out using different PDB (Protein Data Bank) files (2I42, 3EOO, 3D2U and 3D2Y). The structure was optimized prior docking using Gaussian software, and the method followed was Energy (Ground state) Hartree-Fork.

Results: It was observed that the stannane of pyridoxal 5-phosphateinhibited bacterial growth of Staphylococcus aureus (gram positive) and Escherichia coli 1610 (gram negative) in vitro antibacterial study. The complex has shown good docking results on almost all the receptors, with interaction supporting the fitting of the drug to the target molecules. The novel complex has shown good antibacterial activity (theoretically) in insilico studies. It was found to having a good potency to efficiently inhibit the microbes Burkholderia pseudomallei, Human cytomegalovirus, Yersinia enterocolitica and Escherichia coli, based on the interaction profile. The synthesized stannane was found to be effective in halting the undesirable effects of selected PDB files.

Conclusion: On the basis of the above findings in the present research work, the novel complex was found to be a good antimicrobial agent and our future studies will aim design of novel selective and potent inhibitors. Further in vitro studies of this compound against these bacteria will lead to a new pathway to a novel antibacterial drug discovery.
OBESITY: DEVELOPMENT, EPIDEMIOLOGY, FACTORS AFFECTING, QUANTITY, HEALTH HAZARDS, MANAGEMENT AND NATURAL TREATMENT-A REVIEW
Authors: Bollapragada Mani Kumar , Shantaram Manjula , R. Sunil Kumar
Published: February 2017

Due to the advancement in science, enhanced knowledge on the physiological aspects of almost all the tissues and the organs of the human body is gained. One of the most important prevalent topics needed for discussion is obesity and its effect on the metabolic changes leading to disorders in the human body such as diabetes, hypertension, cardiovascular diseases in addition to chronic diseases such as stroke, osteoarthritis, sleep apnea, some cancers, and inflammation-based pathologies. In recent years, obesity is a serious socioeconomic issue, which has become one of the major health problems all over the world, affecting people of all ages, sex, ethnicities and races. Obesity is a complex and multifactorial disease caused by the interaction of a myriad genetics, dietary, lifestyle and environmental factors and it is characterised by an excessive weight for height due to an enlarged fat deposition in the adipose tissue, which is due to a higher calorie intake than the energy expenditure. The pharmaceutical drugs are currently available to treat obesity but generally they have unpleasant side effects. Recent researches demonstrated the potential of natural products to counteract on obesity. Now the novel promising approach is the usage of dietary supplements and plant products and their bioactive compounds that could interfere on pancreatic lipase activity, food intake, lipid metabolism and adipocyte differentiation. In a similar way, hundreds of extracts are currently being isolated from plants, fungi, algae or bacteria and are screened for their potential inhibitions of activity against obesity. Natural products may have a synergistic activity that increases their bioavailability and action on multiple molecular targets.