bluuebunny/crossref_metadata_2025_split huggingface dataset:
UTILITY OF PLACENTAL LEUCINE AMINOPEPTIDASE/OXYTOCINASE IN THE PREDICTION OF PRETERM DELIVERY IN PREGNANT WOMEN WITH THREATENED PRETERM LABOR
Authors: MIAMI ABD–AL HASSAN  , ISRAA TALIB ABD AL KADIR  , NOOR HUMAM MOHAMMED  
Published: October 2019

Objective: The study objective was to assess the utility of placental leucine aminopeptidase (P-LAP) marker for the prediction of delivery in patients presented with threatened preterm labor (TPL).
Setting: This study was conducted at the Obstetrics and Gynaecology Department of Al-Yarmouk Teaching Hospital in the period from March 2017 to June 2018.
Type of Study: This is a prospective case control study.
Methods: This study included 90 pregnant women with gestational age from (28-36+6) weeks; 45 of them who presented with preterm uterine contractions were considered as the study group which was further subdivided into three subgroups according to gestational age 28–31+6 weeks, 32– 33+6 weeks, and 34–36+6 weeks. The other 45 pregnant women who presented to the hospital for regular antenatal care visit at comparable gestational age to the study group were considered as the control group. Hence, this study aimed to assess the serum level of P-LAP in both groups and compare it between those delivered preterm from term to assess its applicability as a predictor of preterm labor.
Results: Serum level of P-LAP in pregnant women presented with TPL was found to be significantly lower in those delivered preterm (p<0.001), compared to those continued to term and control group especially in gestational ages ≥32 weeks, while the study found P-LAP level to be statistically insignificant in gestational age <32 weeks (p=0.052). The cutoff point for P-LAP serum level was = 21 (IU/ml) that below it, the pregnant women with TPL most probably deliver before 37 weeks of gestation with Sensitivity (85.7%) Specificity (90.3%), Positive predictive value (80.0%) Negative predictive (93.3%).
Conclusion: The serum level of P-LAP was lower in women delivered preterm than those delivered at term, so it can be used as one of the markers for the prediction of preterm delivery, especially at gestational age >32 weeks.
EVALUATION OF IN VITRO CYTOTOXIC AND ANTICANCER ACTIVITY OF HEPATOPROTECTIVE POLYHERBAL FORMULATION IN CELL LINE MODEL
Authors: JAYACHANDRA KUNCHA  , THIRUGNANASAMBANTHAM P  , KUMARAN S  , NARAYANAN N  , SHARMILA DEVI V  
Published: October 2019

Introduction: The use of natural products as anticancer agents has a long history that began with folklore medicine and through the years has been incorporated into traditional and allopathic medicine. Several drugs currently used are derived from medicinal plants.
Objective: The main objective of this study is to investigate the cytotoxic potential of hepatoprotective polyherbal formulation in normal and cancer cell lines.
Methods: A 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was utilized to screen the cytotoxic activity.
Results: The results revealed that the formulation does not induce much mortality in normal liver and kidney cell lines, and LC50 value of liver cell lines was found 1716.355 μg/ml and kidney cell lines 2464.910 μg/ml. The in vitro anticancer activity was performed on liver, colon, and prostate cancer cell lines, and IC50 values are found 2.077, 3.850, and 11.989 μg/ml, respectively, which show excellent anticancer activity.
Conclusion: Based on the results obtained, the hepatoprotective polyherbal formulation is safe for normal cells and cytotoxic for cancer cells. Further, identification and quantification of phytoconstituents responsible for the activity are in progress.
COMBINATION OF LEPTIN ANALOG AND SALBUTAMOL: TREATMENT APPROACH FOR OBESITY-INDUCED ASTHMA
Authors: ARUN K SONI  , SHRIKALP S DESHPANDE  
Published: October 2019

Objective: The objective of the study was to investigate the effect of leptin analog and salbutamol in obese asthmatic mice.
Methods: Obese asthmatic condition was induced by administration of hypercaloric diet for 8 weeks followed by ovalbumin-aluminum hydroxide. The animals were treated with leptin analog (0.4 mg/kg, i.p. for 14 days) and salbutamol (2 mg/kg, PO for 14 days). Biochemical parameters such as serum leptin, ghrelin, and tumor necrosis factor-α and physical parameters such as tidal volume and airflow rate were estimated to confirm the state of asthma and obesity, respectively.
Results: Elevated serum leptin and ghrelin were associated with leptin resistance in obese asthmatic mice. It was found that a significant increase in serum leptin level with animal treated with leptin analog and salbutamol when compared to animals treated with leptin analog alone. The result of respiratory parameters and serum parameters also improved with the combination of leptin analog and salbutamol. From our study, we found that salbutamol potentiates the effect of leptin analog in obese asthmatic condition.
Conclusion: Leptin analog and salbutamol are an alternative treatment approach to treat the obese asthmatic condition.
IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITY OF ULVA LACTUCA L.USING MOLT-3 CELL LINE
Authors: CHIDAMBARARAJAN P  , KEERTHANA V  , PRIYADHARSHINI K,  , SAKTHIVEL B  
Published: October 2019

Objective: The aim of the present investigation was to determine the in vitro antioxidant and anticancer activity of the ethanol extract of Ulva lactuca L.
Methods: The present study was to investigate the antioxidant and anticancer activity of U. lactuca L. The extract of U. lactuca L. was extracted by ethanol and subject to analysis. An in vitro antioxidant activity of the ethanol extract of U. lactuca L. was performed by 1, 1-diphenyl-2-picrylhydrazyl free radical scavenging assay. Simultaneously anticancer activity was also performed using blood cancer (MOLT-3) cell line, and the species showed a strong selective cell proliferation inhibition of the cancer cell line.
Results: The scavenging activity was measured and determined to be 78.5%. This might be due to high polyphenolic compounds and flavonoid contents of the extract, which showed maximum growth inhibition of 74.4%.
Conclusion: Thus, the study concludes that the constituents of seaweeds can act as potent in treating various diseases and can be used as an alternative for therapeutic treatment.
STUDIES ON TOXICOLOGICAL AND NEUROBEHAVIORAL PROFILE OF METHANOL EXTRACT OF MUSSAENDA ROXBURGHII HOOK. F. LEAVES IN MICE
Authors: SANJIT NAMASUDRA  , PANKAJ PHUKAN  , MEENAKSHI BAWARI  
Published: October 2019

Objective: The aim of this study was to evaluate the toxicity of Mussaenda roxburghii with special reference to the nervous system.
Methods: For the study, 15 mice were obtained from Pasteur Institute, Shillong. The mice were then divided into three groups containing five mice in each group. The groups were, namely Group I, Group II, and Group III; Group I mice received distilled water and acted as a control group, Group II mice received plant extract at a dose of 600 mg/kg body weight (BWT.), and Group III mice received plant extract at a dose of 800 mg/kg BWT. The doses were administered orally through oral gavage tube for 28 days and the BWT of the mice was measured at 7th, 14th, 21th, and 28th days. The behavior of mice was evaluated for anxiety, locomotion, immobility, learning, and memory with the elevated plus maze test (EPMT), open field test (OFT), forced swim test (FST), and Morris water maze test (MWMT), respectively.
Results: The result of the experiment showed a decrease in the BWT of mice exposed to plant extracts significantly as compared to the control. In the OFT, there is a significant decrease in total distance travel in OFT and also total distance travel in the central zone in mice treated with the plant extracts as compared to the control mice. In the EPMT, the plant extract treated mice showed a decreased in the time spent in open arms. The FST results in increased immobility in mice exposed to plant extracts as compared to control. In the present study, MWMT results in an increased escape latency and path length and in decreased annulus crossovers in plant extract treated group as compared to control.
Conclusion: The results of the present study suggest that the plant extract alters the behavior of the treated mice and possesses neurotoxic activity.
SYNTHESIS, IN SILICO STUDIES AND EVALUATION OF ANTIBACTERIAL ACTIVITY OF 4-SUBSTITUTED BENZYLIDENE-2-(PHENOXYMETHYL) OXAZOL-5(4H)-ONES
Authors: SHAHEEN BEGUM  , ARIFA BEGUM SK  , MANEESHA M  , OME SHANTHI T  , SATYA VARALAKSHMI D  , MANJUSHA RK  , BHARATHI K  , BHARATHI K  
Published: October 2019

Objective: Arylidene-1, 3-oxazol-5-ones represent potential antibacterial agents. In the present work, a series of 4-substituted benzylidene-2- (phenoxymethyl) oxazol-5(4H)-ones were synthesized and screened for antibacterial activity against Gram-negative bacteria Escherichia coli. To explore plausible mechanisms, synthesized compounds were docked with DNA-Gyrase enzyme.
Methods: All the reactants, phenoxy acetyl chloride, acetic anhydride, sodium acetate, substituted aromatic aldehydes, and glycine were triturated in a mortar by mechanical stirring. The antibacterial potentiality of the compounds was screened against E. coli using the disk diffusion method and the activity was recorded as a zone of inhibition.
Results: Compound 2d, possessing 3, 4, 5-trimethoxy functionality on benzylidene ring exhibited the highest activity with 19 mm of the zone of inhibition which might be due to its higher interactions with DNA-Gyrase enzyme (ΔG-8.41 kcal/mol). Compounds 2a, 2b, and 2c exhibited moderate activity in the antimicrobial assay as well as in docking study indicating the positive contribution of substitution on benzylidene ring.
Conclusion: A series of 4-substituted benzylidene-2-(phenoxymethyl) oxazol-5(4H)-ones were synthesized and evaluated for antibacterial activity. Compounds 2a, 2b, and 2c displayed moderate activity whereas 2d showed maximum zone of inhibition (19 mm). The good activity of these derivatives presumed to be due to the conformational flexibility of phenoxy methylene moiety which can be well accommodated in the target binding site.
CYTOTOXICITY AND EXPRESSION STUDIES OF ANGIOGENESIS-PROMOTING GENES IN CANCER CELL LINES UNDER THE TREATMENT OF CANCER CANDIDATE DRUGS
Authors: SALAM ABBAS  , SUDHAKAR MALLA  
Published: October 2019

Objective: Human antigen R (HuR) is a member of the RNA-binding proteins which is a critical factor in mediating the proangiogenic factors resulting in angiogenesis among the tumors. During inflammation and anoxic conditions, cytokine interleukin-1 (IL-1) was found to activate the HuR which, in turn, aids in upregulation or downregulation of the hypoxia-inducible factors (HIF) 1α. The present study was designed to study the correlative effect of the cancer drug docetaxel (Taxotere) on the expression levels of HuR and HIF1α using HeLa cell lines.
Materials and Methods: The drug was tested for cytotoxicity among the cancer cell lines using the lactate dehydrogenase and 3-(4)5-Dimethyl-thiazol-zyl)-2, 5, biphenyl tetrazolium bromide assay. Gene expression and correlation were found by the real-time expression of the gene members under the treatment. The same study was also confirmed using the molecular docking tools to screen for the possible potential anticancer target.
Results: The drug was found to decrease the expression levels of the cytokine IL-1 along with the HuR proteins. This was also found to show a positive inhibition on the expression of HIF1α. The study was also confirmed using the molecular docking studies which are in accordance to the wet lab studies.
Conclusion: The present study confirmed that the two receptors might act as potential anticancer drug targets which might aid in designing more novel drugs.
FORMULATION AND CHARACTERIZATION OF FLOATING BEADS OF ANTIBIOTIC BY EMULSION GELATION TECHNIQUE
Authors: KHALIFA MY  , SHAIKH SIRAJ N  
Published: October 2019

Objective: The study aims at formulation and characterization of floating hydrogel beads of cefdinir for improving its bioavailability.
Methods: Cefdinir is broad-spectrum, oral, third-generation cephalosporin antimicrobial agent active against Gram-positive and Gram-negative bacteria. The floating hydrogel beads of cefdinir were formulated with polymers such as sodium alginate and sodium carboxymethyl cellulose by emulsion gelation technique using olive oil/castor oil. The beads were evaluated for surface morphology, bead size, entrapment efficiency, floating characteristics, in vitro swelling, in vitro drug release, and stability studies.
Results: On the basis of evaluation, all the beads show good swelling up to 12 h in 0.1 N hydrochloric acid. The swelling was followed by values in order of vegetable oil > mineral oil in case of emulsion gelation method. Scanning electron microscopy study shows that beads were spherical in shape. Comparing all the formulations, formulation FB12 was considered as optimized formulation which shows % yield 94.06±0.11, % floating 87.28±0.90, in vitro drug release 94.68, and also stable in stability studies.
Conclusion: From the findings, it may be concluded that cefdinir-loaded floating beads were successfully prepared and proved to be useful for the better bioavailability and patient compliance for enhanced antimicrobial activity.
A POTENT CYTOTOXICITY AND ANTIMICROBIAL ACTIVITY OF ZINC OXIDE NANOPARTICLES SYNTHESIZED BY LEAF OF IPOMOEA PES-CAPRAE (L.) R. BR.
Authors: RAMESH A  , SUNDARRAJ P  , BALAMANI J  
Published: October 2019

Objective: The present study was conducted to investigate the cytotoxicity and antimicrobial activity of zinc oxide nanoparticles (ZnO NPs) synthesized as eco-friendly technique from the leaf extract of Ipomoea pes-caprae (L.) R. Br. against human lung adenocarcinoma (A549), brain tumor (U87) cells, and human pathogens Salmonella typhi, Staphylococcus aureus, Klebsiella pneumonia, Pseudomonas aeruginosa, and Bacillus subtilis.
Materials and Methods: The work was carried out with varying precursor (plant extract) volume to optimize the synthesis of ZnO NPs and it was confirmed by ultraviolet (UV)-visible spectroscopy, Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) analysis, scanning electron microscopy, and atomic force microscope (AFM) characterization techniques and evaluate its cytotoxicity activity by 3-(4,5-dimethyl-2- thiazolyl)-2,5-diphenyl--tetrazolium bromide assay method, antimicrobial activity by disk diffusion method.
Results: A peak at 320 nm with maximum intensity was observed at temperature of 80°C with pH of 8.0 in UV-visible spectroscopy confirmed the formation of ZnO NPs and we calculate the size of ZnO NPs from XRD data found as 15.8 nm. The FTIR analysis evaluated that the presence of different functional groups is carboxyl, amine, and phenolic compounds of leaves extract which are involved in the reduction of zinc ions and acts as capping the ZnO NPs. AFM microgram confirms that ZnO NPs were in nanorange and spherical in nature. The cytotoxicity activity of A549 and U87 cell lines treated with various concentrations of ZnO NPs showed a dose-dependent increase in cell inhibition and the half maximal inhibitory concentration value was calculated to be 7.8 μg/ml. The antibacterial activity of selected pathogens shows higher zone of inhibition.
Conclusion: The present study reveals that synthesized ZnO NPs capping with various bioactive compounds present in the leaf of I. pes-caprae show promising activity of cancer cell lines and antimicrobial agents; hence, further detailed study may lead to develop at a novel phytomedicine for the anticancer and antimicrobial drugs.
FORMULATION AND INVESTIGATION OF POLYMERIC MULTIPLE UNIT PELLET SYSTEMS CONSISTING OF SUSTAINED RELEASE GLIMEPIRIDE AND IMMEDIATE RELEASE ATORVASTATIN CALCIUM
Authors: BHARAT BIJAPUR  , GOWDA DV  , VISHAL GUPTA N  , SHAILESH THIRUMALESHWAR  , PRAVEEN SIVADASU  , MANJUNATH M  
Published: October 2019

Objective: The objective of the present work was to develop novel fixed-dose combinations (FDCs) for improvement of glucose tolerance in type II diabetes mellitus patients associated with dyslipidemia.
Methods: Multiple unit pellet systems (MUPSs) consisting of sustained release (SR) glimepiride and immediate release atorvastatin calcium pellets were formulated. The SR glimepiride pellets were prepared using a combination of locust bean gum and gum ghatti/guar gum. Similarly, the immediate release of atorvastatin calcium pellets was prepared using locust bean gum suspension as a binder.
Results: The formulated pellets were characterized using Fourier transform infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC). Further, surface morphology of the formulated pellets was done by scanning electron microscopy (SEM). FT-IR and DSC studies suggested that there were no chemical interactions between the drug and natural polymers. SEM studies revealed that formulated pellets were in spherical shape. Based on in vitro evaluation, the SR glimepiride formulation developed using a combination of 2% locust bean gum and 2.5% gum ghatti polymers sustained the release of the drug up to 12 h. Similarly, the immediate release atorvastatin calcium formulation containing 1% w/w locust bean gum suspension as a binder and 7% croscarmellose sodium showed fast disintegration of pellets. The in vivo studies in albino Wistar rat revealed that there was an improvement in bioavailability of the drugs. Stability studies showed that there were no significant changes in the drug content and physical appearance of the prepared SR glimepiride and immediate release atorvastatin pellet formulations.
Conclusion: Thus, the formulated FDC as MUPS can be used as an alternative approach for treating diabetes mellitus-induced dyslipidemia.
The ORMULATION OF GLIMEPIRIDE AND ATORVASTATIN CALCIUM NANOPARTICLES BY 1 LIQUID ANTISOLVENT PRECIPITATION METHOD THROUGH DOUBLE STEP COMMINUTION 2 TECHNIQUE AND ITS EVALUATION
Authors: VISHAL S REDDY  , GOWDA DV  , VISHAL GUPTA N  
Published: October 2019

Objective: The present research is to formulate Glimepiride and Atorvastatin Calcium Nanoparticles for the type-2 diabetes mellitus for improvement of glucose tolerance associated with dyslipidemia formulated by liquid antisolvent precipitation technique.
Method: Glimepiride nanoparticles and atorvastatin calcium nanoparticles were prepared by using a liquid antisolvent precipitation technique. Solvent to antisolvent ratio used was 3.5:6.5 and 2.5:7.5 and the drug concentration used was 40 mg/ml and 60mg/ml respectively.
Result: The XRD was determined, the data of the optimized Glimepiride formulation revealed that the prepared nanosized Glimepiride powder was existed in crystalline form. The percent yield for the formulations of Glimepiride and atorvastatin calcium nanoparticles was found to be 72.8±1.8%, 75.3±2.2% respectively. In-vivo studies in albino wistar rats demonstrated that the Cmax and AUC0−24h of optimized Glimepiride and atorvastatin calcium nanosized formulation was found to be 24451.14±2170.5 ng/ml, 162945.12±241.5 ng/ml and 1385.43±153.3 ng/ml,3636.57±65.2 ng/ml respectively. Dissolution study of optimized formulations shows that marked enhancement of dissolution rate. The stability studies of mixture of Glimepiride and atorvastatin calcium powder when stored at 4±3oC refrigerated temperature has shown no significant changes in physical appearance, drug content, particle size and PDI. Conversely the sample stored at room temperature has shown significant increase in particle size and PDI, with no significant changes in drug content and physical appearance.
Conclusion: The Formulation of glimepiride and atorvastatin calcium drug nanoparticles shows increase in the surface-to-volume ratio of API, resulting in better drug solubility and hence increasing the bio-availability when compared to its pure form.
PHYTOCHEMICAL AND PHYSICOCHEMICAL ANALYSIS OF MICROWAVE-ASSISTED EXTRACTION CORIANDRUM SATIVUM L. LEAVES AND ITS BIOLOGICAL EVALUATION
Authors: SAMREEN FATEMA  , MAZAHAR FAROOQUI  , PATHAN MOHD ARIF  , SYED UMMUL KHAIR ASEMA  
Published: October 2019

Objective: The main objective of the present work is to carry out the phytochemical constituent present and physicochemical analysis of microwave-assisted extract (MAE) of Coriandrum sativum leaves and to investigate its antibacterial activity.
Methods: The powdered samples of the leaves were extracted and analyzed for physicochemical properties. Extraction was carried out for C. sativum using different solvents and used for phytochemical investigation. Infrared (IR) spectrum and antibacterial activity of MAE were carried out.
Results: The results show that the percentage extract is different in the different solvents and also differs in phytochemical constituents. Phytochemicals present in the MAE also confirmed by IR spectroscopy. MAE is active against bacteria.
Conclusion: The phytochemicals present in C. sativum is confirmed by IR spectrum and these phytochemicals responsible for antibacterial activity.
IN SILICO DOCKING ANALYSIS OF YOHIMBINE ALKALOIDS FROM CATHARANTHUS ROSEUS AGAINST DENGUE FEVER
Authors: GIRIJA R  , ARUNA S  , SANGEETHA R  
Published: October 2019

Objective: In this docking study was performed by the active site of NS2B-NS3 protease with selected plant alkaloids derived from Catharanthus roseus. On the basis of docking results, out of the nine alkaloids yohimbine might be considered as the best inhibitors of NS2B-NS3 protease protein.
Methods: Lipinski rule was employed to check the ligand likeliness of the compound. The three-dimensional crystallographic structure of NS2B-NS3 protease (ID.2FOM) fetched from the protein data bank. The in silico docking studies were performed by “AutoDock version 4.2” software tool.
Results: Yohimbine is having the best binding score (−7.18 Kcal/mol) than the other eight compounds.
Conclusion: Hence, it has been concluded yohimbine as a novel inhibitor for NS2B-NS3 protease in dengue fever.
A VALIDATED STABILITY-INDICATING REVERSE-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR DACLATASVIR, IDENTIFICATION AND CHARACTERIZATION OF DEGRADATION PRODUCTS USING LC-ESI-QTOF-MS
Authors: SNEHAL V WARGHADE  , KAILAS G BOTHARA  
Published: October 2019

Objective: The objective of this study was to report the stability of antiviral drug, daclatasvir (DCV) based on the information obtained from forced degradation studies and characterization of degradation products (DPs) by tandem mass spectrometry (MS/MS) analysis.
Methods: Chromatographic separation was achieved on Shimadzu liquid chromatography (LC) 20 AD high-performance LC system with photodiode array detector having Kromasil C18 (250 mm×4.6 mm×5 μm) with isocratic elution of a mobile phase composed of ammonium acetate buffer (pH 4.5) and acetonitrile in a ratio of 50:50 at 315 nm. The drug was subjected to forced hydrolytic, oxidative, photolytic, and thermal stress in accordance with the ICH guideline Q1A (R2). The drug showed degradation under acidic and basic hydrolytic conditions by forming two DPs. The DPs were characterized using LC– MS/MS studies and the pathways of fragmentation are proposed. Validation of the developed method was carried out in accordance with ICH guidelines.
Results: Two DPs were identified, DP-1 as (S)-1-((S)-2-(5-(4’-(2-((S)-1-((S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)pyrrolidin-2-yl)-1H-imidazol-5-yl)-[1,1’-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-aminium and DP-2 as (S)-2-(5-(4’-(2-((S)-1-((S)-2- ((methoxycarbonyl)amino)-3-methylbutanoyl)pyrrolidin-2-yl)-1H-imidazol-5-yl)-[1,1’-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidin-1-ium.
Conclusion: The method proved to be simple, accurate, precise, specific, robust, and less time consuming and can be applied for the determination of DCV in bulk and marketed formulation.