bluuebunny/crossref_metadata_2025 huggingface dataset:
ANTIOXIDANT AND ANTI-INFLAMMATORY PROPERTIES OF PTEROSPERMUM RUBIGINOSUM HEYNE EX WIGHT AND ARN AND PTEROSPERMUM RETICULATUM WIGHT AND ARN (STERCULIACEAE): AN IN VITRO COMPARATIVE STUDY
Authors: JACOB JENSON , K SREEJITH
Published: October 2019

Objectives: Plants from the family Sterculiaceae are used as folk medicine for treating various diseases in India. This study aims to determine the antioxidant and anti-inflammatory properties of Pterospermum rubiginosum and Pterospermum reticulatum of the family Sterculiaceae. The barks of P. rubiginosum and P. reticulatum are used in traditional medicine especially in the treatment of wounds, sprains, bone fracture, etc. This study, we compare the antioxidant and anti-inflammatory potentials of the stem bark of these two plants.

Methods: The free radical scavenging assays such as 2,2–diphenyl,1–picrylhydrazyl (DPPH), 2,2’–azino-bis(3-ethylbenzothiozoline-6-sulfonic acid) (ABTS), hydroxyl radical, nitric oxide radical, phosphormolybdenum assay, and reducing power assay are used for the measurement of antioxidant potentials. The in vitro anti-inflammatory activities of the extracts are evaluated by means of lipoxygenase (LOX) and protease inhibition.

Results: Both P. rubiginosum and P. reticulatum scavenge DPPH (70.10% and 91.02%), ABTS (94.48 and 98.19%), hydroxy (76.02 and 87.67%), and nitric oxide (87.02 and 80.84%) radicals. Phosphomolybdenum assay and reducing power assay, used for the measurement of antioxidant potentials also showed good results. Regarding the anti-inflammatory potential, the methanolic extract of the plants shows anti-protease activity (51.29 and 64.93%) and anti-LOX activity (56%) while P. rubiginosum does not exhibit anti-LOX activity.

Conclusion: The above results demonstrate that the plants P. rubiginosum and P. reticulatum are rich source of antioxidant and anti-inflammatory compounds and it is the first report on theantioxidant and anti-inflammatory properties of the barks of these plants.
ISOLATION AND IDENTIFICATION OF NON-POLAR CHEMICAL ENTITY FROM LEPTADENIA RETICULATA AERIAL PARTS
Authors: DHALANI JAYESH , NARIYA PANKAJ
Published: October 2019

Objective: Leptadenia reticulata is the medicinal plant having many biological activities. It is necessary to find out which types of phytochemical constituents are present in the plant. The objective of this investigation was to isolate and identify the non-polar chemical entity of the areal parts of L. reticulata a plant used for medicinal purpose in folklore.

Methods: Petroleum ether extract of the stem bark was used for this study. Non-polar solvent was used to extract non-polar chemical entity from areal parts of leptadeniareticulata. Through the saponification process, saponifiable and unsaponifiable matter was separated. Phytochemical constituents were separated using column chromatography. Separated fractions were analyzed on gas chromatography and mass spectrometry (GC-MS) and nuclear magnetic resonance spectroscopy (NMR).

Results: Hentriacontane compound was isolated and confirmed from GC-MS and NMR whereas phytol, Lupeol, β-amyrin, Campesterol, Stigmasterol, gamma-sitosterol identified through GC and mass spectroscopy.

Conclusion: The present study showed that L. reticulata areal parts three sterols chemical entity Campesterol, Stigmasterol, gamma-sitosterol and phytol (diterpene alcohol), lupeol (triterpenoid), beta-amyrin (triterpene), and hentriacontane (alkane hydrocarbon). Core determination of the experiment was the development efficient method to isolate or identify the non-polar chemical entity through chromatographic technique.
ENDOCRINOLOGICAL ROLE OF LEPTIN IN OBESITY AND ASTHMA
Authors: K SONI ARUN , B PITHADIA ANAND , S DESHPANDE SHRIKALP , N SUHAGIA BHANUBHAI
Published: October 2019

Objective: Role of leptin resistance in correlation between obesity and asthma.

Methods: High-caloric diet was given for 8 weeks to induce obesity. Ovalbumin followed by aluminum hydroxide was given to induce asthma. The animal was treated with leptin analog (0.4 mg/kg, i.p. for 7 days) and leptin antagonist (3 mg/kg, p.o., for 7 days). Biochemical parameters such as serum leptin, ghrelin, and tumor necrosis factor alpha (TNF-α) and physical parameters such as tidal volume and airflow rate were estimated to confirm the state of asthma and obesity, respectively.

Results: It was found that leptin and ghrelin were elevated in obese and obese asthmatic condition, responsible for leptin resistance. Treatment with leptin analog and leptin antagonist significantly increases and decreases serum leptin levels, respectively. There was no significant change in TNF-α and ghrelin level after leptin analog treatment. The result of respiratory parameters improved with leptin analog. From our study, we found beneficial role of leptin analog in obese asthmatic condition.

Conclusion: Leptin is an alternative treatment approach to treat obese asthmatic condition.
CYTOTOXIC EFFECT OF PEPTIDE FUNCTIONALIZED SILVER NANOPARTICLES SYNTHESIZED FROM ALOIN ON BREAST CANCER CELL LINE
Authors: ROSE A LEEMA , S VIDHYA , PRIYA F JANEETA , ASHIFA J SABEENA
Published: October 2019

Objective: The aim of the present study is to synthesize the silver (Ag) nanoparticle using Aloin with a focus on its antibacterial, antioxidant, and anticancer activity.

Methods: The silver nanoparticles were synthesized using Aloin and were determined by UV-Visible spectrum. It was further characterized by scanning electron microscope (SEM), zeta potential, and dynamic light scattering (DLS). The Fourier transform infrared analysis was also carried out for the Aloin.

Results: The UV-Visible absorption spectrum of the synthesized silver nanoparticles has shown the absorption peak at 439nm which proves the formation of silver nanoparticles in the solution. The SEM analysis revealed that the Ag nanoparticles were spherical in shape. The IR spectra showed that there are 6 functional groups are present in Aloin extract. The synthesized nanoparticles are found to be highly stable with an average particle size of 130.7nm which was confirmed by zeta potential and DLS analysis. The synthesized nanoparticles had a good antibacterial and antioxidant activity. It shows a very good cytotoxic effect against breast cancer cell line.

Conclusion: The present study suggests that the synthesis route is free from the requirements such as high energy, extended preparation time, and special equipments and thus can be used for large-scale synthesis in food industries for food preservation and these Ag nanoparticles can be used for its therapeutic purposes for developing a new drug against cancer.
EVALUATION AND COMPARISON OF CYTOTOXIC EFFECT OF VILAZODONE HYDROCHLORIDE WITH 5-FLUOROURACIL IN HT-29 BOWEL CANCER CELL LINE
Authors: PRIYA A LATHA , D ANUSHA , CHELLATHAI K DARLING , A HEMALATHA , MOHAN Y JEGAN
Published: October 2019

Objectives: Vilazodone hydrochloride is a novel selective serotonin reuptake inhibitor (SSRI) used to treat major depressive disorders. There are only sparse data available to know about the SSRI’s and its association with colon cancer. This study aims to evaluate and compare the in vitro cytotoxic effect of vilazodone with 5-fluorouracil (5-FU) in HT-29 cell line.

Methods: Cell viability was tested by the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay (Mosmann, 1983). Test sample and standard drug in variable concentrations were added to the HT-29 cell lines for incubation over 24 h under ideal conditions. After washing the test and standard drug sample from the well with saline, MTT was added and incubated for 4 h. Dimethyl sulfoxide of 1 ml was added in all wells after incubation with MTT. The absorbance at 570 nm was measured with an ultraviolet - spectrophotometer.

Results: The values were tabulated, and the graph was plotted to find the IC-50 value (inhibitory concentration at 50%) which was struck at 28.5 μg/ml and12. 8 μg/ml for vilazodone hydrochloride and 5-FU, respectively.

Conclusion: The results show that vilazodone hydrochloride has good anticancer property comparable with 5-FU, which would probably play a role as a cytotoxic agent in tumor cells. The proposed mechanism of action could be by activation of caspase-3 enzyme, thereby increasing apoptosis and indicates its use in coexisting depression and colon carcinoma. Other mechanism includes suppression of oncogene p53, which can be confirmed by future studies.
DEVELOPMENT AND CHARACTERIZATION OF BIOCOMPATIBLE POLYHYDROXY BUTYRATE IMPREGNATED WITH HERBAL PLANTS AGAINST WOUND HEALING ACTIVITY ON IN VIVO ANIMAL MODEL
Authors: R RAM NARENDRAN , BEGUM SF MALEEKA , S RUBAVATHI
Published: October 2019

Objective: The current study is to evaluate the antimicrobial, antioxidant, anti-inflammatory, and in vitro cytotoxicity activities of polyhydroxybutyrate (PHB) and to develop the herbal impregnated PHB cast film for wound healing activities using Albino Wistar rat model.

Methods: PHB produced by Azotobacter chroococcum A3 strain was synthesized and characterized (previous study). The PHB was subjected to various biocompatibility studies such as antimicrobial, antioxidant, and anti-inflammatory studies. The PHB was also subjected to cytotoxicity study by (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay. PHB films were made using different combinations of plant and algal blends (herbal blends). The herbal blends of PHB films were evaluated for in vivo wound healing activity using Albino Wistar rats.

Results: The turmeric impregnated PHB showed the highest result for antimicrobial with 27.25±0.23 mm against skin pathogens and antioxidant activity with the highest percentage of inhibition of 76%. The result predicts that PHB will not let to any toxic substances rather it acts as a chemoprotective agent followed by the inhibitory concentration value was found to be 1.56 μg/ml for 100 μg. The in vivo study showed better wound healing activity for PHB blended with 2% turmeric leaf and rhizome cast film. Whereas the wound healing activity of control and crude PHB was 90.4±0.4 and 91.3±0.56 respectively.

Conclusion: The results from the present study showed that PHB can act as a good candidate for drug carrier and it is biocompatible in living cells.
DEVELOPMENT AND IN VITRO–IN VIVO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF AN ANTIRETROVIRAL AGENT RITONAVIR
Authors: KIRAN R SHIREESH , SHEKAR B CHANDRA , BABU B NAGENDRA
Published: October 2019

Objective: The present research work concerns the development of the extended release of Ritonavir floating matrix tablets, designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects of irritating drugs.

Methods: The floating tablets of Ritonavir were prepared by direct compression method using different grades of hydroxypropyl methylcellulose (HPMC), crospovidone, Polyox WSR 303, and sodium bicarbonate, as gas generating agent. Evaluation parameters and in vivo radiographic studies were conducted in suitable model.

Results: Among all formulations, F21 was chosen as optimized formulation based on evaluation parameters such as floating lag time (33 s), total floating time (>24 h), and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product were shown 98.67% and 91.46±5.02% of drug release, respectively. The main appliance of medication discharge follows zero-order kinetics and non- Fickian transport by coupled diffusion and erosion. In vivo experiments maintained the potentials in extending the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time of the optimized formulation found to be 330 min±40 in the stomach, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for enhanced bioavailability.

Conclusion: From in vitro and in vivo radiographic studies, Ritonavir floating tablets estimated to provide novel choice for harmless, inexpensive, and extended release for the effective management of AIDS.
EVALUATION OF HEMATINIC ACTIVITY OF NAGA BHASMA IN PHENYLHYDRAZINE-INDUCED ANEMIA IN EXPERIMENTAL RATS
Authors: AV YADAV , VR UNDALE
Published: October 2019

Objective: Bhasmas are biologically produced nanoparticles prescribed with several other medicines of Ayurveda. Metal-based drugs are prepared by transmutation of base metals into noble ones along with the use of plant extracts meant to eradicate the toxic effects of metal. Naga bhasma (NB) is one of such metallic preparation used in various diseases such as diarrhea, spleen enlargement, and diabetes. The present study aims to test the hematinic activity of NB against phenylhydrazine (PHZ)-induced anemia in rats.

Methods: The experiment was carried on Wistar rats of either sex (150–200 g). Anemia was induced by an oral administration of PHZ 40 mg/kg for a period of 2 days. Hemoglobin (Hb) was measured on the 3rd day. Rats with Hb <11 g/dl were selected for the study. The animals were divided into six groups containing six animals each. Group I served as normal control, Group II as anemic control, and Group III was considered as standard that received ferrous sulfate (100 mg/kg), while Groups IV, V, and VI were treated with test NB 100, 200, and 400 mg/kg, respectively, for 15 days. Hb was checked on the 0, 2nd, 7th, and 15th days.

Results: Oral administration of PHZ decreased Hb from 14 g/dl at day 0 to 11 g/dl at day 2. NB induced a significant increase in Hb concentration to 13 at the dose of 100 mg/kg p.o. after 48 h.

Conclusion: PHZ decreased Hb rate inducing anemia. NB caused an increase in the Hb values in anemic rats. Thus, it can be concluded that NB exhibits significant hematinic activity in rats.
QUANTITATIVE DETERMINATION OF CRIZOTINIB IN HUMAN PLASMA WITH HIGHPERFORMANCE LIQUID CHROMATOGRAPHY AND ULTRAVIOLET DETECTION
Authors: NALANDA REVU BABY , RAO ATLA SRINIVASA , DANNANA GOWRI SANKAR
Published: October 2019

Objective: A rapid, sensitive, selective, and reproducible reversed-phase high-performance liquid chromatographic method has been developed and validated for the determination of crizotinib (CRZ), a tyrosine kinase inhibitor for targeted therapy of anaplastic lymphoma kinase-positive non-small-cell lung cancer.
Methods: The chromatographic separation was carried out in an isocratic mode on an YMC ODS C18 column with a mobile phase consisting of methanol and water containing 0.1% orthophosphoric acid in the ratio of 50:50 v/v at a flow rate of 0.6 ml/min. The run time was maintained for 10 min and detection was monitored at 267 nm. The method involved reproducible liquid-liquid extraction of drug from human plasma using diethyl ether as extracting solvent.
Results: CRZ and internal standard retention times were 6.86 and 7.94 min, respectively. Calibration curves were linear over a concentration range of 20.41–2041.14 ng/ml with correlation coefficient 0.9994. The lower limit of quantification for CRZ in plasma was 20 ng/ml. No endogenous substances were found to interfere with the peaks of drug and internal standard. The intra- and inter-day precision was <9.0% and the accuracy ranged from 97% to 112% over the linear range. All stability studies showed that CRZ in plasma sample was stable.
Conclusion: This method was found to be simple, selective, precise, accurate, and cost-effective. Hence, the method can be successfully applied to analyze the CRZ concentration in plasma samples for pharmacokinetic and bioequivalence studies.
FORMULATION AND EVALUATION OF GEL LOADED WITH MICROSPHERES OF APREMILAST FOR TRANSDERMAL DELIVERY SYSTEM
Authors: PRIYANKA N. V. SAI , NEERAJA P. , MANGILAL T. , KUMAR M. RAVI
Published: October 2019

Objective: The main objective of the present research work was to formulate and evaluate gel loaded with microspheres of apremilast to increase bioavailability and to reduce the dosing frequency and to improve patient compliance.

Methods: Gel loaded with microspheres of apremilast was prepared by solvent evaporation method by taking different ratios of polymers. Ethyl cellulose as a polymer, dichloromethane solvent is used as drug solubility, polyvinyl alcohol as a surfactant, and sodium alginate is used as gelling agent. Prepared gel loaded with microspheres was evaluated for drug interactions by Fourier transform infrared (FTIR), differential scanning calorimetry studies, and surface morphology by scanning electron microscopy (SEM), to select effective one among all formulations. The prepared formulations (F1–F6) were evaluated for pre-formulation studies, spreadability, viscosity, pH measurement, gel strength, homogeneity, drug content, in vitro diffusion studies, drug kinetics, and finally for stability studies.

Results: Differential scanning calorimeter studies confirmed that there is no drug interaction between drug and excipients. FTIR spectroscopy studies confirmed that there is compatibility between drug and excipients. Regular and spherical shape particles with smooth surface were observed in the SEM photographs. The optimized gel loaded with microspheres of F4 formulation (drug: polymer in 1:4 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as spreadability (5.86±0.54 g.cm/s), viscosity (568 cps), pH (6.33±0.55), gel strength (38 s) and drug content (90.00±0.71%). In vitro diffusion studies have shown 80.1±1.92% drug release in 10 h. Drug kinetics follows zero order kinetics and n value was found to be 0.721. Stability studies were done for 3 months.

Conclusion: All the results show that the gel loaded with microspheres of apremilast can be effectively used for the treatment of psoriasis and psoriatic arthritis.
PROTECTIVE EFFECT OF CASSIA FISTULA EXTRACTS AGAINST ULTRAVIOLET C INJURY IN HUMAN CORNEAL EPITHELIAL CELLS
Authors: K DEEKSHA , ARUNACHALAM CYNTHIA
Published: October 2019

Objective: The objective of this study was to investigate the antioxidant activity of Indian laburnum (Cassia fistula L. [CF]) leaf extracts and their impact on ultraviolet C (UVC) radiation-induced damage on human corneal epithelial (HCE) cells.

Methods: The antioxidant activity and free radical scavenging ability of CF leaf extracts were determined by in vitro methods such as 1,1-diphenyl- 2-picrylhydrazyl radical scavenging capacity, Total antioxidant capacity (TAC), and reducing power. The total phenolic content (TPC), total flavonoid content (TFC), and preliminary phytochemical screening were done to ensure the pharmacological effects of the extracts. The UVC radiation at wavelength 254 nm was used to irradiate HCE cells and cell viability was assessed by methyl thiazolyl tetrazolium assay.

Results: Extracts at the concentration of 200 μg/ml did not affect the cell viability of HCE cells. Almost 50% cell death was observed after UVC irradiation at a dose of 200 J/m2. Both extracts showed a protective effect by increasing the cell viability of irradiated cells up to 57.28% and 62.39%. A dose-dependent increase in the TAC and reducing power of the extract was observed. The TPC in aqueous and ethanol extracts of CF leaves was 18.8 and 27.80 mg gallic acid equivalent/g sample while TFC was 8.47 and 16.5 mg quercetin equivalent per/gsample, respectively.

Conclusions: CF leaves are a potent source of bioactive compounds with good antioxidant potential. Exposure to UVC radiation cause harmful effects on HCE cells and the extracts have shown to have potent protective effects on UV light-induced oxidative stress in HCE cells.
EVALUATION OF ANTICANCER POTENTIAL OF ETHANOLIC EXTRACT OF ALANGIUM SALVIFOLIUM LEAVES IN ANIMAL MODELS
Authors: C PRATHIMA , SHASHIKUMARA SHASHIKUMARA , T THIPPESWAMY
Published: October 2019

Objective: The present study aims to evaluate the anticancer potential of ethanolic extract of Alangium salvifolium leaves (EASL) against Ehrlich ascites carcinoma (EAC) in animal model.
Methods: The ethanolic extract of A. salvifolium was prepared by continuous method using Soxhlet apparatus. Phytochemical analysis of EASL was conducted. Anticancer activity of the extract was evaluated by EAC model in Swiss albino mice. EASL was administered at the doses of 100 and 200 mg/kg body weight once a day orally for 14 days, after 24 h of tumor inoculation.
Results: A. salvifolium leaves extract treatment produced significant decrease in tumor volume and body weight, and increase in total and non-viable cell count, along with elevated life span of EAC-bearing mice. The EASL exhibited potent dose-dependent antitumor activity. Further, the altered hematological parameters such as red blood cells, hemoglobin, and white blood cells levels as well as biochemical parameters such as serum glutamic oxaloacetic transaminase, serum glutamate pyruvate transaminase, alkaline phosphatase, albumin, and total protein levels in EAC mice were significantly (p<0.05) regained following treatment with EASL. The anticancer potential of EASL can be attributed to the presence of phenols and flavonoids.
Conclusion: Results suggest that EASL possesses significant anticancer activity against EAC tumor-bearing Swiss albino mice.
EFFECT OF LIFESTYLE MODIFICATION IN TYPE II DIABETES MELLITUS INDIVIDUALS
Authors: BHOSALE AVANI , THANGAVELU POOVISHNU DEVI
Published: October 2019

Objectives: The objectives of this study were as follows: (1) To find the effect of conventional physiotherapy along with medications on Type II diabetes mellitus (DM) individuals and (2) to find the effect of lifestyle modification (LSM) and conventional physiotherapy with medications on Type II DM individuals.

Methods: Ethical clearance was obtained from the institutional ethical committee. A total of 70 Type II DM individuals were assessed and 64 were included in this study based on inclusion criteria, the individuals were allocated into two groups: Group A (n=32) received conventional physiotherapy along with prescribed diabetic medications and Group B (n=32) received LSM and conventional physiotherapy with prescribed diabetic medications. Pre- and post-test were done for plasma glucose, serum insulin, glycated hemoglobin (HbA1c), total cholesterol, triglycerides, high-density lipoprotein-C, low-density lipoprotein by blood test, exercise tolerance by 6-min walk test, and quality of life (QOL) by SF-36 questionnaire, and the outcome measures were analyzed after 3 months.

Results: Intergroup statistical analysis for HbA1c (p<0.0001) and QOL (p<0.0001) revealed extremely significant difference post-intervention. Analysis of HbA1c test for Group A (p=0.0652) was not significant and for Group B (p<0.0001) was extremely significant. Moreover, QOL was significant for Group A (p=0.0004) as well as for Group B (p<0.0001).

Conclusion: The study results concluded that LSM was significantly effective in reducing HbA1c levels, exercise tolerance, plasma glucose, serum glycerine, and total cholesterol and improving QOL compared to conventional exercise.
EFFECT OF FLAVONE AND ITS MONOHYDROXY DERIVATIVES ON ANIMAL MODELS OF DEPRESSION IN SWISS ALBINO MICE
Authors: S SHANMUGAPRIYAN , S JAIKUMAR , S VISWANATHAN , K PARIMALA , M RAJESH
Published: October 2019

Objectives: This research was designed to investigate the antidepressant activity of a few structurally related flavones (flavone, 3‑hydroxyflavone, and 7‑hydroxyflavone) and the possible mechanisms involved.

Methods: Antidepressant activity was evaluated in mice by subjecting them to forced swim test and tail suspension test. The involvement of adrenergic, serotonergic, nitric oxide (NO), and opioid mechanisms was investigated using suitable interacting chemicals.

Results: Flavone, 3‑hydroxyflavone, and 7‑hydroxyflavone exhibited a significant and dose‑dependent reduction in total time of immobility in the forced swim test and tail suspension test. Pre‑treatment with alpha‑methyl‑para‑tyrosine and parachlorophenyl alanine attenuated the reduction in immobility period produced by flavone and its derivatives in forced swim test. Naloxone pre‑treatment partially reversed the effect of flavone while L‑arginine pre‑treatment did not alter their effect.

Conclusion: The investigated flavones exhibited promising antidepressant activity in both the animal models of depression. However, the flavone compounds did not alter the motor coordination and ambulatory behavior in the Rotarod and locomotor activity test. The participation of serotonergic, adrenergic, and opioid mechanism in the antidepressant activity of these compounds was elucidated from the results, and the role of NO pathway was excluded.
CHRONIC INTERACTION BETWEEN METFORMIN AND MELOXICAM IN MICE
Authors: AL-REKABI FALAH MUOSA KADHIM
Published: October 2019

Objective: This study is performed for investigation the chronic interaction between metformin and meloxicam from toxicological view.

Methods: Lethal dose 50 after chronic exposure assessed in mice by up and down method. Their interaction analyzed by isobolographic analysis indicated that both medicines exhibited synergism. Assessment of the effects of repeated chronic dosing for 3 months of both medicines also performed on mice. Medicines in question administered orally as therapeutic doses of metformin 14 mg/kg. Body weight (BW) (G1), meloxicam 0.2 mg/kg.BW (G2), and combination of both medicines (G3) while G4 assigned control and dosed DW.

Results: Both G1 and G3 showed significant p˂0.05 decrease in blood glucose and serum cholesterol levels. Meloxicam group (G3) showed statistically significant p˂0.05 increase in triglycerides and alanine aminotransferase (ALT), and aspartate aminotransferase (AST), while group of combination showed statistically significant p≤0.05 decrease in both ALT and AST. Blood urea nitrogen, uric acid, and serum creatinine showed statistically significant p˂0.05 increase in group of meloxicam but decrease in G3 and no changes in G1. Histopathological changes included variable lesions in kidney such as swelling and necrosis in renal tubules of metformin group, cortical vacuolar degeneration in renal tubules, and deterioration of most glomeruli in G2, while G3 showed generalized cortical necrosis of renal tubules and interstitial nephritis. Liver lesions included central venous congestion (VC) and perivascular lymphocytic infiltration and marked necrosis in both groups of metformin and meloxicam, while there were severe VC and necrosis of hepatocytes in group of combination.

Conclusion: Metformin administration with meloxicam may have beneficial important through preventing many deleterious effects of meloxicam after long-standing administration, but adjusting dosing regimen study might be recommended.
PREDICTORS OF MAJOR BLEEDING AMONG ATRIAL FIBRILLATION PATIENTS ON WARFARIN
Authors: M MATALQAH LAILA , YEHYA ALAA , AL-TAANI GHAITH M
Published: October 2019

Objective: Bleeding is the most serious complication associated with anticoagulation therapy. The purpose of this study was to estimate the frequency of major bleeding related to warfarin and to identify its predictors in patients with atrial fibrillation (AF).

Methods: Patients with AF treated with warfarin at Penang General Hospital in Malaysia were identified according to the international classification of disease, Ninth Revision, Clinical Modification (ICD-9). The medical reports of 1611 patients were reviewed, bleeding events were set as primary end point which were identified in 313 patients. Demographic and clinical data were retrieved and warfarin therapy-related parameters including dose, therapy duration, and prothrombin time-international normalized ratio (PT-INR) were recorded and analyzed using descriptive statistics.

Results: Of the 313 patients, 28 patients with major bleeding events were identified. Gastrointestinal bleeding was the major type of bleeding, which accounts for 68% (n = 17) of the cases. The frequency of major bleeding events among all AF patients was 1.7%. High PT-INR value was found in 96.3% (n = 28) of the patients, thereby making it the primary predictor of bleeding events. Other predictors including, advanced age, other comorbidities such as hypertension and multiple anticoagulation therapy were also observed to be significant.

Conclusion: Lower doses of warfarin are recommended to achieve target PT-INR range similar to that reported previously for Asian populations. A regular clinical review for bleeding predictors is essential for maximizing the time spent by the patient taking warfarin in the optimal therapeutic range and for making recommended therapy adjustment.
OXIDATIVE CHANGES AND COGNITIVE FUNCTION DECLINE IN AGING RATS
Authors: FRANCIS RUDIN MUHAMMAD IRFAN NORMAN , MAKPOL SUZANA , WAN NGAH WAN ZURINAH , MOHD YUSOF YASMIN ANUM
Published: October 2019

Objective: This study aims to show that impairment of cognitive function occurred during aging is related to increased oxidative stress.

Methods: A total of 36 Sprague Dawley rats were divided into four groups: Young (3 months), middle (14 months), and old age groups (18 and 23 months). Rats were killed and blood was collected for the measurement of oxidative stress which includes deoxyribonucleic acid (DNA) damage and lipid peroxidation (malondialdehyde [MDA] levels). Cognitive function of rats was measured through open-field experiments, Morris water maze (MWM), and object identification.

Results: Increased DNA damage and MDA levels were found in middle age and old rats compared to young rats (3 months old, p<0.05). There was an increase in anxiety with age as indicated by the increased production of fecal boli and decreased activity of grooming and rearing. For the navigation test, older rats took a long time to search for the hidden platform compared to young rats. In the probe test (spatial memory test 24 h after the last training), the middle- and old-age groups spent less time at the quadrant compared to the young age group.

Conclusion: There is a decline in cognitive function with increased oxidative stress in aging rats.
SYNTHESIS OF SOME NOVEL (E)-METHYL 2,4-DIMETHYL-5-(3-OXO-3-PHENYLPROP-1-EN-1- YL)-1H-PYRROLE-3-CARBOXYLATE DERIVATIVES AS ANTIMICROBIAL AGENT
Authors: HUBLIKAR MAHESH , DIXIT PRASHANT , KADU VIKAS , SHIRAME SACHIN , RAUT DATTATRAYA , BHOSALE RAGHUNATH , `JADHAV SHRAVAN
Published: October 2019

Objective: The objective of the present study was to synthesize a series of some novel (E)-methyl 2,4-dimethyl-5-(3-oxo-3-phenylprop-1-en-1-yl)-1H-pyrrole-3-carboxylate derivatives and to evaluate it’s in vitro antimicrobial activities.

Methods: A novel series of (E)-methyl 2,4-dimethyl-5-(3-oxo-3-phenylprop-1-en-1-yl)-1H-pyrrole-3-carboxylate derivative (8a-l) has been synthesized by cyclization (Knorr reaction) hydrolysis, decarboxylation, and Vilsmeier–Haack formylation reaction. 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate 6 undergo condensation with acetophenone derivatives 7a-l in methanol and potassium hydroxide. The synthesized compounds were screened for in vitro antimicrobial screening.

Results: The structures of the synthesized compounds were characterized by infrared, 1H nuclear magnetic resonance, and mass spectroscopy. The antimicrobial activity data revealed that the synthesized derivatives possess good antibacterial and antifungal activity which is attributed due to the presence of the heterocyclic ring; further, the activity increased with the introduction of a methoxy group in the structure.

Conclusions: New pyrrole chalcone derivatives act as significant antimicrobial agents, easy work-up procedure and reaction take place with minimum side product. Antimicrobial activity report provides an interesting template for the syntheses of new antimicrobial agents and may be helpful for the design of new therapeutic tools.
ANTIOXIDANT ACTIVITY OF SOME NEWLY PREPARED SYMMETRICALLY AZO DYES DERIVED FROM SULFA DRUGS
Authors: MUHAMMAD‑ALI MUNTHER ABDULJALEEL , HAMZA SALMAN HUSSAM , JASIM EKHLASQANBER
Published: October 2019

Objective: Sulfa drugs (sulfonamides) were the first type of drugs largely medically used for preventive and chemotherapeutic agents against various types of diseases. To the date, much research has been directed toward the synthesis sulfa drug derivatives such as azo‑sulfa drug compounds. The aim of the present study is to synthesize of azo‑sulfa compounds as antioxidant agents.

Methods: First, three of sulfa drugs react with 4‑methoxy‑1,2‑Naphthoquinone in aqueous medium by stirring at room temperature to give symmetrically azo‑sulfa compounds. The colored compounds which formed were examined their structures by infrared and proton nuclear magnetic resonance spectral techniques.

Results: Three symmetrically azo‑sulfa compounds were tested as antioxidant agents compared with ascorbic acid (AA) using 2,2‑diphenyl‑1‑picrylhydrazyl method. The results indicated that these compounds had good activities (57.79–73.69%) at 30 μg/ml, which had less activity than AA (81.34%) at the same concentration. These results referred the IC50 which had values (15.23–21.35 μg/ml), whereas AA had 7.59 μg/ml.

Conclusion: Attachment of heterocyclic rings containing nitrogen and oxygen (isoxazole) on the azo‑sulfa compounds can enhance the antioxidant activity as compared with the heterocyclic rings containing nitrogen only (pyrimidine) and without heterocyclic rings, which enhanced the lipophilicity which may increase the bioavailability and efficacy of the drug.
2441 INTERLEUKIN-1B AND CYCLOOXYGENASE-2 PROINFLAMMATION ANALYSIS AND IN SILICO DOCKING NUCLEAR FACTOR KAPPA B ON ENDOMETRIOSIS CELL CULTURE GIVEN HEPTYL GALLATE AND OCTYL GALLATE TREATMENT
Authors: BUSTAMI ARLENI , SULISTYA UTAMI FAJAR , BUDIARTI RAHMI , WIBOWO HERI
Published: October 2019

Objective: The aim of this study is to analyze the effect of octyl gallate and heptyl gallate toward the regulation of interleukin-1β and cyclooxygenase (COX)-2 proinflammatory factor on endometriosis cell culture and analyze its activity toward nuclear factor kappa B (NFkB) target protein through in silico docking technique.

Methods: In vitro study was performed on endometriosis cells cultured treated with two dosages each of heptyl and octyl gallate (51.2 μg/mL and 102.4 μg/mL) for 48 h, then followed by 10 ng/mL lipopolysaccharides (LPS) induction for 24 h. The positive control group was treated by LPS induced and the negative control was treated without LPS. Inflammation regulation was evaluated with enzyme-linked immunosorbent assay technique and in silico docking analyzed using bioinformatics technique.

Results: Molecular docking analysis with gallic acid and their derivatives showed that more stable affinity and stronger binding found on octyl gallate than heptyl gallate and gallic acid at the active site of NFkB.

Conclusions: Based on this study results, octyl gallate and heptyl gallate were proven to be able to reduce COX-2 proinflammatory factor through NFkB pathway as an inflammatory regulator; thus, it has the potential to be developed as a therapy for endometriosis.
DEVELOPMENT AND IN VITRO EVALUATION OF SOLID DISPERSIONS OF CANDESARTAN CILEXETIL
Authors: D.v.r.n. Bhikshapathi
Published: October 2019

Objective

The main objective of the present study is systematic development of solid dispersions of Candesartan cilexetil by solvent evaporation method to enhance the solubility and bioavailability.

Methods

In the present study, eighteen formulations of solid dispersions were prepared with 1:1 and 1:3 ratios of drug: carrier and with and without surfactant. There was significant improvement in the rate of drug release from all 20 solid dispersions and the formulation (SD16) comprising Candesartan: containing Soluplus (1:3 ratio of drug:Â  Soluplus with 2% SLS as surfactant) by solvent evaporation process.

Results

Final optimized design SD16 contained maximum drug content of 99.08%. In in vitro dissolution studies it shows greater dissolution rate i.e. 99.7Â±4.2% associated through additional designs and pure drug. The drug was compatible with all the excipients as per FTIR (Fourier transform infrared spectroscopy). From powder X-ray diffraction (p-XRD) and by (SEM) studies it was evident that crystalline form of Candesartan has been converted into amorphous form within solid dispersion design. 

Conclusion

From these studies we can accomplish solid dispersions are one of the greatest favorable formulation for Candesartan cilexetil for enhancing the solubility and bioavailability of poorly water soluble drugs in the effective group of hypertension and other cardiac problems.
PROTECTIVE EFFECT OF ZILEUTON AND MK-866 AGAINST HEPATIC DAMAGE INDUCED BY DOXORUBICIN
Authors: H SAHIB HUSSAM , M SULTAN AHMED , A SAHEB HUSSEIN
Published: October 2019

Objective: The present study was designed to investigate the protective effect of Zileuton and MK-886 against hepatic damage induced by doxorubicin.

Methods: A total of 30 healthy adult male albino rats were randomized and rats were divided into five groups, six animals in each: Control negative group, Vehicle group: Rats were given ethanol i.p., Dx group: Doxorubicin (15 mg/kg), Mk group: Mk-886-treated rats given 0.6 mg/kg of Mk-886 i.p, and Z group: Zileuton-treated rats given zileuton 10 mg/kg i.p. Biochemical tests of the serum for ASAT and ALAT level were estimated. Serum glutathione (GSH) concentrations (μg/ml) were determined using GSH ELISA Kit, while serum malondialdehyde (MDA) concentrations (ng/ml) were determined using MDA ELISA Kit. Livers were removed from each rat and fixed in 10% neutral-buffered formalin and embedded in paraffin for histopathological studies.

Results: MK- and zileuton-treated groups showed higher GSH levels and lower MDA levels as compared with Dx-treated group. MK-886 associated with significant p<0.05 decreased the liver enzymes in comparison with doxorubicin-treated rats. Zileuton showed insignificant (p>0.05) changes. The liver tissues that treated with Dx only showed several histopathological changes such as moderate sinusoidal dilation, vacuolation, mild-to-moderate hepatocyte necrosis/degeneration and inflammatory cell infiltration, and severe congestion. Liver tissues that treated by zileuton with Dx showed sinusoidal dilation, vacuolation, mild congestion, and inflammatory cell infiltration, while those treated with Mk-886 plus Dx showed nearly normal liver pathophysiology.

Conclusion: It has been concluded that Zileuton and MK-886 have protective effects against hepatic damage induced by doxorubicin.
STANDARDIZED SUPERCRITICAL CO2 EXTRACT OF ACANTHUS ILICIFOLIUS (LINN.) LEAVES INHIBITS THE PRO-INFLAMMATORY CYTOKINE TUMOR NECROSIS FACTOR-Α IN LIPOPOLYSACCHARIDE-ACTIVATED MURINE RAW 264.7 MACROPHAGE CELLS
Authors: THIRUGANASAMBANTHAM RAMANATHAN
Published: October 2019

Objective: Acanthus ilicifolius Linn. (Acanthaceae) is a medicinal mangrove plant used in the treatment of inflammation. Previous phytochemical studies have identified 2-benzoxazolinone (BOA) from the leaves of A. ilicifolius. In the present study, we attempted to standardize the supercritical CO2 leaf extract of A. ilicifolius (SCFE-AI) for BOA content and investigate the tumor necrosis factor-α (TNF-α) inhibitory effect of SCFE-AI and BOA on the lipopolysaccharide (LPS)-induced inflammation in RAW 264.7 macrophages. The acute oral toxicity of SCFE-AI and BOA was also established. Methods: SCFE-AI was standardized for BOA content using high-performance thin-layer chromatography (HPTLC) method. The cytotoxicity of SCFEAI and BOA was evaluated using MTS colorimetric method. The in vitro anti-inflammatory effect of SCFE-AI and BOA on TNF-α production in LPSactivated RAW 264.7 cells was quantified using ELISA method. Acute oral toxicity studies were performed following the Organization for Economic Co-operation and Development test guideline No. 423. Results: The amount of BOA was found 0.8% w/w of SCFE-AI. The RAW 264.7 cell viability was unaffected by SCFE-AI and BOA treatments within a concentration range <1000 mg/ml after 24 h incubation. SCFE-AI decreased the production of TNF-α in a dose-dependent manner compared to BOA. The LD50 value for SCFE-AI was found to be >2000 mg/kg and ranges from 300 to 2000 mg/kg with BOA. Conclusion: The HPTLC chromatogram could serve as an analytical tool for authentication and quantification of BOA content. The anti-inflammatory mechanism of A. ilicifolius might be through the inhibition of TNF-α production.
Reconfiguración de un territorio hidrosocial tras la construcción de la presa El Cajón, en Nayarit
Authors: Pelayo Pérez Mariana Betzabeth , Gasca Zamora José
Published: October 2019

El objetivo de este trabajo es analizar cómo la construcción de la presa El Cajón, ubicada sobre el río Santiago, en Nayarit, generó cambios físico-ambientales que modificaron las formas y medios de vida de una comunidad. El estudio se sustenta en investigación documental, recolección de información directa en campo mediante el método etnográfico, y análisis de las variables cualitativas. Se aportan evidencias de los cambios socioambientales, las tensiones y los conflictos que experimentan los actores de las comunidades contiguas y externas después de la construcción de grandes obras de infraestructura. La investigación es relevante porque el enfoque de territorios hidrosociales utilizado permitió entender la reconfiguración del territorio hídrico, y reveló cambios productivos y conflictos surgidos tras una competencia exacerbada por los recursos de la pesca comercial. Se concluye que es necesario reformular las intervenciones gubernamentales compulsivas que desatan este tipo de procesos, que incluyen las evaluaciones previas y los mecanismos de restitución y compensación social.
Platón, Einstein y el triunfo de la imaginatividad cosmológica
Authors: Robinson T. M.
Published: October 2019

This article argues the following five claims: 1. Plato’s description of the origins of cosmos in the Timaeus is not a myth, nor something unlikely: when he called it an eikos mythos or eikos logos, he meant a likely or trustworthy account on this very subject. 2. Among the details in this account, the following are prominent and surprising: a) the world was fashioned in time, in that precise point that was the beginning of time; b) several kinds of duration can be distinguished in cosmology (mainly eternity, sempiternity, perpetuity and time); and c) space is an entity characterized by movement and tension. 3. In the Statesman, Plato repeats much the same thing, adding this time the strange notion that the universe’s circular movement is periodically reversed. 4. In spite of the important differences in detail, there is a striking similarity between Plato’s account of the origins of the world and the explanation adopted by much of modern cosmology. 5. What Plato shares with so many instances of recent thought is here termed “cosmological imaginativity”. A first section of the paper deals exclusively with the Timaeus. Claims 1 and 2a are supported by a revision of the meanings of mythos and logos, followed by brief reference and discussion of the argument at Timaeus 27d, leading to the conclusion that Plato affirms that the ever-changing world has indeed had a beginning in time. Claim 2b describes five different types of duration, corresponding to Forms, the Demiurge, Space, the [empirical] world and its contents, physical objects. The second section is concerned with the myth in the Statesman, discussing it as a parallel and describing its peculiar turn to the Timaeus’ cosmology and cosmogony, a complex spheric and dynamic model. After digressing into some important ideas in modern cosmology, touching especially on affinities of some of Einstein’s ideas with of Plato’s own, the paper closes with a discussion of cosmological imaginativity, oriented to recover and recognize fully Plato’s greatness as a cosmologist.
Dos fragmentos de Heráclito acerca de psyche y logos
Authors: Hülsz Piccone Enrique Adolfo
Published: October 2019

This is a brief survey and interpretation of the text of the only two Heraclitean fragments that connect explicitly psyche and logos, B45 and B115. Introductory pages deal with the traditional significance of the word psyche, and the meaning and philosophical importance of the complex term of logos, which appears in several other genuine texts. Part I is concerned with B45: “If you go to the soul’s limits, you wouldn’t find them, even if you traveled every path: so deep is its logos”. It is mainly an exploration of its many different resonances and its paradoxical rationality. The focal points of attention are the ideas of “limits” and “searching”, which are then linked to mortality. The second section includes a brief discussion on B36 and concludes that its relevance to the interpretation of B45 is questionable and unclear. The third section tries to recover the general outlines of Heraclitus conception of the [human] soul as the home of knowledge and speech (as a quick glimpse of B107 reveals [“Eyes and ears are bad witnesses for those who have barbarous souls”]), which strongly suggests the idea of self-knowledge as the background of B45. The last section deals with the more difficult B115 (“It belongs to the soul a logos that increases itself”), recognizing first the problem of authenticity, and especially the objection of inconsistency between the idea of a logos that “increases itself” and Heraclitus’ theory of “measures”, venturing a conjectural interpretation that draws attention to the main, common point of both fragments: the inner character of logos, its immanence in psyche, and its most suggestive implication, an idea of self-consciousness, a fundamental philosophical notion that could be thus much more ancient than what is usually thought.
La otredad: ¿real o inventada? El caso de las brujas
Authors: Nathan Bravo Elia
Published: October 2019

The purpose of this paper is two-fold. On the one hand, it offers a general analysis of stigmas (a person has one when, in virtue of its belonging to a certain group, such as that of women, homosexuals, etc., he or she is subjugated or persecuted). On the other hand, I argue that stigmas are “invented”. More precisely, I claim that they are not descriptive of real inequalities. Rather, they are socially created, or invented in a lax sense, in so far as the real differences to which they refer are socially valued or construed as negative, and used to justify social inequalities (that is, the placing of a person in the lower positions within an economic, cultural, etc., hierarchy), or persecutions. Finally, I argue that in some cases, such as that of the witch persecution of the early modern times, we find the extreme situation in which a stigma was invented in the strict sense of the word, that is, it does not have any empirical content.
Metafísica y política en El nacimiento de la tragedia
Authors: Esteban Enguita José Emilio
Published: October 2019

This text aims at throwing light on the political thought which is implicit in The Birth of the Tragedy, and in the Posthumous Writings. Although politics appears not to be important in a work on aesthetics and metaphysics, the author shows that tragic experience is intimately related with the need for a tragic state. The ecstasies of the Dionysian experience form the ethos of the citizen, and nourish the political institutions which, in their turn, allow the artistic liberation of Dionysian forces. Furthermore, the author shows that, to Nietzsche, Euripides represents not only the decadence of tragedy, but also the destruction of the Greek polis and the transformation of the citizen in a mediocre bourgeois. Politics is certainly not the base of existence, but is a mere normativity which changes with aesthetic conceptions. Nevertheless, in his view of politics, Nietzsche responds to the question concerning the value of politics and, accordingly, responds to the essential question of all political philosophy.