Open Access Original Research Article

Comparison of the Effects of Ropivacaine and Bupivacaine on Human Umblical Artery Vasoreactivity

Kayacan Nurten, Dalaklioğlu Selvinaz, Bigat Zekiye, Karsli Bilge, Tasatargil Arda

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2017/32591

The primary aim of the current study was to examine the effect of ropivacaine and bupivacaine on human umblical artery reactivity and on clinical outcomes. Neither bupivacaine nor ropivacaine produce a significant effect on the maternal systolic blood pressure and heart rate during operation. However, ropivacaine and bupivacaine were used by addition of increasing concentrations of agonist (0.2-8 microg/ml) to the baths in a cumulative manner and the isometric tension devoloped by the tissue. In organ bath studies, bupivacaine caused a significant relaxation response in human umblical artery rings precontracted with either KCl or 5-hydroxytriptamine. Conversely, ropivacaine did not induce a relaxation response in umblical vessels which have been previously induced to contract by an activator.  In conclusion, the results of this study have shown that bupivacaine, but not ropivacaine, may cause a significant effect on human umblical vessel tonus.

Open Access Original Research Article

Isolation and Characterization of β-Sitosterol-3-O-β-D-glucoside from the Extract of the Flowers of Viola odorata

Tania Peshin, H. K. Kar

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2017/33160

Isolation from the ethanol extract of the flowers of Viola odorata resulted in the isolation of β-Sitosterol-β-D-glucoside. This compound has not been previously isolated or reported from the flowers of this variety. The isolated β-Sitosterol-3-O-β-D-glucosidewas characterized on the basis of spectroscopic techniques viz. infrared and nuclear magnetic resonance spectroscopy. A tetra acetyl derivative of β-Sitosterol-3-O-β-D-glucoside was synthesized and characterized. On hydrolysis of β-Sitosterol-β-D-glucoside, β-sitosterol was obtained and characterized.

Open Access Original Research Article

Antiangiogenic and Apoptotic Effects of Oleuropein on Breast Cancer Cells

Recep Liman, Funda Karabağ Çoban, Ibrahim Hakkı Ciğerci, İbrahim Bulduk, Selahattin Bozkurt

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2017/33403

Oleuropein is a fundamental polyphenol contained in olive fruit, oil, and leaf, with a bitter taste. A decrease in its level is observed as the fruit ripens. Leaves of oil tree were used in this study as a possible origin of oleuropein. In this study, cytotoxic, genotoxic, apoptotic and antiangiogenic impacts of isolated oleuropein (0.5xIC50, IC50 and 2xIC50) on MCF-7 human breast adenocarcinoma cells were examined by means of 3-[4,5- Dimethylthiazol-2-yl] 1-2,5-diphenyltetrazolium bromide (XTT) kit, Comet assay, Poly (ADP-Ribose) Polymerase (PARP) cleavage ELISA Kit and Vascular Endothelial Growth Factor (VEGF) Human ELISA Kit for 24, 48 and 72 h, respectively. The IC50 value of oleuropein on MCF-7 cells was found to be 11.02±0.52, 9.43±0.41 and 6.81±0.18 µg/mL for 24, 48 and 72 h, respectively. The time and concentration-related cytotoxic impacts of oleuropein were determined to be significant. Cleaved PARP level was significantly increased especially with an increase in the concentration of oleuropein. However, a significant decrease in VEGF level was observed (p<0.05). Furthermore, oleuropein increased damage on DNA for 48 and 72 h. Findings showed oleuropein as a potential antiangiogenic, apoptotic and genotoxic agent for the breast cancer cells.

Open Access Original Research Article

Pyrimethamine Based Anti-protozoan Agents from Isostere and Heuristic Structure-similarity Search

Ronald Bartzatt

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2017/33205

Aims: To generate new medicaments for control and treatment of the parasitic protozoan Toxoplasma gondii.

Study Design: Structure similarity search and isostere search was conducted over a broad range of structure categories. Correlation and highest similarity scores were implemented to select the best drug candidates.

Place and Duration of Study: University of Nebraska, Department of Chemistry, Durham Science Center, 6001 Dodge Street, Omaha Nebraska 68182, from June 2016 to February 2017.

Methodology: Utilizing pyrimethamine as the parent compound, a broad range of similar structures and isosteres were found by applying search methods. The compounds having the highest correlation and similarity scores were selected for the study of molecular properties. The molecular properties were determined and examined for underlying relationships by pattern recognition hierarchical cluster analysis and K-means cluster analysis.

Results: Thirty compounds were identified to have a very high level of structure similarity or isosteric relationship to pyrimethamine. The molecular structures and molecular properties are presented for all compounds, inclusive of pyrimethamine. Hierarchical cluster analysis and K-means cluster analysis indicated compounds with highest underlying similarity to pyrimethamine. Box plots showed the over-all distribution of important pharmaceutical properties, such as molecular weight, Log P, polar surface area, number of rotatable bonds, molecular volume, and number of hydrogen bond donors. Structure components are compared to elucidate potential clinical activity. Multiple regression is applied on all compounds to generate a numerical relationship for prediction of similar compounds. Save for only one isostere, all compounds showed zero violations of the Rule of 5, indicating favorable drug-likeness and bioavailability.

Conclusion: Thirty compounds highly analogous to pyrimethamine were identified following heuristic search course. The molecular properties were determined for all compounds and indicated genuine potential for treatment of toxoplasmosis. Correlation of structure and pattern recognition methods indicated 30 compounds of clinical potential and property analogy to pyrimethamine.

Open Access Original Research Article

Effect of Vitamin D Supplementation in Patients of Moderate Asthma Undergoing Treatment with Inhaled Corticosteroids

Rajendra Sharma, Sanjeev Kumar, D. C. Dhasmana, Juhi Kalra

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2017/32843

Background: Vitamin D is an essential nutrient with significant immunomodulatory effects. There is potential for a protective role of vitamin D against etiopathogenesis of asthma and morbidity. This study evaluated the effect of vitamin D supplementation in patients with moderate asthma.

Aims and Objectives: To evaluate the effect of vitamin D supplementation on lung function improvement in patients of moderate asthma undergoing treatment with inhaled corticosteroids.

Materials and Methods: An interventional prospective study. A total of 60 patients of moderate asthma were enrolled in the study and randomly divided into two groups of 30 patients each. Group A: placed on steroid based treatment regimen (formoterol 6 µg + budesonide 200 µg) + Vitamin D supplementation [60,000IU/week for 8 consecutive weeks]. Group B: placed on steroid based treatment regimen (formoterol 6 µg + budesonide 200 µg) only, as control. The enrolled patients were followed up for 12 weeks and assessed for various parameters of disease severity, asthma control and improvement in lung function by using asthma control test [ACT] questionnaire and Pulmonary function tests (spirometry). Collected data was analyzed using available statistical software [spss ver 20.0].

Results: Statistically significant changes (P<0.001) were seen in pre to post values of FEV1 [2.28±0.41 to 2.64±0.51], FVC [3.37±0.74 to 3.60±0.76] and FEV1/FVC ratio [68.44±5.03 to 73.48±3.52] in Group A as well as in Group B i.e. FEV1 [2.28±0.48 to 2.64±0.52], FVC [3.35±0.67 to 3.58±0.75] and FEV1/FVC ratio [67.87±2.48 to 74.16±4.19]. However there were no significant differences observed in pre and post values of FEV1, FVC and FEV1/FVC ratio in between the two groups.

Conclusion: Vitamin D supplementation failed to show additional benefits in lung function improvement in adults with moderate asthma undergoing treatment with inhaled corticosteroids in the present study.