Open Access Commentary

X-ray Crystal Structure of COX-2 Enzyme as a Tool to Predict Active Sites of Bitter Taste Receptors

Rafik Karaman, Gennaro Mecca, Salma Jumaa

Journal of Pharmaceutical Research International, Page 1-5
DOI: 10.9734/BJPR/2016/28169

This commentary discusses a novel approach to be used in the design of active sites of bitter taste receptors, especially TAS2R14, by using the X-ray crystal structure of the enzyme COX-2 and chemical structures of commonly used non-steroidal anti-inflammatory drugs (NSAIDs) that bind effectively to COX enzymes and activate the bitter taste receptor TAS2R14. The suggested approach consists of docking calculations of the NSAIDs (ligands) to the active site of COX-2 and utilizing the data obtained in better understanding the nature of the interactions between bitter tastants and the chemical groups within the active site of TAS2R14 receptor.

Open Access Original Research Article

Evaluation of Antioxidant and Antiacne Activity of Psorospermum febrifugum (Spach) and Psorospermum corymbiferum (Hochr.)

Taiwo O. Elufioye, Mary O. Bamgbose, Samuel O. Alabi

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/27984

Aim: This study investigated the anti-acne activity, lipase inhibitory effects and antioxidant property of Psorospermum febrifugum and Psorospermum corymbiferum of the family Hypericaceae.

Study Design: Antimicrobial as well as in vitro anti lipase and antioxidant analysis of extracts and fractions of P. febrifugum and P. corymbiferum.

Place and Duration of Study: Faculty of Pharmacy, University of Ibadan, Nigeria between 2014 and 2015.

Methodology: Preliminary antimicrobial assay of the plant extracts was by agar-well diffusion and minimum inhibitory concentration was determined by agar dilution method. The radical scavenging property was determined using DPPH method and the lipase inhibitory assay of the most potent crude extract was done by direct in vitro measurement of lipase inhibition.

Results: Methanolic crude extracts showed antimicrobial activity against Staphylococcus aureus, Staphylococcus epidermidis and Propionibacterium acne with zones of inhibition ranging from 17.00±0.00 to 30.33±1.67. The MIC for the crude extracts was 50, 25, 12.5 and 6.25 mg/mL for P. febrifugum leaf, P. corymbiferum stem, P. corymbiferum leaf and P. febrifugum stem extracts respectively. The IC50 values for P. febrifugum leaf and stem, P. corymbiferum leaf and stem extracts were 0.06, 0.02, 0.12 and 0.04 respectively. At same concentration, the anti-lipase inhibitory activity was higher for P. febrifugum (96%) than Orlistat (82%).

Conclusion: The result confirmed the anti-acne and antioxidant activities of the two plants.

Open Access Original Research Article

Review of Traditionally Used Medicinal Plants by the Kipsigis Community in Kenya

Kemboi Douglas

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/28341

Background: Every community in Kenya have their own ways of providing good health care services for its members. Such services are geared towards providing therapeutic and medical related services for the upkeep of good health and also prevention and treatment of infections. Much before the dawn of modern medicine through sophisticated researches and advances, these societies developed their indigenous medicinal system through interaction with their environment.

Aim: This paper, through secondary literature reviews and survey was aimed at examining the features of commonly used herbal medicine from plants by the Kipsigis community in Kenya.

Place and Duration: The research was carried out at University of Kabianga from January to December 2015.

Methodology: Semi structured interviews, group discussions and observations were used to collect information on traditional knowledge from herbalists. Details of the medical conditions treated, herbal preparations used, treatment methods, local plant names and methods of collection of herbs were recorded. The research team comprised of professionals from the fields of medicine and botany. Local leaders, community elders, church leaders and other stakeholders were used to identify herbalists and convince them to provide information.

Results: The result of this survey revealed that majority of the household, even in urban places; use these commonly available herbs and plants for minor aliments in their families for immediate relief. The study provides information on medicinal and healing methods used by the Kipsigis community. It also revealed that traditional medicines are still widely used in Kericho County. Some of the identified plants have been demonstrated to possess pharmacological activities related to those mentioned by the herbalists.

Conclusion: From the findings it can be concluded that use of traditional herbs as medicine is still common amongst the Kipsigis community but faces numerous challenges and weaknesses. Thus much detailed scientific study on these medicinal plants need to be conducted to ascertain the compounds responsible for such relief.

Open Access Original Research Article

Three Triterpenoids from the Leaf Extract of Vitex doniana (Verbenaceae)

M. Mohammed, A. Danmallam, U. M. Jajere, M. T. Kolo, A. Abubakar, J. M. Babakano

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/24335

Three triterpeniods were isolated from the leaf extract of Vitex doniana (Verbenaceae). Their structures were established mainly by FTIR, FABMS,  highresolution(1Dand 2D) spectroscopic and chemical analysis as 1α, 3β-dihydroxybauer-7-en-28 oicacid(1), 2β, 3β, 19α, 24-tetrahydroxy-23-norus- 12-en- 28-oic acid(2) and (3β, 5a, 7β)-3,7-dihydroxy-4, 4, 14-trimethyl-11, 15-dioxochol-8-en-24-oic acid (3).

Open Access Original Research Article

Effect of Solvent and Crystallization Method on Physicochemical Properties of Aceclofenac and Fenofibrate

Sachinkumar Patil, Shitalkumar Patil, Sachin Navale

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/28489

Aims: Aim of this study was to prepare Aceclofenac and Fenofibrate crystals by cooling crystallization and non-cooling crystallization methods using various solvents. Also to study the effect of crystallization conditions, method of crystallization and type of solvents on physicochemical properties of drug crystals.

Study Design:  By Crystallization method using various solvents.

Place and Duration of Study: The study was performed in Department of Pharmaceutics, Ashokrao Mane College of Pharmacy, Peth-Vadagoan, Tal. Hatkanangale, Dist. Kolhapur, Maharashtra, India-416112 and the duration was two years.

Methodology: Study was performed by cooling crystallization and non-cooling crystallization methods using various solvents like Ethanol, Methanol, Dioxane, Ethyl acetate, Tetrahydrofuran, Butanol, Dichloromethane, Cyclohexane, Hexane and 2- Propanol.

Results: Aceclofenac and Fenofibrate crystals were successfully prepared by cooling crystallization and non-cooling crystallization methods using various solvents. Obtained crystals have shown different particle size and crystal habit with change in method and solvent along with enhanced solubility and dissolution rate. FTIR, DSC and XRD study has indicated no any chemical modification in the drug during process.

Conclusion: Prepared crystals have improved particle size along with enhanced solubility and dissolution than pure drug has signified the commercial applicability of the method in manufacturing the solid dosage forms. Thus optimizing crystallization method in conjunction with appropriate solvent can produce crystals with expected properties for manufacturing ease in pharmaceutical industry.

Open Access Original Research Article

Clinical Outcome Evaluation of Glycaemic Control in a Metformin-based Therapy of Type 2 Diabetes Mellitus Patients Managed Under Ambulatory Care Settings

John David Ohieku, Joy Bitrus Musa, Onoja Ameh

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28232

Background: Short term clinical outcomes evaluation of glycaemic goals or its control are desirable to monitor response to therapy in individual patients and to identify compliance or other problem areas.

Aim and Objectives: The objectives of this study are to determine the levels of glycaemic control between clinic visits, determine changes in diabetes status during consecutive clinic visits and to evaluate the degree of decrease or otherwise in fasting blood sugar of patients.

Results: The fasting blood sugar (FBS) during consecutive clinic visits showed hypoglycaemia increased from 1.0% during the first visit to 3.3% during the fifth visit. Normal glycaemic levels increased from 15.0% during first clinic visits to 23.3% at fifth visits. About 18.2% of the FBS were maintained at impaired glucose concentration range. The proportion of patients whose FBS was in the diabetic range decrease progressively (P<0.05) from 72.0% during the first visit to 50.0% at the fifth visit. The distributions in glycaemic levels during the entire periods are hypoglycaemia (1.4%), normal range (19.4%), impaired glucose concentration (18.2%) and diabetic range (61.4%). In 98 (24.0%) cases, the changes which occurred was from higher diabetic range to lower diabetic range with mean change of 14.12±4.84 to 10.28±3.13 mMol/L. Other changes are from diabetic range to impaired glucose concentration range with mean change of 10.47±3.07 to 6.55±2.98 mMol/L(P<0.01); diabetic range to normal range (mean change from 9.98±3.10 to 4.96±0.61 mMol/L; P<0.01) and from impaired glucose concentration to normal range (mean FBS change from 6.31±0.43 to 4.75±0.74 mMol/L; P<0.01). Changes involving increase in FBS occurs from normal range to diabetic range (4.60±0.66 to 10.76±3.71 mMol/L; P<0.01), impaired glucose concentration to diabetic range (6.43±0.36 to 9.87±2.95 mMol/L; P<0.01) and diabetic range to higher diabetic value (11.66±3.73 to 14.66±5.03 mMol/L; P<0.01).

Conclusion: Most patients recorded decrease in FBS over values recorded in their previous clinic visits but these changes do not translate to good glycaemic control. Several patients experiences poor glycaemic control probably as a result of non-compliance. Multiple clinic visits also do not translate to the desired glycaemic control.

Open Access Original Research Article

Effects of Achyranthes aspera to the Immunity of Rohu (Labeo rohita) against Pseudomonas fluorescens

Md. Hasan-Uj-Jaman, Md. Mer Mosharraf Hossain, Shoumo Khondoker, Md. Eftakher Alam, Md. Farid Uz Zaman, Sanjoy Banerjee Bappa

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28110

Aims: The present study evaluated the efficacy of Achyranthes aspera extract on immunological parameters and disease resistance against Pseudomonas fluorescens infection in Indian major carp, Rohu, Labeo rohita.

Study Design: One hundred and eighty (180) fish with average weight (28.1±1.2 g) were acclimatized and stocked in (6) indoor aquariums (100 L) for three days.

Place and Duration of Study: This experiment was performed in the Laboratory of Fisheries and Marine Bioscience (FMB) and Department of Microbiology, Jessore University of Science and Technology (JUST), on November to April 2014-2015.

Methodology: Fish and management, A. aspera extract preparation, herbal diet preparation with four (4) different doses 0%, 2%, 4% and 6% of A. aspera extract, nonspecific immune response assay, blood and serum collection for hematology and immunology, phagocytic activity and challenges test were performed.

Results: Among the entire dose the 6% doses of A. aspera showed highest significant responses in phagocytic activity, specific and non-specific immune responses on week 4 compared to control diet whereas the changes did not manifest on first week. Further the A. aspera enriched diet at 6% level resulted in lowest mortality (20%) indicating highest protection (relative percent survival 80%) from Pseudomonas fluorescens infection than 0%, 2% and 4% doses t that resulted 73.33%, 46.67% and 33.33% mortalities respectively.

Conclusion: The results are suggested that the dietary supplementation of Achyranthes aspera extract acts as immunostimulants, reduce mortality and increase disease resistance in Labeo rohita against Pseudomonas fluorescens infection.