Open Access Short Research Article

Single-species Allometric Scaling: A Strategic Approach to Support Drug Discovery

Dipal Patel, Elizabeth Dierks

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/JPRI/2018/41693

Aims: Multi-species Allometric Scaling (MSS) from at least three species have been used traditionally to predict human CL and Vss. Single-species Scaling (SSS) can be applied to predict these parameters from a single species using a fixed body weight exponent. SSS is less time- and resource-intense compared to MSS and thus appears to be a very promising method to implement in a screening strategy during the drug discovery phase.

Study Design:  To evaluate SSS predictivity compared to MSS, six discovery compounds were evaluated in pharmacokinetic studies with the intravenous administration to rat, rabbit, dog, and/or cynomolgus monkey. Human CL and Vss were predicted by MSS and SSS, applying protein binding correction. Relative fold difference between these two methods was calculated to define success rate as a percent of the predictions of SSS within two- to four-fold of MSS predictions.

Results: SSS showed a high success rate for human CL prediction with 67% within 2-fold and 94% within 4-fold of MSS. The success rate of human Vss prediction by SSS was also good with 61% within 2-fold and 89% within 4-fold of MSS.

Conclusion: These data demonstrate the potential application of SSS to streamline the screening strategy of drug discovery programs.

Open Access Original Research Article

Antioxidant Activity of Polyphenolic Leaf Extract from Santolina chamaecyparissus L. (Asteraceae) and the Isolated Luteolin-7-O-Glucoside

Chahra Boudoukha, Hamama Bouriche, Mahfuz Elmastas, Huseyin Aksit, Omer Kayir, Nusret Genc, Abderrahmane Senator

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/JPRI/2018/40726

Aim: The present study aimed to investigate the chemical constituents and antioxidant potential of Santolina chamaecyparissus polyphenolic extract (SCPE).

Materials and Methods: The extract containing phenolic compounds, was extracted with ethyl acetate and luteolin-7-O-glucoside was separated and purified using flash chromatography on silica gel column. This isolated compound was identified according to its physicochemical properties and spectral data (UV, LC–TOF-MS, 1H NMR, 13C NMR and 2D NMR). In vitro antioxidant activity of the isolated compound and SCPE was investigated using DPPH•, ABTS+, reducing power, superoxide anion radical scavenging and β-carotene bleaching assays.

Results: Results showed that SCPE and luteolin-7-O-glucoside exhibited significant antioxidant activity. The antioxidant activity of SCPE was comparable to that of luteolin-7-O-glucoside. Luteolin-7-O-glucoside was isolated for the first time from Santolina chamaecyparissus polyphenolic extract.

Conclusion: Results of the present investigation clearly indicate that SCPE and isolated compound (luteolin-7-O-glucoside) have powerful antioxidant capacity against various antioxidant systems in vitro

Open Access Original Research Article

Nutritive and Biological Value of Liver and Blood of Various Slaughtered Animals

Aitbek Kakimov, Anuarbek Suychinov, Aleksandr Tsoy, Nurlan Mustambayev, Nadir Ibragimov, Nazira Kuderinova, Gulmira Mirasheva, Zhanibek Yessimbekov

Journal of Pharmaceutical Research International, Page 1-5
DOI: 10.9734/JPRI/2018/41448

Offal, such as liver, heart, tongue, kidneys, blood, skin, bone, etc., represents an essential source of protein, vitamin and mineral elements. The present study is an attempt at determining the amino acid composition of horse and beef liver and blood.  In general, horse liver was to be a good source of protein (25.06%) compared with beef liver (17.4%). The moisture (74.9%) and fat (3.8) contents were significantly higher (p<0.05) in beef liver, while the ash content of the horse liver was 1.42% compared to 1.30% in beef liver. Total essential amino acid content was higher in beef liver (40.63%) than in horse liver (37.31%).

Open Access Original Research Article

The Prevalence of Asthma and Related Risk Factors in 20-44 Years Old Population in the Kurdistan Provine-Iran, 2014-2015

Rasoul Nasiri Kalmarzi, Mehrnoosh Ataee, Ebrahim Ghaderi, Sairan Nili, Pedram Ataee, Wesam Kooti, Zeinab Kavyani

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/JPRI/2018/38645

Problem Consideration: Asthma has been the most common respiratory disease in human societies in recent decades that lead to frequent coughing, wheezing and shortness of breath. This study was conducted to assess the prevalence of bronchial asthma among 20 to 44 years population at the Kurdistan province-Iran during 2014-2015.

Materials and Methods: In this cross-sectional study (cross-analysis), 489 cases were selected randomly.  Data were collected by directly questioning the statistical units (samples) through interviews. After entering data to SPSS software, comparison of the asthma prevalence in different groups and determination of the relationship between the variables of asthma symptoms was carried out.

Results: The results showed that the asthma prevalence was 5.2% and 15.0% of patients had wheezing during the last 12 months, and 7.6% have been diagnosed with asthma in the last 12 months. Statistically, significant relationship was observed between asthma symptoms and body mass index, contact with animals, hay fever and gastro-esophageal reflux (P <0.05). Hay fever had a significant association with animals contact (P <0.05).

Conclusion:  Determining the risk factors associated with asthma symptoms can be effective in prevention and treatment of the disease.

Open Access Original Research Article

Binding of Procaine Hydrochloride to Hydrocarbon and Fluorocarbon Surfactants: The Role of Hydrophobicity

Sinem Göktürk, Sinem Bektaş

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/JPRI/2018/41732

Aims: The interaction of procaine hydrochloride (PC.HCl) with sodium dodecyl sulfate (anionic hydrocarbon surfactant; SDS), Tween 20 (nonionic hydrocarbon surfactant), cetyltrimethyl ammonium bromide (cationic hydrocarbon surfactant; CTAB), lauryl sulphate betaine (amphoteric hydrocarbon surfactant; LSB) and Zonyl-FSN100 (non-ionic fluorocarbon surfactant; Zonyl FSN) has been aimed to study by UV-vis spectrophotometry.

Methodology: Interactions with a fixed concentration of PC.HCl in the wide concentration range of Tween 20, Zonyl FSN, SDS, CTAB and LSB were studied spectrophotometrically at 298 K. Binding constants of PC.HCl to micelles was determined by using the Benesi-Hildebrand Equation.

Results: Comparison of the binding constants (KB) showed that the most binding tendency of PC.HCl to micelles in case of Zonyl FSN. Due to the electrostatic repulsion between cationic CTAB and cationic PC.HCl the binding constant could not be calculated. The effect of Zonyl FSN on the binding of PC.HCl to hydrocarbon micelles has been also studied in the presence of fixed micelle concentration of Zonyl FSN. The binding tendency has been found to be related to the hydrophobicity of the medium.

Conclusion: Interactions between different surfactants and amphiphilic drug PC.HCl showed that binding tendency of PC.HCl followed the order as; Zonyl FSN > Tween 20 > SDS > CTAB > LSB and presence of Zonyl FSN micelles increased incorporation of PC.HCl to all types of micelles.