Isfahan Pharmaceutical science Research Center

Eşfahān, Iran

Isfahan Pharmaceutical science Research Center

Eşfahān, Iran
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Varshosaz J.,Isfahan University of Medical Sciences | Minayian M.,Isfahan Pharmaceutical science Research Center | Moazen E.,Isfahan University of Medical Sciences
Journal of Liposome Research | Year: 2010

Pentoxifylline (PTX) is a highly water-soluble, hemorheologic drug that undergoes first-pass effect with 20% bioavailability. The solid lipid nanoparticles (SLNs) of PTX were prepared to enhance its oral bioavailability by homogenization, followed by the sonification method. Seven different variables, each at two levels, were studied: lipid type, surfactant type and concentration, speed of homogenizer, acetone:dichloromethane (DCM) ratio, lecithin:lipid ratio, and sonication time. The mean particle size and size distribution, drug entrapment efficiency (EE%), zeta potential, and drug release of the SLNs were investigated. A pharmacokinetic study was conducted in male Wistar rats after oral administration of 10mg kg -1 PTX in the form of free drug or SLNs. The z-average particle size, zeta potential, and EE% of the SLNs were at least 250nm,-30.2 mV, and 70%, respectively. Among the studied factors, the lipid type, surfactant type, and percentage had a significant effect on the particle size. Zeta potential was more affected by lipid type, acetone:DCM ratio, and sonication time. Speed of homogenizer and acetone:DCM ratio had a significant effect on the EE%. The optimized SLN was prepared by 80mg of cetyl alcohol, 10mg of lecithin, acetone:DCM ratio (1:2), 30-second sonication, 3% Tween 20, and a mixing rate of 800rpm. In vitro drug release lasted for about 5 hours. It was found that the relative bioavailability of PTX in SLNs was significantly increased, compared to that of the PTX solution. SLNs offer a promising approach to improve the oral bioavailability of PTX that is affected by a high first-pass effect. © 2010 Informa UK Ltd.


Minaiyan M.,Isfahan University of Medical Sciences | Ghannadi A.,Isfahan University of Medical Sciences | Etemad M.,Isfahan Pharmaceutical science Research Center | Mahzouni P.,Isfahan University of Medical Sciences
Research in Pharmaceutical Sciences | Year: 2012

Cydonia oblonga Miller (Quince) from Rosaceae family is a fruit tree cultivated in many countries mainly in Iran. This study was carried out to investigate the effect of quince juice (QJ) and quince hydroalcoholic extract (QHE) on ulcerative colitis (UC) induced by TNBS (trinitrobenzene sulfonic acid) in rats. Rats were grouped (n=6) and fasted for 36 h before colitis induction. TNBS was instilled into the colon with a hydroalcoholic carrier and then treatments were made for 5 days starting 6 h after colitis induction with different doses of QJ (200, 400, 800 mg/kg), QHE (200, 500 & 800 mg/kg) orally, QJ (400 mg/kg) and QHE (200 and 500 mg/kg) intraperitoneally. The colon tissue was removed and tissue damages were scored after macroscopic and histopathologic assessments. Albeit the examined doses of QJ and QHE were apparently effective to reduce the extent of UC lesions, only the greatest doses (500 and 800 mg/kg) resulted in significant alleviation. Weight/Length ratio as an illustrative of tissue inflammation and extravasation was also diminished with quince treatments while the results correlated with macroscopic and histopathologic evaluations. These data suggest that QJ and QHE were effective to diminish inflammation and ulcer indices in this murine model of acute colitis. Although QHE with different doses was effective in induced colitis, the dose and/or route of administration dependency was not confirmed. So quince fractions could be considered as a suitable anticolitic alternative, however further studies are needed to support this hypothesis for clinical setting.


Hajhashemi V.,Isfahan Pharmaceutical science Research Center | Minaiyan M.,Isfahan Pharmaceutical science Research Center | Movahedian A.,Isfahan University of Medical Sciences | Talebi A.,Isfahan University of Medical Sciences
Inflammation Research | Year: 2010

Objective: To explore the site of action of maprotiline, as an atypical antidepressant, on carrageenan-induced paw edema. Subjects Male Wistar rats were used. Methods: Firstly, the anti-inflammatory effect of systemic maprotiline (12.5, 25 and 50 mg kg-1) was assessed using a paw edema model. Secondly, different doses of maprotiline were administrated intracerebroventricularly, intrathecally and locally before carrageenan challenge. Finally, we tried to reverse the anti-inflammatory effect of maprotiline by propranolol (10 mg kg-1), prazosin (4 mg kg -1), yohimbine (10 mg kg-1), naloxone (4 mg kg -1) and mifepristone (5 mg kg-1). Results Systemic, intracerebroventricular and subplantar application of maprotiline significantly inhibited peripheral edema, but intrathecal maprotiline did not alter the degree of paw swelling. The applied antagonists failed to change the anti-inflammatory activity of maprotiline. Conclusion These results demonstrate that maprotiline has a potent anti-inflammatory effect and this effect is linked to the peripheral and supraspinal actions of the drug. © Springer Basel AG 2010.


Azemikhah M.,Islamic Azad University at Tehran | Ashtiani H.A.,Islamic Azad University at Tehran | Aghaei M.,Isfahan Pharmaceutical science Research Center
Research in Pharmaceutical Sciences | Year: 2015

Discoidin domain receptor (DDR) is a new member of the receptor tyrosine kinase family. There are two isoforms of discoidin domain receptor (DDR), DDR1 and DDR2. These receptors play a major role in the adhesion, motility and cell proliferation. Due to the important role of DDR2 in the development of tumor extension, this receptor is pivotal in the field of carcinogenesis. The aim of this study was to investigate the mRNA and protein expression of DDR2, in the malignant, benign prostatic hyperplasia (BPH) and normal tissues of patients with prostate cancer. In this study the gene and protein expression of DDR2 in adjacent normal (n=40), BPH (n=40), and malignant (n=40) prostate tissue were measured using real-time PCR and Western blotting. Then, the correlation of DDR2 gene and protein expression with prognostic factors such as age, tumor grade, tumor stage, lymph node involvement, and serum prostate-specific antigen (PSA) concentration were evaluated. The relative mRNA and protein expression level of DDR2 in malignant and benign prostate tissue was significantly higher than those of adjacent normal tissues (P0.01). This expression was found to increase approximately 3.5 and 2.1 fold for mRNA and protein levels, respectively. Spearman test indicated a significant correlation between DDR2 mRNA and protein expression with prognostic factors such as tumor grade, stage, lymph node involvement, and serum PSA concentration. However, significant correlation with age was not observed. These findings suggest that DDR2 is a cancerrelated gene associated with the aggressive progression of prostate cancer patients.


Shahlaei M.,Kermanshah University of Medical Sciences | Shahlaei M.,Isfahan University of Medical Sciences | Sabet R.,Isfahan University of Medical Sciences | Ziari M.B.,Islamic Azad University at Shahreza | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2010

Quantitative relationships between molecular structure and methionine aminopeptidase-2 inhibitory activity of a series of cytotoxic anthranilic acid sulfonamide derivatives were discovered. We have demonstrated the detailed application of two efficient nonlinear methods for evaluation of quantitative structure-activity relationships of the studied compounds. Components produced by principal component analysis as input of developed nonlinear models were used. The performance of the developed models namely PC-GRNN and PC-LS-SVM were tested by several validation methods. The resulted PC-LS-SVM model had a high statistical quality (R 2=0.91 and R CV 2=0.81) for predicting the cytotoxic activity of the compounds. Comparison between predictability of PC-GRNN and PC-LS-SVM indicates that later method has higher ability to predict the activity of the studied molecules. © 2010 Elsevier Masson SAS. All rights reserved.


Shahlaei M.,Kermanshah University of Medical Sciences | Shahlaei M.,Isfahan University of Medical Sciences | Madadkar-Sobhani A.,Barcelona Supercomputing Center | Saghaie L.,Isfahan University of Medical Sciences | And 3 more authors.
Expert Systems with Applications | Year: 2012

One strategy to potentially improve the success of drug design and development is to use chemometrics methods early in the process to propose molecules and scaffolds with ideal binding and to clarify physicochemical features influencing in their activity. Adaptive Neuro-Fuzzy Interference System (ANFIS) was used to construct the nonlinear quantitative structure-activity relationship (QSAR) model. The Genetic Algorithm (GA) was used to select descriptors which are responsible for the cathepsin K inhibitory activity of studied compounds. ANFIS regression is a nonlinear regression technique developed to relate many regressors to one or several response variables. The accuracy of the generated QSAR model (R 2 = 0.916) is described using various evaluation techniques, such as leave-one-out procedure (RLOO2=0.875) and validation through an external test set (Rpred2=0.932). © 2011 Elsevier Ltd. All rights reserved.


Sabet R.,Isfahan University of Medical Sciences | Mohammadpour M.,Isfahan University of Medical Sciences | Sadeghi A.,Isfahan University of Medical Sciences | Fassihi A.,Isfahan University of Medical Sciences | Fassihi A.,Isfahan Pharmaceutical science Research Center
European Journal of Medicinal Chemistry | Year: 2010

Quantitative structure activity relationships (QSAR) of anti-cancer isatin derivatives were discovered by multiple linear regressions (MLR) and genetic algorithm partial least squares (GA-PLS) methods. Topological, chemical, geometrical and functional groups descriptors were found to be effective parameters on the cytotoxic activity. The positive effects of the number of halogen atoms and the number of total secondary carbons, and the negative effects of the number of secondary amides, and the number of ketones on the anti-cancer activity were in agreement with previous SAR studies. Hansch analysis showed the importance of lipophilic R3 and R5 substituents. Between MLR and GA-PLS, MLR represented superior results with a high statistical quality (R2 = 0.92 and Q2 = 0.90) for predicting the activity of the compounds. © 2009 Elsevier Masson SAS. All rights reserved.


Razavi A.E.,Isfahan Pharmaceutical science Research Center | Ani M.,Isfahan Pharmaceutical science Research Center | Pourfarzam M.,Isfahan Pharmaceutical science Research Center | Naderi G.A.,Isfahan University of Medical Sciences
Journal of Research in Medical Sciences | Year: 2012

Background: High density lipoprotein (HDL) particles are heterogeneous in composition, structure, size, and may differ in conferring protection against cardiovascular disease. HDL associated enzyme, paraoxonase-1 (PON1), has an important role in attenuation of atherogenic low density lipoprotein (LDL) oxidation. The aim of this study was to investigate the associations between HDL particle size and PON1 activity in relation to serum HDL cholesterol (HDL-C) levels. Materials And Methods: One hundred and forty healthy subjects contributed to this study. HDL was separated by sequential ultracentrifugation and its size was estimated by dynamic light scattering. Paraoxonase activity was measured spectrophotometrically using paraoxon as substrate. Results: Results of this study showed that PON1 activity had negative correlations with HDL mean particle size (r = -0.22, P < 01), HDL2/HDL3 ratio, and serum HDL-C levels (r = -0.25, P < 0.01). HDL mean particle size and HDL2/HDL3 ratio had negative correlation with body mass index (BMI), waist hip ratio (WHR), and serum triglyceride (TG) levels, and positive correlation with serum HDL-C levels. Serum HDL-C levels had significant positive correlations with age, total cholesterol (TC), and apolipoprotein A-I (apo A-I) and significant negative correlation with BMI, WHR, and TG. Conclusion: Based on the results of this study, determination of HDL mean particle size beside the serum PON1 activity may help to better understand the CAD risks, pathogenesis, and prognosis, and may also help to design therapeutic protocols toward beneficial modifications of HDL characteristics.


Shahlaei M.,Isfahan University of Medical Sciences | Shahlaei M.,Kermanshah University of Medical Sciences | Fassihi A.,Isfahan University of Medical Sciences | Fassihi A.,Isfahan Pharmaceutical science Research Center | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2010

Principal component regression (PCR), principal component-artificial neural network (PC-ANN), and principal component-least squares-support vector machine (PC-LS-SVM) as regression methods were investigated for building quantitative structure-activity relationships for the prediction of inhibitory activity of some CCR1 antagonists. Nonlinear methods (PC-ANN and PC-LS-SVM) were better than the PCR method considerably in the goodness of fit and predictivity parameters and other criteria for evaluation of the proposed model. These results reflect a nonlinear relationship between the principal components obtained from molecular descriptors and the inhibitory activity of this set of molecules. The maximum variance in activity of the molecules, in PCR method was 45.5%, whereas nonlinear methods, PC-ANN and PC-LS-SVM, could explain more than 93.7% and 95.6% variance in activity data respectively. © 2010 Elsevier Masson SAS. All rights reserved.


Minaiyan M.,Isfahan University of Medical Sciences | Ghannadi A.,Isfahan University of Medical Sciences | Ghannadi A.,Isfahan Pharmaceutical science Research Center | Mahzouni P.,Isfahan University of Medical Sciences | Jaffari-Shirazi E.,Isfahan Pharmaceutical science Research Center
Iranian Journal of Pharmaceutical Research | Year: 2011

Antioxidant and immunomodulatory effects of anthocyanins are abundant in berberry fruits suggesting that they may have beneficial effects on inflammatory bowel diseases (IBD). The present study was carried out to investigate the anti-colitic effect of Berberis vulgaris fruit extract (BFE) compared to berberine chloride (BEC) and corticosteroids using an animal model of acetic acid induced experimental colitis. BFE with three different doses (375, 750, and 1500 mg/Kg) was administered orally or rectally prior to ulcer induction. BEC (10 mg/Kg), prednisolone (5 mg/Kg), hydrocortisone acetate enema (20 mg/Kg) and normal saline (5 mL/Kg) were considered as respective controls. The tissue was assessed macroscopically for damage scores, area, index and weight/length ratio. They were also examined histopathologically for inflammation extent and severity, crypt damage, invasion involvement and total colitis index. Results indicated that greater doses of oral BFE (750, 1500 mg/Kg) as well as BEC (10 mg/Kg) were effective to protect against colonic damage. By rectal pretreatment, the extract was only effective to diminish the ulcer index and the efficacy was not significant for mucosal inflammation parameters. In conclusion BFE, which is nearly devoid of berberine, was effective to protect against colitis and this might be attributed to its anthocyanin constituents. © 2011 by School of Pharmacy.

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