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Research in Pharmaceutical Sciences

Zohreh Hosseinkhani, Mona Sadeghalvad, Fathemeh Norooznezhad, Reza Khodarahmi, Mohammad Fazilati, Azadeh Mahnam, Ali Fattahi, Kamran Mansouri
Polymorphism in the genes encoding CYP2C9 enzyme and VKORC1 reductase significantly influence warfarin dose requirement since patients with CYP2C9*2 , CYP2C9*3 and VKORC1 mutant alleles require lower warfarin maintenance doses. Studies have reported the ethnic variations in the frequency of these genes within the various populations in Iran and other parts of the world. However, no such study has been done yet on Kurdish population in Kermanshah. From Kurdish population of Kermanshah province in Iran, a total of 110 patients who had heart surgery and taking warfarin, were genotyped for polymorphisms of VKORC1-1639 G>A , CYP2C9*2 , and CYP2C9*3 ...
August 2018: Research in Pharmaceutical Sciences
Amir Nili-Ahmadabadi, Fahimeh Ali-Heidar, Akram Ranjbar, Leila Mousavi, Davoud Ahmadimoghaddam, Amir Larki-Harchegani, Abolfazl Ghafouri-Khosrowshahi
Oxidative stress (OS) is a main mechanism in organophosphorus poisoning. The effects of calcium channel blockers have been confirmed in decreasing of oxidative stress. In the current study, the effects of amlodipine (AM), as a calcium channel blocker, were evaluated on oxidative damages induced by diazinon (DZN) in hippocampus tissue of Wistar rats. Forty-two rats were divided into six groups and treated intraperitoneally for two weeks. Group 1 served as control received vehicle, group 2 was treated with 9 mg/kg of AM, group 3 (positive control) received DZN (32 mg/kg), Groups 4, 5, and 6 were treated with 3, 6, and 9 mg/kg of AM adjunct with DZN (32 mg/kg), respectively...
August 2018: Research in Pharmaceutical Sciences
Zahra Haghighijoo, Zahra Rezaei, Mansooreh Jaberipoor, Samaneh Taheri, Meysam Jani, Soghra Khabnadideh
Quinazoline is one of the most widespread scaffolds amongst natural and synthetic bioactive compounds. Recently the quinazoline derivatives and in particular the 4-anilinoquinazolines have attracted much attention for their anticancer properties due to their capability to stabilize the kinase activity of epidermal growth factor receptor (EGFR). A series of fifteen previously designed and synthesized 4-anilinoquinazoline analogs (4-18) were evaluated for cytotoxic activity on two breast cancer cell lines (MCF-7 and MDA-MB-468)...
August 2018: Research in Pharmaceutical Sciences
Azam Fatahi, Ilnaz Rahimmanesh, Mina Mirian, Fattah Rohani, Maryam Boshtam, Azam Gheibi, Laleh Shariati, Hossein Khanahmad, Shirin Kouhpayeh
Blockade of α4 integrin by antibodies could be an appropriate treatment strategy in multiple sclerosis and Crohn's disease. Considering disadvantages of antibodies, other elements (e.g. aptamers) have been proposed for antibodies replacement. Isolation of aptamers through cell-SELEX (systematic evolution of ligands by exponential enrichment) method requires positive and negative expressing α4 integrin cell lines. For a better isolation, we intended to construct a negative cell line lacking of specific ligand binding site of α4 integrin...
August 2018: Research in Pharmaceutical Sciences
Mozhdeh Iranmanesh, Reza Mohebbati, Fatemeh Forouzanfar, Mostafa Karimi Roshan, Ahmad Ghorbani, Mohammad Jalili Nik, Mohammad Soukhtanloo
The role of angiogenesis in tumor progression and metastasis formation has been well recognized. Recent studies have reported that Trigonella foenum-graecum L. (fenugreek) seed extracts have potential anticancer properties. The current study was planned to investigate the anti-angiogenic activity of hydroalcoholic extract of fenugreek (HAEF) in vitro and in vivo . Effect of HAEF (50-3000 µg/mL) and thalidomide (200-3000 µmol/L), as a positive control, on the viability of human umbilical vein endothelial cells (HUVECs) and 3T3 fibroblast cells was assessed by thiazolyl blue tetrazolium bromide (MTT) assay...
August 2018: Research in Pharmaceutical Sciences
Elham Jafari, Ali Gheysarzadeh, Karim Mahnam, Rezvan Shahmohammadi, Amir Ansari, Hadi Bakhtyari, Mohammad Reza Mofid
Insulin-like growth factor binding protein-3 (IGFBP-3) is a vital protein exist in circulation which interacts with high affinity to insulin-like growth factor (IGFs) altering their activities. Therefore, the interaction between IGFs and IGFBP-3 has a key role altering large spectrum of activities such as cell cycle progression, proliferation and apoptosis. Despite decades of research, the crystal structure of IGFBP-3 has not been identified possibly due to some technical challenge in its crystallizing. The three-dimensional (3D) structure of IGFBP-3 was predicted using homology modeling, Phyre2, and molecular dynamic...
August 2018: Research in Pharmaceutical Sciences
Mozafar Khazaei, Mona Pazhouhi
Natural plants have traditionally been used throughout the world for their anti-diabetic effects. The aim of the present study was to investigate the protective effect of hydroalcoholic extract of Trifolium pratens L . ( T. pratense ) on streptozotocin (STZ) cytotoxicity and insulin concentration from RIN-5F pancreatic β cell line. In this study, possible cytoprotective action of T. pratense extract (using pre-treatment, simultaneous, and post-treatment schedules) against STZ (30 mM) was evaluated using MTT assay...
August 2018: Research in Pharmaceutical Sciences
Iman Fatemi, Morteza Amirteimoury, Ali Shamsizadeh, Ayat Kaeidi
Opiate tolerance and dependence is a worldwide public health problem and gives a significant burden to society. The aim of this study was to evaluate the effects of metformin (MET) on development and expression of morphine tolerance and dependence in rats. For induction of tolerance, morphine sulfate was injected (10 mg/kg, twice a day, s.c.) for 7 days. Animals received metformin (5 and 50 mg/kg, orally, daily) during the examination period for assessing the development of morphine tolerance and dependence...
August 2018: Research in Pharmaceutical Sciences
Nooshin Bijari, Sajad Moradi, Sirous Ghobadi, Mohsen Shahlaei
Human serum albumin (HSA) is the most abundant protein found in human blood and is extensively employed in clinical applications such as hypovolemic shock treatment. Also, there has been a lot of attempt to use HSA as a carrier to deliver various drugs to their specific targets. Thus, clarify of structure, dynamics, functions, and features of HSA-drug complexes play an important role from the viewpoint of pharmaceutical and/or biochemical sciences. In this study, the interaction of letrozole, as a non-steroidal aromatase inhibitor, with HSA has been studied by combining different techniques such as UV-Vis, fluorescence spectroscopy, and computational methods...
August 2018: Research in Pharmaceutical Sciences
Parisa Ghasemiyeh, Soliman Mohammadi-Samani
During the recent years, more attentions have been focused on lipid base drug delivery system to overcome some limitations of conventional formulations. Among these delivery systems solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are promising delivery systems due to the ease of manufacturing processes, scale up capability, biocompatibility, and also biodegradability of formulation constituents and many other advantages which could be related to specific route of administration or nature of the materials are to be loaded to these delivery systems...
August 2018: Research in Pharmaceutical Sciences
Shadi Farshbaf Khalili, Saeed Ghanbarzadeh, Ali Nokhodchi, Hamed Hamishehkar
In the process of quality control of pulmonary drug delivery products, aerosolization efficiency is mainly determined using impactors, e.g. next generation impactor (NGI). However, particle bounce may interfere with the validity and accuracy of results due to the overestimation of the respirable fraction. It is suggested that the coating of impactor's stages may prevent the particle bounce. Therefore, coating materials may influence the results of the aerosolization indexes of pulmonary dosage forms. The aim of this study was to investigate if the aerosolization indices are affected differently by using the different coating materials...
June 2018: Research in Pharmaceutical Sciences
Laleh Maleknia, Mandana Dilamian, Mohammad Kazemi Pilehrood, Hojjat Sadeghi-Aliabadi, Amir Houshang Hekmati
In this paper, polyurethane (PU), chitosan (Cs)/polyethylene oxide (PEO), and core-shell PU/Cs nanofibers were produced at the optimal processing conditions using electrospinning technique. Several methods including SEM, TEM, FTIR, XRD, DSC, TGA and image analysis were utilized to characterize these nanofibrous structures. SEM images exhibited that the core-shell PU/Cs nanofibers were spun without any structural imperfections at the optimized processing conditions. TEM image confirmed the PU/Cs core-shell nanofibers were formed apparently...
June 2018: Research in Pharmaceutical Sciences
Marzieh Rahmani Khajouei, Ahmad Mohammadi-Farani, Aref Moradi, Alireza Aliabadi
Due to resistance of some epileptic patients to the current medications and the general incidence of severe side effects of these drugs, development and discovery of novel antiepileptic drugs is crucial. Isatin-based derivatives are promising compounds as antiepileptic agents. In this study a new series of isatin-containing derivatives were synthesized via the imine formation between isatin and p -aminobenzoic acid. Subsequently, the obtained acidic compound was utilized to prepare the final amidic derivatives ( 4a-4l ) through the reaction with various aniline derivatives...
June 2018: Research in Pharmaceutical Sciences
Mahboobeh Raeiszadeh, Abbas Pardakhty, Fariba Sharififar, Alireza Farsinejad, Mehrnaz Mehrabani, Hossein Hosseini-Nave, Mitra Mehrabani
Myrtus communis (myrtle) is well known for its therapeutic effects pertaining to the major secondary metabolites including essential oils (EOs). EOs are composed of volatile compounds and simply evaporate or decompose leading to their instability. Preparation of EOs niosomal formulation may be a promising approach to deal with these obstacles. Niosomal formulations of myrtle essential oil (nMEO) were provided using non-ionic surfactants and cholesterol (Chol). In the next steps, vesicle size, zeta potential, percentage of entrapment efficiency (EE%) and physical stability of nMEO were investigated...
June 2018: Research in Pharmaceutical Sciences
Amir Hossein Doustimotlagh, Ahmad Reza Dehpour, Shahroo Etemad-Moghadam, Mojgan Alaeddini, Sattar Ostadhadi, Abolfazl Golestani
Chronic liver disease (CLD) affects millions of people and its impact on bone loss has become a subject of interest. Nitric oxide and endogenous opioids are suggested to increase during cholestasis/cirrhosis and may impact bone resorption by different mechanisms. The receptor activator of nuclear factor-κB (RANK)/RANK-ligand (RANKL)/osteoprotegerin (OPG) signaling pathway regulates bone resorption, but its role in metabolic bone disease subsequent to CLD is unknown. We aimed to investigate the involvement of nitrergic and opioidergic systems in bone loss relative to the RANK/RANKL/OPG pathway, in bile duct-ligated (BDL) rats...
June 2018: Research in Pharmaceutical Sciences
Saeed Azadi, Seyed Kazem Sadjady, Seyed Alireza Mortazavi, Nasser Naghdi, Arash Mahboubi, Roya Solaimanian
The methylotrophic yeast Pichia pastoris is a well-established expression host, which is often used in the production of protein pharmaceuticals. This work aimed to evaluate the effect of various concentrations of ascorbic acid in mixed feeding strategy with sorbitol/methanol on productivity of recombinant human growth hormone (r-hGH). The relevant concentration of ascorbic acid (5, 10, or 20 mmol) and 50 g/L sorbitol were added in batch-wise mode to the medium at the beginning of induction phase. The rate of methanol addition was increased stepwise during the first 12 h of production and then kept constant...
June 2018: Research in Pharmaceutical Sciences
Rezvan Rezaee Nasab, Mahboubeh Mansourian, Farshid Hassanzadeh
The quinazolin-4(3H)-one structural motif possesses a wide spectrum of biological activities. DNA gyrase play an important role in induction of bacterial death. It has been shown that many quinazolin-4(3H)-one derivatives have antibacterial effects through inhibition of DNA gyrase. Based on this information we decided to synthesize novel quinazolinone Schiff base derivatives in order to evaluate their antibacterial effects. A series of novel quinazolinone Schiff base derivatives were designed and synthesized from benzoic acid...
June 2018: Research in Pharmaceutical Sciences
Atousa Bonyani, Seyed Ebrahim Sajjadi, Mohammad Rabbani
Lippia citriodora is commonly used in Iranian folk medicine for treatment of many disorders. Since there scientific data to prove the anxiolytic properties of this plant in Iran are scarce, we aimed to evaluate the sedative and anxiolytic activity of the leaf extract and essence of L. citriodora in an animal model of anxiety. The extract and the essence used were obtained after maceration and hydro-distillation of the leaves of L. citriodora , respectively. We evaluated the anti-anxiety profile and sedative activity of diazepam (1 mg/kg i...
June 2018: Research in Pharmaceutical Sciences
Behnam Rasti, Yeganeh Entezari Heravi
Isoform diversity, critical physiological roles and involvement in major diseases/disorders such as glaucoma, epilepsy, Alzheimer's disease, obesity, and cancers have made carbonic anhydrase (CA), one of the most interesting case studies in the field of computer aided drug design. Since applying non-selective inhibitors can result in major side effects, there have been considerable efforts so far to achieve selective inhibitors for different isoforms of CA. Using proteochemometrics approach, the chemical interaction space governed by a group of 4-amino-substituted benzenesulfonamides and human CAs has been explored in the present study...
June 2018: Research in Pharmaceutical Sciences
Mahboubeh Rezazadeh, Vajihe Akbari, Elham Amuaghae, Jaber Emami
In the current study, we aimed to develop a novel injectable thermosensitive hydrogel for simultaneous intra-tumoral administration of paclitaxel (PTX) and doxorubicin hydrochloride (DOX). At first, mixed micelles composed of Pluronic F127 and α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was loaded with PTX and their physicochemical properties including particle size, zeta potential, drug loading content, entrapment efficiency, and the drug release were investigated in details. In the second step, the optimized PTX-loaded micelles prepared in the first step were incorporated into the thermosensitive Pluronic F127/hyaluronic acid (PF127/HA) hydrogel containing fixed amount of DOX...
June 2018: Research in Pharmaceutical Sciences
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