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2014| January-June | Volume 3 | Issue 1
Online since
January 9, 2018
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RESEARCH ARTICLES
Formulation and evaluation of orally disintegrating tablets of captopril using natural super disintegrants
Mohammad Ali Shahtalebi, Majid Tabbakhian, Navid Sarbolookzadeh Harandi
January-June 2014, 3(1):54-64
Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and children. Orally Disintegrating tablets constitute an innovative dosage form that overcomes the problems of swallowing and provides a quicksetof action. The purpose of this study was to formulate and evaluate an orally Disintegrating Tablet (ODT) containing captopril while using croscarmellose sodium, crospovidone and two natural superdisintegrants: karaya gum and natural agar. For the preliminary study 12 batches were prepared. A 3
2
full factorial design was applied to optimize the formulation and 9 batches were prepared and evaluated. From the preliminary study it was found that ODTs containing karaya gum showed a better disintegration time and hence it was considered for further studies. According to the Results of optimized batches, the best concentration of superdisintegrant and binder were obtained. Karaya gum in the concentration of 9% w/w with Avicel PH 102 in25% w/w gave rapid disintegration in 25sec and showed 100% drug release within 5 minuteso it was concluded that orally disintegrating tablets of captopril can be successfully formulated using karaya gum.
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A novel, efficient, fast and inexpensive DNA extraction protocol from whole blood applicable for studying drug-DNA interaction
Mohammad Taher Moradi, Kheirollah Yari, Reza Khodarahmi
January-June 2014, 3(1):80-84
The DNA molecule has been known to be the cellular target for many cytotoxic anticancer agents for several decades. Understanding how drug molecules interact with DNA has become an active research area in the interface between chemistry, molecular biology and medicine. DNA extraction has been suggested as a main step affecting molecular DNA technology such as PCR and PCR-based methods. Therefore, researchers have used several modified protocols for efficient DNA extraction from whole blood. In this study, we focused on a fast and reliable protocol with inexpensive and non-poisonous reagents for DNA extraction from whole blood. Current method was optimized based on a combination of conventional salting-out and boiling methods. Also the quality and quantity of the extracted DNA were surveyed by gel electrophoresis and Nanodrop spectrophotometry methods, respectively. Results showed that high quantity and quality of isolated DNA by this method is enough to do hundreds of PCR-based reactions and also to be utilized in other DNA manipulation assay such as restriction digestion, drug- DNA interaction and methylation detection survey. In conclusion, we described a fast, low-cost, non-toxic and enzyme free protocol for high yield genomic DNA extraction from whole blood.
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Antimicrobial potential of root, stalk and leaves extracts of
Rheum Ribes
Reza Kazemi Darsanaki, Maryam Parsa Lisar
January-June 2014, 3(1):10-13
Plants, as sources of medicinal compounds have continued to play a dominant role in the maintenance of human health since ancient times.
Rheum ribesis
from
Polygonaceae
family which is endemic to Iran and a few neighboring countries. In this investigation, antimicrobial effects of root, stalk and leaves methanol extracts of
R. ribes
against
Staphylococcusaureus
,
Escherichia coli
,
Klebsiellapneumoniae
,
Pseudomonas aeruginosa
,
Shigellaflexneri
were studied, using well diffusion method. Methanol extracts obtained from root, stalk and leaves of
R. ribes
exhibited antimicrobial activity against test micro-organisms.
R. ribes
extracts were found to be more active against
S. flexneri and K. pneumonia
withinhibitory, 13.75 and 13.5 mm. The results suggested that extracts of
R. ribes
could be effectively used against diseases caused by selected human pathogens.
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An electrochemical senor for determination of amlodipine besylate based on graphene–chitosan nanocomposite film modified glassy carbon electrode and application in biological and pharmaceutical samples
Elham Arkan, Ziba Karimi, Mojtaba Shamsipur, Reza Saber
January-June 2014, 3(1):99-107
The graphene–chitosan composite film modified glassy carbon electrode was fabricated and used to determine amlodipine besylate. In 0.1 M pH 7.3 phosphate buffer solutions, the redox peak currents of amlodipine besylate increased significantly at graphene–chitosan composite film modified glassy carbon electrode compared with bare electrode and chitosan modified glassy carbon electrode, indicating that graphene possessed electrocatalytic activity towards amlodipine. The experimental conditions were optimized and the oxidation mechanism was discussed. Under the optimal experimental conditions, the oxidation peak current was proportional to amlodipine concentration in the range from to 1-70 μM with the correlation coefficient of 0.9930. The detection limit was 0.6 μM (S/N=3). Using the proposed method, amlodipine was successfully determined in serum sample, tablets and urine, suggesting that this method can be applied to determine amlodipine in pharmaceuticals.
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Aqueous extract of
Lavandula Angustifolia
alter protein expression in alzheimer rats
Masoud Soheili, Mahmoud Salami, Amirhossein Haghir, Hakimeh Zali, Mostafa Rezaei Tavirani
January-June 2014, 3(1):1-9
Alzheimer's disease (AD) is a progressive and socio-economical form of dementia. The currently available drugs are only able to delay the symptom progression of the disease. This study tries to evaluate protein profile of the effects of aqueous extract of lavender (
Lavandula angustifolia
) on spatial performance of AD rats. Male Wistar rats were divided into control and Alzheimeric groups (CO and ALZ respectively). Rat model of AD was established by intracerebroventricular injection of 10 mg Aβ 1-42 twenty days prior to administration of the lavender extract. All of the groups were introduced to task learning in Morris water maze (MWM). After the first stage of spatial learning, control and Alzheimeric animals received 200 mg/kg of the lavender extract (CE200 and AE200 respectively) for 20 days. After the second stage of MWM, Hippocampus tissues of four groups were separated and protein profile was determined by 2DE. By using progenesis same spot software totally 950 spots were detected in 4 gel groups. Injection of amyloid beta suppresses expression of 111 proteins. Progressive Effects of lavender extract on spatial memory and maze learning task can be clear by finding difference gene expression in both ALZ and AE200 groups. Comparison between CO and CE200 groups show 80 new proteins that expressed and 104 protein that suppressed in CE200. These findings can disclose the efficiency of lavender on improving memory and learning. Applying more proteomics techniques to better understanding of protein changes can lead to the development of new drug treatments for dementia.
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Hepatoprotective effects of pentoxifylline against acrolein-induced mitochondrial dysfunction in rat liver
Jamshid Karimi, Akram Ranjbar, Heidar Tavilani
January-June 2014, 3(1):19-27
Acrolein (ACR) is α, β unsaturated aldehyde that exists extensively in the environment and (thermally processed) foods. It can also be generated through endogenous metabolism. The aim of this study was to investigate the possible protective role of Pentoxifylline (PTX) as a non-selective phosphodiesterase (PDE) inhibitor on toxicity of ACR. In this study, oxidative damages were measured by markers liver mitochondrial, such as, glutathione peroxidase (GPx), superoxide dismutase (SOD), lipid peroxidation (LPO) and total glutathione (GSH) in rats. Effective doses of ACR (2mg/kg/day) and PTX (50mg/kg/day) and vitamin E (15mg/kg/day) were administered alone or in combination for 14 days by intraperitoneal injection. At the end of the experiment, the liver mitochondria of the animals were separated. PTX ameliorated LPO, SOD and GPx in liver mitochondria of ACR-induced changes. Co-administration of PTX with ACR improved LPO in liver mitochondria. In conclusion, intracellular cAMP-elevating agents like PTX, may be considered beneficial for the protection or recovery of ACR-induced toxic damage in liver mitochondria.
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Anti-inflammatory effect of
Kelussia odoratissima
Mozaff. hydroalcoholicextract on acetic acid- induced acute colitis in rats
Mohsen Minaiyan, Seyed-Ebrahim Sajjadi, Nastaran Naderi, Diana Taheri
January-June 2014, 3(1):28-35
Kelussia odoratissima
Mozaff. is an Iranian endangered endemic edible plant with numerous uses in the middle region of Iran as food and spice especially yogurt seasoning, and as medicinal herb for anti-inflammatory and cardiovascular purposes. Antioxidant, anti-inflammatory and antihyperlipidemic properties of
K. odoratissima
suggest that it may have beneficial effects on inflammatory bowel diseases like ulcerative colitis. In the present study, the effect of this plant on a model of acute colitis was evaluated. Different doses of hydroalcoholic extract of
K. odoratissima
(125, 250, 500 mg/kg) were administered orally (p.o.) to the separate groups of male Wistar rats (n = 6). It was started 4h before induction of colitis and continued on a daily basis for 3 consecutive days. Wet colon weight/ length ratio and tissue damage scores and area as well as indices of colitis and tissue myeloperoxidase (MPO) activity were evaluated for each specimen. Two lower doses of extract (125, 250 mg/kg) were effective to reduce all the indices of colitis and MPO activity in different assays. By increasing the dose, (500 mg/kg) the efficacy was declined suggesting a possible reverse dose related effect. It is concluded that
K. odoratissima
has anti-inflammatory action in rat model of colitis but further detailed studies are recommended to identify the mechanisms that are involved and the active constituents that are responsible for these findings.
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Production and secretion of TNF related apoptosis inducing ligand (TRAIL/Apo2L) in the
Escherichia coli
periplasm using PhoA signal peptide
Omid Tavallaei, Mojgan Bandehpour, Nastaran Nafissi-Varcheh, Bahram Kazemi
January-June 2014, 3(1):90-98
The ability of TNF related apoptosis inducing ligand/Apo2 ligand (TRAIL/Apo2L) in order to selectively induce apoptosis in tumor cells but not normal cells makes it an attractive target for development of new cancer therapy. Although TRAIL/Apo2L has been produced in several hosts,
E. coli
is one of the best expression systems among them due to its safety, simplicity, low cultivation cost, and known genetic properties. However, cytoplasmic expression of TRAIL/Apo2L in
E. coli
may be concomitant with some problems such as protease-induced degradation, protein misfolding, diminution in the biological activity and complexity of downstream processing. Therefore, the aim of this study was the development of an expression system to produce and secrete recombinant TRAIL/Apo2L into the
E. coli
periplasmic space. DNA encoding Alkaline Phosphatase (PhoA) signal peptide was added to the TRAIL/Apo2L cDNA using overlapping extension PCR procedure. PhoA-TRAIL construct was subsequently cloned in pET-22b expression plasmid and correct cloning was confirmed by PCR and sequencing. TRAIL/Apo2L expression was induced in
E. coli
BL21 (DE3) and then its periplasmic fraction was isolated through osmotic shock. SDS-PAGE analysis showed that recombinant TRAIL/Apo2L was successfully secreted into
E. coli
periplasm. The periplasmic TRAIL/Apo2L was identified by western blotting analysis. Finally, the biological activity of the purified periplasmic TRAIL/Apo2L was assessed by MTT assay to evaluate its growth inhibitory effect against the HeLa cell line. In conclusion, the results demonstrate that our TRAIL/Apo2L expression system could be an interesting alternative to reduce problems arose from the cytoplasmic production of TRAIL/Apo2L.
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A 3D model for human melanocortin 4 receptor refined with molecular dynamics simulation
Mohsen Shahlaei, Atefeh Mousavi
January-June 2014, 3(1):42-53
Despite a quite short early history, computational drug design and discovery methods can now be efficient in reducing costs and speeding up drug developing procedure. Melanocortin-4 receptor (MC4R) is a G protein-coupled receptor implicated in the regulation of body weight. Despite its clinical reputation, there is a lack of in-depth knowledge about structure and behavior of MC4R in lipid bilayer due to the absence of a crystal structure. In this context, a computational investigation was presented to study the Melnocortin 4 receptor (MC4R) receptor integrating homology modeling (HM) and molecular dynamics (MD) simulations. A homology-based model of the MC4R receptor was produced. The resulting homology model of the receptor was then used for molecular dynamics simulation studies in explicit POPC. The receptor structure that ensued was refined and the final native conformation was obtained.
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In vitro
anti-angiogenic activity of persian shallot (
Allium Hirtifolium
) extract is mediated through inhibition of endothelial cell proliferation/migration and down-regulation of VEGF and MMP expression
Delnia Arshadi, Kamran Mansouri, Reza Khodarahmi, Parivash Seyfi, Yadollah Shakiba, Ali Mostafaie
January-June 2014, 3(1):65-79
Development of phytotherapies aimed at angiogenesis inhibition, in combination with classical anti-cancer therapies, is among the most intensively studied approaches for treatment of cancer. Epidemiological and animal studies have indicated that consumption of
Allium
species like shallot is associated with a reduced risk of cancer development. As a continuation of our efforts to study and characterize the effective anti-angiogenic agents from
Allium
species, here, we investigated the effects of aqueous extract of shallot on critical steps and mediators of
in vitro
angiogenesis. The antiproliferation, -migration, and -tubulogenesis properties of the aqueous extract of shallot (at 100 - 1500 μg/ml) were evaluated using three-dimensional capillary tube formation as well as a wound-healing assay in endothelial cell-based experimental systems. In addition, the effect of the extract on vascular endothelial growth factor (VEGF) secretion and matrix metalloproteinase (MMP-2 and -9) expression was assayed using ELISA, gelatin zymography, and RT-PCR techniques. Treatment with the aqueous extract of shallot at ≥ 500 μg/ml concentrations resulted in significant decreases in endothelial cell proliferation, migration, and tubulogenesis. Moreover, the extract caused a dose-related inhibition of VEGF secretion and MMP-2/-9 expression. Taking all the data into account, the current study indicated that shallot – containing potent anti-angiogenic properties - exerts its inhibitory effect mainly through down-regulation of VEGF and MMP-2/-9; essential angiogenic mediators in many malignant and chronic inflammatory diseases.
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Anti-angiogenic/inflammatory behavior of mushroom
Ganoderma Lucidum
extract could be effective for treatment of corneal neovascularization: A hypothesis
Kamran Mansouri, Leila Mahamed-Khosroushahi, Hassan Rasouli
January-June 2014, 3(1):14-18
Neovascularization of the normally avascular cornea was associated with a notable increase in the expression of the major pro-angiogenic factors, inflammatory cytokines and proteases. The data supporting a causal role for vascular endothelial growth factor (VEGF), inflammatory cytokines and matrix metalloproteinase (MMPs) are extensive. Anti-angiogenic/anti-inflammatory therapy is considered as a possible tool for controlling corneal neovascularization. Mushroom
Ganoderma Lucidum
extracts containing materials that significantly reduced the number of newly formed vessels and expression of inflammatory cytokines and angiogenic factors production from various cells. This study aimed to elucidate anti-angiogenic activity of
Ganoderma Lucidum
extract for inhibiting corneal neovascularization and restoration of corneal neovascularization and restoration.
[ABSTRACT]
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Effect of streptokinase on short-term outcomes in the acute myocardial infarction with ST-segment elevation
Awat Feizi, Ali Nasr, Hamid Sanei, Peyman Mikaili, Afshin Amirpoor, Navab Ghasemi
January-June 2014, 3(1):85-89
Acute coronary syndrome is one of the most prevalent cardiovascular diseases. The acute myocardial infarction is one of its kinds which embodies the indication of fibrinolysis. One of the fibrinolytic types mostly used in Iran is Streptokinase (SK). This study aims to study the short-term clinical outcomes after receiving SK.A prospective cohort study was conducted on 54 patients at hospitals affiliated to Isfahan Medical School. After discharging, within 30 days, patients were followed regarding the morality and major adverse cardiac events (MACE) including Re-MI, unstable Angina, Cerebrovascular Accidents (CVA) and doing revascularization. Results were analyzed in both independent samples and Chi-square by statistical t-tests using SPSS software. Out of 54 patients, 25 individuals received SK versus 29 cases who did not receive that. In 30-day follow-up, no CVA or Re-MI was observed. In patients who did not receive SK, despite more deaths (14.2 % vs. 8 %) and MACE (62% vs. 56 %), it was not statistically significant (P>0.05).In the present study, receiving SK did not cause to reduce the rate of mortality and MACE in the time period of 30 days. However, it is suggested that a similar study with a larger size and also follow-up with long-term outcome be conducted.
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Antimalarial evaluation of cuminaldehyde, an aromatic monoterpenoid, using cell free β-hematin formation assay
Mahdi Mojarrab, Marieh Rezaei, Sayyed-Shahram Miraghaee, Gisya Abdi, Yalda Shokoohinia
January-June 2014, 3(1):36-41
Malaria as one of the most recurrent infectious diseases caused by parasites of the genus
plasmodium
, kills several hundred thousand people especially in the tropical and subtropical regions of the world annually. Terpenoids have served as the lead compounds to develop new antimalarial agents. The aromatic monoterpenoid, cuminaldehyde, isolated from the fruits of
Bunium persicum
was evaluated for antimalarial activity using cell-free β-hematin formation assay. The purified compound showed no inhibitory performance with respect to β-hematin formation. It is presumably due to structural differences between cuminaldehyde and other known active terpenoids.
[ABSTRACT]
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