فهرست مطالب

Research in Pharmaceutical Sciences
Volume:7 Issue: 4, Nov 2012

  • تاریخ انتشار: 1391/04/01
  • تعداد عناوین: 8
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  • B. Zolfaghari, Y. Shokoohinia, P. Ramazanlou, A. Sadeghi, M. Mahmoudzadeh, M. Minaiyan Page 201
    Allium elburzense (A. elborzense, Alliaceae), a plant rich in saponins, is an edible vegetable in northern Iran with a folk background use as antidiabetic which has not yet been examined for this indication. To evaluate the antidiabetic potential of A. elburzense, its hydroalcoholic (HdAE) and butanolic extracts (BuE) were examined. The acute (1, 2, 3, 4, 8 h) and sub-acute (11 days) effects of oral (p.o.) and intraperitoneal (i.p.) administration of HdAE and BuE of A. elburzense bulbs in different doses were evaluated on blood glucose levels of normal and streptozotocin (STZ, 55 mg/kg body weight)-induced diabetic rats. Glibenclamide (1 mg/kg b.w.) was used as reference drug. Sub-acute treatment with HdAE for 11 days reduced significantly blood glucose levels in diabetic rats (at least P<0.05), while BuE was effective only following i.p. administration (P<0.01). Acute administration did not reduce blood glucose level in normal and diabetic animals. It is concluded that HdAE of A. elburzense exhibited a significant antihyperglycemic activity following chronic administration. These results provide evidence for potential use of A. elburzense in diabetes mellitus considering the fact that this plant is endemic to a location of Iran where diabetes is a high prevalence disorder.
  • M. Naderi Maralani, A. Movahedian, Sh Haghjooy Javanmard Page 209
    Oxidative stress has been implicated as a prominent determinant in the development of several diseases such as atherosclerosis. Anti atherosclerotic effects of L-serine have been shown previously but its responsible mechanisms remained unidentified. This study aimed to investigate the antioxidant and cytoprotecrtive effects of L-serine and its possible mechanisms. For this purpose, cell viability analysis and nuclear factor-erythroid 2 (NF-E2)-related factor 2 (Nrf2) activity, heme oxygenase-1 (HO-1) concentration, total Nitric Oxide (NOx) production were evaluated in oxidative stress-induced Human Umbilical Vein Endothelial Cells (HUVECs) pretreated by L-serine. Cytoprotective effects of L-serine was measured through 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Nrf2 activity and HO-1 concentration were determined in the cell lysate by commercial immunoassay methods. NOx was assayed in the supernatant of culture medium through colorimetric Griess method. Pretreatment with L-serine (0.1-3.2 mM) protected endothelial cells from hydrogen peroxide-mediated cell cytotoxicity (H2O2, 0.5 mM) and lead to significant induction of Nrf2 activity, HO-1 expresssion and NOx production. These findings demonstrated that L-serine has antioxidant and cytoprotective effects through the elevation of some crucial antioxidant factors such as Nrf2, HO-1 and NO.
  • A. Jafarian, B. Zolfaghari, M. Parnianifard Page 217
    Pumpkin, as a dietary plant, has been used in traditional medicine around the world. In addition, during the last decade, antidiabetic, antihypertensive, antitumor, intestinal antiparasitic, antibacterial, anti hypercholesterolemia, anti-inflammatory, immunomodulatory and analgic effects of pumpkin has been reported. The aim of the present study was to determine the effects of different extracts of Cucurbita pepo L. on the immune responses. Methanolic, chloroform and ethylacetate extracts of C. pepo fruits was obtained using percolation method. Mice were used to study the effects of C. pepo extracts on the acquired immunity. Sheep red blood cell (SRBC) was injected (S.C., 1×108 cells/ml, 20 ml) and 5 days later, methanolic, chloroform and ethylacetate extracts of C. pepo at diiferent doses (10, 100 and 500 mg/kg), betamethasone and levamisol at equal doses (4 mg/kg) as positive controls and normal saline as a negative control were given i.p. After 1 h SRBC was injected to the footpad (S.C., 1×108 cells/ml, 20 ml) and the footpad swelling was measured up to 72 h. To investigate the effects of C. pepo on the innate immunity the same procedure was used, but animals received only one injection of SRBC 1 h after i.p. injection of test compounds. Our findings showed that SRBC induced an increase in the paw swelling with maximum response at 6-8 h. Betamethasone inhibited the paw swelling in both models. In both innate and acquired immunity models, methanolic, chloroform and ethylacetate extracts of C. pepo fruits significantly reduced the paw swelling dose dependently. The data suggest that the pumpkin extracts may have immunomodulatory effects.
  • J. Shokri, Sh Azarmi, Z. Fasihi, S. Hallaj, Nezhadi, A. Nokhodchi, Y. Javadzadeh Page 225
    A suitable emulgel formulation of piroxicam was prepared and its percutaneous permeation was investigated using Wistar rat skin and diffusion cell technique. The concentrations of the drug in receptor phase of diffusion cells were measured using HPLC method. The effect of three types of penetration enhancers (Myrj 52, cineol and Transcutol P) with different concentrations on transdermal permeation of the drug was also evaluated. Flux, Kp and enhancement ratios (ERs) of piroxicam in the presence of enhancers was measured and compared with emulgel base alone and simple commercial gel. The results showed a significant enhancement in the flux from emulgel base compared to hydroalcoholic gel formulation (9.91 folds over simple gel). The highest enhancement ratio (ER=3.11) was observed for Myrj 52 at the concentration of 0.25%. Higher concentrations of Myrj 52did not show any enhancement in the drug flux due to micelle formation and solubilization of the drug by micelles. The increase in solubility, in turn, increases the saturated concentration and reduces the thermodynamic activity of the drug. Transcutol® P with concentrations higher than 0.25% w/w showed burst transportation of the drug through the skin. All concentrations of cineol and Transcutol did not show any enhancing effects over emulgel base alone (ER <1).
  • J. Esmi Serkani, B. Nasr Isfahani, H. Gh Safaei, R. Kasra Kermanshahi, Gh Asghari Page 235
    The increasing incidence of Multi Drug Resistance Tuberculosis (MDR-TB) and Extensively Drug Resistance TB (XDR-TB) worldwide highlight the urgent need to search for newer anti-tuberculosis compounds. It has been determined that pharmaceutical plant, hops (Humulus lupulus), possesses some antibacterial effect. In this study, the antimycobacterial effect of this plant on rifampin sensitive and resistant strains of Mycobacterium tuberculosis were examined. Sensitivity and resistance of 37 Iranian isolates of M. tuberculosis to rifampin was determined by proportion method. Ethanolic extract of hops was prepared using maceration method. PCR-SSCP and direct sequencing were used for confirming existence of mutations in 193-bp rpoB amplicons related to the rifampin resistance in Mycobacterium tuberculosis isolates. Two different concentrations of hops alcoholic extract (4 and 8 mg/ml) were prepared and its effects against 21 resistant and 15 sensitive isolates was determinate using proportion method. Six different mutations in the 193-bp amplified rpoB gene fragments and seven distinguishable PCR-SSCP patterns in 21 Iranian rifampin resistant isolates were recognized. This study showed that the percentage of resistance and the type of mutations were correlated with the PCR-SSCP patterns and the type of mutations in rpoB gene (P<0.05). The results of hops antimycobacterial effect showed that different concentrations of hops ethanolic extract (4 and 8 mg/ml) had a remarkable inhibitory effect on rifampin sensitive and resistant isolates of Mycobacterium tuberculosis. Identification of the effective fraction of hops against Mycobacterium tuberculosis is a further step to be studied.
  • M. Jalali_M. Mahdavi_H. R Memarian_M. Ranjbar_M. Soleymani_A. Fassihi_D. Abedi Page 243
    The antimicrobial activity of thirty six novel dihydropyrimidine derivatives was evaluated against common pathogenic bacteria. Significant antimicrobial activity (MIC=32, 64 µg/ml) was observed. Escherichia coli and Pseudomonas aeruginosa as Gram-negative bacteria and Staphylococcus aureus as Gram-positive bacteria were determined to be the most susceptible pathogens in this study. The highest inhibitory activity was observed against Gram-negative microorganisms. The widest spectrum of antibacterial activity was exerted by C6 and C22. Most of the compounds had remarkable antifungal activity (MIC=32 µg/ml).
  • G. Bayrami_M. H Boskabadi Page 249
    Previous studies have indicated relaxant, inhibitory effect on histamine (H1) and muscarinic receptors, and stimulatory effect on β-drenoceptor of Crocus sativus on guinea pig tracheal chains. In the present study, the effect of the extract of C. sativus and one of its constituents, safranal, on the inflammatory changes of sensitized guinea pigs was examined. Eight groups of sensitized guinea pigs to ovalbumin were studied. One group was given drinking water alone (group S), while other 7 groups were received drinking water containing; three concentrations of safranal (4, 8 and 16 µg/ml), three concentrations of extract (0.1, 0.2 and 0.4 mg/ml) and one concentration of dexamethasone (S+D group), (six animal in each group). Total and differential white blood cell (WBC) counts in blood were evaluated. Total blood WBC number, eosinophyl and lymphocyte percentage in blood were increased, but neutrophil decreased in sensitized animals compared to those of control groups (P<0.05 to P<0.001). Treatment of animals with dexamethasone, all concentrations of the extract and safranal significantly improved most types of WBCs but total WBC number was only decreased in treated groups with dexamethasone and high concentration of the extract compared to group S (P<0.05 to P<0.001). Safranal was more effective in the improvement of eosinophil and lymphocyte compared to the extracts (P<0.001 for both cases). However, the preventive effect of the extract of C. sativus on total WBC count was more prominent than that of the safranal (P<0.01). These results showed a preventive effect of the extract of C. sativus and its constituent safranal on total and differential count of WBC in blood of sensitized guinea pigs. The results also suggest that the effect of the plant is perhaps due to its constituent of safranal.
  • M. Mansouri, A. Movahedian, M. Rostami, A. Fassihi Page 257
    Biginelli-type pyrimidines contain an interesting moiety which has attracted considerable attention of medicinal chemists in the last few decades. Despite the very diverse pharmacologic effects ascribed to this kind of pyrimidines, there are few reports on the antioxidant evaluation of Biginelli pyrimidines. In this study synthesis of some novel Biginelli-type pyrimidines is reported. The prepared compounds are ester derivatives of 6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate with a simple hetaryl group, furan, at C-4 position of the pyrimidine ring. These compounds were evaluated for free radical and H2O2 scavenging activities. The reducing power of these compounds was also determined. Compound 3c was the most potent one in diphenyl picrylhydrazine scavenging activity assay with the IC50 of 0.6 mg/ml. The results of reducing power assays proved that 3d and 3e are moderate reducing agents. All of the studied compounds were very weak in scavenging hydrogen peroxide compared with gallic acid.