فهرست مطالب

Pharmaceutical Sciences
Volume:26 Issue: 2, Jun 2020

  • تاریخ انتشار: 1399/04/19
  • تعداد عناوین: 13
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  • Alev Önder, Lutfun Nahar*, Sushmita Nath, Satyajit D. Sarker Pages 99-106

    The genus Opopanax W.D.J. Koch is a member of the Apiaceae family, distributed throughout the Mediterranean region and comprises only three recognized and well-defined species, O. chironium (L.) W.D.J. Koch, O. hispidus (Friv.) Griseb. and O. persicus Boiss. The species of this genus with yellow flowers are well-known in traditional medicine and consumed as food. This review critically appraises published literature on the phytochemistry, traditional usages, and pharmacological activities of the genus Opopanax. In addition, it provides evidence to suggest that the plants from this genus have potential phytotherapeutic applications. Previous phytochemical and bioactivity studies revealed that the genus Opopanax predominantly produces coumarins, diterpenes, phenolics, and phthalides, and possesses various biological and pharmacological properties, including anticancer, antioxidant and antimicrobial activities. The phytochemical profile and pharmacological activities of the genus Opopanax could be useful for further study and might find additional medicinal applications in evidence-based phytotherapy.

    Keywords: Anticancer, Apiaceae, Coumarins, Opopanax, Phytochemistry, Phytotherapy
  • Elaheh Rahimpour, Sima Alvani Alamdari, Abolghasem Jouyban* Pages 107-132

    This article summarizes the publishing activities including bioanalytical and pharmaceutical analyses researches carried out in Iran in 2018 in order to connect academic researchers to those in industry, medical care units and hospitals. A wide spectrum of analytical methods has been used to determine and/or evaluate drug levels in the biological samples, based on physical, chemical and biochemical principles. We have compiled a concise survey of the literature covering 125 reports and tabulated the relevant analytical parameters. Chromatographic and electrochemical methods were found to be the technique of choice for many workers and almost 83% studies were performed by using these methods. This is the first annual review of the literature searching in SCOPUS database for published bioanalytical and pharmaceutical analysis researches in Iran.

    Keywords: Iran, Bioanalysis, Pharmaceutical research, Pharmaceutical compounds, Biological samples
  • Elmira Zolali, Sevda Shayesteh, Reza Rahbarghazi, Haleh Vaez, HamidReza Heidari, Alireza Garjani* Pages 133-141
    Background

    Type 2 diabetes mellitus is a chronic metabolic disorder with prominent vascular injuries. In this condition, the levels of multiple pro- and anti-angiogenic factors have been shown to change. This study aimed to investigate the possible effect of metformin on proangiogenic factor, endocan levels, via the modulation of p-AMPK/AMPK axis in diabetic mice.

    Methods

    Mice were randomly assigned to one of 4 groups (n=6): Control (normal saline) and the diabetic group was injected streptozotocin and two groups were given 50 and 100 mg/kg metformin orally, once daily for two weeks after diabetes induction. Endocan protein levels were detected in the liver and kidneys by ELISA and immunofluorescence analysis. Phosphorylation of AMPK was assessed using western blotting. Histological examination was performed to follow the metformin effect on Von Willebrand factor expression and diabetes-related pathologies.

    Results

    ELISA assay showed an elevated levels of endocan in the renal and hepatic tissues of diabetic mice following treatment with metformin (p<0.05). Immunofluorescence and immunohistochemistry examination of kidneys showed that the increase of endocan protein coincided with the promotion of vWF factors in mice treated with metformin (p<0.05). We did not find endocan factor in hepatic tissue of diabetic mice pre- and post-treatment with metformin. Western blotting confirmed the phosphorylation of AMPK by metformin in kidneys (p<0.05), but these changes did not reach statistically significant levels in hepatic tissues (p>0.05).

    Conclusion

    Metformin could change the endocan levels during diabetic condition possibly by the modulation of p-AMPK/AMPK axis.

    Keywords: Diabetes, Metformin, Endocan, p-AMPK AMPK
  • Gohar Eslami, Samad Golshani, Mahmood Moosazadeh, Faezeh Shadfar* Pages 142-149
    Background

    Radial artery spasm (RAS) resulted from decreasing blood flow and activation of vasomotor system leads to a decrease in artery diameter, perfusion and patency, and increase the risk of procedure failure. In this study, we investigated the effects of intra-arterial administration of nitroglycerin and labetalol on radial artery diameter, RAS, and pain intensity in patients undergoing diagnostic radial angiography.

    Methods

    Sixty-four patients randomly enrolled into one of the nitroglycerin (150 μg) or labetalol (500 μg) groups. The radial artery size, and the incidence of RAS were measured before, immediately after puncture, and at the end of treatment. Pain intensity was evaluated using a visual-analog-scale (VAS) at the end of the procedure. Hemodynamic status before, and during the procedure was also recorded.

    Results

    Labetalol causes a significantly larger increase in radial diameter than nitroglycerin immediately after intra-arterial injection (2.24±0.58 mm vs. 1.65±0.39 mm, P-value<0.001). The rate of RAS immediately after vasodilator administration in the labetalol group was 3.1% vs. 12.5% in the nitroglycerin group (P-value=0.355), but the overall incidence (immediately after administration+ at the end of procedure) did not show a statistically significant difference (53.125% vs 31.25% respectively, P-value=0.076). The VAS score did not show a significant difference between two groups (1.15±0.44 in nitroglycerin vs. 1.50±0.91, P-value=0.063).

    Conclusion

    Labetalol increases radial artery diameter more than nitroglycerin. However, the efficacy of labetalol in terms of RAS incidence, and patients’ pain was similar to nitroglycerin. Therefore, intra-arterial labetalol could be considered as one of the therapeutic options in clinical practice in order to reduce RAS and procedure failure.

    Keywords: Angiography, Angiospasm, Labetalol, Nitroglycerin, Radial artery
  • Nafiseh Sadat Alamolhodaei, Hatam Rashidpoor, Melika Ehtesham Gharaee, Javad Behravan, Fatemeh Mosaffa* Pages 150-158
    Background

    TNF-α, as a pro-inflammatory cytokine in the tumor microenvironment is able to regulate the expression and function of various ATP binding cassette (ABC) transporters involved in clinical drug resistance and among them, ABCC2 transporter is represented to contribute to cancer multidrug resistance (MDR) by drug efflux.

    Methods

    In this study, we aimed to evaluate the effects of TNF-α and/or E2 (17β-estradiol) on the mRNA and protein expression levels of ABCC2 and NF-κB (p65) transcription factor in estrogen receptor positive (ER+) MCF-7 cells by QRT-PCR and Western blot analysis. Also, we used MTT assay to study the cell sensitivity against the active form of tamoxifen (4OH-TAM), a hypothetical substrate and Cisplatin (Cis), a well-known substrate for ABCC2 used in endocrine and chemo-therapy of breast cancers, respectively. Data were analyzed by one-way ANOVA and Tukey tests. Significance was considered in P-values < 0.05.

    Results

    The expression levels of ABCC2 and the active form of NF-κB (p65) were significantly increased following 20-day concomitant treatment with TNF-α and E2, compared to untreated cells as control. Also, the viability assay showed that 20-day TNF-α+E2 treatment led to more sensitivity reduction of MCF-7 cells to Cis and 4OH-TAM compared to E2-treated and untreated cells.

    Conclusion

    Based on our findings, there is a positive correlation between ABCC2 overexpression, over-activity of NF-ҡB/p65 and decreasing the sensitivity of MCF-7 cells to Cis and 4OH-TAM following TNF-α treatment in MCF-7 cells. Further experiments are needed to elucidate possible mechanistic relationship of these findings and their clinical significance in order to circumvent the drug-resistance in breast tumors.

    Keywords: Breast cancer, TNF-α, 17β-estradiol, ABCC2, NF, κB, p65, Cisplatin, 4OH, Tamoxifen
  • Seyed Mostafa Mir, Bahman Yousefi*, Abdoljalal Marjani, Mahdi Rahimi, Durdi Qujeq Pages 159-164
    Background

    Investigation of anti-cancer agents with desirable selective toxicity is critical for cancer therapy. The use of natural adjuvants can be a promising option in reducing the toxicity of the anti-cancer agent. The aim of this study was to investigate the potential application of melatonin (MLT) as a natural adjuvant molecule along with doxorubicin (DOX) to induce cytotoxicity in osteosarcoma (OS) cells.

    Methods

    Human OS cell lines included Saos-2, MG-63, and Human Bone Marrow Mesenchymal Stem Cells (hBM-MSCs) were treated with free DOX, free MLT, DOX-loaded NPs (DOX-NPs), MLT-loaded NPs (MLT-NPs), combination of DOX and MLT (DOX-MLT) and combination of DOX and MLT-loaded NPs (DOX-MLT-NPs) in separated cell culture. Cell proliferation of experiments were evaluated by MTT assay after 24 h. Total protein levels were determined by enzyme immunoassay ELISA.

    Results

    Herein, we found the combination of MLT with DOX, especially formulated in nanoform, is resulted in a significant reduction in the protein levels of both X-linked Inhibitor of Apoptosis (XIAP) and Survivin (p<0.0001). Indeed, there was a significant decrease in the expression of XIAP and Survivin when MLT is combined with DOX compared to the individual treatments.

    Conclusion

    Our findings indicated the synergism of the antitumor effect could be due to the down-regulation of XIAP and Survivin in the levels of protein.

    Keywords: -Melatonin, Doxorubicin, Osteosarcoma, Combination therapy
  • Maryam Hamzeh Mivehroud, Zoha Khoshravan Azar, Siavoush Dastmalchi* Pages 165-174
    Background

    In the recent years, histamine H3 receptor (H3R) has been receiving increasing attention in pharmacotherapy of neurological disorders. The aim of the current study was to investigate structural requirements for the prediction of H3 antagonistic activity using quantitative structure-activity relationship (QSAR) and molecular docking techniques.

    Methods

    To this end, genetic algorithm coupled partial least square and stepwise multiple linear regression methods were employed for developing a QSAR model. The obtained QSAR model was stringently assessed using different validation criteria.

    Results

    The generated model indicated that connectivity information and mean absolute charge are two important descriptors for the prediction of H3 antagonistic activity of the studied compounds. To gain insight into the mechanism of interaction between studied molecules and H3R, molecular docking was performed. The most important residues involved in the ligandreceptor interactions were identified.

    Conclusion

    The result of current study can be used for designing of new H3 antagonist and proposing structural modifications to improve H3 inhibitory potency.

    Keywords: GA-PLS, Histamine H3 receptor, H3 antagonists, Molecular docking, MLR -QSAR
  • Shashanka Rajendrachari*, Abdullah Cahit Karaoglanli, Yusuf Ceylan, Orhan Uzun Pages 175-183
    Background

    In the past few years, Magnetite (Fe3O4) nanoparticles have gained a significant research interest in the field of biology, chemistry, metallurgy due to their wide range of applications. Some of their important applications include drug delivery, chemotherapy, lowfriction seals, magnetic fluid, adsorbent, recovery of hazardous wastes, etc.

    Methods

    In the present paper, we reported an eco-friendly route of preparing magnetite nanoparticles by using leaves of Tilia Tomentosa (Ihlamur) followed by calcination at 400 ˚C for 15 minutes.

    Results

    The bandgap energy of the prepared Fe3O4 nanoparticles was studied by UV–Visible spectroscopy and the value was found to be 3.31 eV. The scanning electron microscopy (SEM) image showed the spherical magnetite nanoparticles with an average size of 25 nm. The phases and thermal properties of Fe3O4 nanoparticles were studied by using X-ray diffraction, thermogravimetric (TG) and differential thermal analysis (DTA). The enthalpy change of Fe3O4 nanoparticles was calculated by using the DTA curve and the value was found to be 4.97 kJ/ mol at 8˚C/min heating rate. The antimicrobial activity of Fe3O4 nanoparticles was carried out by the minimum inhibition concentration (MIC) assay method. Except for B. subtilis, Fe3O4 nanoparticles demonstrated significant antibacterial property.

    Conclusion

    The prepared magnetite nanoparticles showed excellent thermal stability and less weight loss over a 30–1000 ˚C temperature range. The size of the prepared magnetite nanoparticles is very less therefore they interacted effectively with the organelle, enzymes, and cells of bacteria and inhibited bacterial growth by killing them.

    Keywords: Antibacterial activity-Fe3O4 nanoparticles, Ihlamur, leaves extract, tilia tomentosa, UV visible spectroscopy
  • Jalal Mardaneh, Hamid Beyzaei, Seyed Hadi Hashemi, Behzad Ghasemi*, Abbas Rahdar Pages 184-192
    Background

    Acinetobacter baumannii is a common infectious agent in hospitals. New antimicrobial agents are identified and prepared to combat these bacterial pathogens. In this context, the blocking potentials of a series of synthesized N-heterocyclic compounds, Cu/ Fe3O4@SiO2 nanocomposites, glycine, poly-L-lysine, nisin and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were evaluated against nonresistant and multidrug-resistant strains of A. baumannii.

    Methods

    Solutions of heterocyclic derivatives and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were prepared at initial concentration of 10240 μg ml-1 in 10% DMSO. Other compounds were dissolved in water at the same concentrations. Their in vitro inhibitory activity was assessed by determination of IZD, MIC and MBC values.

    Results

    Glycine, poly-L-lysine, nisin, Curcuma longa and green tea catechins extracts, and thiazoles 3a, 3d and 3f were ineffective at their initial concentrations. Heterocyclic derivatives 7a-f, 3c, 3e and 3h, Cu/Fe3O4@SiO2 nanocomposites and Trachyspermum ammi extract could block the growth of bacterial strains with IZDs (7.40-15.51 mm), MICs (32-1024 µg ml-1) and MBCs (128-2048 µg ml-1).

    Conclusion

    Among synthetic chemicals and natural products, the best antimicrobial effects were recorded with (E)-2-(5-acetyl-4-methylthiazol-2-yl)-2-(thiazolidin-2-ylidene)acetonitrile (7b) and the extract of Trachyspermum ammi. It is imperative that their toxic and histopathologic effects were assessed in future researches. It is predicted that the essential oil of Trachyspermum ammi will improve its antibacterial activities.

    Keywords: Antibacterial effect, Acinetobacter baumannii, Nanocomposites, Curcuma longa, Green tea catechins, Trachyspermum ammi
  • Fatemeh Dorreh, MohammadHossein Esmaeili, Parsa Yousefichaijan, Mahdyieh Naziri, Aziz Eghbali, Bahador Bagheri* Pages 193-197
    Background

    Upper Respiratory tract infection (URTI) or common cold is very prevalent in children particularly in young children. Leukotriene receptor antagonists (LTRAs) like montelukast are effective drugs in asthma and some other respiratory diseases. Our purpose was to study preventive effects of montelukast on pediatric URTI.

    Methods

    This randomized, placebo-controlled, and double blind trial was performed on 450 healthy children aged 1-5 year in Amir Kabir Hospital, Arak, Iran. Children were randomized 1:1 to placebo group or montelukast group for 12 weeks. Number of URTI episodes and duration were the primary end points and were compared at baseline and after termination of treatment.

    Results

    Mean age was 28 ± 12.3 months. Mean of URTI episodes was 0.7 ± 0.57 in children treated with montelukast and 1.27 ± 0.72 in children treated with placebo, respectively. Differences were statistically significant (P =0.01). A significant difference was seen in URTI duration between two study groups (6.3 ± 6.1 vs 4.1 ± 3.9, P = 0.05). In addition, duration of fever was shorter in children receiving montelukast (P=0.001).

    Conclusion

    Our study indicates that 3 month treatment with montelukast is effective for reducing the incidence of URTI in young children. This treatment has an acceptable safety without any serious concern.

    Keywords: Upper respiratory tract infection, Montelukast, Children, Fever
  • Amin Akbari Ahangar, MohammadReza Delnavazi* Pages 198-202
    Background

    Stachys lavandulifolia Vahl is an herbaceous perennial plant which its flowering aerial parts are used traditionally as gastrotonic, spasmolytic, sedative and for the treatment of gastrointestinal disorders. In the present study the aerial parts of this medicinal plant was investigated for its flavonoid glycosides content.

    Methods

    n-butanol fraction derived from hydroalcoholic extract of S. lavandulifolia was subjected to phytochemical analysis using chromatography on Sephadex LH-20 and RP-18 silica gel columns. The structures of isolated compounds were identified using 1H-NMR, 13C-NMR and UV spectral analysis.

    Results

    Four flavone glycosides, chrysoeriol-7-O-β-D-glucopyranoside (1), apigenin-7-O-(6″O-acetyl)-β-D-glucopyranoside (2), luteolin-7-O-β-D-glucopyranoside (3), apigenin-7-O-β-Dglucopyranoside (4), along with apigenin (5) and chlorogenic acid (6) were isolated from S. lavandulifolia aerial parts.

    Conclusion

    Identification of these phenolic compounds with some known biological activities in S. lavandulifolia explains some medicinal properties reported for this species and make scientific rationale for its traditional uses.

    Keywords: Stachys lavandulifolia Vahl, Flavone glycoside, Apigenin, Luteolin, Chrysoeriol, Chlorogenic acid
  • Parina Asgharian, Abbas Delazar, Solmaz Asnaashari* Pages 203-208
    Background

    Eremostachys macrophylla Montbr. & Auch. is one of the wild growing species of herbs found in East Azerbaijan province of Iran. These species are used in folk medicine for the healing of wound, treatment of snake bites, rheumatism and joint pains. The primary aim of this study was to obtain natural pure compounds and this was done by subjecting the aerial parts of Eremostachys macrophylla Montbr. & Auch. to phytochemical analysis.

    Methods

    The air-dried and crushed aerial parts were respectively extracted with n-hexane, dichloromethane (DCM) and methanol (MeOH) solvents using a soxhlet apparatus. The 10%, 20% and 40% of MeOH in water Sep-Pak fractions of the MeOH extract were subjected to a preparative reversed- phase high performance liquid chromatography (RP-HPLC). Also, the isolated pure compounds were identified by one-dimensional nuclear magnetic resonance (1D-NMR) spectroscopic technique

    Results

    The results obtained in this study showed the presence of seven pure components; (1) Lamalbide, (2) Sesamoside, (3) Phlomiol, (4) Verbascoside, (5) Luteolin-7-O- glucoside, (6) Apigenin-7-O- rutinoside and (7) Kaempferol-3-O- glucoside with iridoid, phenylethanoid and flavonoid structures.

    Conclusion

    The results from the study demonstrated that the aerial parts of E. macrophylla could be a good source of iridoids, phenylethanoids and flavonoids.

    Keywords: Eremostachys macrophylla, Iridoid, Phenylethanoid, Flavonoid
  • Nissha Bharrathi Romes, Wan Mohd Nuzul Hakimi Wan Salleh, Hasnah Mohd. Sirat*, Zaini Assim Pages 209-213
    Background

    Genus Alpinia are commonly used as spices and ingredients in traditional medicines. In the present study, we attempted to isolate the phytochemicals from Alpinia aquatica and evaluate their tyrosinase inhibitory activity.

    Methods

    Phytochemical constituents of the extract were investigated using various chromatographic and spectroscopic methods. The chemical structures of the isolated phytochemicals were established by analysis of their spectroscopic data, as compared to that of reported data. Tyrosinase inhibitory activity was also tested on the extracts and selected compounds using mushroom tyrosinase as the enzyme.

    Results

    Fractionation and purification of the extracts of Alpinia aquatica afforded seven known compounds which are 5-hydroxy-3,7,4’-trimethoxyflavone (1), 4’,5-dihydroxy-3,7-dimethoxyflavone (2), 2-methoxy-8-(2’,4’,5’-trimethoxyphenyl)-1,4-naphthaquinone (3), cis-3S-(2’,4’,5’-trimethoxyphenyl)-4S-[(E)-2’’’,4’’’,5’’’-trimethoxystyryl]cyclohexene (4), 2,4,5-trimethoxybenzaldehyde (5), stigmasterol (6) and β-sitosterol (7). The ethyl acetate extract of pseudostems possessed the highest tyrosinase inhibition of 31.0% among the extracts, while compound (1) gave tyrosinase inhibition of 48.0%.

    Conclusion

    Compounds (3) and (4) were isolated for the first time from A. aquatica and Alpinia genus. These phytochemical results suggest that the extracts could assist as a potential source of bioactive compounds. Further research is needed in which the extract could possibly be exploited for pharmaceutical use.

    Keywords: Zingiberaceae, Alpinia aquatica, Tyrosinase, Flavonoid, Phytochemical