فهرست مطالب

Advanced Pharmaceutical Bulletin
Volume:7 Issue: 4, Dec 2017

  • تاریخ انتشار: 1396/10/27
  • تعداد عناوین: 20
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  • Monica Budu., Gabriel Hancu *, Aura Rusu, Melania CArcu-Dobrin, Daniela Lucia Muntean Pages 495-500
    The majority of modern antidepressants (selective serotonin reuptake inhibitors and selective serotonin and norepinephrine reuptake inhibitors) have one or two centers of asymmetry in their structure; resulting in the formation of enantiomers which may exhibit different pharmacodynamic and pharmacokinetic properties. Recent developments in drug stereochemistry has led to understanding the role of chirality in modern therapy correlated with increased knowledge regarding the molecular structure of specific drug targets and towards the possible advantages of using pure enantiomers instead of racemic mixtures. The current review deals with chiral antidepressant drugs; presenting examples of stereoselectivity in the pharmacological actions of certain antidepressants and their metabolites and emphasizing the differences between pharmacological actions of the racemates and pure enantiomers.
    Keywords: Antidepressants, Selective serotonin reuptake inhibitor (SSRI), Selective serotonin, norepinephrine reuptake in, Stereoselectivity, Chirality
  • Naina Mohamed Pakkir Maideen*, Abdurazak Jumale, Rajkapoor Balasubramaniam Pages 501-504
    Metformin is a most widely used medication all around the world to treat Type 2 diabetes mellitus. It is also found to be effective against various conditions including, Prediabetes, Gestational diabetes mellitus (GDM), Polycystic Ovarian Syndrome (PCOS), Obesity, Cancer, etc. It is a cationic drug and it depends Organic Cation Transporters (OCTs) and Multidrug and Toxin Extruders (MATEs) mostly for its pharmacokinetics movement. The probability of drug interaction increases with the number of concomitant medications. This article focuses the drug interactions of metformin and most of them are linked to the inhibition of OCTs and MATEs leading to increased plasma metformin concentrations and subsequent elevation of risk of Metformin Associated Lactic Acidosis (MALA). By identifying the drugs inhibiting OCTs and MATEs, the healthcare professionals can predict the drug interactions of metformin.
    Keywords: Metformin, Drug interactions, Organic Cation Transporters, Multidrug, Toxin Extruders, Pharmacokinetic interactions
  • Khalil Hajiasgharzadeh, Behzad Baradaran Pages 507-513
    The hepatic vagus branches innervate the liver and serve an important role in liver-brain connection. It appears that brain modulates inflammatory responses by activation of vagal efferent fibers. This activation and subsequent acetylcholine releases from vagus nerve terminals leads to inhibition of inflammatory cytokines through α7 nicotinic acetylcholine receptors (α7nAChRs) which located on the surface of different cell types such as liver Kupffer cells. This protective role of vagus-α7nAChR axis in liver diseases has been shown in several experimental studies. On the other hand, accumulated evidence clearly demonstrate that, autonomic dysfunction which is reduced functioning of both vagal and sympathetic nervous system, occurs during chronic liver disease and is well-known complication of patients suffering from cirrhosis. This review describes the impact and significance of cholinergic anti-inflammatory pathway in the liver and discusses about its disease-related dysfunction on the progression of cirrhosis. Considering the fact that sepsis is major cause of death in cirrhotic patients, convergence of these findings, may lead to designing novel therapeutic strategies in the field of chronic liver diseases management involving selective drug targeting and electrical nerve stimulation.
    Keywords: Hepatic vagus nerve, Autonomic dysfunction, Cirrhosis, Inflammatory reflex
  • Rabinarayan Parhi Pages 515-530
    Hydrogels are promising biomaterials because of their important qualities such as biocompatibility, biodegradability, hydrophilicity and non-toxicity. These qualities make hydrogels suitable for application in medical and pharmaceutical field. Recently, a tremendous growth of hydrogel application is seen, especially as gel and patch form, in transdermal drug delivery. This review mainly focuses on the types of hydrogels based on cross-linking and; secondly to describe the possible synthesis methods to design hydrogels for different pharmaceutical applications. The synthesis and chemistry of these hydrogels are discussed using specific pharmaceutical examples. The structure and water content in a typical hydrogel have also been discussed.
    Keywords: Hydrogel, Cross, linking, Thermoreversible gel, Polymers
  • Hamze Timari, Karim Shamsasenjan, Aliakbar Movassaghpour, Parvin Akbarzadehlaleh, Davod Pashoutan Sarvar, Sara Aqmasheh Pages 531-546
    Hematopoietic stem cells (HSCs) are multipotent stem cells, with self-renewal ability as well as ability to generate all blood cells. Mesenchymal stem cells (MSCs) are multipotent stem cells, with self-renewal ability, and capable of differentiating into a variety of cell types. MSCs have supporting effects on hematopoiesis; through direct intercellular communications as well as secreting cytokines, chemokines, and extracellular vesicles (EVs). Recent investigations demonstrated that some biological functions and effects of MSCs are mediated by their EVs. MSC-EVs are the cell membrane and endosomal membrane compartments, which are important mediators in the intercellular communications. MSC-EVs contain some of the molecules such as proteins, mRNA, siRNA, and miRNA from their parental cells. MSC-EVs are able to inhibit tumor, repair damaged tissue, and modulate immune system responses. MSC-EVs compared to their parental cells, may have the specific safety advantages such as the lower potential to trigger immune system responses and limited side effects. Recently some studies demonstrated the effect of MSC-EVs on the expansion, differentiation, and clinical applications of HSCs such as improvement of hematopoietic stem cell transplantation (HSCT) and inhibition of graft versus host disease (GVHD). HSCT may be the only therapeutic choice for patients who suffer from malignant and non-malignant hematological disorders. However, there are several severe side effects such GVHD that restricts the successfulness of HSCT. In this review, we will discuss the most important effects of MSCs and MSC-EVs on the improvement of HSCT, inhibition and treatment of GVHD, as well as, on the expansion of HSCs.
    Keywords: Expansion, Graft versus host disease, Hematopoietic stem cells, Mesenchymal stem cell, derived extracellular vesicl, Transplantation
  • Negar Saliani, Soheila Montazersaheb, Shideh Montasser Kouhsari Pages 547-556
    MicroRNAs (miRNAs) are endogenous non-coding RNAs that have significant roles in biological processes such as glucose homoeostasis. MiRNAs fine-tune target genes expression via sequence-specific binding of their seed sequence to the untranslated region of mRNAs and degrade target mRNAs. MicroRNAs in islet β-cells regulate β-cell differentiation, proliferation, insulin transcription and glucose-stimulated insulin secretion. Furthermore, miRNAs play key roles in the regulation of glucose and lipid metabolisms and modify insulin sensitivity by controlling metabolic functions in main target organs of insulin such as skeletal muscle, liver and adipose tissue. Moreover, since circulating miRNAs are detectable and stable in serum, levels of certain miRNAs seem to be novel biomarkers for prediction of diabetes mellitus. In this article, due to the prominent impact of miRNAs on diabetes, we overviewed the microRNAs regulatory functions in organs related to insulin resistance and diabetes and shed light on their potential as diagnostic and therapeutic markers for diabetes.
    Keywords: β, cell function, Glucose homeostasis, MicroRNA, MicroRNA biomarkers
  • Rana Refaat Makar, Randa Latif, Ehab Ahmed Hosni, Omaima Naim El Gazayerly Pages 557-567
    Purpose
    Triple solid dispersion adsorbates (TSDads) and spherical agglomerates (SA) present new techniques that extensively enhance dissolution of poorly soluble drugs. The aim of the present study is to hasten the onset of hypoglycemic effect of glimepiride through enhancing its rate of release from tablet formulation prepared from either technique.
    Methods
    Drug release from TSDads or SA tablets with different added excipients was explored. Scanning electron microscopy (SEM) and effect of compression on dissolution were illustrated. Pharmacodynamic evaluation was performed on optimized tablets.
    Results
    TSDads & SA tablets with Cross Povidone showed least disintegration times of 1.48 and 0.5 min. respectively. Kinetics of drug release recorded least half-lives (54.13 and 59.83min for both techniques respectively). Cross section in tablets displayed an organized interconnected matrix under SEM, accounting for the rapid access of dissolution media to the tablet core. Components of tablets filled into capsules showed a similar release profile to that of tablets after compression as indicated by similarity factor. The onset time of maximum reduction in blood glucose in male albino rabbits was hastened to 2h instead of 3h for commercial tablets.
    Conclusion
    After optimization of tablet excipients that interacted differently with respect to their effect on drug release, we could conclude that both amorphisation and spheronization were equally successful in promoting in vitro dissolution enhancement as well as providing a more rapid onset time for drug action in vivo.
    Keywords: Dissolution, Pharmacodynamic study, Blood glucose level, Matrix tablets, Spherical agglomeration, Triple solid dispersion adsorbate
  • Mayank Chaturvedi, Manish Kumar, Kamla Pathak, Shailendra Bhatt, Vipin Saini Pages 569-577
    Purpose
    A comparative study was carried out between surface solid dispersion (SSD) and solid dispersion (SD) of meloxicam (MLX) to assess the solubility and dissolution enhancement approach and thereafter develop as patient friendly orodispersible tablet.
    Methods
    Crospovidone (CPV), a hydrophilic carrier was selected for SSD preparation on the basis of 89% in- vitro MLX adsorption, 19% hydration capacity and high swelling index. SD on the other hand was made with PEG4000. Both were prepared by co-grinding and solvent evaporation method using drug: carrier ratios of 1:1, 1:4, and 1:8. Formulation SSDS3 (MLX: CPV in 1:8 ratio) made by solvent evaporation method showed t50% of 28 min and 80.9% DE50min which was higher in comparison to the corresponding solid dispersion, SDS3 (t50% of 35min and 76.4% DE50min). Both SSDS3 and SDS3 were developed as orodispersible tablets and evaluated.
    Results
    Tablet formulation F3 made with SSD3 with a disintegration time of 11 secs, by wetting time= 6 sec, high water absorption of 78%by wt and cumulative drug release of 97% proved to be superior than the tablet made with SD3.
    Conclusion
    Conclusively, the SSD of meloxicam has the potential to be developed as fast acing formulation that can ensure almost complete release of drug.
    Keywords: Surface solid dispersion, Solid dispersion, Dissolution, Orodispersible tablet
  • Mojtaba Keshavarz, Majid Reza Farrokhi, Atena Amiri Pages 579-584
    Purpose
    Some reports have shown neuroprotective effects of caffeine in several neurodegenerative disorders. However, its mechanism of action is not completely clear. Therefore, the aim of this study was to explore the interference of ryanodine, N-methyl-D-aspartate (NMDA) and adenosine modulators with the neuroprotective effects of caffeine against β-amyloid (Aβ) neurotoxicity in the SHSY5Y cells.
    Methods
    The SHSY5Y cells were treated with Aβ23-35 (20µM) and/or caffeine (0.6 and 1mM), or both for 24 hours. Adenosine (20, 40, 60, 80, 100µM), NMDA (20, 50, 70, 90µM), dantrolene (2, 4, 6, 8, 10µM) were also added to the medium and incubated for 24 hours. The cell viability was measured via the MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) method. The data were analyzed using one-way ANOVA followed by Bonferroni test.
    Results
    Caffeine at all the used concentrations (0.6, 0.8, 0.9, 1, and 3mM) significantly protected neuronal cells against Aβ neurotoxicity. Adenosine at the concentrations of 20, 40, 80 and 100μM diminished the neuroprotective effects of caffeine (0.6 and 1mM) against Aβ neurotoxicity. NMDA at the concentrations of 20, 50, 70 and 90μM blocked caffeine (0.6 and 1mM) neuroprotective effects. Dantrolene at the concentration of 2, 4, 6, 8 and 10μM diminished the neuroprotective effects of caffeine (0.6mM) and at the concentrations of 2 and 10μM impede caffeine (1mM) neuroprotection against Aβ neurotoxicity.
    Conclusion
    Caffeine produced neuroprotective effect against Aβ neurotoxicity. Blockade of adenosine and NMDA receptors, as well as the activation of ryanodine receptors, may contribute to the neuroprotective effects of caffeine.
    Keywords: Caffeine, N, methyl, D, Aspartate, Adenosine, Dantrolene, β, amyloid
  • Tahereh Eteraf-Oskouei, Sevda Mikaily Mirak, Moslem Najafi Pages 585-591
    Purpose
    In the present study, the effects of verapamil on inflammation and angiogenesis in air pouch model were studied.
    Methods
    To create a model of inflammation in the rats, on days 1 and 3 sterile air, and on the sixth day, carrageenan was injected into the pouch subcutaneously. Normal saline as control, diclofenac sodium and dexamethasone as standards and verapamil (0.05, 0.1 and 0.2mg/rat) was injected into the pouch simultaneously with carrageenan and as well as 24 and 48 hours later. After 72 hours, volume of exudate, the leukocytes count, concentration of VEGF and IL-1ß, granulomatous tissue weight, histopathological changes and angiogenesis were considered.
    Results
    Verapamil significantly reduced leukocyte accumulation in all doses, but effect of 0.1mg/rat was more significant (P
    Conclusion
    Verapamil has significant anti-inflammatory and anti-angiogenesis effects in the air pouch model probably due to attenuation effects of verapamil on IL-1β and VEGF.
    Keywords: Verapamil, Air, Pouch, Inflammation, Angiogenesis, VEGF, IL, 1β
  • Roman Akasov, Maria Drozdova, Daria Zaytseva-Zotova, Maria Leko, Pavel Chelushkin, Annie Marc, Isabelle Chevalot, Sergey Burov, Natalia Klyachko, Thierry Vandamme, Elena Markvicheva Pages 593-601
    Purpose
    Multidrug resistance (MDR) of tumors to chemotherapeutics often leads to failure of cancer treatment. The aim of the study was to prepare novel MDR-overcoming chemotherapeutics based on doxorubicin (DOX) derivatives and to evaluate their efficacy in 2D and 3D in vitro models.
    Methods
    To overcome MDR, we synthesized five DOX derivatives, and then obtained non-covalent complexes with human serum albumin (HSA). Drug efficacy was evaluated for two tumor cell lines, namely human breast adenocarcinoma MCF-7 cells and DOX resistant MCF-7/ADR cells. Additionally, MCF-7 cells were entrapped in alginate-oligochitosan microcapsules, and generated tumor spheroids were used as a 3D in vitro model to study cytotoxicity of the DOX derivatives.
    Results
    Due to 3D structure, the tumor spheroids were more resistant to chemotherapy compared to monolayer culture. DOX covalently attached to palmitic acid through hydrazone linkage (DOX-N2H-Palm conjugate) was found to be the most promising derivative. Its accumulation levels within MCF-7/ADR cells was 4- and 10-fold higher than those of native DOX when the conjugate was added to cultivation medium without serum and to medium supplemented with 10% fetal bovine serum, respectively. Non-covalent complex of the conjugate with HSA was found to reduce the IC50 value from 32.9 µM (for free DOX-N2H-Palm) to 16.8 µM (for HSA-DOX-N2H-Palm) after 72 h incubation with MCF-7/ADR cells.
    Conclusion
    Palm-N2H-DOX conjugate was found to be the most promising DOX derivative in this research. The formation of non-covalent complex of Palm-N2H-DOX conjugate with HSA allowed improving its anti-proliferative activity against both MCF-7 and MCF-7/ADR cells.
    Keywords: Aantitumor drug screening assays, Microencapsulation, Multicellular spheroids, Multiple drug resistance, Serum albumin
  • Fatemeh Safari, Solmaz Rahmani Barouji, Ali Mohammad Tamaddon Pages 603-609
    Purpose
    Human telomerase reverse transcriptase (hTERT) plays a crucial role in tumorigenesis and progression of cancers. Gene silencing of hTERT by short interfering RNA (siRNA) is considered as a promising strategy for cancer gene therapy. Various algorithms have been devised for designing a high efficient siRNA which is a significant issue in the clinical usage. Thereby, in the present study, the relation of siRNA designing criteria and the gene silencing efficiency was evaluated.
    Methods
    The siRNA sequences were designed and characterized by using on line soft wares. Cationic co-polymer (polyethylene glycol-g-polyethylene imine (PEG-g-PEI)) was used for the construction of polyelectrolyte complexes (PECs) containing siRNAs. The cellular uptake of the PECs was evaluated. The gene silencing efficiency of different siRNA sequences was investigated and the effect of observing the rational designing on the functionality of siRNAs was assessed.
    Results
    The size of PEG-g-PEI siRNA with N/P (Nitrogen/Phosphate) ratio of 2.5 was 114 ± 0.645 nm. The transfection efficiency of PECs was desirable (95.5% ± 2.4%.). The results of Real-Time PCR showed that main sequence (MS) reduced the hTERT expression up to 90% and control positive sequence (CPS) up to 63%. These findings demonstrated that the accessibility to the target site has priority than the other criteria such as sequence preferences and thermodynamic features.
    Conclusion
    siRNA opens a hopeful window in cancer therapy which provides a convenient and tolerable therapeutic approach. Thereby, using the set of criteria and rational algorithms in the designing of siRNA remarkably affect the gene silencing efficiency.
    Keywords: RNA Interference, hTERT, Gene silencing
  • Atinderpal Kaur, Sonal Gupta, Amit Tyagi, Rakesh Kumar Sharma, Javed Ali, Reema Gabrani, Shweta Dang Pages 611-619
    Purpose
    A nanoemulsion based gel containing Polyphenon 60 (P60) and cranberry (CRB) has been developed to deliver via intravaginal route for the treatment of urinary tract infection.
    Methods
    Polyphenon 60 and cranberry were loaded in a single nanoemulsion gel (NBG) by ultra-sonication method and characterized for particle size, rheological properties, in vitro release and growth curve analysis. P60ऐ NBG were radiolabelled using technetium pertechnetate (99mTc) to perform in vivo pharmacokinetic studies in animals.
    Results
    The finalized NE had a droplet size of 58±1 nm. In vitro release of 90.92 ± 0.6% in 8 hr for P60 and 99.39 ± 0.5% in 6 hr for CRB was observed in simulated vaginal fluid. Growth curve of E. coli indicated the inhibitory action of nanoemulsion based gel at the fifth hour of inoculation. Gamma scintigraphy studies on female Sprague-Dawley rats showed transport of nanoemulsion based gel from the vaginal cavity into the systemic circulation. Further, biodistribution studies with radiolabelled P60ऐ NBG showed significant higher uptake of radiolabelled actives by kidney (3.20±0.16) and urinary bladder (3.64±0.29), when administered intravaginally.
    Conclusion
    The findings suggested 99mTc-P60ऐ NBG can potentially be transported through vaginal cavity and reach the target organs and showed effective distribution in organs affected in urinary tract infection
    Keywords: Cranberry, Gamma scintigraphy, Intravaginal drug delivery, Polyphenon 60, Radiolabelling, Urinary tract infection
  • Maryam Shirdel, Hossein Tajik, Mehran Moradi Pages 621-628
    Purpose
    The aim of this study was to investigate antimicrobial and biofilm removal potential of Zataria multiflora essential oil (ZEO) and silver nanoparticle (SNP) alone and in combination on Staphylococcus aureus and Salmonella Typhimurium and evaluate the mechanism of action.
    Methods
    The minimum inhibitory concentration (MIC), and optimal inhibitory combination (OIC) of ZEO and SNP were determined according to fractional inhibitory concentration (FIC) method. Biofilm removal potential and leakage pattern of 260-nm absorbing material from the bacterial cell during exposure to the compounds were also investigated.
    Results
    MICs of SNP for both bacteria were the same as 25 μg/ mL. The MICs and MBCs values of ZEO were 2500 and 1250 μg/mL, respectively. The most effective OIC value for SNP and ZEO against Salm. Typhimurium and Staph. aureus were 12.5, 625 and 0.78, 1250 μg/ mL, respectively. ZEO and SNP at MIC and OIC concentrations represented a strong removal ability (>70%) on biofilm. Moreover, ZEO at MIC and OIC concentrations did a 6-log reduction of primary inoculated bacteria during 15 min contact time. The effect of ZEO on the loss of 260-nm material from the cell was faster than SNP during 15 and 60 min.
    Conclusion
    Combination of ZEO and SNP had significant sanitizing activity on examined bacteria which may be suitable for disinfecting the surfaces.
    Keywords: Antimicrobial, Sanitizing, Biofilm, Essential oil, Silver nanoparticle, Combination
  • Niloofar Bazazzadegan, Marzieh Dehghan Shasaltaneh, Kioomars Saliminejad, Koorosh Kamali, Mehdi Banan, Reza Nazari, Gholam Hossein Riazi, Hamid Reza Khorram Khorshid Pages 629-636
    Purpose
    Alzheimer’s disease (AD) is pathologically defined by the presence of amyloid plaques and tangles in the brain, therefore, any drug or compound with potential effect on lowering amyloid plaques, could be noticed for AD management especially in the primary phases of the disease. Ectoine constitutes a group of small molecule chaperones (SMCs). SMCs inhibit proteins and other changeable macromolecular structures misfolding from environmental stresses. Ectoine has been reported successfully prohibit insulin amyloid formation in vitro.
    Methods
    We selected eight genes, DAXX, NFκβ, VEGF, PSEN1, MTAP2, SYP, MAPK3 and TNFα genes which had previously showed significant differential expression in Alzheimer human brain and STZ- rat model. We considered the neuroprotective efficacy by comparing the expression of candidate genes levels in the hippocampus of rat model of Sopradic Alzheimer’s disease (SAD), using qPCR in compound-treated and control groups as well as therapeutic effects at learning and memory levels by using Morris Water Maze (MWM) test.
    Results
    Our results showed significant down-regulation of Syp, Mapk3 and Tnfα and up-regulation of Vegf in rat’s hippocampus after treatment with ectoine comparing to the STZ-induced group. In MWM, there was no significant change in swimming distance and time for finding the hidden platform in treated comparing to STZ-induced group. In addition, it wasn’t seen significant change in compound-treated comparing to STZ-induced and control groups in memory level.
    Conclusion
    It seems this compound may have significant effect on expression level of some AD- related genes but not on clinical levels.
    Keywords: Sporadic Alzheimer disease, Ectoine, Gene expression, Morris Water Maze test, STZ, rat model
  • Saiedeh Razi Soofiyani, Akbar Mohammad Hoseini, Ali Mohammadi, Vahid Khaze Shahgoli, Behzad Baradaran, Mohammad Saeid Hejazi Pages 637-643
    Purpose
    Cancerous inhibitor of protein phosphatase 2A (CIP2A) is an identified human oncoprotein which modulates malignant cell growth. It is overexpressed in human prostate cancer and in most of the human malignancies. The aim of this study was to investigate the effects of CIP2A silencing on the sensitivity of PC-3 prostate cancer cells to docetaxel chemotherapy.
    Methods
    PC-3 cells were transfected using CIP2A siRNA. CIP2A mRNA and protein expression were assessed after CIP2A gene silencing using q-RT PCR and Western blotting. Proliferation and apoptosis were analyzed after treatment with docetaxol using MTT assay, DAPI staining, and flow cytometry, respectively.
    Results
    Silencing of CIP2A enhanced the sensitivity of PC-3 cells to docetaxel by strengthening docetaxel induced cell growth inhibition and apoptosis against PC-3 cells.
    Conclusion
    Silencing of CIP2A may potentiate the cytotoxic effects of docetaxel and this might be a promising therapeutic approach in prostate cancer treatment.
    Keywords: CIP2A, Docetaxel, Prostate cancer, siRNA
  • Narjes Khavasi, Mohammad Hosein Somi, Ebrahim Khadem, Elnaz Faramarzi, Mohammad Hossein Ayati, Seyyed Muhammad Bagher Fazljou, Mohammadali Torbati Pages 645-650
    Purpose
    Despite numerous studies on the effects of complementary medicine, to our knowledge, there is no study on the effects of Capparis spinosa on disease regression in non-alcoholic fatty liver disease (NAFLD) patients. We compared the effects of caper fruit pickle consumption, as an Iranian traditional medicine product, on the anthropometric measures and biochemical parameters in different NAFLD patients.
    Methods
    A 12-weeks randomized, controlled, double-blind trial was designed in 44 NAFLD patients randomly categorized for the control (n=22) or caper (n=22). The caper group received 40-50 gr of caper fruit pickles with meals daily. Before and after treatment, we assessed anthropometric measures, grade of fatty liver, serum lipoproteins and liver enzymes.
    Results
    Weight and BMI were significantly decreased in the caper (p
    Conclusion
    Our results suggest that daily caper fruit pickle consumption for 12 weeks may be potentially effective on improving the biochemical parameters in NAFLD patients. Further, additional larger controlled trials are needed for the verification of these results.
    Keywords: Iranian traditional medicine, Non, alcoholic fatty liver, Caper fruit, Lipid profile
  • Mahmood Sadeghi Ataabadi, Sanaz Alaee, Mohammad Jafar Bagheri, Soghra Bahmanpoor Pages 651-654
    Abstract
    Purpose
    Given the antiandrogenic effects of spearmint, in this study we evaluated the effects of its essential oil on polycystic ovarian syndrome in a rat model.
    Methods
    Female rats were treated as follows: Control, normal rats which received 150 mg/kg spearmint oil or 300 mg/kg spearmint oil, or sesame oil; and PCOS-induced rats which received 150 mg/kg spearmint oil or 300 mg/kg spearmint oil, or sesame oil. Then the animals were killed and the levels of LH, FSH, testosterone and ovarian folliculogenesis were evaluated.
    Results
    Spearmint oil reduced body weight, testosterone level, ovarian cysts and atretic follicles and increased Graafian follicles in PCOS rats.
    Conclusion
    Spearmint has treatment potential on PCOS through inhibition of testosterone and restoration of follicular development in ovarian tissue.
    Keywords: PCOS, Mentha spicata, Folliculogenesis, Rat
  • Wafaa Mostafa Elkady, Eman Ahmed Ibrahim, Mariam Hussein Gonaid, Farouk Kamel El Baz Pages 655-660
    Purpose
    the non-edible fruit parts of Casimiroa edulis Llave et were evaluated for their active constituents and their potential as antioxidants, anti-inflammatory and antitumor activity.
    Methods
    Fruits peel (FP) and seeds kernel (SK) of Casimiroa edulis Llave et Lex. were extracted successively with hexane and then methanol. Fatty acids were prepared from hexane extracts and identified by GC. Total flavonoid, phenolic acids and tannins contents in methanol extracts were determined by UV spectrophotometer and identified by HPLC. Antioxidant, in-vitro anti-inflammatory activity and antitumor effect against Caco-2 cell line were determined.
    Results
    GC analysis of hexane extracts showed that oleic acid (47.00%) was the major unsaturated fatty acids in both extracts while lignoceric acid (15.49%) is the most abundant saturated fatty acid in (FP). Total phenolic, flavonoid and tannin contents in (FP) & (SK) methanol extracts were; 37.5±1.5, 10.79±0.66 and 22.28±0.23 for (FP); 53.5±1.5mg/g, 14.44±0.32 mg/g; and 53.73±3.58 mg/g for (SK) respectively. HPLC analysis of methanol extract revealed that; the major phenolic compound was pyrogallol in (FP) and p-hydroxybenzoic acid in (SK), the major flavonoid was luteolin 6-arabinose-8-glucose in (FP) and acacetin in (SK).
    Conclusion
    This study showed that non-edible parts of C. edulis fruit is a rich source of different phenolic compounds and fatty acids which has great antioxidant, anti-inflammatory and antitumor activities; that could be used as a natural source in pharmaceutical industry.
    Keywords: Casimiroa edulis, Fatty acids, Phenolic contents, Antioxidant, Anti, inflammatory, Caco, 2
  • Ali Golestan, Abbas Ghaderi, Zahra Mojtahedi Pages 661-664
    Purpose
    N-myc downstream-regulated gene 2 (NDRG2) is frequently down-regulated in cancer, and plays an important role in the control of tumor growth and metastasis. Its manipulation has been suggested as a therapy in cancer. Here, we examined the outcome of NDRG2 overexpression on proliferation, invasion, migration and MMP activity of HCT116 colorectal cancer cell line.
    Methods
    The HCT116 cell line (human colorectal cancer) was transfected with pCMV6-AC-GFP-NDRG2. 2,5diphenyltetrazolium bromide (MTT) assay was used to detect cell proliferation. The invasion and migration of the transfected cells were examined through transwell chambers while the MMP-9 activity was detected by the ability of the cells to digest gelatin.
    Results
    Overexpression of NDRG2 by stable NDRG2 transfection decreased cell proliferation, migration and invasion ability, along with decreasing MMP-9 activity.
    Conclusion
    Our data indicate that NDRG2 overexpression can suppress several aspect of tumorigenesis. Further investigations are necessitated to verify if NDRG2 molecule can be a therapeutic target in colorectal cancer.
    Keywords: Colorectal cancer, NDRG2, Invasion, Migration, Matrix metalloproteinase