ÖZET: Kişniş (Coriandrum sativum L.), Apiaceae familyasına ait bir bitki olup
Obesity is one of the serious health condition in the world and contributes to many chronic illnesses augmenting to high risk of death rate. With the purpose of obesity treatment, natural sources come to be significant to replace commercial drugs due to their harmful effect to the body. Therefore, a lot of studies were conducted on natural sources due to their potential as medicinal herbs. Aquilaria sp. plants are well known in traditional medicine as a sedative, analgesic and digestive. Even though there were no reports on applications of Aquilaria sp. towards obesity treatment, this plant has traditionally been used as laxative for weight reducing. In this study, the anti-lipase activity of an extract of barks and leaves from A. subintegra and A. malaccensis were investigated. The anti-lipase activity was measured by colorimetric assay on pancreatic lipase activity using porcine pancreatic lipase (PPL; triacylglycerol lipase, EC 3.1.1.3). The result indicated that among these two species of Aquilaria, A. malaccensis bark in dichloromethane crude showed high anti-lipase activity. Thus, these results suggest that Aquilaria sp. plant extracts might be of therapeutic interest with respect to the treatment.
Acne vulgaris is a common inflammatory skin condition, which has been reclassified as a chronic disease. The spectrum of topical acne treatments has expanded substantially in recent years and various topical medications including topical dapsone are available. Dapsone has special physicochemical properties that make its topical formulation challenging. The aim of this study was preparing a hydrogel- thickened microemulsion as a topical delivery system for dapsone. The microemulsions composed of dapsone (5%), isopropyl myristate, tween 80, diethylene glycol monoethyl ether, ethanol and water were prepared. The optimum microemulsion was modified with carbomer 940. Droplet size, pH, refractive index, conductivity, rheology of the optimized formulation, and skin permeation of dapsone through rat skin were evaluated. The optimized formulation significantly increased the skin permeation of dapsone in comparison to that of control gel. Although incorporation of menthol increased the particle size, the flux of microemulgel consisting of menthol (5%) was 2.51 times higher than that of the control. However, the skin absorption of the drug was less than 3%. Six month accelerated studies proved the physicochemical stability of microemulgels. The results of this research indicate that menthol based hydrogel- thickened microemulsion system could be a promising vehicle for topical delivery of dapsone.
Using rarmpril as a model active pharmaceutical ingredient, the focus of the present study was to fabricate low-cost controlled release tablets using combinations of biopolymer and semi-synthetic polymers. Cellulose derivatives are more viscous where biopolymers form gels more easily. Xanthan gum can't shape a solid gel, result in fragmentation of gel around the tablets so that depend upon high concentration. Therefore, a combination was used to formulate tablet by direct compression. This combination of polymer provides low cost product with higher potentiality. Ingredients as per formulations were mixed in small polybag through hand blending. Then tablets were compressed one by one tablet in a hydraulic press. Prepared tablets were evaluated for hardness, weight variation, content uniformity, friability, surface pH and in-vitro dissolution studies. ANOVA was used to analyze the differences between release data. Swelling index, mucoadhesive strength and in-vitro residence time was studied to show gastroretention of the tablets. Formulated products exhibit sufficient quality and strength to formulate as a mucoadhesive tablet. Significant differences were found in drug release among different formulations (p <0.05) in all cases. Among all of formulations, Fll, F12 and F13 containing different ratio of xanthan gum and guar gum showed promising mucoadhesive strength and in-vitro residence time.
Culex pipiena L. (Diptera: Culicidae) is an important vector of West Nile virus in many parts of the world. In this research, the essential oils obtained from Nepeta cadmea Boiss. (endemic for Turkey) and Pimpinella anisum L. were examined for larvicidal activity against second-third instar larvae of Cx. pipiena. The essential oils were distilled from aerial parts of N. cadmea and seeds of P. anisum by water distillation. The chemical composition of these oils was determined by gas chromatography-mass spectrometry (GC-MS). The lethal concentration 50 and 90 values of these essential oils were 28.7 and 49.51 ppm, and 39.82 and 74.57 ppm, respectively. As a result, both essential oils were found highly toxic to larvae of Cx. pipiena. Our results showed that the essential oils obtained from N. cadmea and P. anisum may be suitable for the development of potential new botanical insecticides.
The aim of the study was to increase dissolution rate of atorvastatin by the use of mesoporous silica SYLOID (R) 244 FP. The poorly soluble drug atorvastatin was adsorbed on and/or into SYLOID (R) 244 FP in the ratios 1:1, 1:1.1.5, 1:2, 1:2.5, 1:3 and 1:3.5 via a wetness impregnation method. The absence of crystalline form and presence of hydrogen bond interaction between atorvastatin and SYLOID (R) 244 FP is done by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The atorvastatin loaded matrix lacked in the crystalline form of atorvastatin and it showed improvement in the dissolution rate of ATC. The flowability of the atorvastatin loaded matrix powder was evaluated by bulk density, Carr's index and angle of repose. This matrix was then processed into a tablet by direct compression method. A 3(2) full factorial design was applied to investigate the combined effect of two formulation variables - volume of ethanol and amount of SYLOID (R) 244 FP. The tablets were evaluated for hardness, friability, drug content and drug dissolution studies. The solubility of atorvastatin-loaded matrix was increased up to 4.28 times. Atorvastatin tablet prepared from drug-loaded silica may provide a feasible approach for development of an oral formulation for this poorly water-soluble drug.
Although simulation practice with standard patients became popular in curriculums since years of various countries, it hasn't been used in the education of pharmacists and pharmacy technicians in Turkey yet. In this study, it is aimed to conduct a pilot study with standard patients on students in the simulation laboratory for the first time and get feedback of them. This study was conducted with 22 pharmacy technicians, four pharmacy students and four standard patients in 15-16 December 2015. Six scenarios were used. After the study, video recordings of the "student-standard patient interaction" were watched with the students to improve the simulation laboratory and the practices planned to be. The physical properties of the place, the use of body language, issues related to the needs and feelings during practice for the development of training programs has come to fore during the feedback of the students. It is useful to generalize this pilot study in terms of both student groups for starting their profession with communication skills and achieving the golden standards in education.
In this study, we aimed to develop a novel positive charged nucleic acid delivery system for the treatment of glioblastoma. For this purpose, Epidermal Growth Factor Receptor (EGFR) which plays a prominent role in glioblastoma was selected as a target. Cationic solid lipid nanoparticles (cSLN) were developed by microemulsion dilution method using cetyl palmitate as matrix lipid, Cremephor RH40 and Peceol as surfactants, and ethanol as cosurfactant. Characterization studies showed that obtained nanoparticles are positively charged and has an appropriate particle size for nucleic acid delivery (<20 nm). Gel retardation assay revealed that cSLNs have complexation ability with siRNA EGFR (cSLN:siRNAEGFR) and this complex is able to protect siRNA from serum- mediated degradation up to 6 h. The cytotoxicity evaluation of nanoparticles performed on U87 Human Glioblastoma Cell Line. Furthermore, in vitro delivery of siRNA-EGFR via cSLN inhibited EGFR expression significantly at 50nM siRNA dose compared to free siRNA-EGFR at the same dose on U87 cell line (p<0.05). Based on these findings, we propose that the developed cSLN system may has a potential as a siRNA delivery system for glioblastoma.
We compared different stress conditions on brain BDNF levels, in rats exposed to social isolation test (SIT) and predator scent tests (PST).BDNF expression in the frontal cortex, hippocampus, and amygdala was compared, and effects of chronic fluoxetine (FLU) treatment were evaluated.Rats were exposed to SIT and PST for one month.FLU was given (5 mg/kg/day, ip) throughout stress procedures.Controls, stress, and treatment groups were evaluated in elevated plus maze, anxiety scores were calculated.BDNF expression was determined by Western blot.SIT and PST induced anxiety in both sexes, females had greater anxiety scores than males (p<0.05).FLU restored anxiety scores in both sexes (p<0.01) in both tests.Male and female rats exhibited reduced cortical BDNF levels in SIT (p<0.001).PST reduced cortical BDNF in females, but increased in males.Hippocampal BDNF expression was lowered in SIT (p<0.01) and PST (p<0.001) in both sexes.Female rats had 40% lower BDNF expression than males in the amygdala in SIT.FLU did not restore cortical BDNF in females in both tests, but reduced increased BDNF levels in males in PST (p<0.001).FLU did not restore reduced brain BDNF in males in the hippocampus and amygdala, but restored in hippocampus, in females.Our findings indicate that sex differences must be considered in studies related to mood disorders of animal models, and suggest that BDNF expression in different brain regions are altered differentially in a gender-dependent manner in rats.Antianxiety effect of FLU is not mediated through increasing BDNF activity in cortex in both genders.Increased BDNF in hippocampus and amygdala may reflect antidepressant effect of FLU in female rats, but not in males.
Radiotherapy is an important strategy for cancer treatment, but resistance of tumor cells to ionizing radiation (IR) still remains a main challenging issue related to radiotherapy.The aim of this study was to evaluate the sensitizing effect of cerium oxide nanoparticles (CNPs) on non-small lung cancer (A-549) cells exposure to IR. A-549 cells were treated with CNPs and exposed to IR at dose 2 Gy.The radiosensitizing effect of CNPs was evaluated by clonogenic assay and flowcytometry.The findings of this study showed that CNPs reduced the frequencies of A-549 colony when these cells were exposed to IR. CNPs treatment prior exposure to IR significantly increased the IR-induced apoptotic incidences in A-549 cells.The present study demonstrates that CNPs to be an effective sensitizer on apoptosis and cell death induced by IR in A-549 cells.
A quantitative Structure-Activity Relationship (QSAR) model was applied to the prediction of the activity of iminochromene derivatives.The inhibition activity of 34 carbonyl reductase 1 (CBR1) inhibitors were modeled with the descriptors of quantum-chemical calculations with density functional theory (DFT) method at B3LYP/6-31G level.This study was conducted using the multiple linear regressions (MLR), the partial least square analysis (PLS) and the principal component analysis (PCA) method.Results displayed that the MLR method predicted of activity good enough.The best model, with seven descriptors was selected.Also it indicates very good consistency towards data variations for the validation methods.The predicted values of activities are in suitable agreement with the experimental results.The obtained results suggested that the PCA method could be more helpful to predict the biological activity of iminochromene derivatives.It is anticipated to be useful to predict the activity of other compounds in the same groups.
A key challenge in cancer treatment is the wide range of cancer cells' behavior towards chemotherapy and treatment procedures, which makes the outcomes of treatment often unpredictable, accompanied by cancer resistance and recurrence.One underlying reason is that tumor is a heterogeneous tissue.The cells within a tumor are at different metabolic states and hence behave differently from another and towards the chemotherapeutics.Many of the cells in the inner layers of a tumor lack an appropriate growth condition.However, upon tumor shrinkage, they can regrow and finally cause tumor resistance or recurrence.In the current study, for the first time, long term effects of different levels of metabolic stress on human ovary cancer cell line, A2780, is reported.In this in vitro model, the cells exposed to 10% serum were considered as control and metabolic stress was induced at 0.5, 0.25 and 0% serum for 1-6 days.In this 6-day period, cells' morphology changes, size, cell cycle, mitochondrial function and protein content was measured at 24-hour intervals.Also, cells ability to recur was assessed with the above tests in a 24-hour release in 10% serum.The results of this study showed that A2780 cells show resistant features against metabolic stress and this longterm stress does not stop cells recurrence.These results indicate that in order to have a successful tumor treatment, a modified chemotherapy procedures against different types of cells laying within one tumor is required.
A series of new 4-thiazolidinone derivatives were synthesized and evaluated against diverse DNA- and RNA-viruses in mammalian cell cultures. Some of the compounds were found to exhibit moderate antiviral activity. 3-Propyl-2-[((6-(4-chlorophenyl)imidazo[2,l-b]thiazol-3-yl)acetyl)hydrazono]-5-methyl-4-thiazolidinone 13, displayed modest yet consistent activity against three strains of influenza A virus, including the 2009 pandemic virus A/H1N1 Virginia/ ATCC3/2009 (cytotoxicity >100 mu M). Compounds 6 and 11 displayed activity against vesicular stomatitis virus in HeLa cells (antiviral EC50 values of 9 (cytotoxicity 100 mu M) and 2 mu M (cytotoxicity 20 mu M), respectively). Neither of the compounds was active against HIV.
Schizophrenia is a severe psychiatric disorder with about 1% prevalance.NMDA receptor antagonists such as Phencyclidine (PCP) and MK-801 are commonly used for modeling schizophrenia in rodents.In literature, despite of the concensus about subchronic PCP administration (commonly 7 days, bi-daily administration followed by a 1 week washout period), there are different subchronic administration regimens for MK-801 beside 7 days, bidaily (MK-801-7), such as 14 days (MK-801-14) daily or 28 days daily injections.In this study, we aimed to compare two prevalant MK-801 models (MK-801-7 and MK-801-14, 0.2 mg/kg) in both behavioural and molecular changes.Wistar Hannover rats grouped as control (n=10), MK-801-14 (n=8) and MK-801-7 (n=8).Prepulse inhibition of acustic startle response (PPI), novel object recognition test (NORT), social interaction (SI) and Morris's water maze (MWM) tests were used for behavioural analyzes while real time polimerase chain reaction (Rt-PCR) was conducted for molecular analyzes of glutamic acid decarboxilase 67 (GAD67) and parvalbumin.Our results showed decreased PPI in MK-801-14 and MK-801-7 groups.Moreover, in both models platform finding latencies were increased and swimming time in platform area was decreased in MWM.MK-801-14 and MK-801-7 reduced following and raised avoiding behaviours in SI.In Rt-PCR, GAD67 mRNA levels were decreased by MK-801-14 and MK-801-7 administrations.However, only MK-801-7 decreased discrimination index in NORT and parvalbumin mRNA levels.In this study, it has been showed that although MK-801-14 and MK-801-7 administrations revealed smiliar schizophrenia like symptoms in rats, MK-801-7 has partial superiories in certain aspects.
Due to its geographic location, variable climate and traditional culture, Turkey has a rich flora and the use of plants in folk medicine is very favorable. That practice and knowledge have been passed down from generation to generation. Ethnobotanical surveys are carried out to record traditional treatment methods of plants. In this study, which was prepared by screening of ethnobotanical researches made in Turkey, 241 taxa were recorded in the traditional treatment of hemorrhoids. Information about scientific and local names, families, used parts and usage patterns of these plants are given. According to the research results, the most commonly used plants in hemorrhoid treatment are plants belonging to Asteraceae, Lamiaceae, Rosaceae, Scrophulariaceae, Araceae, Polygonaceae and Cupressaceae families. The species commonly used in different regions of Turkey are Achillea sp., Arum sp., Cichorium intybus L., Dracunculus vulgaris Schott, Ecballium elaterium (L.) A. Rich., Ficus carica L., Hypericum perforatum L., H. scabrum L., Juglans regia L., Peganum harmala L., Rosa canina L., Rubus sp., Sambucus ebulus L., S. nigra L., Teucrium polium L., Urtica dioica L., Verbascum sp..
Ulcers that develop due to alcohol consumption are frequently confronted. The aim of this study was to investigate the protective effects of silk fibroin on the pro-apoptotic and anti-apoptotic protein expression levels on ethanol induced-ulcer models in rats. For three consecutive days, orogastrically either silk fibroin or saline were given to rats. On the 4th day, animals were deprived of food but allowed free access to water for 24 h before the experiment. While control groups were treated with only physiological saline, the ulcer groups were treated orally either with saline or silk fibroin groups. For ulcer induction, 1 ml of absolute ethanol by gavage were given to both group. Firstly, intracardiac blood was taken at 60 min of EtOH or saline administration and immediately animals were decapitated. In blood samples, the amount of TNF-alpha, IL-1 beta were analysed whereas in stomach tissues, the levels of MDA, GSH, and MPO activity and the expression levels of bcl-2, Bax, caspase-3 and -9 were determined. In ulcer groups, the amount of TNF-alpha , IL-l beta, MDA, MPO, caspase-3 and caspase-9 were found to be significantly higher compared to control groups whereas in GSH, Bcl-2/Bax were found to be lower (p < 0.005). In treatment groups it is observed that silk fibroin recovers the amount of TNF-alpha, IL l-beta, MDA, MPO, GSH, caspase-3, caspase-9, and Bcl2/Bax. In conclusion, for the treatment of the gastric ulcer SF thought to be very efficient therapeutic agent.
Delphinidin is an anthocyanidin which is found in fruits and vegetables as a primary plant pigment used for various purposes. The purpose of this study was to investigate the in vitro genotoxic and antigenotoxic effects of delphinidin chloride (DC) in human peripheral blood lymphocytes. Final concentrations of 25 mu M, 50 mu M, 75 mu M and 100 mu M of DC were tested for 24 or 48 hours treatment periods. For detection of possible antigenotoxic potential of DC, human peripheral lymphocytes were co-treated with DC and a known clastogenic agent mitomycin-C (MMC). Genotoxic and antigenotoxic effects of DC were determined with the chromosome aberration (CA) and micronucleus (MN) tests. Cytotoxic effect of DC was determined by measuring the nuclear division index (NDI) and mitotic index (MI). Additionally, total oxidant and antioxidant values were determined by a spectrophotometric method. CA variations resulting from DC treatments did not reveal statistical significance as compared with controls. In tubes treated with DC and MMC together, DC significantly decreased the CA frequency caused by MMC (P <= 0.01). This decrease was almost 50% as compared to the positive control MMC. In this study, DC alone did not lead to the CA and MN formation in all culture tubes. DC did not cause a significant oxidative stress. DC has an antigenotoxic effect against the mutagenic effects of MMC.
Chlorogenic acid (CGA) is a major polyphenol in primary human diet, displaying a wide range of biological activities such as anti-oxidant, anti-inflammatory and anti-cancer effects.Several studies reported the chemopreventive effects of CGA on different types of cancers including breast cancer, which is the most common cancer among women worldwide.In this comprehensive study, we determined the anti-proliferative and cytotoxic effects of pure CGA on the phenotype of various breast cancer cell lines (MCF-7, SKBR-3, MDA-MB-231, MDA-MB-468 and BT-20) with well-defined molecular classification and characteristics, in a time and dose dependent manner by using iCELLigence real-time and label-free cell analysis technology.Cells were plated on iCELLigence system-specific E-plate L8 and treated with CGA for 72 hours at concentrations ranging from 250 μM to 8 mM.Obtained data were analyzed by RTCA data analysis software 1.0 and IC50 values of 952±32.5 μM for MCF-7, 940±21.2μM for SKBR-3, 590.5±10.6 μM for MDA-MB-231, 882.5±12.0μM for MDA-MB-468 and 1095±121.6μM for BT-20 cell lines were calculated at the end of 72-hour assay.Based on our findings, CGA did not have cytotoxic activity on breast cancer cell lines, and IC50 values and growth curves displayed similar anti-proliferative patterns with slight variation.
The current study deals with the development of floating microspheres of venlafaxine hydrochloride. This drag is known as a serotonin-norepinephrine reuptake inhibitor and used to treat depression. Due to the short elimination half life of 4-5 h, the drug has to be administered 2-3 times in a day to maintain the plasma concentration. Thus an attempt was made to decrease the dosing frequency. The microspheres were prepared by non-aqueous solvent evaporation method. The microspheres were evaluated for particle size and morphology using a photomicroscope and scanning electron microscopy, respectively. The incorporation efficiency of microspheres of batch F2 and F6 showed entrapment of 60.6% and 57.2%, respectively. The mean diameters of particles for all batches were found in the range of 226.15 +/- 24.37 to 283.37 +/- 21.56 mu m. The Fourier transform infrared spectroscopy revealed absence of any drug polymer interactions. The microsphers remained buoyant for more than 12 h. The drug release from developed microspheres followed Fickian diffusion with swelling. The results suggested that the developed floating microspheres containing venlafaxine hydrochloride could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.
