Journal of Reports in Pharmaceutical Sciences
Volume:2 Issue: 2, Jul-Dec 2013

Chemical composition of the essential oil of the fruit of Ferula assafoetida L. obtained by steam distillation solvent extraction methodhas been studied by GC/MS for the first time. Fifty-four components, comprising 96.9% of the total oil, were identified.epi-α-Cadinol (23.15 %), germacrene B (10.98 %), α-gurjunene (6.18 %), (Z)-1-propenyl secbutyl disulfide (5.89 %), 5-epi-7-epi-α-eudesmol (4.89 %), -cadinene (4.78 %), -cadinene (3.36 %) and germacrene D (3.09 %) were found to be the major constituents of the oil. The oil of the fruit of F. assafoetidaconsisted of ten monoterpene hydrocarbons (6.14%), twenty-six sesquiterpene hydrocarbons (43.48%), nine oxygenated sesquiterpenes (37.77%), one oxygenated hydrocarbon (0.35%), and nine volatile sulfides (11.18%).

The cytotoxicity activity of the essential oils from the leaves of Achillea wilhelmsii C. Koch were studied on six tumor cell lines and a normal cell line

Dispersive liquid–liquid micro–extraction (DLLME) technique was successfully used as a sample preparation method for the determination of clonazepam in pharmaceutical preparations and water samples. In this method, a suitable mixture of methanol (disperser solvent) and chloroform (extraction solvent) was injected rapidly into a conical test tube that contained an aqueous solution of clonazepam. After centrifuging, phase separation was performed by sedimenting the fine droplets of the micro–extraction solvent on the bottom of a test tube (about 100 μL) and then the absorbance of the enriched extracted phase was determined at the absorption wavelength of clonazepam (307 nm). Some important parameters such as, the type and volume of extraction and dispersive solvents as well as the extraction time were investigated and optimized. Under the optimum conditions, the calibration graph was linear over the range of 0.95 to 18.94 μg/mL of clonazepam with a limit of detection of 0.06 μg/ml.

The genus Hymenocrater, belong to the Lamiaceae family, consist of 21 species throughout the world. In Iran, about 9 species are present, of which some are endemic. Plants belonging to these genuses are pharmacologically active and have been used in folk medicine all around the world. The aim of the present study was to detect the essential oils composition of Hymenocrater longiflorus Benth. collected from Paveh, Kermanshah province. Plant sample was dried in shade condition and the essential oil of the plant obtained by hydrodistillation by Clevenger type apparatus was analyzed by GC/MS. Yield of essential oil was (1.5 % v/w). The major components of the oil of H. longiflorus Benth were Hedycarvol (22.2), α-Cadinol (20.43), β-Bourbonene (5.76%), α-Terpineol (4.95%), Eudesmol<7-Epi-> (4.84%), β-Bourbonene (4.69%), Caryophylene oxide (4.32%) and Geijerene (4.08%), Caryophelen (2.99), Sabinene (2.6%), 1,8-cineole (2.58%), δ-Amorphene (2.58%), δ-Caddinene (2.24%) and α-Pinene (2.07%) were the main compounds with the greatest content.

A green and efficient one-pot, four-component synthesis of 6-Amino-4-aryl-3-methyl-2,4-dihydropyrano[2,3-c]pyrazo-carbonitrile derivatives catalyzed by borax in water is described. This method provides several advantages such as environmental friendliness, shorter reaction time, excellent yields, and simple workup procedure. The in vitro cytotoxic activity of the synthesized test compounds was investigated against cancer cell lines (SW48, A549, KB, HepG2) in comparison with doxorubicin, a well-known anticancer drug, using MTT colorimetric assay. Our compounds showed good and reasonable cytotoxicity than doxorubicin in some studied cell lines. The compounds 5b (2,4-dimethoxy derivative), 5c (3,4,5-trimethoxy derivative), 5g (4-chloro derivative) in KB cell line (IC50 = 8±2.217 µM, 7±2.77 µM, 7.5± 1.49 µM respectively), 5f (3-chloro derivative) in A549 cell line (IC50 = 31.5±2.02 µM), 5g (4-chloro derivative) in HepG2 cell line (IC50 = 22.5±3.09 µM), 5e (2-chloro derivative), and 5i (4-nitro derivative) in SW48 cell line (IC50 = 23± 0.772 µM, 23± 4.97 µM respectively) showed the best results in close to the control drug.

Amphiphilic cationic micelles have recently attracted much attention as non-viral vector. In the current study the retinoic acid-g-chitosan (RA-chitosan) micelles have been used as novel gene carriers. Uptake of micelles, condensation ability and transfection efficiencyof micelle–DNA complexes (miceplexes) in the presence or absence of serum had been investigated on Hela and HepG2 cell lines. Uptake of micelles in Hela cells was faster and more effective than HepG2. After 1.5 hours, micelles were up-taken by Hela cells while no uptake was observed in HepG2 cells. Miceplexes showed lower transfection efficiency in both Hela and HepG2 cells grown in the serum free medium than chitosan polyplexes, with 7.25 × 105 versus 1.47 × 105 and 7.76 × 105 versus 2.16 × 105, respectively. Lower transfection efficiency of miceplexes could be attributed to their stronger complexation. Transfection in the presence of serum was increased in both of the cell lines. These properties all together, make RA-chitosan micelles as a potential gene carrier for active gene delivery into cells, particularly for transfection in the presence of serum.

A precise and feasible reversed-phase high-performance liquid chromatographic method for the determination of an antipsychotic drug quetiapine fumarate (QTF) in pharmaceuticals and spiked human urine sample has been developed and validated. The analysis was carried out using a ODS (250 mm × 4.6 mm i.d., 5 µm particle size) chromatopack column. Mobile phase containing a mixture of acetonitrile and 0.1% phosphate buffer (pH 3.1) (40:60) was pumped at a flow rate of 1 mL/min with UV detection at 240 nm at ambient column temperature (25 ºC). The method showed good linearity in the range of 0.09 – 18 µg/mL QTF with limits of detection (LOD) and quantification (LOQ) values of 0.03 and 0.09 µg/mL, respectively. The suggested method was successfully applied for the analysis of QTF in bulk drug, tablets and human urine with average recoveries of 100.06, 100.26 and 98.83%, respectively. The intra- and inter-day RSD values were less than 5%. The method is accurate, precise, sensitive and selective for routine analysis in quality control laboratories.

The main objective of this study was to design, formulate and evaluate the physicochemical properties of 500 mg acetaminophen effervescent tablets, in order to accelerate its analgesic and antipyretic effects in patients with pill swallowing problems. Formulations with 500 mg of acetaminophen were prepared with effervescent bases including tartaric acid, citric acid, sodium bicarbonate, and PEG6000. Flowability of powders and granules was determined by measurement of bulk and tapped density, compressibility index and Hausner's ratio. Three methods were applied to prepare tablets: direct compression, wet granulation and fusion. The effervescence time, hardness, pH, thickness, CO2 content, water content, weight variation, and content uniformity of the prepared tablets were investigated. In order to overcome the bitter taste of acetaminophen, different sweeteners and fruity essences such as orange, lemon, and cherry flavors were applied. Panel taste was performed using 20 volunteers. The physicochemical characteristics of three different methods of preparing tablets were pretty similar. Wet granulated formulations had higher hardness and better flowability while direct compressed tablets had stable effervescence time and better solubility. According to the panel taste, orange flavor was more acceptable. Wet granulated tablets which were prepared using alcohol and PVP had higher hardness and variable effervescence time in comparison to direct compressed tablets. Flowability of wet granulated formulations was better than the one of direct compressed formulations.

Different species of Artemisia (Asteraceae) have shown to exhibit antitumor activity. The aim of this study was to identify the antiproliferative effect of Artemisia aucheri Boiss (A.aucheri) from Iran on cultured human cancer cells. Aerial parts of Artemisia aucheri Boiss. were collected from Chahar Bagh region (2150 m altitude, Sep. 2011),Golestan province, Iran.The dried powdered aerial parts of A.aucheri were extracted with petroleum ether (40-60), dichloromethane, ethyl acetate, ethanol and ethanol-water (1:1 v/v), respectively.For biological investigation different concentrations of extracts were added to cultured cells and incubated for 24 h. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was employed to assess the cell viability.In addition,morphological changes of cells were assayed using phase contrast inverted microscope. Different extracts exert various growth inhibitory effects. In case of SKNMC,MCF-7 and A2780 cells, pertroleum ether extracts (IC50 values: 21.0, 26.0 and 28.0 µg/ml, respectively) showed the highest growth inhibitory effects. Dichloromethane extracts showed IC50 values: 27.0, 35.0 and 55.0 µg/ml, respectively.This study shows the antiproliferative effects of A.aucheri petroleum ether extract on malignant cell lines. Thus, may be considered as a promising chemotherapeutic agent in cancer treatment.

Polyphenol oxidase (PPO), also known as tyrosinase (EC 1.14.18.1), is a copper-containing enzyme widely distributed in microorganisms, animals, and plants. This enzyme is responsible not only for browning in plants but also for melanization in animals. Thus, tyrosinase inhibitors have a huge impact on industry and the economy. In the current study, we first purified the enzyme, then evaluated inhibitory potency of three benzaldehyde derivatives: 2,4-dihydroxybenzaldehyde, 3,4-dihydroxybenzaldehyde and 4-dimethylaminobenzaldehyde on diphenolase activity of the purified mushroom tyrosinase, compared to kojic acid. Despite their close structural similarity, 2,4-dihydroxybenzaldehyde was found as potent competitive inhibitor while uncompetitive inhibition was observed for 4-dimethylaminobenzaldehyde. Further complementary studies on these types of inhibitors, as potential drugs for treating abnormal melanin pigmentation, are needed.

The composition of the essential oil from the stalks and flowers of Rheum ribes L., growing in Iran, were extracted by hydrodistillation and analyzed by GC-MS. Thirty constituents representing 93.84% of Rheum oil were identified. The oil was found to be rich in hydrocarbons especially long-chain n-alkanes (80.81%). The most abundant components in the oil included tricosane (26.29%), heneicosane (26.07%), pentacosane (10.63%), heptacosane (10.37%) and palmitic acid (3.64%). The essential oil was also evaluated for general toxicity bioassay using brine shrimp lethality method. The toxicity profile of the oil indicated some degree of toxicity in comparison with podophyllotoxin.

Thermo-sensitive polymers were prepared by graft copolymerization of gelatin with N-Isopropylacrylamide via gamma radiation. Characterization of polymers such as DSC analysis, swelling in different ratios and cell assays were investigated. DSC and solubility analysis showed gelatin and NIPAAm monomer were grafted via gamma radiation successfully. Results show swelling of samples increased with to gelatin increasing. Swelling ratio and curves results administrated hydrophilicity / hydrophobicity of hydrogel that this property is due to presence of PNIPAAm in different temperatures. The polymer was tested for harvesting epithelial cells after carrying out cell culture at 37 °C and incubating the confluent cells at 10°C for spontaneous detachment of cell sheet from polymer surface without enzyme treatment. These unique properties of the hydrogel would make it a promising support for drug delivery systems and tissue regeneration.

Multi-drug therapy in high blood pressure is appreciated to achieve a normalblood pressure.A simple spectrophotometric method based on principal component analysis has been proposed for simultaneous determination of amlodipine (Amd) and metoprolol(Met) in pharmacutical preparations. Calibration matrix contains 3.402 µgml-1to 170.130 µgml-1and from 13.060 µgml-1to 65.3 µgml-1amlodipine and metoprolol, respectively. The proposedmethod was validated by using a set of synthetic sample mixtures and subsequently applied to simultaneousdetermination of amlodipine (Amd) and metoprololin different pharmaceutical preparations.

Gastric emptying is a complex and extremely variable process. This causes the unpredictability of the bioavailability of drug delivery systems. Gastro retentive drug delivery systems (GRDDS)s have received significant interest in the past decades as they can overcome the limitation of conventional oral controlled release drug delivery systems related to fast gastric emptying time. An optimum GRDDS can be defined as a system which remains in the stomach for a sufficient time interval and releases active ingredients in a controlled manner. This, significantly extends the duration of drug release, prolongs dosing interval and increases bioavailability of drugs and therefore improves compliance of the patients and effectiveness of pharmacotherapy.This article gives an overview of the main concepts used to design pharmaceutical dosage forms with prolonged gastric residence times as well as the parameters effecting gastric emptying, advantages, shortcomings, formulation considerations and, factors effecting gastro retentive systems. The main emphasis is on the entire classification and different types of GRDDSs. Finally evaluation methods of these systems have been summarized.

Molecular Chaperones or Amyloid-binding compounds? Perspective on Their Application as Possible Therapeutic Agents in Reduction of Cytotoxicity of Amyloid Oligomers