Iranian Journal of Pharmaceutical Sciences

In different folk medicine Ziziphus spina-christi is used for different purposes such as pneumonia, dysentery, scorpion stings, cough, constipation, intestinal worms and fever. The aim of this study was evaluation and comparing the antibacterial activity of methanolic and ethanolic extracts of Ziziphus spina –christi as well as subsequent structural changes in affected bacteria. For this purpose, ethanolic and methanolic extracts were prepared by 80% alcoholic solution. Antibacterial activity of these extracts was assessed using standard disc diffusion method against pathogenic bacteria. Sterile filter paper discs (6mm) were saturated by four different concentrations of each extract. The prepared discs were placed on lawn cultures of test bacteria and incubated at 37 0C for 24 h. After incubation the inhibition zone diameter around each disc was measured in millimeter. The induced changes in shape of affected bacteria were discovered using scanning electron microscopy (SEM). As a result of this study maximum
inhibition zone diameter in case of methanolic extract were 18 and 14 against Staphylococcus aureus, Bacillus cereu, and in case of ethanolic extract was 15 mm for S. aureus and Proteus mirabilis. The methanolic extract of this plant was more effective against S. aureus and B. cereus than the ethanolic extract even at high concentration. While the ethanolic extract was more active on Proteus mirabilis. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) indexes of both extracts were equal (MIC= MBC=8 mg/ml) for S. aureus. The SEM analysis revealed cell deformation and irregular shape in both S. aureus and B. cereus. These results suggest significant antibacterial activity of this plant especially against S. aureus, which its resistant strains are currently a great hazard in infection treatment. So, this plant should be considered as a potential source for finding new antibacterial agents.

Liver is a major organ of the body which can be exposed to various chemicals, drugs, and many other xenobiotics such as bromobenzene. Bromobenzene must be converted to its active metabolites to produce liver and kidney toxicity. Livergol is an herbal product which contains silymarin. The objective of this study was to find out the protective effect of livergol against liver toxicity induced by bromobenzene in mice. In this study, doses: 50, 100, 200, 300 mg/kg of livergol were administrated to mice orally 2 hours after bromobenzene(460 mg/kg) administration for 7 days (test groups). The negative control group received normal saline. The positive control group received 460 mg/kg of bromobenzene orally. 24 hours after the last administration animals were sacrificed; their blood was collected to determine serum enzyme activities of aspartate aminotransferase (AST) , alanine aminotransferase (ALT) and alkaline phosphatase (ALP). The livers were removed for histological examination.The results showed that livergol at doses 200 and 300 mg/kg cause significant reduction in the level of enzymes (p > 0.05). The histopathological study of liver tissues showed that doses of 200 and 300 mg/kg are more effectively restore tissue damage to the normal state. Our finding indicated that livergol in the high doses (200 and 300 mg/kg) have protective effects and cause significant improvement in the liver tissue and biochemical markers in bromobenzene intoxicated mice.

Pathogenic infections and inflammation are very common ailments humans suffer. Upsurge of resistant pathogens has impeded the antimicrobial drug development process in recent years and the search of new antimicrobial agents is clearly evident from the literature. In line with these developments the synthesis of N-substituted aryl-2-({4-[(substituted aryl carbamoyl) methyl]-5-(pyridin-4-yl)-4H-1, 2, 4-triazol-3-yl} sulfanyl) acetamide derivatives as antimicrobial, antioxidant and anti-inflammatory had been undertaken. The synthesis of target derivatives was achieved in three steps viz. potassium-pyridine-dithiocarbazate (II) obtained from base catalyzed reaction of isoniazide with CS2 which was further cyclized with hydrazine hydrate and CS2 to afford 4-amino-5-(pyridine-4-yl)-4H-1,2,4-triazole-3-thiol (III). This compound upon reaction with different aromatic N-substituted-α-chloroacetanilide afforded title compound N-substituted aryl-2-({4-[(substituted aryl carbamoyl) methyl]-5-(pyridin-4-yl)-4H-1, 2, 4-triazol-3-yl} sulfanyl) acetamides IV (KA1-KA15). All the newly synthesized derivatives were screened for in vitro antibacterial activity carried out against four bacterial strains viz. E.coli, K.pneumonia, S.aureus, and B. Subtilis and antifungal activity against two fungal strains viz. A.niger and S. cerevisiae by minimum inhibitory concentration (MIC) method, in vitro antioxidant activity was carried out by hydrogen peroxide radical scavenging method, and in vitro anti-inflammatory activity by inhibition of protein denaturation method. From the results of screening, it is evident that most of the derivatives KA3, KA4, KA7, KA9, KA11, and KA14 were found to possess promising biological activities and the derivatives with presence of electron-withdrawing groups at o-, m- and p- position of the phenyl ring improve the activity considerably.

Tumor growth is characterized by uncontrolled cell division. For centuries, silver kushta powder, composed of nano and submicro silver particles, has been used in traditional Iranian and Pakistani medicine for the treatment of melanoma and breast cancer. We have found that these nanocomposite particles are similar to silver nanoparticles (AgNps) in size and shape and that there are so differences in their physicochemical properties such as silver content.In the present study, a comparison of cytotoxic effects of nanosilver(AgNps) and two silver kushtas [Iranian silver kushta (IKAg) and Pakistan silver kushta (PKAg)]have been conductedindifferent concentrations against tumor cell lines (MCF-7, HepG2, A549) and a normal cell line (MDBK) using MTT andTrypan blue exclusion tests.At first, Particle size was analyzed using the Malvern Zetasizer. The Z average diameters of samples (AgNps, PKAg, and IKAg) were64.08, 51.72 and 190.4 nm, respectively.The result of MTTtest showed no toxicity of both silver kushtas (IKAg&PKAg) toward the cancer cell lines and MDBK cells. The IC50 values of AgNpsdetermined for A549, HPG2, MCF-7, and MDBK were 5.94, 1.41, 3.68, and, 1.9 ppm, respectively. According to trypan blue (0.2% w/v) exclusion test, the cytotoxicity of the silver materials toward primary rat hepatocytes followed the order AgNps (100%) >AgNO3 (80.9%) >Pakistani silver kushta (48.35%)>Iranian silver kushta (45%).This result illustrated that the silver components [(IKAg) & (PKAg)] of the traditional kushtas do not penetrate the cancer cell membrane and do not show cytotoxicity. Therefore, kushtas are ineffective as anti-cancer agents. However, AgNps shows good anticancer properties.

The aim of the present study was to investigate the relationship between the polar surface area and other molecular properties of the model drugs and their transdermal permeability across the rat skin. Few model drugs which are weakly acidic (ibuprofen, aceclofenac and glipizide) and weakly basic (olanzapine, telmisartan and sildenafil citrate) were selected for the study based on Polar surface area (PSA). Ex- vivo studies were carried out in franz diffusion cell. The skin permeation parameters of the model drugs were correlated to the physicochemical properties. The physicochemical properties considered for the study have shown to be synonymous with the pre-established ideal properties for the transdermal permeation. In acidic drugs, the order of correlation of the physicochemical properties to flux was mol. wt. > total no. of hydrogen bonds > M.P > PSA > Log P > Log D > solubility. In basic drugs, the order of correlation of the physicochemical properties to flux was mol. wt > PSA > solubility > log P > log D> total no. of hydrogen bonds> M.P. The property considered for the study PSA has acquired 4th rank in acidic drugs with R2= 0.9465 and 2nd in basic drugs with R2= 0.9477. The prime important factor for the study PSA, has shown a tortuous effect on the permeation of the selected drugs, whereas further study of PSA in relation to skin permeability parameters by considering larger drug data sets may impart a clearer image of its influence on transdermal permeation.

Researchers have found a big interest in biological application of Fourier Transform Infrared (FTIR) spectroscopy. Evaluating many diseases, staging them and studying the chemical structures of different formed compounds in diseases are some of the research applications of FTIR. Cancer is also one of these diseases. Researchers are trying to set up FTIR methods to detect and diagnose cancer cells and follow up the treatment steps using FTIR. In this regard, cancer cells and tissues are under investigation. In order to study cancer cells in lab, it is important to find out the proper cell density on the disk, at the first step. In this regard, the effect of different densities and positioning of cancer cells on FTIR supporting disk are studied in the present project. At the first step calibration of the instrument is checked using bovine serum albumin (BSA). Cancer cells were collected from culture dishes and washed with normal saline, twice. Different concentrations of cells (10000-320000 cells/uL) were located on ZnSe disks and dried prior to spectroscopy. The samples were scanned in the mid-infrared range of 4000-400 cm-1, with the resolution of 2 cm-1. Each spectrum was collected by 100 sample scans. Microscopic images of the disk were also taken to find out the distribution of the cells on the disk. The results of this study showed that the right amount of cell number and positioning on the disk is a very important parameter in bio-spectroscopic quality for biological purposes.

The synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one was achieved in two steps, In first step, pyrazine-2-carboxamide dissolved in EtOH, 10% KOH solution with ClCH2COOH produced compound 2-(pyrazine-2-carboxamido) acetic acid (II) and in second step, compound (II) in (CH3CO)2O with aromatic aldehyde, and catalyst potassium acetate produced title compounds 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one (PA1-PA14). All the newly synthesized compounds structure were elucidated using various spectral techniques viz. FT-IR, 1H-NMR, GC-MS spectroscopy, and CHN elemental analysis data and screened for in vitro antimicrobial and antifungal activity. In vitro anti bacterial activity was carried out against organisms E.coli, K.pneumonia, S.aureus, and B. Subtilis as well as antifungal activity were carried out against A.niger and S. cerevisiae activity by minimum inhibitory concentration method. The most promising broad spectrum compounds PA3, PA4, and PA5 were observed and study data reveals that additions of different functional groups had varying effects on activity. In addition, the greater biological activities were observed when the electron-withdrawing groups like fluorine, bromine and chlorine were incorporated at p-position of the phenyl ring.

Miconazole is an imidazole antifungal agent, commonly applied topically to the skin or mucous membranes. The aim of this study was to examine the alternative method for gaining mechanism or the bimolecular changes caused by the possible teratogenic effects of Miconazole on mice fetus brain tissueusing FTIR-Microspectroscopy.The mice were injected with Miconazole(60 mg/Kg) on gestation day 9. Fetuses were dissected on day 15 of gestation and morphological and histological studies on thefetus were carried out. Sections (10 μm) of controland Miconazoletreated fetus brain tissue were used for FTIR measurement in the mid-infraredregion. The results were shown by spectra2ndderivativeand also subtracting from control spectra.A lower intensity in the lipid (2800–3000 cm-1) and amid I (1600–1800 cm-1) regions of Miconazole treated mice fetus brain tissue was observed compared to the control mice fetus brain tissue. No major spectral shifting was observed at amide I band, amide II band and nucleic acid regions.As a conclusion, FTIR-Microspectroscopycan be a useful tool forteratogenic measurement with a unique ability to identify the modified bimolecular structuresin mice fetus tissues.