Journal Of Pharmaceutical and Health
Volume:4 Issue: 2, Summer 2016

HIE-124 is a new member of ultra-short acting hypnotics’ drug family. In this research, the synthesis of analogues of HIE-124 drug in the heterocyclic thiazole ring replaced to thiadiazole, will be presented. Thiadiazolodiazepines during a two-step reaction starting from the amino thiadiazole resulted from-various derivatives of benzoic acid and thiosemicarbazide were synthesized. In the first step, the reaction of synthetic raw material 2-amino thiadiazole and 4-chlorobutyrilchloride in toluene solvent give the 4-chloro-N-(5-(methyl/aryl)-1,3,4-thiadiazol-2-yl) butanamide intermediate. In the next step, from the cyclization reaction of this intermediate ring in the presence of base under reflux, the target products are synthesized. Structure of products was identified based on IR, HNMR and CNMR spectroscopy analysis. Then, the procedure of docking of ligands were performed on the active site of GABAA that the common residues involved in allosteric modulators such as benzodiazepines and HIE-124 include ASN82, ASN81, PHE79, MET1, TYR106, ALA38 and AlA168. Consequently, These Docking calculations suggest that these new compounds might be having better interaction results between receptor (GABAA) than HIE-124.

Breast cancer affects Iranian women at least one decade younger than their counterparts in other countries and the incidence of breast fibroadenoma is growing in the last two decades in Tehran. This study aimed to compare the AhR levels in premenopausal breast cancer and breast fibroadnemo with appropriate normal groups. Possible associations of AhR with lifestyle and reproductive risk factors and other fundamental genes of breast cancer and reproductive disorders were the other major goals of present study. To conduct the comparisons all possible reproductive, environmental and lifestyle risk factors of mentioned diseases were recorded in 100 breast cancer, 100 breast fibroadenoma and compared with 400 women in normal group from 2009 to 2011. AhR overexpression in epithelial cells of premenopausal patients emphasized the susceptibility of these cells to environmental induced reproductive disorders. The AhR overexpression was contributed to ER-/PgR- immunophenotype in malignant tissues. Weight gain (after 18 and after pregnancy), long term (>5yrs) OCP consumption, smoking, severe stress ,history of ovarian cysts, hormonal deregulations, living near PAHs producing sources, were correlated with increased risk of breast cancer and reproductive disorders and were correlated with elevated tissue levels of AhR. It seems that increased risk of breast cancer and other reproductive tumours in Tehran may be the result of exposure to environmental endocrine disruptors. Long term exposure to environmental estrogens can increase the tissue levels of AhR and deregulate the expression pattern of sex steroid receptors and other genes in target tissues.

Chronic kidney disease (CKD) is a major public health problem that often goes unrecognized until late-stage disease. Patients with chronic kidney disease face with uremic toxins and hyperkalemia. Also fluid overload in CKD patients is associated with rapid decline in kidney function. Lactulose is a hyper osmotic agent and as a prebiotic plays an important role in regulating serum urea and potassium levels and have some effects on fluid overload. The aim of this study was to evaluate effect of lactulose on serum levels of biochemical products in patients with CKD. In this interventional study 17 patients with end stage of CKD (76.47 % men; mean age 65.88 ± 13.4) were evaluated. All patients received lactulose, 10 ml, 3 times per day for 3 months. Blood samples from all participants were collected before and at the end of intervention to examine changes in biochemical parameters, including potassium, urea, creatinine and uric acid. Lactulose significantly decreased urea levels (p=0.001), blood potassium (0.001) and fluid overload(with due attention to patient’s weight p=0.001) in patients with end-stage renal failure. The decrease in serum creatinin anduric acidwere not significant. Lactulose administration in CKD patients could decrease levels of various deleterious elements especially urea and blood potassium, and its daily use can be recommended in these patients.

In this research, acute toxicity (LC) of zinc oxide nanoparticle on Beluga (Huso huso) and common carp (Cyprinus carpio) was studied. The experiment was conducted using the Organization for Economic Co-operation and Development (No. 202) method. For both species, 96hLC10 was determined to be more than 200 mg/l. To assess the effects of zinc oxide nanoparticles on blood factors, leukocyte index count (Lymphocyte, Monocytes, Neutrophils, Eosinophil, and Basophils) was performed, and the results were analyzed using IBM SPSS software version. According to the results and based on the ANOVA test, there is no significant difference among mean values of leukocyte index responses (p>0.05), and one should note that the amount of lymphocyte had decreased while that of neutrophils and monocytes had increased. Furthermore, with regard to concentration levels, this decrease or increase has not followed a systematic trend. In Beluga based on ANOVA test, there is a significant difference between mean values of lymphocytes and neutrophils (p

Plants are almost reach sources of phenolic compounds such as flavonoids which are the most important natural antioxidants. Antioxidant compounds are essential for protecting human body against oxidative stress. However use elicitors could increase the antioxidant activity of plant. The purpose of this study was to evaluate the effects of Chitosan on the content of phenolic and flavonoid compounds and also antioxidant activity Mentha piperita L.In this study, firstly the Mentha piperita L. were grown up for 6-week period at greenhouse conditions and then were treated with 50-100 µm of chitosan, then total phenolic and flavonoid contents were determined using spectrophotometry and finally antioxidant activities of extracts were evaluated with 2,2-diphenyl-1-picryl hydrazyl (DPPH) method and the results were analyzed with Excel software and Variance analysis testing method with SPSS software. The results showed the content of phenolic compounds in the methanol extract based on sample mg of Gallic acid /g for control with water, 50µm and 100µm treatments respectively were 146.8,233.1,339.1. Meanwhile the total volume of flavonoid content of the methanol extract per mg of Rutin/g respectively were 9.88,12.11,14.06 and concentration of the said extracts respectively were 196.3,147.7,128.62. In regard to the above results it can be concluded that due to having phenolic and flavonoid contents, Mentha piperita L showed that antioxidant activity could be stimulated upon Chitosan treatment moreover, antioxidant activity increased by increasing Chitosan treatment content. Therefore, this method can be used to increase antioxidant effect of plant as a natural antioxidant and all the phenolic and flavonoid contents.

Given the inappropriate use of antibiotics and prevalence of resistant bacteria, there is urgent need for antibacterial drugs that have fewer side effects than antibiotics. Satureja bachtiarica is a medicinal plant which had many uses in traditional medicine. In this research, the ethanol extract of leave of Satureja bachtiarica is tested on coagulase-negative staphylococcus strains. Materials and Methods In this experimental study, after collecting and drying the plant extract, the ethanolic extract of the plant was extracted by soxhelet method. Then, the antibiotic resistance pattern of coagulasenegative staphylococcus strains to Cefoxitin, Tobramycin, Kanamycin, Amikacin, Gentamicin, was assessed. To evaluate the antibacterial activity, the minimum inhibitory concentration was assessed by using micro dilution broth method. The results of this study showed that the antimicrobial effect of Satureja extract is concentration dependent. The results of the antimicrobial activity of extracts, indicate that alcoholic extract in all dilutions have an antimicrobial effect on the coagulase-negative staphylococcus strains. The results show that coagulase-negative staphylococcus strains have highest resistance against Cefoxitin (0.39 mg/ml) and highest sensitivity to Amikacin (0.035 μl/ml). However, in 200 and 100 mg/ml concentrations the extract has higher antibacterial effect. According to the results of this study, ethanol extracts of leave of Satureja bachtiarica had growth inhibitory effect on coagulase-negative staphylococcus strains. Therefore this plant has the potential to be evaluated as an alternative or adjunct to antibiotics to treat coagulase-negative staphylococcus infections.

Because of inappropriate use of antibiotics and prevalence of resistant bacteria, there is urgent need for antibacterial drugs that have fewer side effects than antibiotics. Myrtus communis is a medicinal plant which had many uses in traditional medicine. In this study, ethanol leave extract of this plant is tested on Acinetobacter baumannii. In the case of antimicrobial evaluation of plants, one of the effecting factors on effectiveness of the microbial inhibition is extraction techniques. In the presents study, the antibacterial activity of the Ethanol, Methanol, and Ethyl acetate extracts of M. communis plant was evaluated at seven different concentrations by broth microdilution method. The results of this study showed that the antimicrobial effect of M. communis extract is concentration dependent. Different extracts were obtained by the maceration method. Extracts of the plant exhibited antibacterial activity at varied levels against A. baumannii. Obtained results from our antibacterial experiments showed that all extracts have anti-bacterial activity against tested bacterial isolates According to the results, the ethyl acetate extracted fraction showed the highest level of activity at a MIC 400 mg/ml for A. baumannii. The results of this study indicate that, different extracts had growth inhibitory effect on A. baumannii. Therefore this plant has the potential to be evaluated as an alternative or adjunct to antibiotics to treat Acinetobacter infections.

The adsorption of a number of amino acids on a defected single-walled carbon nanotube (SWCNT) is investigated by using the density-functional theory (DFT) calculations. The adsorption energies and equilibrium distances are calculated for various configurations such as amino acid attaching to defect sites heptagon, pentagon and hexagon in defective tube and also for several molecular orientations with respect to the nanotube surface. The results showed that amino acids prefer to be physisorbed on the outer surface of the defected nanotube with different interaction strength following the hierarchy histidine > glycine > phenylalanine > cysteine. Comparing these findings with those obtained for perfect SWCNTs reveals that the adsorption energy of the amino acids increase for adsorption onto defected CNTs. The adsorption nature has also been evaluated by means of electronics structures analysis within the Mulliken population and DOS spectra for the interacting entities.