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Background and objectives: Trametes species have been used for centuries in traditional medicine of Asian countries. Recently, some of the bioactive compound have been isolated and evaluated for therapeutic purposes from these species. The aim of this study was to report the isolation and structure elucidation of major sterols from fruiting bodies of Trametes gibbosa. Volatile compounds and antioxidant activities of the different mushroom extracts of mushroom were also examined. Methods: The fruiting bodies of T. gibbosa were extracted with n-hexane, methanol, and hot water, respectively. For isolation of sterols, the n-hexane extract was subjected to column chromatography and fractionated by step gradient of n-hexane: ethyl acetate. The volatile oil was prepared by hydrodistillation and analyzed by GC-MS. For evaluation of the antioxidant activity, 2,2-diphenyl-1-picrylhydrazyl and ferric reducing antioxidant power assays were used. Moreover, the phenolic and carbohydrate contents were assessed using spectrophotometry methods. Results: The column chromatography of the n-hexane extract led to the isolation of three sterols. These compounds were identified for the first time in T. gibbosa as follows: ergosta-5,7,22-trien-3β-ol (ergosterol); 5,8-epidioxy-ergosta-6,22-dien-3-ol; 5,9-epidioxy-8,14-epoxy-ergosta-6,22-dien-3-ol. The most abundant volatile compounds were identified as aldehydes (29.01%), fatty acids (21.2%) and alcohols (12.07%). Based on antioxidant results, methanol and hot water extracts showed the highest activities in DPPH (EC50=588.56±36.37 µg/mL) and FRAP (432±6.6 mmol Fe2+/g DW) methods, respectively. Conclusion: Trametes gibbosa is a valuable source of mycochemicals such as sterols, carbohydrate and phenolics. Further investigations are required for evaluation of the therapeutic potentials of the isolated compounds.

Background and purpose: In medicinal chemistry, molecules containing rhodanine(2-thiazolidine-4-one) ring as a magic multifunctional privileged structural and functional scaffold show a broad range of potent pharmacological properties containing anti-microbial, antiviral, anti-diabetic, and anti-convulsant effects. Evidence suggests that the activity of the rhodanine derivative correlates with the size and the nature of the substituents at C-5 and N-3 positions. In this study, we synthesized new N-substituted rhodanine derivatives with arylidene substituent at the C-5 position via solvent-free Knoevenagel condensation reaction. We also investigated the antifungal activity of the compounds. Materials and methods: A mixture of aromatic aldehyde (1 mmol) and rhodanin derivatives (1 mmol) was stirred in choline chloride (ChCl)/urea deep eutectic solvent (1 mL) at 100C in an oil bath for 1 hour. The progress of the reaction was monitored by TLC (2:1 n-hexane/ethyl acetate). Then, the crude compound was collected by vacuum filtration and washed using ice-cold solvent. Results: Novel products were elucidated on the basis of elemental analyses as well as FTIR, Mass and 1H NMR, 13CNMR spectroscopy. Conclusion: A green, comfortable and rapid procedure has been developed for the synthesis of N-substituted rhodanine derivatives using ChCl/Urea Deep Eutectic Ionic Liquid (DEILs) under solvent-free conditions.

Background: Bioremediation of groundwater and soil contamination is more economical than physicochemical remediation. The present study focused on the bioremediation capability of two bacterial species (Klebsiella planticola and Enterobacter cloacae) from the family Enterobacteriaceae. These bacteria have been identified as new species with capability of degrading methyl tertiary-butyl ether (MTBE). In order to enhance their degradation capability, selected concentrations and retention time were investigated. Methods: The bacteria were cultured on the nutrient agar (NA) medium at room temperature. pH of the medium was adjusted to 7. The medium was autoclaved at 121°C for 15 minutes and incubated for 24 hours at 35°C. After 24 hours, the mixture was inoculated into 50 mL of Luria Bertani (LB) liquid medium containing 50 and 150 ppm MTBE. The cultures were incubated for 2 and 5 days at 35°C and shacked on a shaker at 150 rpm. Cell concentrations of the bacteria in pure culture were determined from the optical density at 600 nm using a UV–VIS spectrophotometer. Then, the culture was centrifuged at 3800 rpm for 20 minutes. In the next step, the MTBE concentration in the supernatant was measured by gas chromatography/mass spectrometry (GC/MS, Agilent Technologies, 5975, US10304411, 5.02.07). Results: The results showed that both strains are able to grow in the presence of 50 and 150 ppm MTBE. In the best conditions, when cell density was 3×108 CFU/mL during 5 days, the highest rate of MTBE degradation for K. planticola and E. cloacae, was 43% and 40%, respectively. It was also revealed that Escherichia coli can degrade 50 and 150 ppm MTBE about 19.8% and 13.65%, respectively. Conclusion: It seems that E. coli can be a good candidate for MTBE degradation at high concentrations for a time longer than that in the present study. It was also found that the species have high performance at 50 ppm than 150 ppm. So, these bacteria can remove MTBE from the environment.

Background and purpose: Increasing resistance of microbes to antimicrobial drugs necessitates the production of new compounds of more extensive activity together with low toxicity. Compounds containing quinoxaline and pyrazole cycles comprise important group of nitrogen-bearing heterocyclic compounds. These scaffolds possess a wide spectrum of biological effects including antimicrobial and anticancer effects. Materials and methods: Three steps procedure were designed to prepare the title compound. 3-(glycerol-1-yl)-1-phenyl flavazole was prepared by adding D-glucose, and ortho-phenylenediamine to phenylhydrazine in presence of acetic acid. Then, the desired aldehyde was obtained by adding sodium periodate to the solution. Finally, adding 4-aminoantipyrine gave the target product. Results: The considered imine compound was synthesized and its structure was confirmed using NMR, IR, and GC- Mass spectroscopy techniques. Conclusion: In this study, (1-H) pyrazolo [4, 5-b] quinoxaline was prepared using inexpensive and widely available materials. In present research, not only the reaction performance was improved, but also some time and resource savings along with enhanced efficiency were achieved. The method proposed is an efficient, simple, and fast method to synthesize the aforementioned compound with antibacterial potential.

Abstract With the aim of making specific targeting of silver nanoparticles as a drug for tumor cells and developing new anticancer agents, a novel nano-composite was developed. Albumin coated silver nanoparticles (ASNPs) were synthesized, and their anti-cancerous effects were evaluated against MDA-MB 231, a human breast cancer cell line. The synthesized ASNPs were characterized by spectroscopic methods. The morphological changes of the cells were observed by inverted, florescent microscopy and also by DNA ladder pattern on gel electrophoresis; the results revealed that the cell death process occurred through the apoptosis mechanism. It was found that ASNPs with a size of 90 nm and negatively charged with a zeta-potential of about −20 mV could be specifically taken up by tumor cells. The LD50 of ASNPs against MDA-MB 231 (5 μM), was found to be 30 times higher than that for white normal blood cells (152 μM). The characteristics of the synthesized ASNPs included; intact structure of coated albumin, higher cytotoxicity against cancer cells than over normal cells, and cell death based on apoptosis and reduction of gland tumor sizes in mice. This work indicates that ASNPs could be a good candidate for chemotherapeutic drug.

Objective(s):The mechanism of hypothermia action of acetaminophen (APAP) remains unclear even 125 years after its synthesis. Acetaminophen produces hypothermia. The mechanism of this reduction in core body temperature is not clear but evidence shows that it is not dependent on opioid and cannabinoid receptors. Because of strong documents about the roles of GABA and benzodiazepine receptors in hypothemic activity of some drugs such as diazepam, we determined if these receptors also contributes to the hypothermic effect of APAP. Materials and Methods: Diazepam (5 mg/kg, IP) was used for induction of hypothermia. Flumazenil (10 mg/kg, IP) or picrotoxin (2 mg/kg, IP) used for reversal of this effect. Rats injected with APAP (100, 200 or 300 mg/kg, IP). Baseline temperature measurements were taken with a digital thermometer via rectum. To evaluate the structural correlation between APAP and benzodiazepine receptor ligands, numerous models are selected and studied at HF/6-31G* level of theory. Relative energies, enthalpies and Gibbs free energies were calculated for all selected drugs. Results:Diazepam induced hypothermia was reversed by flumazenil or picrotoxin. Rats injected with APAP displayed dose- and time-related hypothermia. For combined administration, the hypothermic effect of APAP (200 mg/kg) was strongly reduced by pretreatment with picrotoxin or flumazenil P