Microwave assisted solid support synthesis of novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazepines as potent antimicrobial agents

An environmentally benign and economic synthesis of 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazepines is described from readily accessible substituted 2-mercapto-1-amino triazoles and substituted chalcones on basic alumina that are accelerated by exposure to microwaves. The reaction time has been brought down from hours to seconds with improved yield as compared to conventional heating. The method reported herein is devoid of the hazards of solution phase reactions. All the synthesised compounds were tested for their in vitro antibacterial and antifungal activity. Some compounds showed significant antimicrobial properties. The best activity was observed with compounds 3a, 3c, 4a and 4d.     

Acetylation of amino groups and its effect on the conformation and immunological activity of obalbumin.

A procedure is described for the specific acetylation of the lysine residues of ovalbumin. Six acetylated ovalbumins varying in the degree of modification from 21 to 98% were prepared and were found to be homogeneous by polyacrylamide gel electrophoresis, immunodiffusion, and immunoelectrophresis. As expected, the anodic movement of ovalbumin increased and the isoionic point shifted to lower pH values with progressive acetylation of the protein. Measurements on ultraviolet absorption, fluorescence, tryptic digestion, intrinsic viscosity, gel filtration behavior, and immunological reactivity demonstrated that the native folded conformation of ovalbumin was appreciably altered by acetylation. However, even the maximally modified ovalbumin retained considerable residual structure consisting of regions of ordered structure containing antigenic determinants.     

The use of TMA for interlaboratory validation of FISH testing for detection of HER2 gene amplification in breast cancer.

HER2 fluorescence in situ hybridization (FISH) testing for breast cancer is largely limited to academic centers and commercial laboratories. As testing demands increase, methods for rapid and cost-effective technical validation and quality assessment will be required. Tissue microarray (TMA), a technique for high-throughput biomarker evaluation, could help facilitate these needs. Our objective was to assess the usefulness of TMA technology for validation of HER2 FISH testing. Two TMA blocks containing paired cores from 41 breast cancers were constructed. HER2 FISH was performed in parallel at two institutions and the results compared. One institution, with considerable HER2 FISH experience, served as the reference laboratory. HER2 chromogenic in situ hybridization (CISH) and immunohistochemistry (IHC) were compared to the FISH results. For positive and negative results, the concordance rate between laboratories was 100%. Using kappa statistical analysis to determine interobserver agreement, HER2 to chromosome 17 gene copy ratios showed strong agreement between laboratories with kappa = 0.85 (perfect agreement = 1.0). Four cases displaying low-level amplification by CISH contained chromosome 17 polysomy and gene copy ratios of <2.0 by FISH. Good concordance was observed between HER2 IHC and in situ hybridization testing. TMA is a robust and effective method for the technical validation of HER2 FISH testing and should be considered for use by quality assessment programs.     

Production of ganoderic acid by Ganoderma lucidum RCKB-2010 and its therapeutic potential

The newly isolated basidiomycetous fungus, identified as Ganoderma lucidum RCKB-2010 was tested for production of ganoderic acid (GA) under submerged fermentation conditions. Production of GA under liquid static cultivation condition was found to be 2,755.88 mg L^?1 on the 25th day of incubation, whereas under shaking cultivation conditions the maximum production of GA was observed to be 373.75 mg L^?1. ¹H NMR analysis revealed clearly that the fungal extracts possessed a lanostane skeleton, confirming the presence of GA. Interestingly, GA was found to have potential to inhibit the proliferation of HeLa cells and U87 human glioma cells in a dose dependent manner. In addition, GA was also found to possess antibacterial activity, exhibiting a minimal inhibitory concentration of 0.25 mg mL^?1 against standard strains of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus epidermidis. GA produced in the present study holds potential as a potent anticancer agent.     

Components of fast and slow phases of axoplasmic flow

Abstract— Cat ventral roots removed at times from hours to days after injection of [³H]leucine into the seventh lumbar and first sacral spinal cord segments were homogenized and subjected to sub-cellular fractionation. The soluble fraction was further analysed for protein content by column chromatography with Sephadex. The fast phase of axoplasmic flow carries down labelled free leucine, polypeptide, and soluble protein. The slow phase of axoplasmic flow carries down labelled soluble protein. The sub-cellular components were labelled with the small particulate fraction showing a higher specific activity than the other sub-cellular fractions.     

Deacylation of Cephalosporins by Lipase Catalysis and Microwave Assisted Transformation on a Solid Support

Deacylation of cephalosporins has been investigated using enzymatic and microwave activated solid phase techniques. The lipase calatysed deacylation was achieved under cooling with good yields but the microwave method was much faster with better yields. All the synthesised compounds were screened for their antibacterial activity and showed good results.     

1-Aryl-4,6-diamino-1,2-dihydrotriazine as antimalarial agent: a new synthetic route

Some novel derivatives of 1-aryl-4,6-diamino-1,2-dihydrotriazines have been synthesized using neat technology under microwaves. These were tested in vitro against both sensitive and resistant Plasmodium falciparum strains for antimalarial activity.     

A rapid method for preparation of sarcolemma from frog skeletal muscle

A rapid method for the preparation of sarcolema from frog skeletal muscle has been described. The purified cell segments were transparent and devoid of contractile material. The Na⁺, K⁺ -ATPase and 5'-nucleotidase activities in sarcolemma purified by this method were comparable to those reported for sarcolemmal preparations purified by density gradient centrifugation. The preparation also possessed acid phosphatase, alkaline phosphatase and K⁺ -activated, ouabain-sensitive p-nitrophenyl phosphatase activities. The cholesterol to phospholipid ratio of the sarcolemma was 0.33, indicating its high purity; further, the preparation was free from mitochondria and contractile proteins.