Indolocarbazole glycosides related to rebeccamycin represent a promising category of antitumor agents targeting DNA and topoisomerase I. These drugs prefer to adopt a closed conformation with an intramolecular hydrogen bond between the indole NH group and the pyranose oxygen atom. Three pairs of indolocarbazole monoglycosides bearing an NH or an N-methyl indole moiety were synthesized and their biological properties investigated at the molecular and cellular level. Replacing the indole NH proton with a methyl group reduces DNA interaction and abolishes activity against DNA topoisomerase I. Surface plasmon resonance studies performed with a pair of water-soluble indolocarbazole glycosides and two hairpin oligonucleotides containing an [AT]4 or a [CG]4 sequence indicate that both the NH and the N-methyl derivative maintain a relatively high affinity for DNA (Keq = 2 - 6 x 10(5) M(-1)) but the incorporation of the methyl group restricts access to the DNA. The number of ligand binding sites (n) on the oligonucleotides is about twice as high for the NH compound compared to its N-methyl analogue. Modeling and 1H NMR studies demonstrate that addition of the N-methyl group drives a radical change in conformation in which the orientation of the aglycone relative to the beta-glucoside is reversed. The loss of the closed conformation by the N-methyl derivatives perturbs thir ability to access DNA binding sites and prevents the drug from inhibiting topoisomerase I. As a consequence, the NH compounds exhibit potent cytotoxicity against CEM leukemia cells with an IC50 value in the 1 microM range, whereas the N-methyl analogues are 10 to 100 times less cytotoxic. These studies offer circumstantial evidence supporting the importance of the closed conformation in the interaction of indolocarbazole glycosides with their molecular targets, DNA and topoisomerase I. 相似文献
Spent brewery grains (SBG), a by-product of the brewing process, were tested as an adsorbent of acid orange 7 dye (AO7), a monoazo acid dye currently used in paper and textile industries. The presence of AO7 in these effluents causes obvious environmental problems.
Kinetics studies of adsorption of AO7 to SBG (3.75%, m/v) were carried out at 20 °C, using aqueous solutions with different AO7 concentrations (30–834 mg/L). For every situations tested, no significant variation in residual AO7 concentration in solution was detected after 1 h contact between the dye and the adsorbent. The adsorption process followed a pseudo-first order model.
The equilibrium process showed to be well described by both Freundlich and Langmuir isotherm models, at 20 and 30 °C. The maximum adsorption capacity was estimated to be 30.5 mg AO7/g SBG, at 30 °C.
Free energy of adsorption (ΔG°), enthalpy (ΔH°), and entropy (ΔS°) changes were calculated to predict the nature of adsorption. The estimated values for ΔG° were −22.78 and −24.53 kJ/mol, respectively, at 293.3 K (20 °C) and 303.3 K (30 °C), which are rather low indicating that a spontaneous process occurred. The enthalpy changes and entropy of adsorption were 28.66 and 175.36 J/mol K, respectively. The positive value for ΔH° indicates that the adsorption of AO7 dye to SBG is an endothermic process. The positive value of entropy reflects the affinity of the adsorbent for AO7 dye.
The obtained results are very promising since: (i) high levels of colour removal (>90%) were achieved with low contact times adsorbent/dye (less than 1 h contact); and (ii) the whole SBG can be successfully used as adsorbent of AO7 dye in aqueous solution without needing any previous treatments such as milling and/or sieving. Spent grains, being a cheap, and easily available material, can be an alternative for more costly adsorbents used for dye removal in wastewater treatment processes. 相似文献
Bacteria from the genus Enterococcus sp. were isolated and identified from nonpasteurized milk samples obtained from the Costa Rican Metropolitan Area, in order to evaluate its sensitivity pattern to common use antibiotics. One hundred five milk samples were collected from suppliers of a national dairy industry. The initial isolation was done in EVA (Ethyl violet agar). Isolated colonies were initially characterized phenotypically as Enterococcus sp. using biochemical tests, species' identification was done using the Api 20 Strep kit. The different Enterococci species were tested for their antibiotic sensitivity using the plate diffusion method; the minimal inhibition concentration (MIC) to vancomycin was determined using E test. 38% of the milk samples were positive for Enterococcus; 48 different strains were isolated, where E. faecalis corresponded to 71%, E. faecium to 19%, E. durans to 4%, E. gallinarum to 4% and E. avium to 2%. The geographical distribution analysis of the species isolated did not show significant statistical differences according to the origin of the samples. All isolates identified showed an important resistance rate to the antibiotics tested. The aminoglycoside family showed the lower resistance rate, the resistance to eritromicin, tetracycline and chloranphenicol was lower than 50% and all strains were sensitive to bacitracin. An 8% resistance rate to vancomycin was determined. No relationship between the resistance rate of samples and the province of origin was found, but it is important to emphasize that the strains resistant to vancomycin came from Cartago, one of the Costa Rican regions with highest milk production. 相似文献
Many metal-manufacturing industries include oxyfuel cutting among their manufacturing processes because cutting and welding
are often required in metal-cutting processes, specifically in the fabrication of pressure vessels and storage tanks. The
oxyfuel cutting process uses controlled chemical reactions to remove preheated metal by rapid oxidation in a stream of pure
oxygen. Previous research has demonstrated that metal cutting surfaces varied depending on the gas used for the combustion
as well as the cutting speed (Vc) used during the process. In this research, AISI 1045 carbon steel was cut using an oxyacetylene
and an oxypropane cutting process. Different tests, such as surface roughness, cut drag displacement, groove width, microhardness,
and microstructure, were used to analyze the influence of the Vc and the combustion flame (oxyacetylene and oxypropane). The
results showed, in general, better cut surfaces when using propane gas. Also, it was demonstrated that oxyacetylene cutting
is almost 85% more expensive than oxypropane cutting. 相似文献
The chemical compositions (organic and inorganic contents) and mechanical behaviors of the dentin of permanent and deciduous teeth were analyzed and compared using X‐ray fluorescence spectrometry (µ‐EDXRF) Fourier transform Raman spectroscopy (FT‐Raman) and a microhardness test (HD). Healthy fresh human primary and permanent molars (n = 10) were selected, The buccal surfaces facing upwards were stabilized in an acrylic plate, flattened, polished, and submitted to the µ‐EDXRF, FT‐Raman, and HD analysis. The results of the analysis were subjected to ANOVAs and Mann‐Whitney U/Student's t multiple comparisons tests. The data showed similar values for the dentin of the primary and permanent teeth in P content, organic content (amide I peak), inorganic content ( – 430 and 590), and microhardness, Nevertheless, Ca content and Ca/P weight ratio were higher, and the peak was lower in the dentin of the permanent teeth compared to primary teeth. It be concluded that despite permanent teeth showed more Ca element, both substrates showed similar behavior of chemical and physical properties. 相似文献
Automated Guided Vehicles (AGVs) are among various advanced material handling techniques that are finding increasing applications
today. They can be interfaced to various other production and storage equipment and controlled through an intelligent computer
control system. Both the scheduling of operations on machine centers as well as the scheduling of AGVs are essential factors
contributing to the efficiency of the overall flexible manufacturing system (FMS). An increase in the performance of the FMS
under consideration would be expected as a result of making the scheduling of AGVs an integral part of the overall scheduling
activity. In this paper, simultaneous scheduling of parts and AGVs is done for a particular type of FMS environment by using
a non-traditional optimization technique called the adaptive genetic algorithm (AGA). The problem considered here is a large
variety problem (16 machines and 43 parts) and combined objective function (minimizing penalty cost and minimizing machine
idle time). If the parts and AGVs are properly scheduled, then the idle time of the machining center can be minimized; as
such, their utilization can be maximized. Minimizing the penalty cost for not meeting the delivery date is also considered
in this work. Two contradictory objectives are to be achieved simultaneously by scheduling parts and AGVs using the adaptive
genetic algorithm. The results are compared to those obtained by conventional genetic algorithm. 相似文献