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2-Deamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) is a potent in­hibitor of thymidylate synthase. Its analogue, Nα-[4-[N-[(3,4-dihydro 2-methyl-4 -oxo- 6-quinazolinyl)methyl]-N-propargylamino]phenylacetyl]-L-glutamic acid, containing p-aminophenylacetic acid residue substituting p-aminobenzoic acid residue, was syn­thesized. The new analogue exhibited a moderately potent thymidylate synthase inhi­bition, of linear mixed type vs. the cofactor, N5,10 -methylenetetrahydrofolate. The K value of 0.34 uM, determined with a purified recombinant rat hepatoma enzyme, was about 30-fold higher than that reported for inhibition of thymidylate synthase from mouse leukemia L1210 cells by ICI 198583 (Hughes et al., 1990, J. Med. Chem. 33, 3060). Growth of mouse leukemia L5178Y cells was inhibited by the analogue (IC50 = 1.26 mM) 180-fold weaker than by ICI 198583 (IC50 = 6.9 uM).
 Poly(ADP-ribose) polymerase (PARP) plays a crucial role in DNA repair. Modulation of its activity by stimulation or inhibition is considered as a potentially important strategy in clinical practice, especially to sensitize tumor cells to chemo- and radiotherapy through inhibition of DNA repair. Here we studied the effect of the three PARP inhibitors, 5-iodo-6-amino-benzopyrone (INH2BP), 1,5-isoquinolinediol (1,5-dihydroxyisoquinolinediol (1,5-IQD) and 8-hydroxy-2-methylquinazolin-4-[3H]one (NU1025), and for two of them the efficiency in slowing the rejoining of DNA strand breaks induced by H2O2 was compared. Inhibition of PARP changed its intranuclear localization markedly; cells exposed to the inhibitor NU1025 showed a significant tendency to accumulate PARP in large foci, whereas in untreated cells its distribution was more uniform. The speed and efficiency of rejoining of H2O2-induced DNA strand breaks were lower in cells incubated with a PARP inhibitor, and the kinetics of rejoining were modulated in a different manner by each inhibitor. At a concentration of 100 µM the efficiency of the inhibitors could be ranked in the order NU1025 > IQD > INH2BP. The two first compounds were able to decrease the overall PARP activity below the level detected in control cells, while INH2BP showed up to 40% PARP activity after exposure to H2O2.
The list of species of the plant parasitic nematodes presented in this paper (133 species belonging to 14 families) is based on the results of faunistic research conducted in the Wielkopolska region by Polish nematologists up until the year 2010, and the results obtained from the project “Elaboration of Innovative Methods for Rapid Identification of Nematodes Causing Damage to the Economy” managed by the Museum and Institute of Zoology of the Polish Academy of Sciences. During the two years of the project (2010-2011) we found 21 species of nematodes which had not yet been reported in the list of species from the Wielkopolska region. Two of them were reported for the first time in Poland.
This paper reports the results of an investigation of the effect of Zn2+, Mg2+, Cu2+, Ni2+, Fe2+, Fe3+, Mn2+ and Cr3+ ions present in the media on the kinetics of dissimilatory reduction of sulfates in Desulfotomaculum ruminis bacteria. It has been shown that the range of the optimum concentration of studied elements is different; sometimes very wide but sometimes very narrow. After a certain threshold concentration of a given element has been reached, its presence either causes total inhibition of the process or has a toxic effect.
Polyphenol oxidase (PPO) from hawthorn was extracted and partially purified through (NH4)2SO4 precipitation, dialysis and ion exchange chromatography. The activity of polyphenol oxidase was investigated in Crataegus spp. Spectrophotometric method was used to assay the enzyme activity and the kinetic constants - maximum enzyme velocity (Vmax) and Michealis - Menten constant (Km). Of the substrates tested, catechol was the best substrate for PPO with a Km value of 2.2 mM. The optimum pH for PPO activity was found to be 7. The enzyme showed high activity over a broad pH range of 4 - 8. The optimal pH and temperature for enzyme activity were found to be 7 and 40-45 °C, respectively. km value for hawthorn PPO is calculated 22 mM for catechol and 6.7 mM for pyrogallol and 9.7 mM for L-dopa. As can be seen, affinity of PPOs for various substrates varies widely. The enzyme showed a broad activity over a broad pH and temperature range. The thermal inactivation studies showed that the enzyme is heat resistant. The enzyme showed the highest activity toward pyrogallol and no activity toward tyrosine. Of the inhibitors tested, the most potent inhibitors were kojic acid, cysteine and glycine , respectively.
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Mannose inhibition of nitrate uptake by wheat roots

75%
The effect of mannose on nitrate uptake was investigated by a new non-invasive technique. Under normal condition, nitrate uptake by wheat (Triticum aestivum L.) roots was about 1-7 µmol gfwt-1 h-1. After the addition of 10 mM mannose, net nitrate influx by wheat roots started to decrease and reached a new steady state at -40 ±50% of the control value after 73 min. After mannose supplied for 2 h, its removal caused net nitrate influx to be recovered to an original rate. Therefore, the inhibition of mannose on nitrate uptake is not due to the onset of programmed cell death because it starts too rapidly and it is reversible, however, it is probably due to Pi and consequent ATP depletion.
Background. Pullulan is a water-soluble polysaccharide produced by fungi Aureobasidium pullulans. This glucan was applied for coating of food products. The aim of this study was obtaining of a pullulan coating and checking its effect on growth of microorganisms responsible for spoilage of food. Materials and methods. Pullulan produced by the white mutant A. pullulans B-1 was applied. Permeability of oxygen and carbon dioxide through film produced from 10% water solution of pullulan was checked as well as degree of inhibition of chosen microorganisms through pullulan coating formed on surface of growth‟s media. Results. Low permeability of gases through pullulan film and a considerable growth‟s limitation of all tested microorganisms were found. A total growth‟s inhibition of 21 from 36 tested strains and a partial growth‟s limitation of the remaining 15 strains was observed. The inhibitory effect was diverse and it was from 63 to 100%. Conclusions. These results proved that pullulan coating applied in these tests revealed big barrier characteristics in relation to oxygen and carbon dioxide, which had effect upon growth‟s inhibition of most of the tested microorganisms, responsible for spoilage of food
The influence of free base of quinolinilporphyrin and its Zn complex on infectivity of lactophages E3, E5 and E17 has been studied. The results of our investigations show that inhibition of lactophage activity by Zn complex of quinolinilporphyrin at concentration 10 μM and 20 μM was in the range 53–62% and 65–85%, respectively. The presence of this porphyrin in nutrient medium prevents the propagation of bacteriophage infection in Lactococcus lactis, but does not affect the phage adsorption process. The free base of quinolinilporphyrin slightly inhibits the activity of lactophages.
In this paper the effect of Mo6+, W6+, and Cu2+ ions on kinetics of denitrification and growth of Bacillus licheniformis is presented. The absence lack of Mo6+ and Cu2+ in the growth medium appeared to have no effect on the kinetics of the process. This fact suggests that these ions are not a part of the active centers of denitrification enzymes. Additionaly tungsten (VI) which is competitive to molybdenum (VI) does not inhibit denitrification in concentrations up to 0.1 g/dm3. Molibdenum (VI) starts to inhibit denitrification from 5.0 g/dm3 and copper (II) starting from 0.03 g/dm3.
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