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1.
We report the synthesis and the biological evaluation of two new analogues of the potent dimeric opioid peptide biphalin. The performed modification is based on the replacement of two key structural elements of the native biphalin, namely: the hydrazine bridge which joins the two palindromic moieties and the phenylalanine residues at the 4,4′ positions of the backbone. The new analogues 9 and 10 contain 1,2-phenylenediamine and piperazine, respectively, in place of the hydrazidic linker and p-fluoro-l-phenylalanine residues at 4 and 4′ positions. Binding values are: K\textim = 0.51 \textnM K_{\text{i}}^{\mu } = 0.51\,{\text{nM}} and K\textid = 12.8 \textnM K_{\text{i}}^{\delta } = 12.8\,{\text{nM}} for compound 9, K\textim = 0.09 \textnM K_{\text{i}}^{\mu } = 0.09\,{\text{nM}} and K\textid = 0.11 \textnM K_{\text{i}}^{\delta } = 0.11\,{\text{nM}} for analogue 10.  相似文献   

2.
3.
The research into kinetics of styrene biodegradation by bacterial strain Pseudomonas sp. E-93486 coming from VTT Culture Collection (Finland) was presented in this work. Microbial growth tests in the presence of styrene as the sole carbon and energy source were performed both in batch and continuous cultures. Batch experiments were conducted for initial concentration of styrene in the liquid phase changed in the range of 5–90 g m−3. The Haldane model was found to be the best to fit the kinetic data, and the estimated constants of the equation were: μ m = 0.1188 h−1, K S = 5.984 mg l−1, and K i = 156.6 mg l−1. The yield coefficient mean value Y\textxs\textapp Y_{\text{xs}}^{\text{app}} for the batch culture was 0.72 gdry cells weight (gsubstrate)−1. The experiments conducted in a chemostat at various dilution rates (D = 0.035–0.1 h−1) made it possible to determine the value of the coefficient for maintenance metabolism m d = 0.0165 h−1 and the maximum yield coefficient value Y\textxs\textM = 0.913 Y_{\text{xs}}^{\text{M}} = 0.913 . Chemostat experiments confirmed the high value of yield coefficient Y\textxs\textapp Y_{\text{xs}}^{\text{app}} observed in the batch culture. The conducted experiments showed high activity of the examined strain in the styrene biodegradation process and a relatively low sensitivity to inhibition of its growth at higher concentrations of styrene in the solution. Such exceptional features of Pseudomonas sp. E-93486 make this bacterial strain the perfect candidate for technical applications.  相似文献   

4.
The activation mechanism of Pseudomonas stutzeri cytochrome c peroxidase (CCP) was probed through the mediated electrochemical catalysis by its physiological electron donor, P. stutzeri cytochrome c-551. A comparative study was carried out, by performing assays with the enzyme in the resting oxidized state as well as in the mixed-valence activated form, using cyclic voltammetry and a pyrolytic graphite membrane electrode. In the presence of both the enzyme and hydrogen peroxide, the peak-like signal of cytochrome c-551 is converted into a sigmoidal wave form characteristic of an \textE\textr \textC\texti {\text{E}}_{\text{r}} {\text{C}}_{\text{i}}^{\prime } catalytic mechanism. An intermolecular electron transfer rate constant of (4 ± 1) × 105 M−1 s−1 was estimated for both forms of the enzyme, as well as a similar Michaelis–Menten constant. These results show that neither the intermolecular electron transfer nor the catalytic activity is kinetically controlled by the activation mechanism of CCP in the case of the P. stutzeri enzyme. Direct enzyme catalysis using protein film voltammetry was unsuccessful for the analysis of the activation mechanism, since P. stutzeri CCP undergoes an undesirable interaction with the pyrolytic graphite surface. This interaction, previously reported for the Paracoccus pantotrophus CCP, induces the formation of a non-native conformation state of the electron-transferring haem, which has a redox potential 200 mV lower than that of the native state and maintains peroxidatic activity.  相似文献   

5.
The chlorophyll a-specific absorption coefficient ( a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) ) in a highly eutrophic lake can show characteristics distinct from that in the ocean due to the differences in the structure and composition of phytoplankton. In this study, investigated the variation of a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) in Lake Kasumigaura, a highly eutrophic lake in Japan, in association with the package effect and the effect of accessory pigments, and carried out the parameterization of a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) . Although a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) did not vary spatially, it did show significant temporal variation, with a particularly high value after spring-bloom. This high a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) in spring was attributed to a lower package effect and a higher proportion of carotenoid than the other samples. Although the value of a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) was correlated with the concentration of chlorophyll-a (Chl-a), the correlation coefficient was lower than those reported in the ocean. Some lake-water samples showed variations of the package effect and the effect of accessory pigments that were independent of the concentration of Chl-a, and these independent variations resulted in the weak correlation between a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) and the concentration of Chl-a. Together, these results suggest that the factors controlling a\textph* ( l) a_{\text{ph}}^{*} \left( \lambda \right) in highly eutrophic lakes are distinct from that in ocean samples.  相似文献   

6.
Mammalian metallothioneins ( \textM7\textIIMTs {\text{M}}_7^{\text{IIMTs}} ) show a clustered arrangement of the metal ions and a nonregular protein structure. The solution structures of Cd3-thiolate cluster containing β-domain of mouse β-MT-1 and rat β-MT-2 show high structural similarities, but widely differing structure dynamics. Molecular dynamics simulations revealed a substantially increased number of \textNH - \textSg {\text{NH - }}{{\text{S}}^\gamma } hydrogen bonds in β-MT-2, features likely responsible for the increased stability of the Cd3-thiolate cluster and the enfolding protein domain. Alterations in the \textNH - \textSg {\text{NH - }}{{\text{S}}^\gamma } hydrogen-bonding network may provide a rationale for the differences in dynamic properties encountered in the β-domains of MT-1, -2, and -3 isoforms, believed to be essential for their different biological function.  相似文献   

7.
The effects of UVB radiation on the different developmental stages of the carrageenan-producing red alga Iridaea cordata were evaluated considering: (1) carpospore and discoid germling mortality; (2) growth rates and morphology of young tetrasporophytes; and (3) growth rates and pigment content of field-collected plant fragments. Unialgal cultures were submitted to 0.17, 0.5, or 0.83 W m−2 of UVB radiation for 3 h per day. The general culture conditions were as follows: 12 h light/12 h dark cycles; irradiance of 55 μmol photon.per square meter per second; temperature of 9 ± 1°C; and seawater enriched with Provasoli solution. All UVB irradiation treatments were harmful to carpospores ( 0.17  \textW \textm - 2 = 40.9 ±6.9% 0.17\;{\text{W}}\,{{\text{m}}^{ - 2}} = 40.9 \pm 6.9\% , 0.5  \textW \textm - 2 = 59.8 ±13.4% 0.5\;{\text{W}}\,{{\text{m}}^{ - 2}} = 59.8 \pm 13.4\% , 0.83  \textW \textm - 2 = 49 ±17.4% 0.83\;{\text{W}}\,{{\text{m}}^{ - 2}} = 49 \pm 17.4\% mortality in 3 days). Even though the mortality of all discoid germlings exposed to UVB radiation was unchanged when compared to the control, those germlings exposed to 0.5 and 0.83 W m−2 treatments became paler and had smaller diameters than those cultivated under control treatment. Decreases in growth rates were observed in young tetrasporophytes, mainly in 0.5 and 0.83 W m−2 treatments. Similar effects were only observed in fragments of adult plants cultivated at 0.83 W m−2. Additionally, UVB radiation caused morphological changes in fragments of adult plants in the first week, while the young individuals only displayed this pattern during the third week. The verified morphological alterations in I. cordata could be interpreted as a defense against UVB by reducing the area exposed to radiation. However, a high level of radiation appears to produce irreparable damage, especially under long-term exposure. Our results suggest that the sensitivity to ultraviolet radiation decreases with increased algal age and that the various developmental stages have different responses when exposed to the same doses of UVB radiation.  相似文献   

8.
Total height, diameter, index volume, stem straightness, apical dominance, and survival were assessed at 8 years from seed in an open-pollinated progeny test of 36 families of European chestnut (Castanea sativa Miller) established at two sites in the Atlantic area of Galicia, Spain. Iterative spatial analysis was applied to eliminate the effect of the spatial dependence in the original data and to estimate accurately genetic parameters for evaluating the potential for selection of the measured trees. Spatial analysis was very beneficial for growth traits and survival, but less so if at all for form traits. Estimated individual heritabilities ranged from moderate to high for growth traits ([^(h)]i2 = 0.29 - 0.42 \widehat{h}_i^2 = 0.29 - 0.42 ) and stem straightness ([^(h)]i2 = 0.24 - 0.42 \widehat{h}_i^2 = 0.{24} - 0.{42} ). High coefficients of additive genetic variance were obtained for volume ( [^(\textC)]\textV\textA = 36.5 - 41.5% \widehat{\text{C}}{{\text{V}}_{\text{A}}} = {36}.{5} - {41}.{5}\% ) and straightness ( [^(\textC)]\textV\textA = 44.26 - 53.84% \widehat{\text{C}}{{\text{V}}_{\text{A}}} = {44}.{26} - {53}.{84}\% ). Phenotypic and estimated genetic correlations between growth traits were very high, and correlations between sites indicated that there was no important family × site interaction. No adverse correlations between traits were evident. The results indicate the ample potential for selection in the current progeny trial, where responses to within-family and combined selection for growth traits may be high. Accordingly, three selection scenarios were addressed with the aim to initiate the selection of individuals for implementing the Forest Breeding Plan of Galicia for European chestnut.  相似文献   

9.
Pseudomonas aeruginosa phosphorylcholine phosphatase (PchP) catalyzes the hydrolysis of phosphorylcholine, which is produced by the action of hemolytic phospholipase C on phosphatidylcholine or sphyngomielin, to generate choline and inorganic phosphate. Among divalent cations, its activity is dependent on Mg2+ or Zn2+. Mg2+ produced identical activation at pH 5.0 and 7.4, but Zn2+ was an activator at pH 5.0 and became an inhibitor at pH 7.4. At this higher pH, very low concentrations of Zn2+ inhibited enzymatic activity even in the presence of saturating Mg2+ concentrations. Considering experimental and theoretical physicochemical calculations performed by different authors, we conclude that at pH 5.0, Mg2+ and Zn2+ are hexacoordinated in an octahedral arrangement in the PchP active site. At pH 7.4, Mg2+ conserves the octahedral coordination maintaining enzymatic activity. The inhibition produced by Zn2+ at 7.4 is interpreted as a change from octahedral to tetrahedral coordination geometry which is produced by hydrolysis of the [ \textZn 2+ \textL 2 - 1 \textL 20 ( \textH 2 \textO ) 2 ] \left[ {{\text{Zn}}^{ 2+ } {\text{L}}_{ 2}^{ - 1} {\text{L}}_{ 2}^{0} \left( {{\text{H}}_{ 2} {\text{O}}} \right)_{ 2} } \right] complex.  相似文献   

10.
11.
Although nitrate is a macronutrient and can serve as good nitrogen source for many species of phytoplankton, high nitrate concentrations do not benefit the growth of phytoplankton. We hypothesise that algae cultured under high nitrate concentrations can accumulate intracellular nitrite, which is produced by nitrate reductase (NR) and can inhibit the growth of algae. To assess the validity of this hypothesis, Microcystis aeruginosa was grown under different nitrate concentrations from 3.57 to 21.43 mM in low CO2 and high CO2 conditions for 15 days. We observed that, with increasing nitrate concentrations, the intracellular nitrite concentrations of the alga increased and the growth rates and photosynthesis declined. When grown under high CO2 conditions, M. aeruginosa showed lower intracellular nitrite concentrations and higher growth rates and \textP\textm\textchla {\text{P}}_{\text{m}}^{{\text{chl}}a} , \textR\textd\textchla {\text{R}}_{\text{d}}^{{\text{chl}}a} , αchla than under low CO2 conditions. These results suggest that the accumulation of intracellular nitrite could be the cause of inhibition of algal growth under high nitrate concentrations.  相似文献   

12.
Existing correlations of Power law consistency index with Penicillium chrysogenum biomass concentration and morphology were revised using a microscope magnification of 50 times to characterize the latter, rather than the 80 times used previously. This allowed tests of the correlations on broths of Aspergillus oryzae and Aspergillus niger, which have such large mycelial sizes that a lower magnification is required for accurate morphological analysis. The new correlations were successful at predicting the rheology of A. oryzae broths but not A. niger broths, which may be because of a change in the exponent on the biomass concentration in the correlations for the latter. Because the mean maximum dimension of clumps is magnification independent, the preferred correlation was:
K = C\textm2 ×[4×10-5 D-9 ×10-4] K = C_{\text{m}}^{2} \times \left[{4\times 10^{-5}\,D-9 \times 10^{-4}}\right]  相似文献   

13.
Others have shown that exposing oocytes to high levels of (10–20 mM) causes a paradoxical fall in intracellular pH (pHi), whereas low levels (e.g., 0.5 mM) cause little pHi change. Here we monitored pHi and extracellular surface pH (pHS) while exposing oocytes to 5 or 0.5 mM NH3/NH4 +. We confirm that 5 mM causes a paradoxical pHi fall (−ΔpHi ≅ 0.2), but also observe an abrupt pHS fall (−ΔpHS ≅ 0.2)—indicative of NH3 influx—followed by a slow decay. Reducing [NH3/NH4 +] to 0.5 mM minimizes pHi changes but maintains pHS changes at a reduced magnitude. Expressing AmtB (bacterial Rh homologue) exaggerates −ΔpHS at both levels. During removal of 0.5 or 5 mM NH3/NH4 +, failure of pHS to markedly overshoot bulk extracellular pH implies little NH3 efflux and, thus, little free cytosolic NH3/NH4 +. A new analysis of the effects of NH3 vs. NH4 + fluxes on pHS and pHi indicates that (a) NH3 rather than NH4 + fluxes dominate pHi and pHS changes and (b) oocytes dispose of most incoming NH3. NMR studies of oocytes exposed to 15N-labeled show no significant formation of glutamine but substantial accumulation in what is likely an acid intracellular compartment. In conclusion, parallel measurements of pHi and pHS demonstrate that NH3 flows across the plasma membrane and provide new insights into how a protein molecule in the plasma membrane—AmtB—enhances the flux of a gas across a biological membrane.
Walter F. Boron (Corresponding author)Email:
  相似文献   

14.
The goal of the present paper was to assess a method for estimating the thermal radiation absorbed by dairy cows (0.875 Holstein–0.125 Guzerath) on pasture. A field test was conducted with 472 crossbred dairy cows in three locations of a tropical region. The following environmental data were collected: air temperature, partial vapour pressure, wind speed, black globe temperature, ground surface temperature and solar radiation. Average total radiation absorbed by animals was calculated as Rabs = 640.0 ±3.1 W.m - 2 {R_{abs}} = 640.0 \pm 3.1\, W.{m^{ - 2}} . Absorbed short-wave radiation (solar direct, diffuse and reflected) averaged 297.9 ± 2.7 W m−2; long wave (from the sky and from terrestrial surfaces) averaged 342.1 ± 1.5 W m−2. It was suggested that a new environmental measurement, the effective radiant heat load (ERHL), could be used to assess the effective mean radiant temperature ( T\textmr* ) \left( {T_{\text{mr}}^* } \right) . Average T\textmr* T_{\text{mr}}^* was 101.4 ± 1.2°C, in contrast to the usual mean radiant temperature, Tmr = 65.1 ±0.5° C {T_{mr}} = 65.1 \pm 0.5^\circ C . Estimates of T\textmr* T_{\text{mr}}^* were considered as more reliable than those of T mr in evaluating the thermal environment in the open field, because T mr is almost totally associated only with long wave radiation.  相似文献   

15.
Nitschke U  Ruth AA  Dixneuf S  Stengel DB 《Planta》2011,233(4):737-748
The emission of molecular iodine (I2) from the stipe, the meristematic area and the distal blade of the brown macroalga Laminaria digitata (Hudson) Lamouroux (Phaeophyceae) was monitored under low light and dark conditions. Photosynthetic parameters were determined to investigate both the extent of stress experienced by different thallus parts and the effects of emersion on photosynthesis. Immediately after air exposure, intense I2 emission was detectable from all thallus parts. I2 emission declined continuously over a period of 180 min following the initial burst, but was not affected by the light regime. The total number of mole of I2 emitted by stipes was approximately 10 times higher than those emitted from other thallus parts. Initial I2 emission rates (measured within 30 min of exposure to air) were highest for stipes (median values: 2,999 and 5,222 pmol g−1 dw min−1 in low light and dark, respectively) and lower, by one order of magnitude, for meristematic regions and distal blades. After exposure to air for between 60 and 180 min, I2 emission rates of all thallus parts were reduced by 70–80%. Air exposure resulted in a decrease of the maximum photosystem II (PSII) efficiency (F v/F m) by 3%, and in a 25–55% increase of the effective PSII quantum efficiency ( \Updelta F/F\textm \Updelta F/F^{\prime}_{\text{m}} ); this was caused by a higher fraction of open reaction centres (qP), whereas the efficiency of the latter in capturing energy ( F\textv /F\textm F^{\prime}_{\text{v}} /F^{\prime}_{\text{m}} ) remained constant. The results indicate the presence of an iodine pool which is easily volatilised and depleted due to air exposure, even under apparently low stress conditions.  相似文献   

16.
17.
Rye (Secale cereale L.) chromosome arm 1RS could delay leaf senescence, and change in H2O2 content is a useful index for weighing the ability to delay the senescence. Two wheat cultivars, Chuannong12 (CN12) and Chuannong 18 (CN18), harboring the wheat–rye 1BL/1RS translocated chromosome were investigated for H2O2 change and physiological index after flowering under field conditions, and MY11, the agronomical parent of both CN12 and CN18, was used as the control. A combined change in the peak value of CdSe/ZnS quantum dot (QD) fluorescence and morphological observation indicated that the H2O2 contents in CN12 and CN18 were generally lower than that in MY11. They both had higher values for net photosynthetic rate (P n), stomatal conductance (G s), F\textv /F\textm F_{\text{v}} /F_{\text{m}}^{\prime } F\textv /F\textm F_{\text{v}}^{\prime } /F_{\text{m}}^{\prime } , and photochemical quenching of PSII (qP) than MY11 only in the late measurement stage. Some small differences were also observed, such as CN12 and CN18 wheat cultivars having higher and longer photosynthetic competence than MY11 during the grain filling stage, which perhaps resulted from a mechanism for removing oxidative species, especially H2O2.  相似文献   

18.
Escherichia coli AFP111, a pflB, ldhA, ptsG triple mutant of E. coli W1485, can be recovered for additional succinate production in fresh medium after two-stage fermentation (an aerobic growth stage followed by an anaerobic production stage). However, the specific productivity is lower than that of two-stage fermentation. In this study, three strategies were compared for reusing the cells. It was found when cells were aerobically cultivated at the end of two-stage fermentation without supplementing any carbon source, metabolites (mainly succinate and acetate) could be consumed. As a result, enzyme activities involved in the reductive arm of tricarboxylic acid cycle and the glyoxylate shunt were enhanced, yielding a succinate specific productivity above 1 2 5  \textmg  \textgDCW - 1  \texth - 1 1 2 5\;{\text{mg}}\;{\text{g}}_{\rm DCW}^{ - 1} \,{\text{h}}^{ - 1} and a mass yield above 0.90 g g−1 in the subsequent anaerobic fermentation. In addition, the intracellular NADH of cells subjected to aerobic cultivation with metabolites increased by more than 3.6 times and the ratio of NADH to NAD+ increased from 0.4 to 1.3, which were both favorable for driving the TCA branch to succinate.  相似文献   

19.
A series of 35 triazolopyrimidine analogues reported as Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors were optimized using quantum mechanics methods, and their binding conformations were studied by docking and 3D quantitative structure–activity relationship studies. Genetic algorithm-based criteria was adopted for selection of training and test sets while maintaining structural diversity of training and test sets, which is also very crucial for model development and validation. Both the comparative molecular field analyses ( q\textLOO2 = 0.841 q_{\text{LOO}}^2 = 0.{841} , r\textncv2 = 0.99 r_{\text{ncv}}^2 = 0.{99} ) and comparative molecular similarity indices analyses ( q\textLOO2 = 0.757 q_{\text{LOO}}^2 = 0.{757} , r\textncv2 = 0.943 r_{\text{ncv}}^2 = 0.{943} ) show excellent correlation and high predictive power. Furthermore, molecular dynamics simulations were performed to explore the binding mode of the two of the most active compounds of the series, 10 and 14. Harmonization in the two simulation results validate the analysis and therefore applicability of docking parameters based on crystallographic conformation of compound 14 bound to receptor molecule. This work provides useful information about the inhibition mechanism of this class of molecules and will assist in the design of more potent inhibitors of PfDHODH.  相似文献   

20.
Silicone oil 20 and 200 cSt, a perfluorocarbon (FC40TM), heptamethylnonane, Kraton, Elvax, and Desmopan were evaluated for their ability to enhance oxygen transfer in stirred tank and airlift reactors (STR and ALR, respectively). None of the vectors tested was either toxic or biodegradable and they exhibited a moderate affinity for oxygen (gas/vector partitioning coefficients K\textg/\textv = C\textg ·C\textv- 1 K_{{{\text{g}}/{\text{v}}}} = C_{\text{g}} \cdot C_{\text{v}}^{- 1} ranging from 3 to 5.1). FC40 was highly volatile, while KratonTM and ElvaxTM exhibited a low thermal stability, which constitutes a serious handicap for their implementation in fermentations. Silicone oil 20 cSt and Desmopan supported the highest oxygen transfer rates under abiotic conditions in both STR and ALR designs, with enhancement factors of up to 90% and 250%, respectively, compared to control tests (deprived of vector). The fact that these vectors showed the highest K g/v proved that, besides the classical selection criteria, the in situ hydrodynamic behavior (which affects K L a) must be considered for vector selection. The use of silicone oil 20 cSt and Desmopan in glucose-supplemented Saccharomyces cerevisiae fermentations resulted in a two- and threefold increase in biomass productions, respectively. The better performance of Desmopan in terms of biomass growth enhancement, together with the absence of the operational problems inherent to the use of liquid vectors (such as intensive foaming, high cost, and difficult solvent recovery), make solid vectors a promising and cost-effective alternative in the future developments of two-phase partitioning bioreactors.  相似文献   

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