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Wyszukujesz frazę "Inhibition" wg kryterium: Temat


Tytuł:
The role of alkyl chain length in the inhibitory effect n-alkyl xanthates on mushroom tyrosinase activities
Autorzy:
Saboury, Ali
Alijanianzadeh, Mahdi
Mansoori-Torshizi, Hasan
Powiązania:
https://bibliotekanauki.pl/articles/1041136.pdf
Data publikacji:
2007
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
mushroom tyrosinase
mixed inhibition
uncompetitive inhibition
alkyl xanthate
competitive inhibition
inhibition constant
Opis:
Sodium salts of four n-alkyl xanthate compounds, C2H5OCS2Na (I), C3H7OCS2Na (II), C4H9OCS2Na (III), and C6H13OCS2Na (IV) were synthesized and examined for inhibition of both cresolase and catecholase activities of mushroom tyrosinase (MT) in 10 mM sodium phosphate buffer, pH 6.8, at 293 K using UV spectrophotemetry. 4-[(4-methylbenzo)azo]-1,2-benzendiol (MeBACat) and 4-[(4-methylphenyl)azo]-phenol (MePAPh) were used as synthetic substrates for the enzyme for catecholase and cresolase reactions, respectively. Lineweaver-Burk plots showed different patterns of mixed, competitive or uncompetitive inhibition for the four xanthates. For the cresolase activity, I and II showed uncompetitive inhibition but III and IV showed competitive inhibition pattern. For the catecholase activity, I and II showed mixed inhibition but III and IV showed competitive inhibition. The synthesized compounds can be classified as potent inhibitors of MT due to their Ki values of 13.8, 11, 8 and 5 µM for the cresolase activity, and 1.4, 5, 13 and 25 µM for the catecholase activity for I, II, III and IV, respectively. For the catecholase activity both substrate and inhibitor can be bound to the enzyme with negative cooperativity between the binding sites (α > 1) and this negative cooperativity increases with increasing length of the aliphatic tail of these compounds. The length of the hydrophobic tail of the xanthates has a stronger effect on the Ki values for catecholase inhibition than for cresolase inhibition. Increasing the length of the hydrophobic tail leads to a decrease of the Ki values for cresolase inhibition and an increase of the Ki values for catecholase inhibition.
Źródło:
Acta Biochimica Polonica; 2007, 54, 1; 183-191
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Evaluation of p-phenylene-bis and phenyl dithiocarbamate sodium salts as inhibitors of mushroom tyrosinase
Autorzy:
Amin, Ehsan
Saboury, Ali
Mansouri-Torshizi, Hassan
Zolghadri, Samane
Bordbar, Abdol-Khalegh
Powiązania:
https://bibliotekanauki.pl/articles/1040368.pdf
Data publikacji:
2010
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
phenyl dithiocarbamate
mushroom tyrosinase
mixed inhibition
p-phenylene-bis (dithiocarbamate)
noncompetitive inhibition
inhibition constant
Opis:
Two structurally related compounds, phenyl dithiocarbamate sodium salt (I) and p-phenylene-bis (dithiocarbamate) sodium salt (II) were prepared by reaction of the parent aniline and p-phenylenediamine with CS2 in the presence of sodium hydroxide. These water soluble compounds were characterized by spectroscopic techniques, IR, 1H NMR and elemental analysis. The inhibitory effects of both compounds on both activities of mushroom tyrosinase (MT) from Agricus bisporus were studied at two temperatures, 27°C and 37°C. L-3, 4-dihydroxyphenylalanine (L-DOPA), and l-tyrosine were used as natural substrates for the catecholase and cresolase enzyme reactions, respectively. Kinetic analysis confirmed noncompetitive inhibition mode of I and mixed type of II on both activities of MT; I and II inhibit MT with inhibition constants (KI) of 300 µM and 4 µM, respectively. Analysis of thermodynamic parameters indicated predominant involvement of hydrophobic interactions in binding of I and electrostatic ones in binding of II to MT. It seems that II is a more potent MT inhibitor due to its two charged head groups able to chelate copper ions in the enzyme active site. Intrinsic fluorescence studies as a function of concentrations of both compounds showed unexpectedly quenching of emission intensity without any shift of emission maximum. Extrinsic ANS-fluorescence indicated that only binding of I induces limited changes in the tertiary structure of MT, in agreement with the postulated hydrophobic nature of the binding mechanism.
Źródło:
Acta Biochimica Polonica; 2010, 57, 3; 277-283
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Aba Sensitivity as a Criterion for Drought Tolerance in Wheat (Triticum Aestivum L.) Cultivars
Autorzy:
Razzaq, Abdul
Rashid, Madiha
Shfique, Talal Ahmad
Hafeez, Abdul
Jhanzab, Hafiz Muhammad
Shabir, Ghulam
Shah, Zahid Hussain
Powiązania:
https://bibliotekanauki.pl/articles/2199671.pdf
Data publikacji:
2016-12-20
Wydawca:
Instytut Hodowli i Aklimatyzacji Roślin
Tematy:
ABA
chlorophyll
inhibition
proline
Opis:
Criteria used for evaluating drought tolerance of wheat cultivars demanding more time and efforts are usually not efficient and conclusive. Present study was conducted to evaluate ABA sensitivity as a criterion for evaluating drought tolerance of wheat cultivars at an early stage. Ten cultivars of wheat were subjected to drought at 3-leaf stage to select the most sensitive and two tolerant cultivars using mortality rate. Tatara was found the most susceptible whereas GA-2002 and Chakwal-50 were the cultivars with maximum drought tolerance. These cultivars were used to study sensitivity to applied absicic acid (based on germination index and relative growth inhibition rate) and physiological responses (leaf water content, chlorophyll stability index, coefficient of relative inhibition and proline accumulation) under drought stress. Highest ABAsensitivity was recorded in GA-2002 and Chakwal-50 whereas Tatara manifested minimum sensitivity. ABAsensitivity corresponded to physiological indices of drought tolerance. Results show that ABA-sensitivity is an efficient criterion that can be used to evaluate drought tolerance of wheat cultivars at early stage.
Źródło:
Plant Breeding and Seed Science; 2016, 74; 73-84
1429-3862
2083-599X
Pojawia się w:
Plant Breeding and Seed Science
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Inhibition study of adenosine deaminase by caffeine using spectroscopy and isothermal titration calorimetry.
Autorzy:
Saboury, A
Divsalar, A
Ataie, G
Amanlou, M
Moosavi-Movahedi, A
Hakimelahi, G
Powiązania:
https://bibliotekanauki.pl/articles/1043464.pdf
Data publikacji:
2003
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
calorimetry
inhibition
caffeine
adenosine deaminase
Opis:
Kinetic and thermodynamic studies were made on the effect of caffeine on the activity of adenosine deaminase in 50 mM sodium phosphate buffer, pH 7.5, using UV spectrophotometry and isothermal titration calorimetry (ITC). An uncompetitive inhibition was observed for caffeine. A graphical fitting method was used for determination of binding constant and enthalpy of inhibitor binding by using isothermal titration microcalorimetry data. The dissociation-binding constant is equal to 350 μM by the microcalorimetry method, which agrees well with the value of 342 μM for the inhibition constant that was obtained from the spectroscopy method. Positive dependence of caffeine binding on temperature indicates a hydrophobic interaction.
Źródło:
Acta Biochimica Polonica; 2003, 50, 3; 849-855
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
The impact of polyphenols on Bifidobacterium growth
Autorzy:
Gwiazdowska, Daniela
Juś, Krzysztof
Jasnowska-Małecka, Joanna
Kluczyńska, Katarzyna
Powiązania:
https://bibliotekanauki.pl/articles/1038940.pdf
Data publikacji:
2015
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
dietary polyphenol
probiotic
inhibition
stimulation
Opis:
Polyphenols are a common group of plant based bioactive compounds, that can affect human health because of their antioxidant and antimicrobial properties as well as free-radical scavenging activity. An increasing interest is observed in the interaction between polyphenols and microbiota occurring in food and the human gut. The aim of the work presented here, was to evaluate the effect of some polyphenolic compounds on the growth of two strains of Bifidobacterium: B. adolescentis and B. bifidum. The influence of some flavonoids: naringinin, hesperidin, rutin, quercetin as well as phenolic acids: gallic, caffeic, p-coumaric, ferulic, chlorogenic, vanillic and sinapic was determined by a 96-well microtiter plate assay. In the experiments the effect of three different concentrations of polyphenols: 2, 20 and 100 µg/ml on the growth of Bifidobacterium strains was investigated. All tested compounds influenced the growth of the examined bacteria. Both stimulatory and inhibitory effects were observed in comparison to the positive control. The strongest impact on the growth of bifidobacteria was observed during the first hours of incubation. The constant inhibitory effect was observed for hesperidin and quercetin addition and was dose-dependent. B. bifidum showed a stronger dependence on phenolic acids content in the medium than B. adolescentis during the first hours of incubation.
Źródło:
Acta Biochimica Polonica; 2015, 62, 4; 895-901
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Odbiór bodźców środowiskowych przez glony Characeae sygnalizowany za pomocą ultrasłabej luminescencji
Reception of environmental stimuli by Characeae algae manifested by ultraweak luminescence
Autorzy:
Jaśkowska, A.
Dudziak, A.
Borc, R
Powiązania:
https://bibliotekanauki.pl/articles/1819387.pdf
Data publikacji:
2012
Wydawca:
Politechnika Koszalińska. Wydawnictwo Uczelniane
Tematy:
photon emission
heavy metals
inhibition
Opis:
Protecting the environment requires ensuring such conditions that organisms living in it did not suffer permanent damage to their structures and life functions. This also applies to algae living in the aquatic environment. Some species of water flora especially quickly react to negative stimuli arriving from the environment. Their reactions to experienced stress may be a subtle criterion for assessing the condition of aquatic environment. To this kind of plants belong Chara, which are bioindicators of water quality. Their response to applied environmental stimuli is rapid changes of the electrical parameters of the cell membrane. Our research shows that there is also a change in the intensity of ultraweak luminescence (UWL) generated by these plants. UWL is a phenomenon that continuously accompanies processes occurring in living cells and its intensity is less than the threshold sensitivity of the human eye. The method of measurement of this little known way of Chara's response to environmental stimuli has the advantage that it is completely non-invasive for the test material. Non-invasiveness is due to the fact that the radiation emitted from the samples is measured outside the cell membrane separating the living matter from the surrounding environment. In our study, after exposure to a selected stimulus, three types of responses of plant cells were observed: 1) - after a temporary increase of UWL, there is a return to the level of light corresponding to undisturbed homeostasis (e.g. when ascorbic acid is added to the environment); 2) - after a temporary increase in the UWL, the emission of photons slightly falls and stabilizes at a new higher level of illumination (when the stress stimulus is e.g. lead acetate, the emission intensity is 2.2 times larger than in the beginning); 3) - after a sudden and significant increase of UWL, the high emission level is maintained for many hours (e.g. after adding sucrose follows a 20-fold increase of UWL). UWL curves obtained in our experiments correlate with the changes of entropy corresponding to the disturbance of homeostasis in individual cases, depending on the applied stimulus. Respectively: for 1) - an increase of entropy is temporary and is followed by a return to values before the application of the stimulus, 2) - a lasting change occurs, which consists in an increase of entropy to a new fixed level, 3) - change in entropy is so large that its value exceeds the so-called point of no return, which means that the disorder of homeostasis leads to cell death. The application of luminescence imaging technique Single Photon Counting Imaging (SPCI) to the test cells have revealed that the emission of photons from different parts of the plant has a different intensity. When the plant suffered mechanical damage by cutting pseudoleaves, the emission from the damaged sites increased dramatically. This observation allows the damage to be located. Thanks to SPCI technique, it is also possible to track over time any repair processes. The clear differentiation of UWL kinetics leads to the conclusion that monitoring its intensity can be a good research tool in environmental protection. It makes it possible to determine whether chemicals found in the aquatic environment are harmful to a given species of plants. It can be also assessed whether the degree of the harm threatens the entire population with extinction. Thus, the presented method can be used as an ecotoxicity test.
Źródło:
Rocznik Ochrona Środowiska; 2012, Tom 14; 380-392
1506-218X
Pojawia się w:
Rocznik Ochrona Środowiska
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Inhibicja enzymatyczna wolnowiążąca
Enzymatic slow-binding inhibition
Autorzy:
Pawełczak, M.
Hurek, J.
Powiązania:
https://bibliotekanauki.pl/articles/142333.pdf
Data publikacji:
2014
Wydawca:
Stowarzyszenie Inżynierów i Techników Przemysłu Chemicznego. Zakład Wydawniczy CHEMPRESS-SITPChem
Tematy:
kinetyka enzymatyczna
inhibicja wolnowiążąca
mechanizmy inhibicji wolnowiążącej
enzymatic kinetics
slow-binding inhibition
slowbinding inhibition mechanisms
Opis:
Inhibitory enzymów otrzymywane są głównie w celu ich zastosowania w medycynie, ochronie plonów, czy przemyśle spożywczym. Wolnowiążące się z enzymem inhibitory stanowią grupę inhibitorów nieklasycznych i ten typ inhibicji wymaga bardziej złożonej analizy danych kinetycznych. Znajomość mechanizmów hamowania enyzmów przez inhibitory jest kluczowa dla projektowania nowych, bardziej efektywnych związków tego typu. Poniżej przedstawiono algorytm pozwalający na rozstrzygnięcie jaki jest mechanizm inhibicji wolnowiążącej oraz oryginalny sposób obliczenia stałej Ki dla każdego z tych mechanizmów.
Enzyme inhibitors are produced mostly for applications in medicine, crop protection and food industry. Inhibitors slow-binding with enzyme are a group of non-classical inhibitors and such type of inhibition requires more complex analysis of kinetic data. The knowledge of enzyme inhibition mechanisms by inhibitors plays essential role for designing new, more effective compounds of such type. Below, the algorithm is presented that allows to find out what is a mechanism of slow-binding inhibition and the original method for calculating constant Ki for each individual mechanism is shown.
Źródło:
Chemik; 2014, 68, 4; 377-384
0009-2886
Pojawia się w:
Chemik
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Effect of natural phenols on the catalytic activity of cytochrome P450 2E1
Autorzy:
Mikstacka, Renata
Gnojkowski, Jerzy
Baer-Dubowska, Wanda
Powiązania:
https://bibliotekanauki.pl/articles/1043696.pdf
Data publikacji:
2002
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
resveratrol
tannic acid
polyphenols
inhibition kinetics
mechanism-based inhibition
CYP2E1
protocatechuic acid
Opis:
The effect of protocatechuic acid, tannic acid and trans-resveratrol on the activity of p-nitrophenol hydroxylase (PNPH), an enzymatic marker of CYP2E1, was examined in liver microsomes from acetone induced mice. trans-Resveratrol was found to be the most potent inhibitor (IC50 = 18.5 ± 0.4 mM) of PNPH, while protocatechuic acid had no effect on the enzyme activity. Tannic acid with IC50 = 29.6 ± 3.3 mM showed mixed- and trans-resveratrol competitive inhibition kinetics (Ki = 1 mM and 2.1 mM, respectively). Moreover, trans-resveratrol produced a NADPH-dependent loss of PNPH activity, suggesting mechanism-based CYP2E1 inactivation. These results indicate that trans-resveratrol and tannic acid may modulate cytochrome P450 2E1 and influence the metabolic activation of xenobiotics mediated by this P450 isoform.
Źródło:
Acta Biochimica Polonica; 2002, 49, 4; 917-925
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Modelling of the cometabolic decomposition of 4-chlorophenol and phenol by the Stenotrophomonas maltophilia KB2 strain
Modelowanie kometabolicznego rozkładu 4-chlorofenolu i fenolu przez szczep Stenotrophomonas maltophilia KB2
Autorzy:
Szczyrba, E.
Gąszczak, A.
Bartelmus, G.
Janecki, D.
Powiązania:
https://bibliotekanauki.pl/articles/126703.pdf
Data publikacji:
2017
Wydawca:
Towarzystwo Chemii i Inżynierii Ekologicznej
Tematy:
cometabolism
kinetics
phenol
4-chlorophenol
self-inhibition
competitive inhibition
kometabolizm
kinetyka
fenol
4-chlorofenol
inhibicja
Opis:
The present study investigated the degradation kinetics of growth (phenol) and non-growth (4-chlorophenol, 4-CP) substrates, present alone and in cometabolic system. Batch experiments were performed using very active Stenotrophomonas maltophilia KB2 strain. The methods of determining the model parameters describing the kinetics of changes in biomass and both substrates concentrations in a cometabolic system were presented.
Zaprezentowano model rozkładu 4-chlorofenolu przez szczep Stenotrophomonas maltophilia KB2 w obecności fenolu jako substratu wzrostowego. Opracowanie tego modelu wymagało wykonania czterech serii badań: biodegradacji różnych dawek czystego fenolu, biodegradacji różnych dawek czystego 4-CP, biodegradacji 4-CP w obecności fenolu przy różnym stosunku stężeń obu substratów oraz biodegradacji 4-CP przez komórki w fazie spoczynku, indukowane wstępnie fenolem. Szczegółowo omówiono sposoby wyznaczania poszczególnych parametrów równań opisujących szybkość degradacji substratów wzrostowego i niewzrostowego oraz przyrostu biomasy. W oparciu o stworzoną bazę danych obliczono m.in. stałe półnasycenia KSg i KSc, stałe inhibicji KIg i KIc, współczynnik zamierania endogennego b oraz wydajność transformacyjną substratu wzrostowego w stosunku do kometabolitu Tcg.
Źródło:
Proceedings of ECOpole; 2017, 11, 2; 421-431
1898-617X
2084-4557
Pojawia się w:
Proceedings of ECOpole
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Adsorption behavior of pharmaceutically active dexketoprofen as sustainable corrosion Inhibitor for API X80 carbon steel in acidic medium
Autorzy:
Nkem, B. Iroha
Abosede, O. James
Powiązania:
https://bibliotekanauki.pl/articles/1076601.pdf
Data publikacji:
2019
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
Adsorption
Carbon steel
Dexketoprofen
Inhibition
SEM
Opis:
The inhibition of X80 carbon steel corrosion in 1 M HCl solution by dexketoprofen (DKP) was studied using weight loss (WL), electrochemical impedance spectroscopy (EIS), potentiodynamic polarization (PDP) and scanning electron microscopy (SEM) techniques. The results indicated that DKP acts by way of adsorption as an effective protective inhibitor in the aggressive acid medium. The inhibition efficiency of DKP increased with concentration but was lower at higher temperature. The results of potentiodynamic polarization showed that DKP molecule behaved as a mixed type inhibitor by reducing both the anodic and the cathodic electrochemical reactions. Dexketoprofen was adsorbed on the X80 steel surface in accordance with Langmuir adsorption isotherm. SEM analyses supported formation of protective film on the X80 steel in the presence of DKP.
Źródło:
World News of Natural Sciences; 2019, 27; 22-37
2543-5426
Pojawia się w:
World News of Natural Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Signal transduction in confluent C3H 10T1/2 cells. The role of focal adhesion kinase.
Autorzy:
Miłoszewska, Joanna
Trembacz, Halina
Janik, Przemysław
Powiązania:
https://bibliotekanauki.pl/articles/1044183.pdf
Data publikacji:
2001
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
integrins
FAK
ERK
fibronectin
contact inhibition
Opis:
The activities of extracellular signal-regulated kinases (ERK1/ERK2) is required for proliferation of several types of cells. The performed analysis showed stimulation of ERK's by fetal calf serum (FCS) or fibronectin in the C3H 10T1/2 cell cultures at logarithmic phase of growth. The ERKs activity was not stimulated in confluent cells. This could not be accounted for a partial down regulation of ERK since its level was stable in both types of cells regardless of their density and kind of stimulation. Searching for ERK upstream elements we studied the integrin receptor gene transcript by RT-PCR and focal adhesion kinase (FAK) by Western blotting and phosphorylation assays. It was found that FCS and fibronectin stimulated phosphorylating activity of FAK in the cells at the logarithmic phase of growth, but were inefficient in the confluent cells. RT-PCR showed the presence of α5 and β1 integrin transcripts, and p125FAK was at the same level regardless of the type of stimulation. These data indicate that the ability of FAK to be activated plays an important role in ERK regulation and, in consequence in proliferation and growth inhibition during confluence.
Źródło:
Acta Biochimica Polonica; 2001, 48, 1; 175-181
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Effective flotation separation of scheelite and calcite by applying methylene phosphonic acid sodium as a novel and green depressant
Autorzy:
Zhou, Hepeng
Wu, Handan
Guo, Jiangfeng
Tang, Xuekun
Huang, Wen
Luo, Xianping
Powiązania:
https://bibliotekanauki.pl/articles/24086193.pdf
Data publikacji:
2023
Wydawca:
Politechnika Wrocławska. Oficyna Wydawnicza Politechniki Wrocławskiej
Tematy:
scheelite
calcite
inhibition mechanism
flotation separation
Opis:
It is known that the flotation separation of scheelite and calcite is quite difficult due to their similar surface properites. To slove the problem, ethylenediaminetetra (methylene phosphonic acid) sodium (EDTMPS), an environmentally friendly reagent, was employed as an efficient depressant for flotation separation of calcite for the first time. In flotation experiments, it demonstrates that EDTMPS could strongly inhibit the flotation of calcite but barely affect the flotaiton behavior of scheelite, showing excellent dpress ability and selectivity. Based on a series of measurements including contact angle analysis, zeta potential, and XPS analysis, it was found that large amout of EDTMPS could be absorbed on the surface of calcite through strong chemical chelation reaction and thus inhibiting the further adsorption of NaOL. On the contrary, little EDTMPS was absorbed on that of scheelite owing to the negatively charged tungstate ions on the surface in relative terms. All in all, these results exhibit EDTMPS has excellent selective inhibition ability on calcite, which can be potentially applied in actual scheelite and calcite flotation separation process.
Źródło:
Physicochemical Problems of Mineral Processing; 2023, 59, 3; art. no. 168517
1643-1049
2084-4735
Pojawia się w:
Physicochemical Problems of Mineral Processing
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and biological activity of Nα-[4-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-propargylamino]phenyl-acetyl]-L-glutamic acid.
Autorzy:
Kusakiewicz-Dawid, Anna
Bugaj, Marta
Dzik, Jolanta
Gołos, Barbara
Wińska, Patrycja
Pawełczak, Krzysztof
Rzeszotarska, Barbara
Rode, Wojciech
Powiązania:
https://bibliotekanauki.pl/articles/1043826.pdf
Data publikacji:
2002
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
ICI 198583 analogue
inhibition
thymidylate synthase
Opis:
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 Ki value of 0.34 μM, 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 μM) 180-fold weaker than by ICI 198583 (IC50 = 6.9 μM).
Źródło:
Acta Biochimica Polonica; 2002, 49, 1; 197-202
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Experimental and computational study of levofloxacin as corrosion inhibitor for carbon steel in acidic media
Autorzy:
Ikpi, M. E.
Abeng, F. E.
Okonkwo, B. O.
Powiązania:
https://bibliotekanauki.pl/articles/1118353.pdf
Data publikacji:
2017
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
Corrosion Inhibition
Polarization
levofloxacin and Adsorption
Opis:
The corrosion inhibition behaviour of levofloxacin was investigated on carbon steel by means of a 2 M HCl solution, using potentiodynamic polarization measurement and Quantum chemical studies. The inhibitive effect of the studied compound was found to increase with increasing concentration and to increase with increasing temperature. The study reveals that levofloxacin is a mixed-type corrosion inhibitor. The adsorption of levofloxacin on carbon steel surface obeys the Langmuir adsorption isotherm and involves physical adsorption mechanisms. Quantum chemical studies corroborate experimental results.
Źródło:
World News of Natural Sciences; 2017, 9; 79-90
2543-5426
Pojawia się w:
World News of Natural Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Correlation between butyrylcholinesterase variants and sensitivity to soman toxicity
Autorzy:
Dimov, Dimo
Kanev, Kamen
Dimova, Ivanka
Powiązania:
https://bibliotekanauki.pl/articles/1039756.pdf
Data publikacji:
2012
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
enzyme inhibition/reactivation
soman toxicity
Butyrylcholinesterase variants
Opis:
Butyrylcholinesterase (BChE) is synthesized in the liver and found in high concentrations in blood plasma, liver, heart, pancreas, vascular endothelium, skin, brain white matter, smooth muscle cells and adipocytes. BChE is a non specific enzyme that hydrolyzes different choline esters (succinylcholine, mivacurium) and many other drugs such as aspirin, cocaine and procaine. The enzyme is also considered as a bioscavenger due to its ability to neutralize the toxic effects of organophosphorus compounds (nervous system fs agents) such as soman. BChE displays several polymorphisms that influence its serum activity; therefore they could determine the individual sensitivity to chemical nerve agents. In this study, we investigated the correlation between BChE variants and the degree of enzyme inhibition and reactivation after soman application on blood samples of 726 individuals. The blood samples of individuals expressing abnormal variants, were more sensitive to soman compared to variants of homozygotes and heterozygotes for U-allele. We found significant differences in the degree of enzyme reactivation between different variants (with and without U-presence).
Źródło:
Acta Biochimica Polonica; 2012, 59, 2; 313-316
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł

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