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Keywords = oxidoreductive enzyme activities

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12 pages, 2196 KiB  
Article
Effect of Glyoxal on Plasma Membrane and Cytosolic Proteins of Erythrocytes
by Michal Kopera, Malgorzata Adamkiewicz and Anna Pieniazek
Int. J. Mol. Sci. 2025, 26(9), 4328; https://doi.org/10.3390/ijms26094328 - 2 May 2025
Cited by 1 | Viewed by 456
Abstract
Glyoxal (GO) is a reactive dicarbonyl derived endogenously from sugars and other metabolic reactions within cells. Numerous exogenous sources of this compound include tobacco smoking, air pollution, and food processing. GO is toxic to cells mainly due to its high levels and reactivity [...] Read more.
Glyoxal (GO) is a reactive dicarbonyl derived endogenously from sugars and other metabolic reactions within cells. Numerous exogenous sources of this compound include tobacco smoking, air pollution, and food processing. GO is toxic to cells mainly due to its high levels and reactivity towards proteins, lipids, and nucleic acids. We speculate that glyoxal could be involved in erythrocyte protein damage and lead to cell dysfunction. The osmotic fragility and level of amino and carbonyl groups of membrane proteins of erythrocytes incubated for 24 h with GO were identified. The amount of thiol, amino, and carbonyl groups was also measured in hemolysate proteins after erythrocyte treatment with GO. In hemolysate, the level of glutathione, non-enzymatic antioxidant capacity (NEAC), TBARS, and activity of antioxidant enzymes was also determined. The study’s results indicated that GO increases erythrocyte osmotic sensitivity, alters the levels of glutathione and free functional groups in hemolysate proteins, and modifies the activity of antioxidant enzymes. Our findings indicate that GO is a highly toxic compound to human erythrocytes. Glyoxal at concentrations above 5 mM can cause functional changes in erythrocyte proteins and disrupt the oxidoreductive balance in cells. Full article
(This article belongs to the Section Molecular Biology)
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35 pages, 4345 KiB  
Review
Can Compounds of Natural Origin Be Important in Chemoprevention? Anticancer Properties of Quercetin, Resveratrol, and Curcumin—A Comprehensive Review
by Elżbieta Cecerska-Heryć, Zofia Wiśniewska, Natalia Serwin, Aleksandra Polikowska, Małgorzata Goszka, Weronika Engwert, Jaśmina Michałów, Maja Pękała, Marta Budkowska, Anna Michalczyk and Barbara Dołęgowska
Int. J. Mol. Sci. 2024, 25(8), 4505; https://doi.org/10.3390/ijms25084505 - 19 Apr 2024
Cited by 17 | Viewed by 3576
Abstract
Malignant tumors are the second most common cause of death worldwide. More attention is being paid to the link between the body’s impaired oxidoreductive balance and cancer incidence. Much attention is being paid to polyphenols derived from plants, as one of their properties [...] Read more.
Malignant tumors are the second most common cause of death worldwide. More attention is being paid to the link between the body’s impaired oxidoreductive balance and cancer incidence. Much attention is being paid to polyphenols derived from plants, as one of their properties is an antioxidant character: the ability to eliminate reactive oxygen and nitrogen species, chelate specific metal ions, modulate signaling pathways affecting inflammation, and raise the level and activity of antioxidant enzymes while lowering those with oxidative effects. The following three compounds, resveratrol, quercetin, and curcumin, are polyphenols modulating multiple molecular targets, or increasing pro-apoptotic protein expression levels and decreasing anti-apoptotic protein expression levels. Experiments conducted in vitro and in vivo on animals and humans suggest using them as chemopreventive agents based on antioxidant properties. The advantage of these natural polyphenols is low toxicity and weak adverse effects at higher doses. However, the compounds discussed are characterized by low bioavailability and solubility, which may make achieving the blood concentrations needed for the desired effect challenging. The solution may lie in derivatives of naturally occurring polyphenols subjected to structural modifications that enhance their beneficial effects or work on implementing new ways of delivering antioxidants that improve their solubility and bioavailability. Full article
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15 pages, 1847 KiB  
Article
Biochemical and Quality Parameter Changes of Wheat Grains during One-Year Storage under Different Storage Conditions
by Ivica Strelec, Vladimir Mrša, Dragana Šoronja Simović, Jovana Petrović, Jana Zahorec and Sandra Budžaki
Sustainability 2024, 16(3), 1155; https://doi.org/10.3390/su16031155 - 30 Jan 2024
Cited by 4 | Viewed by 2645
Abstract
The selection of suitable storage conditions and monitoring of changes in the wheat grains using suitable parameters are of great importance for the sustainability of technological quality and utilization of the entire stored quantity of wheat grains without waste generation until the next [...] Read more.
The selection of suitable storage conditions and monitoring of changes in the wheat grains using suitable parameters are of great importance for the sustainability of technological quality and utilization of the entire stored quantity of wheat grains without waste generation until the next harvest. Wheat grains of three varieties, stored for 12 months at three different conditions of environmental temperature and relative humidity (% RH): (1) 40 ± 1.06 °C; 45 ± 3% RH; (2) 4 ± 1.05 °C; 45 ± 4% RH, (3) 15 ± 8.51 °C; and 67 ± 4% RH, were compared for germination percentage, protein and advanced glycation end products content, oxidoreductive and proteolytic enzyme activity, wet gluten content and falling number. A decrease in the activity of guaiacol peroxidase and polyphenol oxidase, as well as an increase in the content of advanced glycosylation end products and the falling number, was observed in wheat grains during storage conditions at 40 ± 1.06 °C; 45 ± 4% RH. On the other hand, storage of wheat grains at lower temperatures resulted in much lower changes in examined parameters, among which advanced glycation end-product content, peroxidase activity and falling number values were the greatest. Based on the obtained results, it can be assumed that changes in guaiacol peroxidase activity and falling number might be used as indicators of improper wheat grain storage. Full article
(This article belongs to the Special Issue Agricultural Product Quality Safety and Sustainable Development)
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20 pages, 3550 KiB  
Article
Immobilisation of Cellobiose Dehydrogenase and Laccase on Chitosan Particles as a Multi-Enzymatic System for the Synthesis of Lactobionic Acid
by Justyna Sulej, Wiktoria Piątek-Gołda, Marcin Grąz, Katarzyna Szałapata, Piotr Waśko, Ewa Janik-Zabrotowicz and Monika Osińska-Jaroszuk
J. Funct. Biomater. 2023, 14(7), 383; https://doi.org/10.3390/jfb14070383 - 21 Jul 2023
Cited by 8 | Viewed by 2280
Abstract
Lactobionic acid (LBA) is a bioactive compound that has become increasingly popular in medicine in recent years due to its unique properties. This chemical can be formed via the enzymatic oxidation of lactose using fungal oxidoreductive enzymes. This study aimed to intensify the [...] Read more.
Lactobionic acid (LBA) is a bioactive compound that has become increasingly popular in medicine in recent years due to its unique properties. This chemical can be formed via the enzymatic oxidation of lactose using fungal oxidoreductive enzymes. This study aimed to intensify the synthesis of LBA using immobilised enzymes (cellobiose dehydrogenase from Phanerochaete chrysosporium (PchCDH) and laccase from Cerrena unicolor (CuLAC)) on chitosan microspheres. We used three different crosslinking agents: genipin, glutaraldehyde, and polyethyleneimine to activate the chitosan. The FTIR and CellDrop techniques were used to characterise the activated microspheres. Quantitative (HPLC) and qualitative (TLC) methods were used to determine the obtained LBA. The results show that the type of activator used influences the efficiency of the binding of the enzyme to the matrix. Furthermore, the amount of LBA formed depends on the type of system used. The use of a system in which one of the enzymes is immobilised on a PEI-activated carrier (PchCDH) and the other is free (CuLAC) proved to be the most optimal, as it yielded almost 100% conversion of lactose to lactobionic acid. Summarising the data obtained the following: lactobionic acid immobilised on chitosan microspheres has great potential for medical applications. Full article
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22 pages, 1650 KiB  
Article
Influence of Plant Growth Retardants and Nitrogen Doses on the Content of Plant Secondary Metabolites in Wheat, the Presence of Pests, and Soil Quality Parameters
by Joanna Lemanowicz, Bożena Dębska, Robert Lamparski, Agata Michalska, Jarosław Pobereżny, Elżbieta Wszelaczyńska, Agata Bartkowiak, Małgorzata Szczepanek, Magdalena Banach-Szott and Tomasz Knapowski
Agriculture 2023, 13(6), 1121; https://doi.org/10.3390/agriculture13061121 - 25 May 2023
Cited by 4 | Viewed by 2348
Abstract
Wheat is the cereal most susceptible to lodging, particularly during the flowering period and at the early ripening stage. The use of plant growth retardants (PGRs) is especially recommended when intensive nitrogen (N) fertilisation is applied, which increases the susceptibility of plants to [...] Read more.
Wheat is the cereal most susceptible to lodging, particularly during the flowering period and at the early ripening stage. The use of plant growth retardants (PGRs) is especially recommended when intensive nitrogen (N) fertilisation is applied, which increases the susceptibility of plants to lodging. This paper presents the results of tests into the effects of PGRs (PGR0—control; PGR1—chlormequat chloride (CCC) + trinexapac-ethyl (TE); PGR2—chlormequat chloride (CCC) + ethephon (ET)), and N dose—N0, N20, N40, and N60 [0, 20, 40, and 60 kg N ha−1] on the content of selected plant secondary metabolites (PSM) in the Indian dwarf wheat (Triticum sphaerococcum Percival) of the Trispa cultivar, and on the abundance of insect pests. In the developmental stage of wheat (BBCH 39), insects were collected with an entomological net. The study also investigated the effect of experimental factors on the physicobiochemical properties of the soil (pH in KC, granulometric composition, total organic carbon TOC, total nitrogen TN, fractional composition of humus, and the activity of enzymes). An increase in the plant secondary metabolite (PSM) and FRAP (ferring reducing ability of plasma) contents following the application of PGRs and N fertilisation already from as low a rate as 20 kg ha−1 was demonstrated. A significant positive correlation was noted between the abundance of Oulema spp. and the contents of total polyphenols, chlorogenic acid, and FRAP. No such relationship was noted for Aphididae or Thysanoptera. TOC content was higher on the plots on which N fertilisation was applied at the highest rate and after the application of PGRs. The factor determining the TN content was N fertilisation. Soil samples of the PGR0 N0 treatment were characterised by the greatest proportion of carbon in the humic and fulvic acid fractions and by the smallest proportion of carbon in the humin fraction. N fertilisation increased the proportion of carbon in the humin fraction on the plots on which no PGRs were applied. The study demonstrated an increase in the activity of oxidoreductive enzymes following the application of higher N rates. The application of PGRs resulted in no inhibition of enzymes in the soil compared to the control (PGRs0). Full article
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18 pages, 910 KiB  
Review
The Role of Selected Trace Elements in Oxidoreductive Homeostasis in Patients with Thyroid Diseases
by Marcin Wróblewski, Joanna Wróblewska, Jarosław Nuszkiewicz, Marta Pawłowska, Roland Wesołowski and Alina Woźniak
Int. J. Mol. Sci. 2023, 24(5), 4840; https://doi.org/10.3390/ijms24054840 - 2 Mar 2023
Cited by 28 | Viewed by 5836
Abstract
Impaired levels of selenium (Se), zinc (Zn), copper (Cu), iron (Fe), manganese (Mn) and iodine (I) in the organism may adversely affect the thyroid endocrine system. These trace elements play a role in the fight against oxidative stress as components of enzymes. Oxidative–antioxidant [...] Read more.
Impaired levels of selenium (Se), zinc (Zn), copper (Cu), iron (Fe), manganese (Mn) and iodine (I) in the organism may adversely affect the thyroid endocrine system. These trace elements play a role in the fight against oxidative stress as components of enzymes. Oxidative–antioxidant imbalance is considered a possible factor in many pathological conditions, including various thyroid diseases. In the available literature, there are few scientific studies showing a direct correlation of the effect of supplementation of trace elements on slowing down or preventing the occurrence of thyroid diseases in combination with the improvement of the antioxidant profile, or through the action of these elements as antioxidants. Among the available studies, it has been shown that an increase in lipid peroxidation levels and a decrease in the overall antioxidant defense status occur during such thyroid diseases as thyroid cancer, Hashimoto’s thyroiditis and dysthyroidism. In studies in which trace elements were supplemented, the following were observed: a decrease in the level of malondialdehyde after supplementation with Zn during hypothyroidism and reduction in the malondialdehyde level after Se supplementation with a simultaneous increase in the total activity status and activity of antioxidant defense enzymes in the course of autoimmune thyroiditis. This systematic review aimed to present the current state of knowledge about the relationship between trace elements and thyroid diseases in terms of oxidoreductive homeostasis. Full article
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19 pages, 4126 KiB  
Article
Rational Engineering of 3α-Hydroxysteroid Dehydrogenase/Carbonyl Reductase for a Biomimetic Nicotinamide Mononucleotide Cofactor
by Yan-Liang Chen, Yun-Hao Chou, Chia-Lin Hsieh, Shean-Jaw Chiou, Tzu-Pin Wang and Chi-Ching Hwang
Catalysts 2022, 12(10), 1094; https://doi.org/10.3390/catal12101094 - 21 Sep 2022
Cited by 3 | Viewed by 2544
Abstract
Enzymes are powerful biological catalysts for natural substrates but they have low catalytic efficiency for non-natural substrates. Protein engineering can be used to optimize enzymes for catalysis and stability. 3α-Hydroxysteroid dehydrogenase/carbonyl reductase (3α-HSD/CR) catalyzes the oxidoreduction reaction of NAD+ with androsterone. Based [...] Read more.
Enzymes are powerful biological catalysts for natural substrates but they have low catalytic efficiency for non-natural substrates. Protein engineering can be used to optimize enzymes for catalysis and stability. 3α-Hydroxysteroid dehydrogenase/carbonyl reductase (3α-HSD/CR) catalyzes the oxidoreduction reaction of NAD+ with androsterone. Based on the structure and catalytic mechanism, we mutated the residues of T11, I13, D41, A70, and I112 and they interacted with different portions of NAD+ to switch cofactor specificity to biomimetic cofactor nicotinamide mononucleotide (NMN+). Compared to wild-type 3α-HSD/CR, the catalytic efficiency of these mutants for NAD+ decreased significantly except for the T11 mutants but changed slightly for NMN+ except for the A70K mutant. The A70K mutant increased the catalytic efficiency for NMN+ by 8.7-fold, concomitant with a significant decrease in NAD+ by 1.4 × 104-fold, resulting in 9.6 × 104-fold cofactor specificity switch toward NMN+ over NAD+. Meanwhile, the I112K variant increased the thermal stability and changed to a three-state transition from a two-state transition of thermal unfolding of wild-type 3α-HSD/CR by differential scanning fluorimetry. Molecular docking analysis indicated that mutations on these residues affect the position and conformation of the docked NAD+ and NMN+, thereby affecting their activity. A70K variant sterically blocks the binding with NAD+, restores the H-bonding interactions of catalytic residues of Y155 and K159 with NMN+, and enhances the catalytic efficiency for NMN+. Full article
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21 pages, 1620 KiB  
Article
Potential of Trichoderma harzianum and Its Metabolites to Protect Wheat Seedlings against Fusarium culmorum and 2,4-D
by Julia Mironenka, Sylwia Różalska and Przemysław Bernat
Int. J. Mol. Sci. 2021, 22(23), 13058; https://doi.org/10.3390/ijms222313058 - 2 Dec 2021
Cited by 18 | Viewed by 3440
Abstract
Wheat is a critically important crop. The application of fungi, such as Trichoderma harzianum, to protect and improve crop yields could become an alternative solution to synthetic chemicals. However, the interaction between the fungus and wheat in the presence of stress factors [...] Read more.
Wheat is a critically important crop. The application of fungi, such as Trichoderma harzianum, to protect and improve crop yields could become an alternative solution to synthetic chemicals. However, the interaction between the fungus and wheat in the presence of stress factors at the molecular level has not been fully elucidated. In the present work, we exposed germinating seeds of wheat (Triticum aestivum) to the plant pathogen Fusarium culmorum and the popular herbicide 2,4-dichlorophenoxyacetic acid (2,4-D) in the presence of T. harzianum or its extracellular metabolites. Then, the harvested roots and shoots were analyzed using spectrometry, 2D-PAGE, and MALDI-TOF/MS techniques. Although F. culmorum and 2,4-D were found to disturb seed germination and the chlorophyll content, T. harzianum partly alleviated these negative effects and reduced the synthesis of zearalenone by F. culmorum. Moreover, T. harzianum decreased the activity of oxidoreduction enzymes (CAT and SOD) and the contents of the oxylipins 9-Hode, 13-Hode, and 13-Hotre induced by stress factors. Under the influence of various growth conditions, changes were observed in over 40 proteins from the wheat roots. Higher volumes of proteins and enzymes performing oxidoreductive functions, such as catalase, ascorbate peroxidase, cytochrome C peroxidase, and Cu/Zn superoxide dismutase, were found in the Fusarium-inoculated and 2,4-D-treated wheat roots. Additionally, observation of the level of 12-oxo-phytodienoic acid reductase involved in the oxylipin signaling pathway in wheat showed an increase. Trichoderma and its metabolites present in the system leveled out the mentioned proteins to the control volumes. Among the 30 proteins examined in the shoots, the expression of the proteins involved in photosynthesis and oxidative stress response was found to be induced in the presence of the herbicide and the pathogen. In summary, these proteomic and metabolomic studies confirmed that the presence of T. harzianum results in the alleviation of oxidative stress in wheat induced by 2,4-D or F. culmorum. Full article
(This article belongs to the Special Issue Plant-Microbe Interactions)
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12 pages, 1174 KiB  
Article
Changes in Antioxidative, Oxidoreductive and Detoxification Enzymes during Development of Aphids and Temperature Increase
by Roma Durak, Jan Dampc, Monika Kula-Maximenko, Mateusz Mołoń and Tomasz Durak
Antioxidants 2021, 10(8), 1181; https://doi.org/10.3390/antiox10081181 - 25 Jul 2021
Cited by 26 | Viewed by 3697
Abstract
Temperature, being the main factor that has an influence on insects, causes changes in their development, reproduction, winter survival, life cycles, migration timing, and population dynamics. The effects of stress caused by a temperature increase on insects may depend on many factors, such [...] Read more.
Temperature, being the main factor that has an influence on insects, causes changes in their development, reproduction, winter survival, life cycles, migration timing, and population dynamics. The effects of stress caused by a temperature increase on insects may depend on many factors, such as the frequency, amplitude, duration of the stress, sex, or the developmental stage of the insect. The aim of the study was to determine the differences in the enzymatic activity of nymphs and adult aphids Aphis pomi, Macrosiphum rosae and Cinara cupressi, and changes in their response to a temperature increase from 20 to 28 °C. The activity of enzymatic markers (superoxide dismutase (SOD), catalase (CAT), glutathione S-transferase (GST), β-glucosidase, polyphenol oxidase (PPO) and peroxidase (POD)) in aphid tissues was analysed for three constant temperatures. The results of our research showed that the enzymatic activity of aphids (measured as the activity of antioxidant, detoxifying and oxidoreductive enzymes) was mainly determined by the type of morph. We observed a strong positive correlation between the activity of the detoxifying and oxidoreductive enzymes and aphids’ development, and a negative correlation between the activity of the antioxidant enzymes and aphids’ development. Moreover, the study showed that an increase in temperature caused changes in enzyme activity (especially SOD, CAT and β-glucosidase), which was highest at 28 °C, in both nymphs and adults. Additionally, a strong positive correlation between metabolic activity (heat flow measured by microcalorimeter) and longevity was observed, which confirmed the relationship between these characteristics of aphids. The antioxidant enzyme system is more efficient in aphid nymphs, and during aphid development the activity of antioxidant enzymes decreases. The antioxidant enzyme system in aphids appears to deliver effective protection for nymphs and adults under stressful conditions, such as high temperatures. Full article
(This article belongs to the Special Issue Oxidative Stress Response in a Wide Variety of Insect Species)
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19 pages, 1780 KiB  
Article
Mild Abiotic Stress Affects Development and Stimulates Hormesis of Hemp Aphid Phorodon cannabis
by Roma Durak, Malgorzata Jedryczka, Beata Czajka, Jan Dampc, Katarzyna Wielgusz and Beata Borowiak-Sobkowiak
Insects 2021, 12(5), 420; https://doi.org/10.3390/insects12050420 - 8 May 2021
Cited by 10 | Viewed by 4412
Abstract
The hemp aphid Phorodon cannabis Passerini is a well- known (Asia, Europe) or newly emerging (North America) insect. It is a monophagous insect pest causing considerable damage in field and glasshouse cultivations. The aim of this work was to study the effects of [...] Read more.
The hemp aphid Phorodon cannabis Passerini is a well- known (Asia, Europe) or newly emerging (North America) insect. It is a monophagous insect pest causing considerable damage in field and glasshouse cultivations. The aim of this work was to study the effects of meteorological (temperature) and agronomical (herbicide) factors on the biology of the hemp aphid. In one experiment, hemp plants were kept at constant temperatures ranging from 20 to 30 °C, and aphid survival and fecundity were measured. In a related experiment conducted at 20 °C, plants were treated with field-appropriate rates of a selective graminicide containing quizalofop-P-tefuryl (40 gL−1, 4.38%, HRAC group 1), commonly used to control weeds in hemp, and aphid enzyme activity was measured in addition to population parameters. We found that hemp aphids could live, feed and reproduce within the whole studied range of temperatures, demonstrating its great evolutionary plasticity. However, the optimal temperature for development was 25 °C, at which the insect lived and reproduced for 25 and 15 days, respectively, with an average fecundity of 7.5 nymphs per reproduction day. The herbicide treatment increased the activity of superoxide dismutase (SOD), catalase (CAT), β-glucosidase, S-glutathione transferase (GST), oxidoreductive peroxidase (POD), and polyphenol oxidase (PPO) in the aphids, but only on certain days after treatment, which indicates a mild stress in aphid tissues, related to a higher reproduction and changed feeding behavior; aphids moved from the actively growing tips compared to untreated plants. The results of these experiments are discussed in terms of the impact on the future management of this pest. Full article
(This article belongs to the Collection Biology and Management of Sap-Sucking Pests)
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17 pages, 5468 KiB  
Article
Biochemical Background in Mitochondria Affects 2HG Production by IDH2 and ADHFE1 in Breast Carcinoma
by Jitka Špačková, Klára Gotvaldová, Aleš Dvořák, Alexandra Urbančoková, Kateřina Pospíšilová, David Větvička, Alberto Leguina-Ruzzi, Petra Tesařová, Libor Vítek, Petr Ježek and Katarína Smolková
Cancers 2021, 13(7), 1709; https://doi.org/10.3390/cancers13071709 - 4 Apr 2021
Cited by 7 | Viewed by 3626
Abstract
Mitochondrial production of 2-hydroxyglutarate (2HG) can be catalyzed by wild-type isocitrate dehydrogenase 2 (IDH2) and alcohol dehydrogenase, iron-containing 1 (ADHFE1). We investigated whether biochemical background and substrate concentration in breast cancer cells promote 2HG production. To estimate its role in 2HG production, we [...] Read more.
Mitochondrial production of 2-hydroxyglutarate (2HG) can be catalyzed by wild-type isocitrate dehydrogenase 2 (IDH2) and alcohol dehydrogenase, iron-containing 1 (ADHFE1). We investigated whether biochemical background and substrate concentration in breast cancer cells promote 2HG production. To estimate its role in 2HG production, we quantified 2HG levels and its enantiomers in breast cancer cells using analytical approaches for metabolomics. By manipulation of mitochondrial substrate fluxes using genetic and pharmacological approaches, we demonstrated the existence of active competition between 2HG producing enzymes, i.e., IDH2 and ADHFE1. Moreover, we showed that distinct fractions of IDH2 enzyme molecules operate in distinct oxido-reductive modes, providing NADPH and producing 2HG simultaneously. We have also detected 2HG release in the urine of breast cancer patients undergoing adjuvant therapy and detected a correlation with stages of breast carcinoma development. In summary, we provide a background for vital mitochondrial production of 2HG in breast cancer cells with outcomes towards cancer biology and possible future diagnosis of breast carcinoma. Full article
(This article belongs to the Section Molecular Cancer Biology)
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23 pages, 3307 KiB  
Article
Enzymatic Activity as New Moorsh-Forming Process Indicators of Peatlands
by Lech W. Szajdak, Teresa Meysner and Marek Szczepański
Agronomy 2021, 11(1), 113; https://doi.org/10.3390/agronomy11010113 - 8 Jan 2021
Cited by 3 | Viewed by 2689
Abstract
The aim of this study is to comprehensively assess the change in oxidoreductive enzyme activities, due to the potential in catalyzing oxidation and reduction reactions, as the basic processes on undrained and drained peat soils. On undrained peatlands, a significant decrease of enzyme [...] Read more.
The aim of this study is to comprehensively assess the change in oxidoreductive enzyme activities, due to the potential in catalyzing oxidation and reduction reactions, as the basic processes on undrained and drained peat soils. On undrained peatlands, a significant decrease of enzyme activities was observed such as xanthine oxidase, urate oxidase, phenol oxidase, and peroxidase with an increase in depth. It was connected with significantly higher porosity values, hot water extractable organic carbon, and total organic nitrogen contents, ammonium and nitrate ions concentrations, and significantly lower ash and bulk density values in the upper layers. On drained peatlands, a significant increase of enzyme activities in depth was measured. Enzyme activities such as xanthine, urate, phenol oxidase, and peroxidase were documented to be effective as new indicators and tools for changes of the moorsh-forming process in association with the oscillation of the water table caused by the drainage of the peatlands. Full article
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16 pages, 45362 KiB  
Article
In Silico Discovery of a Substituted 6-Methoxy-quinalidine with Leishmanicidal Activity in Leishmania infantum
by Strahinja Stevanović, Andrej Perdih, Milan Senćanski, Sanja Glišić, Margarida Duarte, Ana M. Tomás, Filipa V. Sena, Filipe M. Sousa, Manuela M. Pereira and Tom Solmajer
Molecules 2018, 23(4), 772; https://doi.org/10.3390/molecules23040772 - 27 Mar 2018
Cited by 28 | Viewed by 6295
Abstract
There is an urgent need for the discovery of new antileishmanial drugs with a new mechanism of action. Type 2 NADH dehydrogenase from Leishmania infantum (LiNDH2) is an enzyme of the parasite’s respiratory system, which catalyzes the electron transfer from NADH [...] Read more.
There is an urgent need for the discovery of new antileishmanial drugs with a new mechanism of action. Type 2 NADH dehydrogenase from Leishmania infantum (LiNDH2) is an enzyme of the parasite’s respiratory system, which catalyzes the electron transfer from NADH to ubiquinone without coupled proton pumping. In previous studies of the related NADH: ubiquinone oxidoreductase crystal structure from Saccharomyces cerevisiae, two ubiquinone-binding sites (UQI and UQII) were identified and shown to play an important role in the NDH-2-catalyzed oxidoreduction reaction. Based on the available structural data, we developed a three-dimensional structural model of LiNDH2 using homology detection methods and performed an in silico virtual screening campaign to search for potential inhibitors targeting the LiNDH2 ubiquinone-binding site 1—UQI. Selected compounds displaying favorable properties in the computational screening experiments were assayed for inhibitory activity in the structurally similar recombinant NDH-2 from S. aureus and leishmanicidal activity was determined in the wild-type axenic amastigotes and promastigotes of L. infantum. The identified compound, a substituted 6-methoxy-quinalidine, showed promising nanomolar leishmanicidal activity on wild-type axenic promastigotes and amastigotes of L. infantum and the potential for further development. Full article
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