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19 pages, 476 KB  
Article
Evaluation of Different Sensor Systems for Classifying the Behavior of Dairy Cows on Pasture
by Barbara Pichlbauer, Jose Maria Chapa Gonzalez, Martin Bobal, Christian Guse, Michael Iwersen and Marc Drillich
Sensors 2024, 24(23), 7739; https://doi.org/10.3390/s24237739 - 3 Dec 2024
Cited by 5 | Viewed by 2116
Abstract
Monitoring animal behavior using sensor technologies requires prior testing under varying conditions because behaviors can differ significantly, such as between grazing and confined cows. This study aimed to validate several sensor systems for classifying rumination and lying behaviors in cows on pasture under [...] Read more.
Monitoring animal behavior using sensor technologies requires prior testing under varying conditions because behaviors can differ significantly, such as between grazing and confined cows. This study aimed to validate several sensor systems for classifying rumination and lying behaviors in cows on pasture under different environmental conditions, compare the sensors’ performance at different time resolutions, and evaluate a correction algorithm for rumination data. Ten Simmental dairy cows were monitored on pasture, each simultaneously equipped with an ear-tag accelerometer (ET), two different leg-mounted accelerometers (LMs), and a noseband sensor (NB). Indirect visual observations using drone-recorded video footage served as the gold standard for validation. The concordance correlation coefficient (CCC) for rumination time was very high for both the ET and NB (0.91–0.96) at a 10 min time resolution. Applying the correction algorithm to 1 min data improved the CCC for the NB from 0.68 to 0.89. For lying time, the CCC was moderate for the ET (0.55) but nearly perfect for both LMs (0.99). In conclusion, both sensors evaluated for classifying rumination are suitable for cows on pasture. We recommend using a correction algorithm for 1 min NB data. For the measurement of lying time, the LMs significantly outperformed the ET. Full article
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15 pages, 287 KB  
Article
Alternatives to Traditional Aging of Bobal Red Wines from Semi-Arid Climate: Influence on Phenolic Composition and Related Properties
by María Osorio Alises, Eva Sánchez Palomo and M. Ángel González-Viñas
Beverages 2024, 10(3), 89; https://doi.org/10.3390/beverages10030089 - 13 Sep 2024
Cited by 1 | Viewed by 1636
Abstract
The effect of oak chips on the phenolic composition, color characteristics, and antioxidant capacity of Bobal red wines caused by contact with oak chips at different stages of the winemaking process has been studied. Performance liquid chromatography–diode array detection (HPLC-DAD) was used to [...] Read more.
The effect of oak chips on the phenolic composition, color characteristics, and antioxidant capacity of Bobal red wines caused by contact with oak chips at different stages of the winemaking process has been studied. Performance liquid chromatography–diode array detection (HPLC-DAD) was used to determine the detailed phenolic composition of wines and antioxidant activity, and chromatic characteristics were determined by spectrophotometric methods. Standard red winemaking process was applied to make the Bobal control wine. The rest of the wines were elaborated with oak chip contact at two dose levels (3 and 6 g/L) in different phases of the winemaking process: during alcoholic fermentation (AF), during malolactic fermentation (MLF), and in young wines. The phenolic composition, antioxidant activity, and chromatic characteristics of Bobal control wines were slightly but significantly modified by contact with the oak chips. Wines in contact with oak chips during malolactic fermentation showed a decrease in the concentration of resveratrol-monomer stilbenes, monomeric anthocyanins, and pyranoanthocyanins. In general, the concentration of total resveratrol is influenced by the dose level used, resulting in a 10% decrease when the dose level is 6 g/L compared to the 3 g/L dose. Full article
(This article belongs to the Section Wine, Spirits and Oenological Products)
8 pages, 562 KB  
Technical Note
Field Evaluation of a Rising Plate Meter to Estimate Herbage Mass in Austrian Pastures
by Jose Maria Chapa, Barbara Pichlbauer, Martin Bobal, Christian Guse, Marc Drillich and Michael Iwersen
Sensors 2023, 23(17), 7477; https://doi.org/10.3390/s23177477 - 28 Aug 2023
Cited by 4 | Viewed by 1926
Abstract
Pasture management is an important topic for dairy farms with grazing systems. Herbage mass (HM) is a key measure, and estimations of HM content in pastures allow for informed decisions in pasture management. A common method of estimating the HM content in pastures [...] Read more.
Pasture management is an important topic for dairy farms with grazing systems. Herbage mass (HM) is a key measure, and estimations of HM content in pastures allow for informed decisions in pasture management. A common method of estimating the HM content in pastures requires manually collected grass samples, which are subjected to laboratory analysis to determine the dry matter (DM) content. However, in recent years, new methods have emerged that generate digital data and aim to expedite, facilitate and improve the measurement of HM. This study aimed to evaluate the accuracy of a rising plate meter (RPM) tool in a practical setting to estimate HM in Austrian pastures. With this study, we also attempted to answer whether the tool is ready for use by farmers with its default settings. This study was conducted on the teaching and research farm of the University of Veterinary Medicine in Vienna, Austria. Data were collected from May to October 2021 in five different pastures. To evaluate the accuracy of the RPM tool, grass samples were collected and dried in an oven to extract their DM and calculate the HM. The HM obtained from the grass samples was used as the gold standard for this study. In total, 3796 RPM measurements and 203 grass samples yielding 49 measurement points were used for the evaluation of the RPM tool. Despite the differences in pasture composition, the averaged HM from the RPM tool showed a strong correlation with the gold standard (R2 = 0.73, rp = 0.86, RMSE = 517.86, CV = 33.67%). However, the results may not be good enough to justify the use of the tool, because simulations in economic studies suggest that the error of prediction should be lower than 15%. Furthermore, in some pastures, the RPM obtained poor results, indicating an additional need for pasture-specific calibrations, which complicates the use of the RPM tool. Full article
(This article belongs to the Special Issue Crop and Animal Sensors for Agriculture 5.0)
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22 pages, 2606 KB  
Article
First Approach to the Aroma Characterization of Monovarietal Red Wines Produced from Varieties Better Adapted to Abiotic Stresses
by Francesco Agostinelli, Ilda Caldeira, Jorge M. Ricardo-da-Silva, Miguel Damásio, Ricardo Egipto and José Silvestre
Plants 2023, 12(10), 2063; https://doi.org/10.3390/plants12102063 - 22 May 2023
Cited by 4 | Viewed by 2889
Abstract
Adaptation strategies in the wine sector consist of the use of cultural techniques to limit damages caused by climate change, using, among other resources, varieties better adapted to the scenarios of abiotic stress exacerbation, namely water and thermal stress, as well as those [...] Read more.
Adaptation strategies in the wine sector consist of the use of cultural techniques to limit damages caused by climate change, using, among other resources, varieties better adapted to the scenarios of abiotic stress exacerbation, namely water and thermal stress, as well as those more tolerant to heatwaves. With the intention to determine the aromatic characterization of ten monovarietal wines produced from cultivars with high productive performance in a global warming scenario (‘Petit Verdot’, ‘Marselan’, ‘Merlot’, ‘Touriga Franca’, ‘Syrah’, ‘Vinhão’, ‘Bobal’, ‘Preto Martinho’, ‘Trincadeira’, and ‘Alicante Bouschet’), grown in Esporão vineyard (Alentejo, Portugal) and submitted to deficit irrigation (Ks ± 0.5), their aromatic character has been analyzed. Each grape variety was vinified at a small scale, in duplicate, and the wines were evaluated by a sensory panel, which rated several sensory attributes (visual, olfactory, and gustatory). Sensory analysis revealed a discrete appreciation for the monovarietal wines tasted, showing a differentiation at the olfactory level that was not too marked, although present, between the samples. The free volatile compounds were analysed using gas chromatography-olfactometry (GC-O), identified using a gas chromatography-mass spectrometry (GC-MS) technique and semi-quantified using the gas chromatography-flame ionization detector (GC-FID) technique. Based on the interpolation of the results of the various statistical analyses carried out, 49 probable odor active compounds (pOACs) were identified and based on the odor activity values (OAVs), 24 of them were recognized as odor active compounds (OACs) originated mainly during the fermentation processes. An aromatic characterization of the varieties has been proposed. Full article
(This article belongs to the Special Issue Grapevine Response to Abiotic Stress)
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16 pages, 2071 KB  
Article
Agronomic Response of 13 Spanish Red Grapevine (Vitis vinifera L.) Cultivars under Drought Conditions in a Semi-Arid Mediterranean Climate
by A. Sergio Serrano, Jesús Martínez-Gascueña, Gonzalo L. Alonso, Cristina Cebrián-Tarancón, M. Dolores Carmona, Adela Mena and Juan L. Chacón-Vozmediano
Agronomy 2022, 12(10), 2399; https://doi.org/10.3390/agronomy12102399 - 4 Oct 2022
Cited by 7 | Viewed by 2598
Abstract
Drought is perhaps the most important abiotic stressor affecting plants. Grapevine (Vitis vinifera L.) is a drought-tolerant species, and this feature makes it a traditional crop in semi-arid climate areas. However, not all cultivars respond to drought in the same way. Many [...] Read more.
Drought is perhaps the most important abiotic stressor affecting plants. Grapevine (Vitis vinifera L.) is a drought-tolerant species, and this feature makes it a traditional crop in semi-arid climate areas. However, not all cultivars respond to drought in the same way. Many studies on grapevine drought response have focused on physiological traits. This study mainly used agronomic indicators to assess the drought response of 13 red cultivars. Our results revealed high variability in must isotope ratios (δ13C and δ18O), yield components, and grape must quality. Bobal, Garnacha Peluda, Garnacha Tinta, Mazuela, and Moribel cultivars responded well to drought conditions, simultaneously maintaining high yields and must quality. By contrast, Garnacha Tintorera, Forcallat Tinta, and Tempranillo cultivars showed high water use efficiency but had low yield and must quality. Therefore, these cultivars can be considered poorly adapted to drought conditions. By knowing which cultivars perform well under drought conditions, viticulturists can reduce their reliance on water irrigation and continue to maintain vineyard sustainability in current and future semi-arid climatic conditions. This research also contributes novel information about the Castilla-La Mancha region, where there have been no previous similar assays. Full article
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16 pages, 2082 KB  
Article
Characterization of Local Mediterranean Grapevine Varieties for Their Resilience to Semi-Arid Conditions under a Rain-Fed Regime
by Carmina Gisbert, Jaume X. Soler, Mariano Fos, Diego S. Intrigliolo, Alberto Yuste, Belén Picó, Daniel Torrent and Rosa Peiró
Agronomy 2022, 12(9), 2234; https://doi.org/10.3390/agronomy12092234 - 19 Sep 2022
Cited by 9 | Viewed by 3086
Abstract
Viticultural adaptations to climate change are needed, and the utilization of grapevine varieties that are better-adapted to water scarcity could contribute to finding grape varieties that are adapted to climate change. The present research was carried out to expand the limited knowledge on [...] Read more.
Viticultural adaptations to climate change are needed, and the utilization of grapevine varieties that are better-adapted to water scarcity could contribute to finding grape varieties that are adapted to climate change. The present research was carried out to expand the limited knowledge on the minor varieties Arcos and Forcallat in comparison with three other more widespread traditional Mediterranean cultivars (Bobal, Garnacha, and Monastrell). An ampelographic characterization was carried out and provided with the characteristics for the cv. Arcos, which have not been previously described, as well as traits that are useful for differentiating it from the cv. Forcallat. Both varieties maintained low stomatal conductance, having the highest number of small stomata in comparison to the rest of varieties. Arcos and Forcallat also showed the highest intrinsic water use efficiency in addition to being late ripening, a characteristic that could be of interest in the context of water scarcity and warm climates for better coupling of technological and phenolic maturity. In parallel, we analyzed Veremeta plants considered a synonym of Monastrell, which were growing in the same field. The synonymy was confirmed by SSR markers, but phenotypic differences between plant materials were determined in relation to their ampelographic, agronomical, and physiological traits. Indeed, both accessions are very interesting as materials to be studied in agronomic trials under different watering regimes in order to deepen our understanding of the mechanisms underlying the drought tolerance of the evaluated Mediterranean varieties. Full article
(This article belongs to the Special Issue Current Progress in Improving Water Use Efficiency of Vineyards)
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19 pages, 728 KB  
Article
Preliminary Studies on Endotherapy Based Application of Ozonated Water to Bobal Grapevines: Effect on Wine Quality
by Ana Campayo, Cristina Cebrián-Tarancón, María Mercedes García-Martínez, María Rosario Salinas, Gonzalo L. Alonso and Kortes Serrano de la Hoz
Molecules 2022, 27(16), 5155; https://doi.org/10.3390/molecules27165155 - 12 Aug 2022
Cited by 3 | Viewed by 2127
Abstract
The application of ozonated water in the vineyard is an increasingly popular tool for disease management, but the quality of grapes and resulting wines is likely to be affected. Endotherapy, or trunk injection, is a particularly useful method to apply phytosanitary products since [...] Read more.
The application of ozonated water in the vineyard is an increasingly popular tool for disease management, but the quality of grapes and resulting wines is likely to be affected. Endotherapy, or trunk injection, is a particularly useful method to apply phytosanitary products since many fungal pathogens colonize the grapevine woody tissues. Thus, the present study aimed to evaluate the effect on wine quality of the ozonated water applied to Bobal grapevines, one of the most cultivated red varieties in Spain, through endotherapy (E) or its combination with spraying (E + S). Endotherapy was carried out four times before harvest for both E and E + S treatments, and spraying was performed 2 days before and after each endotherapy application. Grapes were harvested, vinified, and the quality of the finished wines was evaluated through several enological parameters and the phenolic and volatile composition. Both treatments resulted in less alcoholic and more acidic wines. The E treatment, although it reduced the content of phenolic acids, stilbenes and flavanols, significantly increased anthocyanins, whereas E + S decreased the overall amount of phenolics, which had different implications for wine colour. In terms of aroma, both treatments, but E to a greater extent, reduced the content of glycosylated precursors and differentially affected free volatiles, both varietal and fermentative. Thus, the dose of ozonated water, frequency and/or method of application are determining factors in the effect of these treatments on wine quality and must be carefully considered by winegrowers to establish the optimum treatment conditions so as not to impair the quality of wines. Full article
(This article belongs to the Collection Wine Chemistry)
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18 pages, 1742 KB  
Review
The Role of ATRA, Natural Ligand of Retinoic Acid Receptors, on EMT-Related Proteins in Breast Cancer: Minireview
by Pavel Bobal, Marketa Lastovickova and Janette Bobalova
Int. J. Mol. Sci. 2021, 22(24), 13345; https://doi.org/10.3390/ijms222413345 - 12 Dec 2021
Cited by 10 | Viewed by 4816
Abstract
The knowledge of the structure, function, and abundance of specific proteins related to the EMT process is essential for developing effective diagnostic approaches to cancer with the perspective of diagnosis and therapy of malignancies. The success of all-trans retinoic acid (ATRA) differentiation [...] Read more.
The knowledge of the structure, function, and abundance of specific proteins related to the EMT process is essential for developing effective diagnostic approaches to cancer with the perspective of diagnosis and therapy of malignancies. The success of all-trans retinoic acid (ATRA) differentiation therapy in acute promyelocytic leukemia has stimulated studies in the treatment of other tumors with ATRA. This review will discuss the impact of ATRA use, emphasizing epithelial-mesenchymal transition (EMT) proteins in breast cancer, of which metastasis and recurrence are major causes of death. Full article
(This article belongs to the Section Molecular Oncology)
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5 pages, 387 KB  
Proceeding Paper
Investigation of the Effect of Selected Piperazine-2,5-Diones on Cartilage-Related Cells
by Josef Jampilek, Jan Hosek and Pavel Bobal
Chem. Proc. 2022, 8(1), 108; https://doi.org/10.3390/ecsoc-25-11650 - 13 Nov 2021
Viewed by 1335
Abstract
Various chronic inflammatory diseases have become a problem, especially in the Western world. Whether it concerns inflammation of visceral organs, joints, bones, etc., it is always a physiological reaction of the body, which always tries to eradicate harmful substances and restore tissue homeostasis. [...] Read more.
Various chronic inflammatory diseases have become a problem, especially in the Western world. Whether it concerns inflammation of visceral organs, joints, bones, etc., it is always a physiological reaction of the body, which always tries to eradicate harmful substances and restore tissue homeostasis. Unfortunately, prolonged or chronic inflammation often results in damage to the affected tissues. Diseases such as osteoarthritis, rheumatoid arthritis, and arthrosis, as well as cartilage damage, are very common. In addition to suppressing inflammation in the joints and around the cartilage, it is advantageous to administer compounds that are capable of stimulating cartilage growth and regenerating damaged tissue. Variously substituted piperazine-2,5-dione derivatives were investigated as compounds with a potential effect on cartilage regeneration. A series of assays were performed to evaluate their cytotoxicity, anti-inflammatory activity, and ability to potentiate chondrocyte proliferation and suppress synovial cell growth. The compounds proved to be completely non-toxic for all used types of cells up to the concentration of 20 µM. Unfortunately, their evaluated biological activity proved to be insignificant based on the comparison with untreated cells. Full article
18 pages, 1559 KB  
Article
Novel Endotherapy-Based Applications of Ozonated Water to Bobal Grapevines: Effect on Grape Quality
by Ana Campayo, Kortes Serrano de la Hoz, M. Mercedes García-Martínez, M. Rosario Salinas and Gonzalo L. Alonso
Agronomy 2020, 10(9), 1218; https://doi.org/10.3390/agronomy10091218 - 19 Aug 2020
Cited by 9 | Viewed by 4652
Abstract
Ozonated water has recently been incorporated in the management of grapevine diseases, which in turn can alter the fruit quality. When wood-inhabiting pathogens are involved, trunk injection or “endotherapy” represents a promising application method. Thus, the present study aimed to evaluate the effect [...] Read more.
Ozonated water has recently been incorporated in the management of grapevine diseases, which in turn can alter the fruit quality. When wood-inhabiting pathogens are involved, trunk injection or “endotherapy” represents a promising application method. Thus, the present study aimed to evaluate the effect on grape quality of ozonated water applied to Vitis vinifera L. cv. Bobal grapevines through endotherapy (E) or its combination with spraying (E + S). Grape quality at harvest was evaluated through several enological and chromatic parameters, the phenolic maturity, the varietal aroma potential index (IPAv) and the phenolic and volatile composition. The E treatment improved the chromatic characteristics and favored the accumulation of phenolic compounds. Conversely, E + S had a detrimental effect on the color and phenolic content and, although their synthesis was enhanced, the extractability of anthocyanins was negatively affected. In terms of aroma, both treatments reduced the content of glycosylated precursors but increased certain free volatiles. The application of ozonated water to grapevines, even when injected into the trunk, results in changes in fruit quality and a possible impact on wine attributes. Our findings and those in the literature support that, with the appropriate dose, frequency and method of application, ozonated water could be used with a twofold objective: disease management and grape quality improvement. Full article
(This article belongs to the Special Issue Ozone Effects on Crop Production)
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20 pages, 329 KB  
Article
Spraying Ozonated Water on Bobal Grapevines: Effect on Wine Quality
by Ana Campayo, Kortes Serrano de la Hoz, M. Mercedes García-Martínez, M. Rosario Salinas and Gonzalo L. Alonso
Biomolecules 2020, 10(2), 213; https://doi.org/10.3390/biom10020213 - 1 Feb 2020
Cited by 16 | Viewed by 3755
Abstract
Ozonated water is being introduced as an alternative phytosanitary treatment to control grapevine diseases in a context in which the reduction of chemical pesticides has become an urgent necessity. In this study, we evaluated the effect of spraying grapevines with ozonated water on [...] Read more.
Ozonated water is being introduced as an alternative phytosanitary treatment to control grapevine diseases in a context in which the reduction of chemical pesticides has become an urgent necessity. In this study, we evaluated the effect of spraying grapevines with ozonated water on the enological, phenolic, and aromatic qualities of Bobal wines during two consecutive growing seasons. In the first season, ozonated water was applied once during the ripening period on grapevines trained on the traditional gobelet system (S1). In the second season, three applications were performed between fruit set and harvest on grapevines grown on a vertical trellis system (S2). The S1 treatment led to a wine with an increased alcoholic degree and a remarkably higher phenolic content, which resulted in preferable chromatic characteristics. The S2 treatment maintained the total phenolic content but significantly enhanced stilbenes and flavanols and also reduced anthocyanins, which negatively affected the wine colour. Regarding aroma, both treatments reduced the content of glycosylated precursors and had different effects on free volatiles, both varietal and fermentative. Thus, the metabolic response of grapevines to the ozonated water stress, and therefore the quality of wines, depended on the ozone dose received by the plants. Full article
(This article belongs to the Special Issue Biochemistry of Wine and Beer)
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29 pages, 4248 KB  
Article
SAR-mediated Similarity Assessment of the Property Profile for New, Silicon-Based AChE/BChE Inhibitors
by Andrzej Bak, Hana Pizova, Violetta Kozik, Katarina Vorcakova, Jiri Kos, Jakub Treml, Klara Odehnalova, Michal Oravec, Ales Imramovsky, Pavel Bobal, Adam Smolinski, Zdeněk Trávníček and Josef Jampilek
Int. J. Mol. Sci. 2019, 20(21), 5385; https://doi.org/10.3390/ijms20215385 - 29 Oct 2019
Cited by 12 | Viewed by 4468
Abstract
A set of 25 novel, silicon-based carbamate derivatives as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors was synthesized and characterized by their in vitro inhibition profiles and the selectivity indexes (SIs). The prepared compounds were also tested for their inhibition potential on photosynthetic electron [...] Read more.
A set of 25 novel, silicon-based carbamate derivatives as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors was synthesized and characterized by their in vitro inhibition profiles and the selectivity indexes (SIs). The prepared compounds were also tested for their inhibition potential on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. In fact, some of the newly prepared molecules revealed comparable or even better inhibitory activities compared to the marketed drugs (rivastigmine or galanthamine) and commercially applied pesticide Diuron®, respectively. Generally, most compounds exhibited better inhibition potency towards AChE; however, a wider activity span was observed for BChE. Notably, benzyl N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(2-hydroxyphenyl)carbamoyl]ethyl]-carbamate (2) and benzyl N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(3-hydroxyphenyl)carbamoyl]ethyl]-carbamate (3) were characterized by fairly high selective indexes. Specifically, compound 2 was prescribed with the lowest IC50 value that corresponds quite well with galanthamine inhibition activity, while the inhibitory profiles of molecules 3 and benzyl-N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(4-hydroxyphenyl)carbamoyl]ethyl]carbamate (4) are in line with rivastigmine activity. Moreover, a structure–activity relationship (SAR)-driven similarity evaluation of the physicochemical properties for the carbamates examined appeared to have foreseen the activity cliffs using a similarity–activity landscape index for BChE inhibitory response values. The ‘indirect’ ligand-based and ‘direct’ protein-mediated in silico approaches were applied to specify electronic/steric/lipophilic factors that are potentially valid for quantitative (Q)SAR modeling of the carbamate analogues. The stochastic model validation was used to generate an ‘average’ 3D-QSAR pharmacophore pattern. Finally, the target-oriented molecular docking was employed to (re)arrange the spatial distribution of the ligand property space for BChE and photosystem II (PSII). Full article
(This article belongs to the Special Issue QSAR and Chemoinformatics Tools for Modeling)
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13 pages, 2393 KB  
Article
Genotoxic Effects of Tributyltin and Triphenyltin Isothiocyanates, Cognate RXR Ligands: Comparison in Human Breast Carcinoma MCF 7 and MDA-MB-231 Cells
by Luba Hunakova, Eva Horvathova, Karolina Majerova, Pavel Bobal, Jan Otevrel and Julius Brtko
Int. J. Mol. Sci. 2019, 20(5), 1198; https://doi.org/10.3390/ijms20051198 - 9 Mar 2019
Cited by 18 | Viewed by 3544
Abstract
The cytotoxicity of two recently synthesized triorganotin isothiocyanate derivatives, nuclear retinoid X receptor ligands, was tested and compared in estrogen-receptor-positive MCF 7 and -negative MDA-MB-231 human breast carcinoma cell lines. A 48 h MTT assay indicated that tributyltin isothiocyanate (TBT-ITC) is more cytotoxic [...] Read more.
The cytotoxicity of two recently synthesized triorganotin isothiocyanate derivatives, nuclear retinoid X receptor ligands, was tested and compared in estrogen-receptor-positive MCF 7 and -negative MDA-MB-231 human breast carcinoma cell lines. A 48 h MTT assay indicated that tributyltin isothiocyanate (TBT-ITC) is more cytotoxic than triphenyltin isothiocyanate (TPT-ITC) in MCF 7 cells, and the same trend was observed in the MDA-MB-231 cell line. A comet assay revealed the presence of both crosslinks and increasing DNA damage levels after the 17 h treatment with both derivatives. Differences in cytotoxicity of TBT-ITC and TPT-ITC detected by FDA staining correspond to the MTT data, communicating more pronounced effects in MCF 7 than in the MDA-MB-231 cell line. Both derivatives were found to cause apoptosis, as shown by the mitochondrial membrane potential (MMP) depolarization and caspase-3/7 activation. The onset of caspase activation correlated with MMP dissipation and the total cytotoxicity more than with the amount of active caspases. In conclusion, our data suggest that the DNA damage induced by TBT-ITC and TPT-ITC treatment could underlie their cytotoxicity in the cell lines studied. Full article
(This article belongs to the Section Molecular Toxicology)
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14 pages, 1274 KB  
Article
Investigation of Permeation of Theophylline through Skin Using Selected Piperazine-2,5-Diones
by Aneta Pokorna, Pavel Bobal, Michal Oravec, Lucie Rarova, Janette Bobalova and Josef Jampilek
Molecules 2019, 24(3), 566; https://doi.org/10.3390/molecules24030566 - 4 Feb 2019
Cited by 10 | Viewed by 5103
Abstract
Transdermal administration of drugs that penetrate, in this case directly into the blood circulation, has many advantages and is promising for many drugs thanks to its easy application and good patient compliance. (S)-8-Methyl-6,9-diazaspiro[4.5]decan-7,10-dione (alaptide), has been studied as a potential chemical [...] Read more.
Transdermal administration of drugs that penetrate, in this case directly into the blood circulation, has many advantages and is promising for many drugs thanks to its easy application and good patient compliance. (S)-8-Methyl-6,9-diazaspiro[4.5]decan-7,10-dione (alaptide), has been studied as a potential chemical permeation enhancer. Based on its structure, four selected piperazine-2,5-diones were synthesized by means of multi-step synthetic pathways. All the compounds were investigated on their ability to enhance the permeation of the model drug theophylline from the hydrophilic medium propylene glycol:water (1:1). In vitro experiments were performed using vertical Franz diffusion cells at constant temperature 34 ± 0.5 °C and using full-thickness pig (Sus scrofa f. domestica) ear skin. Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline. All the compounds were applied in ratio 1:10 (w/w) relative to the amount of theophylline. One hour after application, the permeated amount of theophylline from formulations with alaptide and (3S,6S)-3,6-dimethylpiperazine-2,5-dione, was ca. 15- and 12-fold higher, respectively, than from the formulation without the tested compounds. Despite the enhancement ratio of both enhancers in a steady state was ca. 2.3, the pseudo-enhancement ratio in the time range from 1 to 3 h was 4.4. These enhancement ratios indicate that the compounds are able to enhance the permeation of agents through the skin; however, the short-term application of both compound formulations seems to be more advantageous. In addition, the screening of the cytotoxicity of all the prepared compounds was performed using three cell lines, and the compounds did not show any significant toxic effect. Full article
(This article belongs to the Special Issue Heterocycles in Medicinal Chemistry)
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16 pages, 2574 KB  
Article
Triorganotin Derivatives Induce Cell Death Effects on L1210 Leukemia Cells at Submicromolar Concentrations Independently of P-glycoprotein Expression
by Viera Bohacova, Mario Seres, Lucia Pavlikova, Szilvia Kontar, Martin Cagala, Pavel Bobal, Jan Otevrel, Julius Brtko, Zdena Sulova and Albert Breier
Molecules 2018, 23(5), 1053; https://doi.org/10.3390/molecules23051053 - 1 May 2018
Cited by 12 | Viewed by 4737
Abstract
The acceleration of drug efflux activity realized by plasma membrane transporters in neoplastic cells, particularly by P-glycoprotein (P-gp, ABCB1 member of the ABC transporter family), represents a frequently observed molecular cause of multidrug resistance (MDR). This multiple resistance represents a real obstacle in [...] Read more.
The acceleration of drug efflux activity realized by plasma membrane transporters in neoplastic cells, particularly by P-glycoprotein (P-gp, ABCB1 member of the ABC transporter family), represents a frequently observed molecular cause of multidrug resistance (MDR). This multiple resistance represents a real obstacle in the effective chemotherapy of neoplastic diseases. Therefore, identifying cytotoxic substances that are also effective in P-gp overexpressing cells may be useful for the rational design of substances for the treatment of malignancies with developed MDR. Here, we showed that triorganotin derivatives—tributyltin-chloride (TBT-Cl), tributyltin-bromide (TBT-Br), tributyltin-iodide (TBT-I) and tributyltin-isothiocyanate (TBT-NCS) or triphenyltin-chloride (TPT-Cl) and triphenyltin-isothiocyanate (TPT-NCS)—could induce the death of L1210 mice leukemia cells at a submicromolar concentration independently of P-gp overexpression. The median lethal concentration obtained for triorganotin derivatives did not exceed 0.5 µM in the induction of cell death of either P-gp negative or P-gp positive L1210 cells. Apoptosis related to regulatory pathway of Bcl-2 family proteins seems to be the predominant mode of cell death in either P-gp negative or P-gp positive L1210 cells. TBT-Cl and TBT-Br were more efficient with L1210 cells overexpressing P-gp than with their counterpart P-gp negative cells. In contrast, TBT-I and TPT-NCS induced a more pronounced cell death effect on P-gp negative cells than on P-gp positive cells. Triorganotin derivatives did not affect P-gp efflux in native cells measured by calcein retention within the cells. Taken together, we assumed that triorganotin derivatives represent substances suitable for suppressing the viability of P-gp positive malignant cells. Full article
(This article belongs to the Section Medicinal Chemistry)
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