Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases

A series of novel N-benzyl substituted amides of 1H-indole-5-carboxylic acid were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The target compounds (6bñ6e) displayed moderate potency to inhibit BuChE. One of the compounds tested, i.e., 1- benzylpiperidine amide of 1H-indole-5-carboxylic acid (6a) was a weak, non-selective inhibitor for both enzymes. The highest inhibitory activity towards BuChE (30.06% [10 μM]) was determined for compound (6c) which is 1-(3-chloro)benzylpiperidine amide of 1H-indole-5-carboxylic acid

The Effect of Pre-Drying Treatment and Drying Conditions on Quality and Energy Consumption of Hot Air-Dried Celeriac Slices: Optimisation

Celeriac is a good source of fibre, trace minerals, and phenolic compounds; it has a pleasant aroma but is a perishable material, prone to discolouration. This research investigated the optimisation of the quality and energy demand in hot-air dried celeriac slices. The experiment utilised the I-optimal design of response surface methodology with 30 experiment runs. Pre-drying treatments (blanching at 85 °C, three minutes; dipping in 1% citric acid solution, three minutes; no pre-drying treatment), drying temperatures (50, 60, and 70 °C), air velocities (1.5, 2.2, and 2.9 m/s), and thickness (three-, five, and seven-mm) were applied. The drying conditions affected drying time significantly (p < 0.0001). The model by Midilli and others and the logarithmic model fitted best with celeriac slices drying kinetics. Blanched samples had a higher ΔE*ab (total colour difference) and BI (browning index) but lower WI (whiteness index) than samples with other pre-drying treatments. The rehydration ratio decreased with the increase of sample thickness and blanching (p < 0.0001). A quadratic model described the specific energy consumption (Es) best. The dried samples compared with fresh samples had increased antioxidant activity but decreased total phenolic compound value. The optimisation solution chosen was 58 °C drying temperature, 2.9 m/s air velocity, and 4.6 mm sample thickness with acid pre-drying treatment

The effect of intermittent drying on drying kinetics and quality change dynamics of organic carrot (daucus carota v. laguna)

The objective of this research was to investigate the effect of intermittent drying on drying kinetics and quality of organic carrots. Drying time can be reduced by 18.2 % to 25.5% after tempering for 1 and 3 hours.Tempering for 3 hours at 30% moisture levels had shown shorter drying time, minimal color changes at 8.43 and the highest retention of total carotenoids of up to 7 8%.The Page, Midili and Two term equations were found to be appropriate to describe the drying kinetics of organic carrot

Prediction of total carotenoids, color, and moisture content of carrot slices during hot air drying using non‐invasive hyperspectral imaging technique

The objective of this paper was to evaluate the performance of Partial Least Square Regression (PLSR) model and to assess the statistical agreement between two different measurement techniques, that is, Vis–NIR hyperspectral imaging (HSI) and standard laboratory methods for quality evaluation of dried carrots throughout the hot‐air drying process. Carrots at commercial maturity of 3.5 months after planting were harvested in two seasons (2017 and 2018) and dried in a convective hot air dryer at 50°C, 60°C, and 70°C. Quality measurements were examined at intervals of 30 minutes. PLSR was performed as a regression model to predict quality attributes in carrots, while Passing–Bablok and Deming regressions alongside Blant–Altman analysis were applied as method comparisons. Excellent prediction performance for moisture content was observed with high R2T and R2v at 0.92 and 0.90 with values of RMSET and RMSEv at 8.15% and 8.16%. Satisfactory prediction accuracies were observed for total carotenoids (R2v = 0.64 and RMSEv = 32.62) μg/g, L* (R2v = 0.68 and RMSEv = 32.62), a* (R2v = 0.69 and RMSEv = 1.18), and b* (R2v = 0.60 and RMSEv = 1.45). Selected wavelengths for total carotenoids, moisture content, L*, a*, and b* based on the highest score of VIP loadings were 531, 973, 531, 531, and 680 nm, respectively. An adequate agreement of Blant–Altman analysis between the two methods within the upper and lower limits of 95% confidence interval (CI) were obtained for total carotenoids from 95.68 μg/g to 82.34 μg/g, moisture content (25.18% to 22.93%), L* (2.88 to −3.30), a* (4.15 to 3.43), and b* (4.53 to −3.11) with mean differences at 6.67, 1.12, −0.21, 0.36, and 0.71, respectively. Good correlation coefficients (r) were also observed at 0.89, 0.91, 0.78, and 0.83 for moisture content, L*, a*, and b* with a moderate correlation of total carotenoids at 0.69. The results indicate the potential feasibility of using non‐invasive measurement of quality attributes using hyperspectral imaging during the drying of carrots. Novelty impact statement non‐invasive measurement using hyperspectral imaging for quality determination in carrots during convective drying demonstrated promising results. Multivariate analysis of Partial Least Square Regression showed a good modeling performance for quality prediction in dried carrots. A good statistical agreements between non‐invasive quality measurements using hyperspectral imaging and standard laboratory analysis were achieved by comparative analysis using Blant–Altman plot, Deming, and Passing–Bablok regression.Bundesanstalt für Landwirtschaft und Ernährung http://dx.doi.org/10.13039/501100010771German Research Foundation (DFG‐Deutsche Forschungsgemeinschaft) http://dx.doi.org/10.13039/501100001659Institut Penyelidikan dan Kemajuan Pertanian Malaysia http://dx.doi.org/10.13039/501100007702Federal Ministry of Food and Agriculture http://dx.doi.org/10.13039/501100005908Coordination of European Transnational Research in Organic Food and Farming Systems http://dx.doi.org/10.13039/501100011598the Universität KasselPeer Reviewe

Evaluation of TLR4 expression and chosen parameters of oxidative-antioxidative balance in young children with food allergy.

The authors evaluated mRNA TLR4 expression on neutrophils and the chosen parameters of oxidative-antioxidative balance in blood of 35 children with food allergy (17 of them with IgE-dependent allergy and 18 with IgE-independent allergy) and 15 healthy children without any allergy. The age of these children ranged from 1 to 36 months. Children with food allergy in comparison with healthy children were found to have lower mRNA TLR4 expression, higher average value of chemiluminescence (CL) and its increase after stimulation by fMLP, PMA and OZ as well as lower TAS values. Disturbances of oxidative-antioxidative balance were found in children with food allergy. We suggest that natural immunity is involved in the development of food allergy mechanisms. Moreover, chemiluminescence can be used as an additional diagnostic test

Investigating the Effect of Different Drying Strategies on the Quality Parameters of Daucus carota L. Using Dynamic Process Control and Measurement Techniques

The present work aims to improve the understanding of the effect of different drying strategies at varying temperatures on the dynamic drying behaviour and quality of organic products such as carrots using non-invasive measurement techniques. For this purpose, carrot slices of 3 mm thickness were dried under three different strategies namely air temperature controlled (A), product temperature controlled (P) and stepwise temperature controlled (S) at different temperatures (50 °C, 60 °C and 70 °C) to measure and analyse the changes in moisture content, colour, total carotenoid retention, water activity, rehydration ratio and specific energy consumption. From the investigation performed, it was incurred that the application of different drying strategies influences rather significantly both the product quality as well as the overall process efficiency. Modelling the drying curves deemed Page model to be a good fit for all the strategies with R2adj = 0.99 and RMSE = 0.01. The results also show that implementing strategy P not only led to shorter drying times but also led to higher total carotenoid retention within the samples (TCR = 0.59–0.73). Colour changes, however, were observed to be maximum with strategy P as compared to strategy A and strategy S. Furthermore, the use of a non-invasive measurement technique such as infrared camera proved to be reliable in order to detect the phase transition of the product during the drying process

Influence of storage time on essential oil components in dried hops

Hop processors often store fresh hops in silos prior to drying. There has been little knowledge regarding the effect of storage on hops. To investigate the effects on product quality, freshly harvested hop cones were stored for 5 and 24 hr respectively and dried for 210 min at 65°C thereafter. The results obtained from gas chromatography (GC) investigations show an increase in linalool, ß-carophyllen, humulen and geraniol content and decrease in myrcene content based on the period of storage

Badanie wieloośrodkowe rozpoznań raka tarczycy

Introduction: In the front of the problems related to the differentiation between benign and malignant thyroid tumors we decided to perform a multicentre study in order to validate diagnoses of malignant thyroid tumors and assess the inter-observer variability. Material and methods: Material included 690 cases of malignant and benign thyroid lesions with primary histopathology established in 1985-1999. These cases were selected to multicentre study. The studies were sent from centres which agreed to participate in the project and than coded in the independent centre - Department of Nuclear Medicine and Endocrine Oncology. 40 pathologists from 25 centres provided their diagnoses which were compared with the reference ones. Results: 10 547 diagnoses were evaluated, both on their accuracy of the distinction between malignant and benign lesions and on their accuracy of cancer histotype definition. The reference diagnosis was made by an agreement between four expert pathologists (D.L., S.S., J.S. and A.K.). The participants diagnosed 21% of cases differently than experts. Concerning the diagnosis of cancer histotype, the difference between participants diagnosis and the reference one was even higher. The best concordance was achieved in the diagnosis of papillary thyroid cancer, however, on the cost of cancer overdiagnosis by some participants. Follicular cancer was diagnosed accurately only in 75.4% of cases. Conclusion: The study documents a high inter-observer variability of thyroid cancer diagnosis and confirms the lesser accuracy of diagnosis of follicular cancer.Wstęp: Histopatologia guzów tarczycy należy do jednych z trudniejszych działów patomorfologii. Wzrostowi liczby badań towarzyszy wiele problemów diagnostycznych, w tym najistotniejszych dotyczących różnicowania zmian łagodnych od złośliwych. Uważa się, że powtarzalność rozpoznania histopatologicznego w rakach tarczycy jest zdecydowanie niższa od spodziewanej. To stanowiło podstawę dla zaplanowania i realizacji wieloośrodkowego badania w celu sprawdzenia powtarzalności, wiarygodności i stopnia niezgodności histopatologicznej diagnostyki raków tarczycy. Materiał i metoda: Materiał stanowiły 690 rozpoznania pierwotne nadesłanych przypadków, rozpoznania referencyjne ustalone przez 4 ekspertów oraz rozpoznania uczestników prowadzonego w latach 2000-2002 badania wieloośrodkowego. Preparaty dostarczone z ośrodków, które wyraziły chęć uczestniczenia w grancie zostały zakodowane w ośrodku niezależnym - Zakładzie Medycyny Nuklearnej i Endokrynologii I.O. w Gliwicach. Preparaty po zakodowaniu były sukcesywnie rozsyłane do ośrodków uczestniczących w badaniu i oceniane przez uczestników badania jak i niezależnie przez czterech ekspertów. Na podstawie tych ostatnich rozpoznań było możliwe ustalenie puli rozpoznań referencyjnych bez konieczności powtórnej analizy preparatów. Rozpoznania te stanowiły "złoty standard", do którego odnoszono rozpoznania uczestników. Wyniki: 40 uczestników grantu postawiło łącznie 10 547 rozpoznań, diagnozując przeciętnie 264 przypadki. Rozpoznań niezgodnych co do złośliwości zmiany było 2262, co stanowi 21,44%. Sześciu z uczestników wykazało ponad 33% rozpoznań niezgodnych z rozpoznaniem referencyjnym. Odsetek rozpoznań niezgodnych wzrósł znacznie, gdy w analizie uwzględniono szczegółowy typ histologiczny raka i w tym przypadku co trzeci uczestnik nie zgadzał się z rozpoznaniem referencyjnym. Najwyższą zgodność rozpoznań, sięgającą 90%, odnotowano w ocenie raków brodawkowatych Uczestnicy stawiający rozpoznanie raka zgodne w wysokim procencie z rozpoznaniami referencyjnymi zdecydowanie rzadziej diagnozowali zgodnie z ekspertami zmiany łagodne. Rak pęcherzykowy zgodnie oceniono w 75,4% jednak aż 1/5 uczestników diagnozowała ponad 40% przypadków inaczej niż eksperci. Wniosek: Porównanie zgodności rozpoznań raka tarczycy między poszczególnymi patologami pozwala uściślić źródła błędów diagnostycznych oraz wyznaczyć kryteria dla poprawnej diagnostyki, które różnią się w zależności od typu raka

Glucagon-like peptide-1 receptor imaging with [Lys^{40}(Ahx-HYNIC-^{99m}Tc/EDDA)NH_2]-exendin-4 for the detection of insulinoma

PURPOSE: The objective of this article is to present a new method for the diagnosis of insulinoma with the use of [Lys(40)(Ahx-HYNIC-(99m)Tc/EDDA)NH(2)]-exendin-4. METHODS: Studies were performed in 11 patients with negative results of all available non-isotopic diagnostic methods (8 with symptoms of insulinoma, 2 with malignant insulinoma and 1 with nesidioblastosis). In all patients glucagon-like peptide-1 (GLP-1) receptor imaging (whole-body and single photon emission computed tomography/CT examinations) after the injection of 740 MBq of the tracer was performed. RESULTS: Both sensitivity and specificity of GLP-1 receptor imaging were assessed to be 100 % in patients with benign insulinoma. In all eight cases with suspicion of insulinoma a focal uptake in the pancreas was found. In six patients surgical excision of the tumour was performed (type G1 tumours were confirmed histopathologically). In one patient surgical treatment is planned. One patient was disqualified from surgery. In one case with malignant insulinoma pathological accumulation of the tracer was found only in the region of local recurrence. The GLP-1 study was negative in the other malignant insulinoma patient. In one case with suspicion of nesidioblastosis, a focal accumulation of the tracer was observed and histopathology revealed coexistence of insulinoma and nesidioblastosis. CONCLUSION: [Lys(40)(Ahx-HYNIC-(99m)Tc/EDDA)NH(2)]-exendin-4 seems to be a promising diagnostic tool in the localization of small insulinoma tumours, but requires verification in a larger series of patients