http://hdl.handle.net/20.500.12603/46 Přírodovědecká fakulta 2026-08-16T07:37:32Z http://hdl.handle.net/20.500.12603/2849 Immobilized animal liver microsomes: A versatile tool for efficient ester hydrolysis in chemo-enzymatic synthesis☆ Monnier, Charline; Andrýs, Rudolf; Castellino, Irene; Mičková, Veronika; Halečková, Annamária; Loskot, Jan; Benek, Ondřej; Zemanová, Lucie Animal liver microsomes are a rich source of carboxylesterases with potential for biocatalytic applications. However, their instability and difficulty in reuse limit their practical application. This study investigates the immobilization of animal liver microsomes from four species Mus musculus (house mouse), Sus scrofa (wild boar), Dama dama (fallow deer), and Capreolus capreolus (roe deer) on Perloza MG microparticles for enhanced stability and reusability. Immobilization significantly improved the stability and pH tolerance of the microsomes, particularly those from D. dama, maintaining esterase activity across a broad pH range (5-9) and enabling the reusability over ten consecutive cycles. The immobilized D. dama microsomes were successfully employed in a preparative-scale chemo-enzymatic synthesis of a cyclophilin D inhibitor, achieving a total reaction yield of 68% with 98% final product purity, demonstrating their potential for sustainable organic synthesis. 2025-01-01T00:00:00Z http://hdl.handle.net/20.500.12603/2846 Experimental investigations on cryogenic friction- stir welding of similar ZE42 magnesium alloys Trojovský, Pavel; Dhasarathan, Vigneswaran; Boopathi, Sampath In this research, the cryogenic friction stir welding (CFSW) process has been performed using a liquid nitrogen medium to join two similar ZE42 magnesium alloy plates. The new experimental setup has been designed and fabricated to supply low-temperature (−196 °C) liquid nitrogen into the welding zone. The effects of welding parameters (tool pin profile, tool rotational speed, welding speed, and axial load) on the welding characteristics (tensile strength, hardness, and wear rate) have been investigated by the Taguchi technique. The impacts of welding parameters have been analysed to predict the optimum welding characteristics. The predicted best welding settings have been utilized to compare the CFSW and normal friction stir welding (NFSW) performances. The fractography of tensile-tested specimens, hardness distributions, and microstructure of worn-out CFSW welding surfaces have been examined by scanning electron microscopy (SEM) analysis. When compared to the NFSW process, the tensile strength and hardness of CFSW are improved by 41.36 % and 35.13 %, respectively, and the wear rate has decreased by 23.53 %. 2023-01-01T00:00:00Z http://hdl.handle.net/20.500.12603/2844 Serval Optimization Algorithm: A New Bio-Inspired Approach for Solving Optimization Problems Dehghani, Mohammad; Trojovský, Pavel This article introduces a new metaheuristic algorithm called the Serval Optimization Algorithm (SOA), which imitates the natural behavior of serval in nature. The fundamental inspiration of SOA is the serval’s hunting strategy, which attacks the selected prey and then hunts the prey in a chasing process. The steps of SOA implementation in two phases of exploration and exploitation are mathematically modeled. The capability of SOA in solving optimization problems is challenged in the optimization of thirty-nine standard benchmark functions from the CEC 2017 test suite and CEC 2019 test suite. The proposed SOA approach is compared with the performance of twelve well-known metaheuristic algorithms to evaluate further. The optimization results show that the proposed SOA approach, due to the appropriate balancing exploration and exploitation, is provided better solutions for most of the mentioned benchmark functions and has superior performance compared to competing algorithms. SOA implementation on the CEC 2011 test suite and four engineering design challenges shows the high efficiency of the proposed approach in handling real-world optimization applications. 2022-01-01T00:00:00Z http://hdl.handle.net/20.500.12603/2843 Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities Chrienová, Žofia; Nepovimová, Eugenie; Andrýs, Rudolf; Dolezal, R.; Janockova, J.; Muckova, L.; Fabova, L.; Soukup, O.; Olekšák, Patrik; Valis, M.; Korabecny, J.; Marco-Contelles, J.; Kuča, Kamil Twenty-four novel compounds bearing tetrahydroacridine and N-propargyl moieties have been designed, synthesised, and evaluated in vitro for their anti-cholinesterase and anti-monoamine oxidase activities. Propargyltacrine 23 (IC50 = 21 nM) was the most potent acetylcholinesterase (AChE) inhibitor, compound 20 (IC50 = 78 nM) showed the best inhibitory human butyrylcholinesterase (hBChE) profile, and ligand 21 afforded equipotent and significant values on both ChEs (human AChE [hAChE]: IC50 = 0.095 ± 0.001 µM; hBChE: IC50 = 0.093 ± 0.003 µM). Regarding MAO inhibition, compounds 7, 15, and 25 demonstrated the highest inhibitory potential towards hMAO-B (IC50 = 163, 40, and 170 nM, respectively). In all, compounds 7, 15, 20, 21, 23, and 25 exhibiting the most balanced pharmacological profile, were submitted to permeability and cell viability tests. As a result, 7-phenoxy-N-(prop-2-yn-1-yl)-1,2,3,4-tetrahydroacridin-9-amine hydrochloride (15) has been identified as a permeable agent that shows a balanced pharmacological profile [IC50 (hAChE) = 1.472 ± 0.024 µM; IC50 (hBChE) = 0.659 ± 0.077 µM; IC50 (hMAO-B) = 40.39 ± 5.98 nM], and consequently, as a new hit-ligand that deserves further investigation, in particular in vivo analyses, as the preliminary cell viability test results reported here suggest that this is a relatively safe therapeutic agent. 2022-01-01T00:00:00Z