Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The data indicated, depending on the IC50 values, that some of the prepared compounds have anti-prostate cancer activity. The results indicate that compounds 1d and 2d have good anti-prostate cancer activity compared to the rest of the compounds. The prepared series of compounds were also studied against selected types of bacteria and fungi, as the results showed that some of the compounds in the series had anti-bacterial and anti-fungal activity.
Activation of farnesoid X receptor (FXR) markedly attenuates development of atherosclerosis in animal models. However, the underlying mechanism is not well elucidated. Here, we show that the FXR agonist, obeticholic acid (OCA), increases fecal cholesterol excretion and macrophage reverse cholesterol transport (RCT) dependent on activation of hepatic FXR. OCA does not increase biliary cholesterol secretion, but inhibits intestinal cholesterol absorption. OCA markedly inhibits hepatic cholesterol 7α‐hydroxylase (
Despite extensive investigations, an effective treatment for sepsis remains elusive and a better understanding of the inflammatory response to infection is required to identify potential new targets for therapy. In this study we have used RNAi technology to show, for the first time, that the inducible lysophosphatidylcholine acyltransferase 2 (LPCAT2) plays a key role in macrophage inflammatory gene expression in response to stimulation with bacterial ligands. Using siRNA- or shRNA-mediated knockdown, we demonstrate that, in contrast to the constitutive LPCAT1, LPCAT2 is required for macrophage cytokine gene expression and release in response to TLR4 and TLR2 ligand stimulation but not for TLR-independent stimuli. In addition, cells transfe
... Show MoreThe rise of edge-cloud continuum computing is a result of the growing significance of edge computing, which has become a complementary or substitute option for traditional cloud services. The convergence of networking and computers presents a notable challenge due to their distinct historical development. Task scheduling is a major challenge in the context of edge-cloud continuum computing. The selection of the execution location of tasks, is crucial in meeting the quality-of-service (QoS) requirements of applications. An efficient scheduling strategy for distributing workloads among virtual machines in the edge-cloud continuum data center is mandatory to ensure the fulfilment of QoS requirements for both customer and service provider. E
... Show MoreUnconfined Compressive Strength is considered the most important parameter of rock strength properties affecting the rock failure criteria. Various research have developed rock strength for specific lithology to estimate high-accuracy value without a core. Previous analyses did not account for the formation's numerous lithologies and interbedded layers. The main aim of the present study is to select the suitable correlation to predict the UCS for hole depth of formation without separating the lithology. Furthermore, the second aim is to detect an adequate input parameter among set wireline to determine the UCS by using data of three wells along ten formations (Tanuma, Khasib, Mishrif, Rumaila, Ahmady, Maudud, Nahr Um
... Show MoreThis work aims to investigate the integrated ultra-dense wavelength division multiplexing (UDWDM) and polarization division multiplexing (PDM) schemes incorporated in the free space optic (FSO) communication system. Erbium-doped fiber amplifiers (EDFAs) are used as post and pre-amplifiers in the proposed UDWDM–PDM–FSO system to boost the transmission power for increasing the distance. Thirty-two channels are transported over the FSO link to realize the total data transmission of 160 and 320 Gbps with 0.08 and 0.1 nm channel spacing, respectively. Results are also reported with non-return to zero modulation schemes. The performance of the proposed UDWDM–PDM–FSO transmission sys
Amputation of the upper limb significantly hinders the ability of patients to perform activities of daily living. To address this challenge, this paper introduces a novel approach that combines non-invasive methods, specifically Electroencephalography (EEG) and Electromyography (EMG) signals, with advanced machine learning techniques to recognize upper limb movements. The objective is to improve the control and functionality of prosthetic upper limbs through effective pattern recognition. The proposed methodology involves the fusion of EMG and EEG signals, which are processed using time-frequency domain feature extraction techniques. This enables the classification of seven distinct hand and wrist movements. The experiments conducte
... Show More