Pancreatic lipase inhibitory activity of selected pharmaceutical agents

Twenty-five structurally diverse compounds have been tested in vitro for their pancreatic lipase (PL) inhibitory activity. Despite the diversity of tested compounds, the relationship comprising structural attributes of the compounds could be established to correlate with the observed inhibitory activity. Compounds that exerted inhibitory action through surface activity were of different profile from the rest of compounds. When co-incubated with orlistat (OsT), important synergistic effects for some compounds (orphenadrine, gliclazide, cefuroxime and sulfacetamide) were revealed, while antagonistic effects were demonstrated for others (camphor sulfonic acid and dinitro salicylic acid). Docking studies for the most active molecules were performed and molecular interaction forces with the PL active site were identified. The results suggested co-binding of OsT along with the other inhibitor in the binding site in cases of synergistic effect but not in the case of antagonistic effect. These results were additionally supported by affinity capillary electrophoresis. In conclusion, synergistic lipase inhibitory activity between OsT and some other pharmaceutical compounds was demonstrated for the first time, which might help improve the pharmacological effect of OsT

Tuning the K value in K-nearest neighbors for malware detection

Malicious software, also referred to as malware, poses a serious threat to computer networks, user privacy, and user systems. Effective cybersecurity depends on the correct detection and classification of malware. In order to improve its effectiveness, the K-nearest neighbors (KNN) method is applied systematically in this study to the task of malware detection. The study investigates the effect of the number of neighbors (K) parameter on the KNN's performance. MalMem-2022 malware datasets and relevant evaluation criteria like accuracy, precision, recall, and F1-score will be used to assess the efficacy of the suggested technique. The experiments evaluate how parameter tuning affects the accuracy of malware detection by comparing the performance of various parameter setups. The study findings show that careful parameter adjustment considerably boosts the KNN method's malware detection capability. The research also highlights the potential of KNN with parameter adjustment as a useful tool for malware detection in real-world circumstances, allowing for prompt and precise identification of malware

PET Molecular Targets and Near-Infrared Fluorescence Imaging of Atherosclerosis

PURPOSE OF REVIEW: With this review, we aim to summarize the role of positron emission tomography (PET) and near-infrared fluorescence imaging (NIRF) in the detection of atherosclerosis. RECENT FINDINGS: (18)F-FDG is an established measure of increased macrophage activity. However, due to its low specificity, new radiotracers have emerged for more specific detection of vascular inflammation and other high-risk plaque features such as microcalcification and neovascularization. Novel NIRF probes are engineered to sense endothelial damage as an early sign of plaque erosion as well as oxidized low-density lipoprotein (oxLDL) as a prime target for atherosclerosis. Integrated NIRF/OCT (optical coherence tomography) catheters enable to detect stent-associated microthrombi. Novel radiotracers can improve specificity of PET for imaging atherosclerosis. Advanced NIRF probes show promise for future application in human. Intravascular NIRF might play a prominent role in the detection of stent-induced vascular injury

Multi-biological activity evaluation of Sn(П), Zn(П) and Fe(П) complexes based on thiocarbohydrazide schiff bases: synthesis, spectroscopic investigations and fluorescence studies

Abstract Two new Schiff base ligands (L1 and L2) were synthesized by condensing thiocarbohydrazide (TCH) with o-anisaldehyde or p-anisaldehyde in ethanol. Their mono- and bi-nuclear complexes with Sn(II), Zn(II), and Fe(II) were prepared for potential fluorescence and biological applications. Characterization was performed using FT-IR, NMR, UV-Vis spectroscopy, mass spectrometry, molar conductance, TGA, X-ray diffraction and SEM. XRD results indicated good crystallinity with crystallite sizes of 20–50 nm. Fluorescent intensity of free TCH ligands increased upon complexation with Sn, Zn, and Fe, suggesting their potential as fluorescence chemosensors. The compounds exhibited variable antimicrobial activities against Staphylococcus aureus, Escherichia coli, and Candida albicans, but lower than commercial drugs. L1Fe and L1Zn enhanced L1’s cytotoxicity in four colorectal malignancy cells and L1Zn in skin cancer cells (A375), lung cancer cells (A549), uterine cervix cells (HeLa), and glioblastoma cells (U87). L1Fe showed enhanced activity in mammary adenocarcinoma cells (T47D) and triple-negative breast cancer cells (MDA-MB-231). L2Sn exhibited 70fold increase in L2’s DPPH radical scavenging compared to the antioxidant ascorbic acid. L1Zn and L2Zn complexes outperformed indomethacin in reducing inflammation in RAW macrophages, enhancing the nanomolar efficacy of L1 and L2. These complexes have promising utility in cancer diagnosis, monitoring and highly selective duality of anti-inflammatory/cytotoxicity treatments

Pancreatic lipase inhibitory activity of selected pharmaceutical agents

Twenty-five structurally diverse compounds have been tested in vitro for their pancreatic lipase (PL) inhibitory activity. Despite the diversity of tested compounds, the relationship comprising structural attributes of the compounds could be established to correlate with the observed inhibitory activity. Compounds that exerted inhibitory action through surface activity were of different profile from the rest of compounds. When co-incubated with orlistat (OsT), important synergistic effects for some compounds (orphenadrine, gliclazide, cefuroxime and sulfacetamide) were revealed, while antagonistic effects were demonstrated for others (camphor sulfonic acid and dinitro salicylic acid). Docking studies for the most active molecules were performed and molecular interaction forces with the PL active site were identified. The results suggested co-binding of OsT along with the other inhibitor in the binding site in cases of synergistic effect but not in the case of antagonistic effect. These results were additionally supported by affinity capillary electrophoresis. In conclusion, synergistic lipase inhibitory activity between OsT and some other pharmaceutical compounds was demonstrated for the first time, which might help improve the pharmacological effect of OsT