Synthesis and Radiolabeling of Glu-Urea-Lys with 99mTc-Tricarbonyl-Imidazole-Bathophenanthroline Disulfonate Chelation System and Biological Evaluation as Prostate-Specific Membrane Antigen Inhibitor.

Background: The Glu-Urea-Lys (EUK) pharmacophore as prostate-specific membrane antigen (PSMA)-targeted ligand was synthesized, radiolabeled with 99mTc-tricarbonyl-imidazole-BPS chelation system, and biological activities were evaluated. The strategy [2 + 1] ligand is applied for tricarbonyl labeling. (5-imidazole-1-yl)pentanoic acid as a monodentate ligand and bathophenanthroline disulfonate (BPS) as a bidentate ligand formed a chelate system with 99mTc-tricarbonyl. EUK-pentanoic acid-imidazole and EUK were evaluated for PSMA active site using AutoDock 4 software. Materials and Methods: EUK-pentanoic acid-imidazole was synthesized in two steps. BPS was radiolabeled with 99mTc-tricarbonyl at 100°C for 30 min. The purified 99mTc(CO)3(H2O)BPS was used to radiolabel EUK-pentanoic acid-imidazole at 100°C, 30 min. Radiochemical purity, Log P, and stability studies were carried out within 24 h. Affinity of 99mTc(CO)3BPS-imidazole-EUK was performed in the saturation binding studies using LNCaP cells at 37°C for 1 h with a range of 0.001-1000 nM radiolabeled compound range. Internalization studies were performed in LNCaP cells with 1000 nM radiolabeled compound incubated for (0-2) h at 37°C. Biodistribution was studied in normal male Balb/c mice. The artificial intelligence predicts the uptake of radiolabeled compound in tumor. Results: The structures of synthesized compounds were confirmed by mass spectroscopy. Radiochemical purity, Log P, and protein binding were ≥95%, -0.2%, and 23%, respectively. The radiolabeled compound was stable in saline and human plasma within 24 h with radiochemical purity ≥90%. There was no release of 99mTc within 4 h in competition with histidine. The affinity was 82 ± 26.38 nM, and the activity increased inside the cells over time. Biodistribution studies showed radioactivity accumulation in kidneys less than 99mTc-HYNIC-PSMA. There was a moderate accumulation of radioactivity in the liver and intestine. Conclusion: Based on the results, 99mTc(CO)3BPS-imidazole-EUK can potentially be used as an imaging agent for studies at prostate bed and distal areas. The chelate system can be potentially labeled with rhenium for imaging studies (fluorescent or scintigraphy) and therapy.

Scaling purely elastic instability of strongly shear thinning polymer solutions.

Flow of viscoelastic polymer solutions in curved channels exhibits instability caused by the elastic nature of polymers even at low Reynolds numbers. However, scaling of the onset of this purely elastic instability in semidilute polymer solutions has not been previously reported. Here we experimentally investigate the flow of highly elastic polymer solutions above their overlap concentrations using pressure measurements and particle image velocimetry. We demonstrate that the onset of instability can be scaled by including shear dependent rheological properties of the polymer solutions in the nonlinear stability analysis. As a result, a universal criterion as function of normalized polymer concentration is provided for scaling the onset of purely elastic instability in the semidilute regime regardless of the type and molecular weight of the polymer.

Structure-Property Relationships of Nanosheeted 3D Hierarchical Roughness MgAl-Layered Double Hydroxide Branched to an Electrospun Porous Nanomembrane: A Superior Oil-Removing Nanofabric.

A straightforward approach was successfully developed to fabricate a well-designed three-dimensional rough sheetlike MgAl-layered double hydroxide (LDH) array to stand vertically on poly(acrylonitrile) porous nanofibrous membranes based on an electrospun-nanofiber-templated in situ hydrothermal strategy, and then the surface was modified with cyclohexanecarboxylic acid. The as-spun highly dense ordered sheetlike LDH porous nanofabric exhibited a superior durability in superhydrophobicity and superoleophilicity, which has achieved high oil-removing capability including both oil harvesting and oil separation to harvest/separate a wide range of organic solvents and oils from an oil-water mixture and, especially, exhibited a very good recycling and reusing performance. Interestingly, a steady water repellency was obtained against both drinkable hot (about 95 °C) and cool water. Outstanding oil harvesting, oil separation, and highly durable water repellant can be attributed to an effective synergistic effect between the high-density roughness of LDH nanosheets modified with acid and the very high porosity in the electrospun nanofibers, as well as the interspace between LDH nanosheets that acted as both a textile for selective oil separation and a container for penetrated oil storage, leading to special wettability, making the as-spun nanofabric a promising textile for large-scale removal and recollection of hydrophobic spillage on the water surface.