Evaluation of the C biodistribution in mice in a micellar ExtraOx form and in an oil solution.

The article is devoted to the study of the pharmacokinetics of fullerene C in oil and micellar forms, analysis of its content in blood, liver, lungs, kidneys, heart, brain, adrenal glands, thymus, testicles, and spleen. The highest accumulation of C was found in the liver and adrenal glands. As a result of the studies carried out, it was shown that the bioavailability of C in the micellar form is higher than that in an oil solution.

Physicochemical properties, biological activity and biocompatibility of water-soluble C-Hyp adduct.

Amino acid adducts of light fullerenes have a potential of application in a variety of fields of biomedicine, that is reactive oxygen species scavenging activity, anticancer activity, viruses and bacteria inactivation etc. In this work, the water-soluble C fullerene derivative with l-hydroxyproline (C(CHNO), C-Hyp) was studied. Extensive biomedical investigation of this compound, namely, antiradical activity in the reaction with stable diphenylpicrylhydrazyl radical, the binding to human serum albumin, photodynamic properties, cytotoxicity in glioblastoma A172 and lung carcinoma A549 cell lines, erythrocytes haemolysis, platelet aggregation, genotoxicity on human peripheral blood mononuclear cells was conducted.

Prodrug Approach for Posterior Eye Drug Delivery: Synthesis of Novel Ganciclovir Prodrugs and in Vitro Screening with Cassette Dosing.

Because of poor ocular drug bioavailability, intravitreal injections have become the gold standard for drug delivery to the posterior eye. The prodrug approach can be used for optimizing the biopharmaceutical properties of intravitreal drugs. The preclinical screening of prodrugs' properties, such as hydrolysis and bioconversion, should be conducted in a resource-efficient way for an extensive set of synthesized compounds with validated methods.

Regression algorithm for calculating second-dimension retention indices in comprehensive two-dimensional gas chromatography.

Gas chromatography-mass spectrometry (GC-MS) is one of the most accurate, well developed, and reliable analytical tools for the analysis of volatile and semivolatile compounds. The GC-MS data have been extensively improved by enhancing the separation capacity via comprehensive two-dimensional gas chromatography (GC × GC). The reliability of the identification of the analytes in GC × GC-MS can be notably improved by applying the second-dimension retention index (I) as additional analytical parameter along with the commonly used first dimension retention index (I) and mass spectrum.

Light-Induced Reactions of Diazotetrahydrofuranone without Elimination of Nitrogen: Experimental and Mechanistic Study.

The energies and lifetimes of the excited states (S, S, S, T) of a diazotetrahydrofuranone were determined using experimental and computational methods. It was shown that direction of the diazoketone photochemical transformations without elimination of nitrogen is determined by multiplicity and energy of the excited state, generated by UV irradiation of diazo compound: isomerization to α-ketodiazirine proceeds from the singlet S state, whereas the alternative process of C-H insertion with hydrazone formation occurs through the triplet T state. The most probable excited state that leads to elimination of nitrogen and Wolff rearrangement is one of the highest singlet excited states of diazotetrahydrofuranone.

Coordination to Imidazole Ring Switches on Phosphorescence of Platinum Cyclometalated Complexes: The Route to Selective Labeling of Peptides and Proteins via Histidine Residues.

In this study, we have shown that substitution of chloride ligand for imidazole (Im) ring in the cyclometalated platinum complex Pt(phpy)(PPh)Cl (1; phpy, 2-phenylpyridine; PPh, triphenylphosphine), which is nonemissive in solution, switches on phosphorescence of the resulting compound. Crystallographic and nuclear magnetic resonance (NMR) spectroscopic studies of the substitution product showed that the luminescence ignition is a result of Im coordination to give the [Pt(phpy)(Im)(PPh)]Cl complex. The other imidazole-containing biomolecules, such as histidine and histidine-containing peptides and proteins, also trigger luminescence of the substitution products.