Deuterium- and tritium-labeled pharmaceutical compounds are pivotal diagnostic tools in drug discovery research, providing vital information about the biological fate of drugs and drug metabolites. Herein we demonstrate that a photoredox-mediated hydrogen atom transfer protocol can efficiently and selectively install deuterium (D) and tritium (T) at α-amino sp carbon-hydrogen bonds in a single step, using isotopically labeled water (DO or TO) as the source of hydrogen isotope. In this context, we also report a convenient synthesis of TO from T, providing access to high-specific-activity TO. This protocol has been successfully applied to the high incorporation of deuterium and tritium in 18 drug molecules, which meet the requirements for use in ligand-binding assays and absorption, distribution, metabolism, and excretion studies.
Hepatocellular carcinoma (HCC) is one of the most common malignancies. The currently available clinical drugs for HCC frequently cause serious side effects and the treatment outcomes are unsatisfactory. It is urgent to develop effective drugs with high selectivity and low adverse effects for HCC.
Introduction: This study investigates the synthesis of silver nanoparticles (Ag NPs) using Helianthemum lippii extract and evaluates their photoprotective, anti-hemolytic, antibacterial, and anti-inflammatory properties compared to various extract fractions, including total aqueous extract (AE), flavonoid monoglycosides (FMG), flavonoid diglycosides/triglycosides (FDG/FTG), tannins (TN), and anthocyanins (AC). Helianthemum lippii is rich in bioactive compounds such as caffeic acid, p-coumaric acid, and gallic acid, known for their therapeutic potential. This study aims to determine whether embedding these phytochemicals into Ag NPs enhances their biomedical applications compared to the natural extract fractions.
With no effective treatments for functional recovery after injury, spinal cord injury (SCI) remains one of the unresolved healthcare challenges. Human induced pluripotent stem cell (hiPSC) transplantation is a versatile patient-specific regenerative approach for functional recovery after SCI. Injectable electroconductive hydrogel (ECH) can further enhance the cell transplantation efficacy through a minimally invasive manner as well as recapitulate the native bioelectrical microenvironment of neural tissue.
Abnormal proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) leading to pulmonary vascular remodeling are critical factors in the development of pulmonary hypertension (pH). Dehydrodiisoeugenol (DEH), a natural phenolic compound, is renowned for its antioxidant and anti-inflammatory properties. However, the precise role and mechanisms of DEH in PH remain unclear.
Stanislav Iosofatovich Zalesky - the first head of the Department of General Medical Chemistry of the Imperial Tomsk University (currently the Department of Chemistry of the Siberian State Medical University), a versatile scientist and public figure, acknowledged expert in medical, chemical, hydrogeological and balneological sciences. Professor S.I.
