Ru(III)-PhI(OAc)─A Combination for Generation of Isocyanate Intermediate from Benzimidate through a Rearrangement: Synthesis of Unsymmetrical Urea, Carbamate, and Chiral Analogues.

Ru(III)-PhI(OAc), an unprecedented combination, is a highly efficient reagent system for the in situ generation of a valuable isocyanate intermediate from benzimidate synthons through a rearrangement. It unlocks a powerful platform for forming diverse C-N bonds, enabling the one-pot synthesis of an expansive array of valuable unsymmetrical ureas, carbamates, and their chiral analogues toward complex molecular structures with high selectivity and excellent yields. This new strategy not only exemplifies efficiency but also serves as a versatile tool for the construction of valuable molecular architectures, enhancing the scope and impact of modern synthetic chemistry.

Designing Nano-Hemin for Ferroptosis-Mediated Cell Death via Enzymatic Hemin Digestion.

Hemin is a protoporphyrin complex of ferric ion which catalyzes HO degradation and produces reactive oxygen species (ROS). This ROS generation property induces oxidative stress to hemin-exposed cells that can lead to various situations such as intracellular Fenton reaction, ferroptosis, or autophagy. Therapeutic performance of hemin is hindered due to low bioavailability of the active monomeric form with an intact ROS generation property.

Designed Nanodrugs for Ultrasonic Removal of Toxic Polyglutamine Aggregates from Neuron Cells.

Clearing of toxic polyglutamine aggregates from neuronal cells is crucial for ameliorating Huntington's disease. However, such clearance is challenging, requiring the targeting of affected neuron cells in the brain, followed by the removal of polyglutamine from cells. Here we report a designed nanodrug that can be used for the ultrasound-based removal of toxic polyglutamine aggregates from neuron cells.

New routes towards azomethine ylide generation from prolines to synthesize diverse -heterocycles: a DFT supported -selective mechanism.

Azomethine ylides are generated using either organocatalysts or metal catalysts a ballet of decarboxylative C-N coupling choreographed by prolines. These strategies enable diastereoselective [3 + 2] cycloaddition, C-C coupling, and ring annulation, providing sustainable routes. The synthesized pyrrolizines and other heterocycles have potential applications in the development of crucial biomolecules and pharmaceuticals.

Ultrasound-Responsive Nanodroplet-Based Targeted Therapy via Conversion to Microbubbles.

Ultrasound-based therapy is appealing as it can be used via a wireless approach at remote parts of the body including the brain. Microbubbles are commonly used in such therapy due to their highly sound-responsive property. However, the larger size of microbubbles limits selective targeting /.

Protein Delivery to the Cytosol and Cell Nucleus via Micellar Nanocarrier-Based Nonendocytic Uptake.

Although efficient cell nucleus delivery of exogenous materials can greatly improve their biochemical activity, this is strictly restricted by cellular uptake and intracellular trafficking processes. In the current approach, synthetic carriers are designed for cell delivery of exogenous materials via endocytosis, and nucleus delivery can be achieved via endosomal escape. Here, we demonstrate that a nonendocytic cell uptake approach can be adapted for protein delivery to the cell nucleus.

Nuclear Transport of the Molecular Drug via Nanocarrier-Based Nonendocytic Cellular Uptake.

Although subcellular targeting can enhance the therapeutic performance of most drugs, such targeting requires appropriate carrier-based delivery that can bypass endosomal/lysosomal trafficking. Recent works show that nanocarriers can be designed for direct cell membrane translocation and nonendocytic uptake, bypassing the usual endocytosis processes. Here we show that this approach can be adapted for the rapid cell nucleus delivery of molecular drugs.

Biodegradable Poly(trehalose) Nanoparticle for Preventing Amyloid Beta Aggregation and Related Neurotoxicity.

Trehalose is a disaccharide that is capable of inhibiting protein aggregation and activating cellular autophagy. It has been shown that a polymer or nanoparticle form, terminated with multiple trehalose units, can significantly enhance the anti-amyloidogenic performance and is suitable for the treatment of neurodegenerative diseases. Here, we report a trehalose-conjugated polycarbonate--lactide polymer and formulation of its nanoparticles having multiple numbers of trehalose exposed on the surface.

Efficient Synergistic Antibacterial Activity of α-MSH Using Chitosan-Based Versatile Nanoconjugates.

The application of antimicrobial peptides has emerged as an alternative therapeutic tool to encounter against multidrug resistance of different pathogenic organisms. α-Melanocyte stimulating hormone (α-MSH), an endogenous neuropeptide, is found to be efficient in eradicating infection of various kinds of , including methicillin-resistant (MRSA). However, the chemical stability and efficient delivery of these biopharmaceuticals (i.

Direct Cellular Delivery of Exogenous Genetic Material and Protein via Colloidal Nano-Assemblies with Biopolymer.

Direct cytosolic delivery of large biomolecules that bypass the endocytic pathways is a promising strategy for therapeutic applications. Recent works have shown that small-molecule, nanoparticle, and polymer-based carriers can be designed for direct cytosolic delivery. It has been shown that the specific surface chemistry of the carrier, nanoscale assembly between the carrier and cargo molecule, good colloidal stability, and low surface charge of the nano-assembly are critical for non-endocytic uptake processes.

Co-assembly of charge complementary peptides and their applications as organic dye/heavy metal ion (Pb, Hg) absorbents and arsenic(iii/v) detectors.

Learning from nature, molecular self-assembly has been used extensively to generate interesting materials using a bottom up approach. The enthusiasm in this field of research stems from the unique properties of these materials and their diverse applications. The field has not been limited to studying assembly of similar types of molecules but extended to multi component systems the co-assembly phenomenon.

Peptide Hydrogels as Platforms for Sustained Release of Antimicrobial and Antitumor Drugs and Proteins.

A charged synthetic peptide-based noncytotoxic hydrogelator was employed in encapsulation, storage, and sustainable release of different kinds of drugs, namely, ciprofloxacin (CP), an antibiotic; 5-fluorouracil (5-FU), an anticancer drug and proteins like lysozyme and bovine serum albumin (BSA). Hydrogelation of the peptide and its coassembly with the drug molecules were studied to obtain mechanistic details. All of the different cargos were capable of sustained and efficient release from the delivery platform.