Bufalin-Loaded Multifunctional Photothermal Nanoparticles Inhibit the Anaerobic Glycolysis by Targeting SRC-3/HIF-1α Pathway for Improved Mild Photothermal Therapy in CRC.

Purpose: Compared with traditional photothermal therapy (PTT, >50°C), mild PTT (≤45°C) is a promising strategy for tumor therapy with fewer adverse effects. Unfortunately, its anti-tumor efficacy is hampered by thermoresistance induced by overexpression of heat shock proteins (HSPs). In our previous study, we found bufalin (BU) is a glycolysis inhibitor that depletes HSPs, which is expected to overcome thermotolerance of tumor cells.

Surface chemistry mediates the tumor entrance of nanoparticles probed using single-molecule dual-imaging nanodots.

The active transport of nanoparticles into solid tumors through transcytosis has been recognized as a promising way to enhance tumor accumulation and penetration, but the effect of the physicochemical properties of nanoparticles remains unclear. Herein, we develop a type of single-molecule dual imaging nanodot by divergent growth of perylenediimide (PDI)-dye-cored polylysine dendrimers and internal orthogonal conjugation of Gd(III)-based macrocyclic probes for fluorescence imaging and magnetic resonance imaging (MRI) of surface chemistry-dependent tumor entrance. The MRI and fluorescence imaging show that sixth-generation nanodots with acetylated (G6-Ac) and oligo ethylene glycol (G6-OEG) surfaces exhibit similar high tumor accumulation but different intratumor distribution.

High-Throughput Screening of Surface Engineered Cyanine Nanodots for Active Transport of Therapeutic Antibodies into Solid Tumor.

The successful delivery of therapeutic biomacromolecules into solid tumor holds great challenge due to their high resistance to penetrate through the complex tumor microenvironments. Here, active-transporting nanoparticles are harnessed to efficiently deliver biomacromolecular drugs into solid tumors through cell transcytosis. A series of molecularly precise cyanine 5-cored polylysine G5 dendrimers (Cy5 nanodots) with different peripheral amino acids (G5-AA) is prepared.

Spatiotemporally controllable diphtherin transgene system and neoantigen immunotherapy.

Individualized immunotherapy has attracted great attention due to its high specificity, effectiveness, and safety. We used an exogenous antigen to label tumor cells with MHC I molecules, which allowed neoantigen-specific T cells to recognize and kill tumor cells. A neoantigen vaccine alone cannot achieve complete tumor clearance due to a tumor immunosuppressive microenvironment.

Bufalin exacerbates Photodynamic therapy of colorectal cancer by targeting SRC-3/HIF-1α pathway.

Photodynamic therapy (PDT) induces tumour cell death by producing reactive oxygen species (ROS), and hypoxia is one of the main factors that limits its efficiency. In our previous study, bufalin (BU) enhanced photosensitizer mTHPC-mediated PDT therapy in colorectal cancer (CRC) cells, but its mechanism was not elucidated. To explore a strategy for improving the efficacy of PDT, we designed iRGD-modified nanoparticles to co-capsuled mTHPC and BU for simultaneous delivery to the tumour site and explored the underlying mechanism of the synergistic anti-CRC effect.

Light-switchable diphtherin transgene system combined with losartan for triple negtative breast cancer therapy based on nano drug delivery system.

Breast cancer is a common malignancy in women. The abnormally dense collagen network in breast cancer forms a therapeutic barrier that hinders the penetration and anti-tumor effect of drugs. To overcome this hurdle, we adopted a therapeutic strategy to treat breast cancer which combined a light-switchable transgene system and losartan.

Synthesis and Structural Characterization of Amidine, Amide, Urea and Isocyanate Derivatives of the Amino--dodecaborate Anion [BHNH₃].

The synthesis and structural characterization of new derivatives of [BH] is of fundamental interest and is expected to allow for extended applications. Herein we report on the synthesis of a series of amidine, amide, urea and isocyanate derivatives based on the amino--dodecaborate anion [BHNH₃]. Their structures have been confirmed by spectroscopic methods, and nine crystal structures are presented.

Rh -Catalyzed Functionalization of closo-Dodecaborates by Selective B-H Activation: Bypassing Competitive C-H Activation.

The closo-dodecaborate dianion is a fundamental icosahedral boron cage with 12 identical B-H vertices. The chemistry and applications of boron clusters have inspired researchers ever since their discovery several decades ago, and the selective modification of the cage positions has remained a major synthetic challenge. A rhodium(III)-catalyzed B-H functionalization-cyclization cascade of closo-dodecaborate amides is reported.

The closo-Dodecaborate Dianion Fused with Oxazoles Provides 3D Diboraheterocycles with Selective Antimicrobial Activity.

The synthesis and application of icosahedral boron cluster compounds has been studied extensively since their discovery several decades ago; however, two aspects of their chemistry have received little attention: The possibility to form inorganic/organic fused boraheterocycles and their potential to act as antimicrobial agents. This work comprises the preparation of a class of 3D diborabenzoxazole analogues with the closo-dodecaborate in place of the benzene moiety. The presented synthetic procedures provide access to a wide range of diboraheterocycles under mild conditions.

Fusing Carborane Carboxylic Acids with Alkynes: 3D Analogues of Isocoumarins via Regioselective B-H Activation.

An iridium-catalyzed alkenylation/annulation sequence between monocarba-closo-dodecaborate carboxylic acids and diarylacetylenes is reported. Regioselective activation of the B2 position, followed by B-C bond formation and ring closure, affords 3D bora-analogues of isocoumarins. The reaction tolerates a variety of functional groups on the aromatic rings and can be extended to B12-substituted derivatives.

Rhodium(III)-Catalyzed Alkenylation-Annulation of closo-Dodecaborate Anions through Double B-H Activation at Room Temperature.

1,2,3-Trisubstituted closo-dodecaborates with B-O, B-N, and B-C bonds as well as a fused borane oxazole ring have been synthesized by rhodium-catalyzed direct cage B-H alkenylation and annulation of ureido boranes in the first reported example of regioselective B-H bond functionalization of the [B H ] cage by transition-metal catalysis. This reaction proceeded at room temperature under ambient conditions and exhibited excellent selectivity for efficient monoalkenylation with good functional-group tolerance. The urea moiety enabled B-H activation by acting as a directing group, was incorporated in the oxazole ring in situ, and also avoided multiple alkenylation.

Facile synthesis of enantioenriched phenol-sulfoxides and their aluminum complexes.

Chiral phenolic p-tolylsulfoxides and t-butylsulfoxides were prepared by several short synthetic routes starting from readily available starting materials. The key synthetic step was the reaction of lithiated arenes with menthyl sulfinates or enantioselective oxidation of a t-butyl sulfide. Well-defined neutral ligand-AlMe2 complexes were obtained by stoichiometric treatment with AlMe3.