Core-Shell Chitosan Particles Targeting Membrane-Bound Heat Shock Protein 70 for Cancer Therapy.

Anti-cancer targeted therapy is a promising approach. However, the identification of target molecules over-expressed in a wide range of tumors remains a significant challenge. The aim of this study was to analyze the expression of cell membrane-exposed heat shock protein 70 kDa (mHSP70) on different tumor cells and to develop a nanoscale delivery system based on a monoclonal antibody (mAb) that recognizes mHSP70 and uses chitosan core-shell nanoparticles (NPs).

Exploring the properties of theVB-defect in hBN: optical spin polarization, Rabi oscillations, and coherent nuclei modulation.

Optically active point defects in semiconductors have received great attention in the field of solid-state quantum technologies. Hexagonal boron nitride, with an ultra-wide band gapEg= 6 eV, containing a negatively charged boron vacancy (VB-) with unique spin, optical, and coherent properties presents a new two-dimensional platform for the implementation of quantum technologies. This work establishes the value ofVB-spin polarization under optical pumping with= 532 nm laser using high-frequency (= 94 GHz) electron paramagnetic resonance (EPR) spectroscopy.

Design of an aryne-platform for the synthesis of non-racemic heterocyclic allocolchicinoids.

A four-step semisynthetic approach towards a highly versatile allocolchicine-related chiral aryne intermediate starting from naturally occurring colchicine was developed, and some of its synthetic transformations were studied. The generated benzyne intermediate afforded a number of non-racemic heterocyclic allocolchicinoids, which were shown to exhibit potent cytotoxicity towards COLO 357, OSA and Raji cells. The proposed methodology is attractive for the synthesis of libraries of new cytotoxic tubulin inhibitors.

Design, Synthesis and In Vitro Biological Activity of Novel C-7 Methylene Congeners of Furanoallocolchicinoids.

A series of novel heterocyclic colchicine derivatives bearing a C-7 methylene fragment were synthesized via Wittig, Horner-Wadsworth-Emmons and Nenajdenko-Shastin olefination approaches. The in vitro biological activities of the most promising compounds were investigated using MTT assays and cell cycle analyses. Compounds with an electron withdrawing group on the methylene fragment exhibited substantial antiproliferative activity towards COLO-357, BxPC-3, HaCaT, PANC-1 and A549 cell lines.

Size-Dependent Biodistribution of Fluorescent Furano-Allocolchicinoid-Chitosan Formulations in Mice.

The aim of this study was to compare the biodistribution in mice of functionalized rhodamine B (Rh) labeled colchicine derivative furano-allocolchicinoid (, ) either conjugated to 40 kDa chitosan (, ) or encapsulated into chitosan nanoparticles (). AC-NPs were formed by ionotropic gelation and were 400-450 nm in diameter as estimated in mice by dynamic light scattering and confocal microscopy. AC-Chi and AC-NPs preserved the specific colchicine activity in vitro.