Discovery of Fatty Acid Translocase CD36-Targeting Near-Infrared Fluorescent Probe Enables Visualization and Imaging-Guided Surgery for Glioma.

Despite therapeutic advances in glioma, glioma-related mortality rates remain high due to its extremely poor prognosis and high recurrence. Near-infrared (NIR) fluorescence imaging technologies, using the clinically approved fluorescent probe 5-ALA, have gained prominence in facilitating visualization of glioma resection. However, the false-positive and false-negative results of 5-ALA decrease its sensitivity and specificity in detecting glioma, thereby hampering its use in glioma surgical navigation.

Photothermally Enhanced Cascaded Nanozyme-Functionalized Black Phosphorus Nanosheets for Targeted Treatment of Infected Diabetic Wounds.

Due to the limitations of H O under physiological conditions and defective activity, nanozyme-catalyzed therapy for infected diabetic wound healing is still a huge challenge. Here, this work designs a novel multifunctional hybrid glucose oxidase (GOx)-CeO @black phosphorus (BP)/Apt nanosheet that features GOx and CeO dual enzyme loading with photothermal enhancement effect and targeting ability for the treatment of infected wounds in type II diabetic mice. Combined with the photothermal properties of the BP nanosheets, the cascade nanozyme effect of GOx and CeO is extremely enhanced.

A Hemin-Graphene Nanocomposite-Based Aptasensor for Ultrasensitive Colorimetric Quantification of Leukaemia Cells Using Magnetic Enrichment.

Diagnostic blood cell counting is of limited use in monitoring a minimal number of leukaemia cells, warranting further research to develop more sensitive and reliable techniques to identify leukaemia cells in circulation. In this work, a hemin-graphene nanocomposite-based aptasensor was developed for ultrasensitive colorimetric detection of leukaemia cells (CEM) using magnetic enrichment. Hemin-conjugated graphene oxide nanocomposites (HGNs) were prepared by hydrazine reduction using graphene oxide nanosheets and hemins.

Biomineralized Cascade Enzyme-Encapsulated ZIF-8 Nanoparticles Combined with Antisense Oligonucleotides for Drug-Resistant Bacteria Treatment.

The unrestrained use of antibiotics accelerates the development of drug-resistant bacteria and leads to an increasing threat to human health. Therefore, there is an urgent need to explore novel and effective strategies for the treatment of bacterial infections. Herein, zeolite imidazole framework-8 (ZIF-8) material was utilized to construct biomineralized nanomaterial (GOx&HRP@ZIF-8/ASO) by encapsulating biological cascade enzymes and combining with antisense oligonucleotides (ASOs), which achieved effective and synergistic antidrug-resistant bacteria therapy.

Synthesis and bioevaluation of thienopyrimidines bearing a pyrazoline unit as selective PI3Kα inhibitors.

A series of thienopyrimidines containing a pyrazoline unit (4a-d, 7a-d and 13a-l) were designed and synthesized. The target compounds were evaluated for antiproliferative activity against A549, HepG2 and MCF-7 cancer cell lines. Among the twenty target compounds, most of them exhibited excellent antiproliferative activity against one or several cancer cell lines.

Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors.

Aimed at discovering effective EGFR inhibitors, six series of quinazoline derivatives bearing a semicarbazone moiety were designed, synthesized and evaluated in different cancer cell lines (A549, HepG2, MCF-7 and PC-3). Most of the selected compounds showed remarkable cytotoxicity with IC values reaching the nanomole range. Further, the inhibition efficacy of 11 compounds against EGFR kinases was tested, which demonstrated excellent IC values in nanomolar level.