In silico screening and synthesis of stable tilmicosin-hydrazone derivatives as potential DNA disruptors towards Staphylococcus aureus.

In this study, 30 tilmicosin-hydrazone derivatives were designed using MOE software. Six candidate molecules with strong binding affinity to DNA or DNA-Topo II complexes, as indicated by molecular docking results, were synthesized. These candidates were evaluated for their in vitro antibacterial activities against common Gram-positive and Gram-negative bacteria.

Biocompatible -carbazoleacetic acid decorated CuO nanoparticles as self-cascading platforms for synergistic single near-infrared triggered phototherapy treating microbial infections.

In this work, positively charged -carbazoleacetic acid decorated CuO nanoparticles (CuO-CAA NPs) as novel biocompatible nanozymes have been successfully prepared through a one-step hydrothermal method. CuO-CAA can serve as a self-cascading platform through effective GSH-OXD-like and POD-like activities, and the former can induce continuous generation of HO through the catalytic oxidation of overexpressed GSH in the bacterial infection microenvironment, which in turn acts as a substrate for the latter to yield ˙OH Fenton-like reaction, without introducing exogenous HO. Upon NIR irradiation, CuO-CAA NPs possess a high photothermal conversion effect, which can further improve the enzymatic activity for increasing the production rate of HO and ˙OH.

Rational design and synthesis of triazene-amonafide derivatives as novel potential antitumor agents causing oxidative damage towards DNA through intercalation mode.

In this work, we rationally designed and synthesized two novel triazene-amonafide derivatives 2-(2-(diisopropylamino)ethyl)-5-(3,3-dimethyltriaz-1-en-1-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (D-11) and 5-(3,3-diethyltriaz-1-en-1-yl)-2-(2-(diisopropylamino)ethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (D-12) as potential antitumor agents. The DNA damage induced by the intercalation mode of D-11 (D-12) towards DNA was electrochemically detected through the construction of efficient biosensors. The consecutive processes of reversible redox of naphthylimide ring and irreversible oxidation of triazene moiety were elucidated on the surface of glassy carbon electrode (GCE) by CV, SWV, and DPV methods.

Construction of Mn-N-C nanoparticles with multienzyme-like properties and photothermal performance for the effective treatment of bacterial infections.

In this work, we successfully constructed Mn-coordinated nitrogen-carbon nanoparticles (Mn-N-C NPs) exhibiting multienzyme-like activities. In a bacterial infectious microenvironment, the POD-like and OXD-like activities of Mn-N-C NPs could synergistically trigger the generation of ROS (˙OH and O˙), causing oxidative damage to the bacterial cell membrane for killing bacteria. Alternatively, in neutral or weak alkaline normal tissues, the excessive O˙ could be converted into O and HO the SOD-like ability of Mn-N-C NPs, and subsequently their CAT-like activity catalyzed excess HO into HO and O for protecting normal cells through the antioxidant defense.

Electrochemical detection of genetic damage caused by the interaction of novel bifunctional anthraquinone-temozolomide antitumor hybrids with DNA modified electrode.

In this work, novel potential anthraquinone-temozolomide (TMZ) antitumor hybrids N-(2-((9,10-dioxo-9,10-dihydroanthracen-1-yl)amino)ethyl)-3-methyl-4-oxo-3,4-dihydroimidazo [5, 1-d][1,2,3,5]tetrazine-8-carboxamide (C-1) and 2-(9,10-dioxo-9,10-dihydroanthracen-1-yl)amino) ethyl-3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylate (C-9) were designed and synthesized successfully. The electrochemical behaviors of C-1 (C-9) involved the reversible processes of 9,10-anthraquinone ring, the irreversible reduction and oxidation processes of TMZ ring. Electrochemical biosensors were constructed with ctDNA, poly (dG) and poly (dA) modifying the surface of glassy carbon electrode (GCE) to evaluate the DNA oxidative damage caused by the interaction of C-1 (C-9) with DNA.

Cuprous oxide-demethyleneberberine nanospheres for single near-infrared light-triggered photoresponsive-enhanced enzymatic synergistic antibacterial therapy.

In this work, novel cuprous oxide-demethyleneberberine (CuO-DMB) nanomaterials are successfully synthesized for photoresponsive-enhanced enzymatic synergistic antibacterial therapy under near-infrared (NIR) irradiation (808 nm). CuO-DMB has a spherical morphology with a smaller nanosize and positive potential, can trap bacteria through electrostatic interactions resulting in a targeting function. CuO-DMB nanospheres show both oxidase-like and peroxidase-like activities, and serve as a self-cascade platform, which can deplete high concentrations of GSH to produce O˙ and HO, then HO is transformed into ˙OH, without introducing exogenous HO.

Iron Phosphate Nanozyme-Hydrogel with Multienzyme-like Activity for Efficient Bacterial Sterilization.

Pathogenic bacteria infections have posed a threat to human health worldwide. Nanomaterials with natural enzymatic activity provide an opportunity for the development of new antibacterial pathways. We successfully constructed iron phosphate nanozyme-hydrogel (FePO-HG) with the traits of positive charge and macropores.

Metal-Organic Framework Modified MoS Nanozyme for Synergetic Combating Drug-Resistant Bacterial Infections via Photothermal Effect and Photodynamic Modulated Peroxidase-Mimic Activity.

Bacterial infections have become major threats to public health all over the world. With the emergence of antibiotic resistance, it is urgent to develop novel antimicrobial materials to efficiently overcome drug resistance with high bactericidal activity. In this work, UiO-66-NH-CO-MoS nanocomposites (UNMS NCs) are constructed through the amidation reaction.