Tianfeng Chen

Photothermal therapy has attracted much interest for use in cancer treatment in recent years. In this study, Cu₂Se nanoparticles as a novel photothermal agent modified by chitosan (CS‐Cu₂SeNPs) were successfully synthesized through a facile route at room temperature. The as‐synthesized CS‐Cu₂SeNPs exhibited good water solubility and significant stability. CS‐Cu₂SeNPs can efficiently convert near‐infrared (NIR) light into heat and exhibit excellent thermostability. In vitro experiments showed that CS‐Cu₂SeNPs had selective cellular uptake between cancer and normal cells and expressed clear anticancer activity on A375 and HeLa human cancer cells. In addition, the anticancer activity was increased to about 400 % by combination with a laser at 808 nm, which acted through induction of apoptosis with the involvement of intrinsic and extrinsic pathways. CS‐Cu₂SeNPs irradiated with a laser effectively triggered the intracellular reactive oxygen species (ROS) overproduction that promoted cell apoptosis. Therefore, the developed CS‐Cu₂SeNPs could be used as a novel phototherapeutic agent for the photothermal therapy of human cancers.

Nanorods have been utilized in targeted therapy, controlled release, molecular diagnosis, and molecule imaging owing to their large surface area and optical, magnetic, electronic, and structural properties. However, low stability and complex synthetic methods have substantially limited the application of tellurium nanorods for use as antioxidant and anticancer agents. Herein, a facile one‐pot synthesis of functionalized tellurium nanorods (PTNRs) by using a hydrothermal synthetic system with a polysaccharide–protein complex (PTR), which was extracted from Pleurotus tuber‐regium, as a capping agent is described. PTNRs remained stable in water and in phosphate‐buffered saline and exhibited high hemocompatibility. Interestingly, these nanorods possessed strong antioxidant activity for scavenging 2,2′‐azinobis‐(3‐ethylbenzothiazoline‐6‐sulfonic acid radical cation (ABTS^.+) and 2,2‐diphenyl‐1‐picrylhydrazylhydrate (DPPH) free radicals and demonstrated novel anticancer activities. However, these nanorods exhibited low cytotoxicity toward normal human cells. In addition, the PTNRs effectively induced a decrease in the mitochondrial membrane potential in a dose‐dependent manner, which indicated that mitochondrial dysfunction might play an important role in PTNR‐induced apoptosis. Therefore, this study provides a one‐pot strategy for the facile synthesis of tellurium nanorods with novel antioxidant and anticancer application potentials.

Construction of bioresponsive drug‐delivery nanosystems could enhance the anticancer efficacy of anticancer agents and reduce their toxic side effects. Herein, by using transferrin (Tf) as a surface decorator, we constructed a cancer‐targeted nanographene oxide (NGO) nanosystem for use in drug delivery. This nanosystem (Tf‐NGO@HPIP) drastically enhanced the cellular uptake, retention, and anticancer efficacy of loaded drugs but showed much lower toxicity to normal cells. The nanosystem was internalized through receptor‐mediated endocytosis and triggered pH‐dependent drug release in acidic environments and in the presence of cellular enzymes. Moreover, Tf‐NGO@HPIP effectively induced cancer‐cell apoptosis through activation of superoxide‐mediated p53 and MAPK pathways along with inactivation of ERK and AKT. Taken together, this study demonstrates a good strategy for the construction of bioresponsive NGO drug‐delivery nanosystems and their use as efficient anticancer drug carriers.

Aquation has been proposed as crucial chemical action step for ruthenium (Ru) complexes, but its effects on the action mechanisms remain elusive. Herein, we have demonstrated the aquation process of a potent Ru polypyridyl complex (RuBmp=[Ru^II(bmbp)(phen)Cl]ClO₄, bmbp=2,6‐bis(6‐methylbenzimidazol‐2‐yl) pyridine, phen=phenanthroline) with a chloride ligand, and revealed that aquation of RuBmp effectively enhanced its hydrophilicity and cellular uptake, thus significantly increasing its anticancer efficacy. The aquation products (H‐RuBmp=[Ru^II(bmbp)(phen)Cl]ClO₄, [Ru^II(bmbp)(phen)(H₂O)]ClO₄, bmbp) exhibited a much higher apoptosis‐inducing ability than the intact complex, with involvement of caspase activation, mitochondria dysfunction, and interaction with cell membrane death receptors. H‐RuBmp demonstrated a higher interaction potency with the cell membrane and induced higher levels of ROS overproduction in cancer cells to regulate the AKT, MAPK, and p53 signaling pathways. Taken together, this study could provide useful information for fine‐tuning the rational design of next‐generation metal medicines.

Polymer‐surface decoration has been found to be an effective strategy to enhance the biological activities of nanomedicine. Herein, three different types of polymers with a cancer‐targeting ligand Arg‐Gly‐Asp peptide (RGD) have been used to decorate mesoporous silica nanoparticles (MSNs) and the functionalized nanosystems were used as drug carriers of oxaliplatin (OXA). The results showed that polymer‐surface decoration of the MSNs nanosystem by poly(ethylene glycol) (PEG) and polyethyleneimine (PEI) significantly enhanced the anticancer efficacy of OXA, which was much higher than that of chitosan (CTS). This effect was closely related to the enhancement of the cellular uptake and cellular drug retention. Moreover, PEI@MSNs‐OXA possessed excellent advantages in penetrating ability and inhibitory effects on SW480 spheroids that were used to simulate the in vivo tumor environments. Therefore, this study provides useful information for the rational design of a cancer‐targeted MSNs nanosystem with polymer‐surface decoration.