Mitochondria-targeted photodynamic therapy (PDT) has recently been recognized as a promising strategy for effective cancer treatment. In this work, a mitochondria-targeted near-infrared (NIR) aggregation-induced emission (AIE)-active phosphorescent Ir(III) complex (Ir1)...
Combinatory photodynamic and chemotherapy
have demonstrated superior
performance in cancer ablation over singular therapeutics. However,
photodynamic therapy (PDT) often exhibits suboptimal efficacy for
deep-seated tumors, owing to the limited penetration depth of illumination
light, while chemotherapy is generally accompanied by severe side
effects. Therefore, it is imperative to develop a functional nanoplatform
for combinatory PDT and chemotherapy, which could, for PDT, achieve
enhanced light penetration and, for chemotherapy, realize reduced
therapeutic threshold dosage and a controllable drug release profile
(e.g., minimized release in blood circulation but bursting release
in the tumor microenvironment). Herein, we demonstrate a therapeutic
nanoplatform composed of poly(acrylic acid) (PAA)-modified silica-coated
Nd3+-doped upconversion nanoparticles decorated with methylene
blue (MB) and doxorubicin (DOX) in silica and a PAA layer, respectively.
Notably, 808 nm light is used to excite upconversion nanoparticles
and further trigger the photosensitization behavior of MB in PDT,
while the quick acid response of the PAA layer in the tumor acid environment
introduces DOX bursting for optimized chemotherapy with significantly
decreased therapeutic threshold dosage and minimized side effects.
Importantly, the anticancer efficiency of the nanoplatform in vitro and in vivo shows an IC50 and a tumor inhibition rate of 12.55 μg mL–1 and 89.81%, respectively. This study provides a strategy for combinatory
cancer therapy.
In this study, 2-chloro-1,3-dimethoxy-5-methylbenzene (CDM), a natural product with anti-Candida albicans activity, was discovered from the Hericium erinaceus mycelium. The minimum inhibitory concentration of CDM was 62.5 μg/mL. Moreover, structural analogues of CDM obtained from chemical synthesis were applied to explore the structure−activity relationship (SAR) of CDM against C. albicans. It was found that methoxy groups, halogen atoms (except fluorine atoms), and methoxy-meta-position methyl groups in the structure of CDM were the key active groups. Furthermore, we investigated the anti-C. albicans mechanism of CDM. Experiments suggested that CDM destroyed the cell membrane of C. albicans, including the cytoplasmic membrane and mitochondrial membrane, and caused the accumulation of reactive oxygen species and mitochondrial dysfunction, which ultimately led to apoptosis of C. albicans. In addition, CDM had no toxicity on human normal gastric mucosal epithelial cells exposed to a concentration of 125 μg/mL. Experiments showed that CDM reduced the damage of C. albicans to the visceral tissue of infected mice and improved the survival rate of mice. Our research provides a scientific basis for the discovery of effective and safe anti-C. albicans drugs from H. erinaceus.
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