RESUMO
Compared with normal cells, cancer cells usually exhibit an increase in glucose uptake as part of the Warburg effect. To take advantage of this hallmark of cancer, glucose transporters could be a good candidate for cancer targeting. Herein, we report novel glycoconjugate aza-BODIPY dyes (AZB-Glc and AZB-Glc-I) that contain two glucose moieties conjugated to near-infrared dyes via the azide-alkyne cycloaddition reaction. As anticipated, a higher level of AZB-Glc uptake was observed in breast cancer cells that overexpressed glucose transporters (GLUTs), especially GLUT-1, including the triple-negative breast cancer cell line (MDA-MB-231) and human breast adenocarcinoma cell line (MCF-7), compared to that of normal cells (human fetal lung fibroblasts, HFL1). The cellular uptake of AZB-Glc was in a dose- and time-dependent manner and also depended on GLUT, as evidenced by the decreased uptake of AZB-Glc in the presence of d-glucose or a glucose metabolism suppressor, combretastatin. In addition, light triggered cell death was also investigated through photodynamic therapy (PDT), since near-infrared (NIR) light is known to penetrate deeper tissue than light of shorter wavelengths. AZB-Glc-I, the analog of AZB-Glc containing iodine for enhanced singlet oxygen production upon NIR irradiation, was used for all treatment assays. AZB-Glc-I showed significant NIR light-induced cytotoxicity in cancer cells (IC50 = 1.4-1.6 µM under 1 min irradiation), which was about 20-times lower than that in normal cells (IC50 = 32 µM) under the same conditions, with negligible dark toxicity (IC50 > 100 µM) in all cell lines. Moreover, the singlet oxygen was detected inside the cancer cells after exposure to light in the presence of AZB-Glc-I. Therefore, our glucose conjugated systems proved to efficiently target cancer cells for enhanced photodynamic cancer therapy.
Assuntos
FotoquimioterapiaRESUMO
Leaf spot is one of the most important cassava diseases. Nanotechnology can be applied to control diseases and improve plant growth. This study was performed to prepare chitosan (CS) nanoparticle (NP)-loaded salicylic acid (SA) or silver (Ag) by the ionic gelation method, and to evaluate their effectiveness on reducing leaf spot disease and enhancing the growth of cassava plants. The CS (0.4 or 0.5%) and Pentasodium triphosphate (0.2 or 0.5%) were mixed with SA varying at 0.05, 0.1, or 0.2% or silver nitrate varying at 1, 2, or 3 mM to prepare three formulations of CS-NP-loaded SA named N1, N2, and N3 or CS-NP-loaded Ag named N4, N5, and N6. The results showed that the six formulations were not toxic to cassava leaves up to 800 ppm. The CS-NP-loaded SA (N3) and CS-NP-loaded Ag (N6) were more effective than the remaining formulations in reducing the disease severity and the disease index of leaf spot. Furthermore, N3 at 400 ppm and N6 at 200, 400, and 800 ppm could reduce disease severity (68.9-73.6% or 37.0-37.7%, depending on the time of treatment and the pathogen density) and enhance plant growth more than or equal to commercial fungicide or nano-fungicide products under net-house conditions. The study indicates the potential to use CS-NP-loaded SA or Ag as elicitors to manage cassava leaf spot disease.
RESUMO
By 2050, population growth and climate change will lead to increased demand for food and water. Nanoparticles (NPs), an advanced technology, can be applied to many areas of agriculture, including crop protection and growth enhancement, to build sustainable agricultural production. Ionic gelation method is a synthesis of microparticles or NPs, based on an electrostatic interaction between opposite charge types that contains at least one polymer under mechanical stirring conditions. NPs, which are commonly based on chitosan (CS), have been applied to many agricultural fields, including nanopesticides, nanofertilizers, and nanoherbicides. The CS-NP or CS-NPs-loaded active ingredients (Cu, saponin, harpin, Zn, hexaconazole, salicylic acid (SA), NPK, thiamine, silicon, and silver (Ag)) are effective in controlling plant diseases and enhancing plant growth, depending on the concentration and application method by direct and indirect mechanisms, and have attracted much attention in the last five years. Many crops have been evaluated in in vivo or in greenhouse conditions but only maize (CS-NP-loaded Cu, Zn, SA, and silicon) and soybean (CS-NP-loaded Cu) were tested for manage post flowering stalk rot, Curvularia leaf spot, and bacterial pustule disease in field condition. Since 2019, five of eight studies have been performed in field conditions that have shown interest in CS-NPs synthesized by the ionic gelation method. In this review, we summarized the current state of research and provided a forward-looking view of the use of CS-NPs in plant disease management.
RESUMO
Ineffective site-specific delivery has seriously impeded the efficacy of nanoparticle-based drugs to a disease site. Here, we report the preparation of three different shapes (sphere, scroll, and oblate) to systematically evaluate the impact of the marginative delivery on the efficacy of magnetic resonance (MR) imaging-guided X-ray irradiation at a low dose of 1 Gy. In addition to the shape effect, the therapeutic efficacy is investigated for the first time to be strongly related to the structure effect that is associated with the chemical activity. The enhanced particle-vessel wall interaction of both the flat scroll and oblate following margination dynamics leads to greater accumulation in the lungs, resulting in superior performance over the sphere against lung tumor growth and suppression of lung metastasis. Furthermore, the impact of the structural discrepancy in nanoparticles on therapeutic efficacy is considered. The tetragonal oblate reveals that the feasibility of the charge-transfer process outperforms the orthorhombic scroll and cubic sphere to suppress tumors. Finally, surface area is also a crucial factor affecting the efficacy of X-ray treatments from the as-prepared particles.