ABSTRACT
BACKGROUND: Although microencapsulation technology is an effective pesticide formulation method, the correlation between the release properties of microcapsules and pesticide concentrations in soil and their efficacy has not been thoroughly investigated. Here, the effects of the release properties of the nematicide Fosthiazate (FTZ) from microcapsules on their efficacy against the nematode Meloidogyne incognita were examined using experimental and mathematical approaches. RESULTS: Gradual release of FTZ from both polyurea microcapsules (PU-MC) and melamine-formaldehyde microcapsules (MF-MC) was observed over 30 days in the release test, and each release curve was completely distinct. In the biological test, the efficacy of both microcapsules against M. incognita 42 days after the application was 8-15% higher than that of the non-encapsulated FTZ at a concentration of 2.0 mg FTZ kg-1 soil. Soil degradation experiments suggested that the microcapsules worked effectively to protect the FTZ from degradation, which resulted in higher efficacy at a later stage. A simulation study to predict the concentration of FTZ outside the microcapsule found that the timing of supplying FTZ was important and suggested that the mixture of non-encapsulated FTZ (non-MC) and MF-MC showed enhanced efficiency for the entire cultivation period in the biological test; the efficacy against nematodes was also confirmed by the measurement of nematode density using the Bearman funnel method. CONCLUSION: The release properties of FTZ from microcapsules are critical for their effective application against M. incognita, and the established simulation study is a useful step in designing suitable release properties under complex soil conditions. © 2024 Society of Chemical Industry.
ABSTRACT
Curcumin, which can exist in an equilibrium between keto and enol tautomers, binds to beta-amyloid (Abeta) fibrils/aggregates. The aim of this study was to assess the relationship between the tautomeric structures of curcumin derivatives and their Abeta-binding activities. Curcumin derivatives with keto-enol tautomerism showed high levels of binding to Abeta aggregates but not to Abeta monomers. The binding activity of the keto form analogue of curcumin to Abeta aggregates was found to be much weaker than that of curcumin derivatives with keto-enol tautomerism. The color of a curcumin derivative with keto-enol tautomerism, which was substituted at the C-4 position, changed from yellow to orange within 30 min of being combined with Abeta aggregates in physiological buffer. This resulted from a remarkable increase in the enol form with extended conjugation of double bonds upon binding. These findings suggest that curcumin derivatives exist predominantly in the enol form during binding to Abeta aggregates, and that the enolization of curcumin derivatives is crucial for binding to Abeta aggregates. The keto-enol tautomerism of curcumin derivatives may be a novel target for the design of amyloid-binding agents that can be used both for therapy and for amyloid detection in Alzheimer's disease.
Subject(s)
Alzheimer Disease/drug therapy , Amyloid beta-Peptides/metabolism , Curcumin/analogs & derivatives , Curcumin/therapeutic use , Amyloid beta-Peptides/chemistry , Curcumin/chemistry , Curcumin/metabolism , Magnetic Resonance Spectroscopy , Methanol/chemistry , Protein Binding/drug effects , Protein Structure, Quaternary , Solutions , Spectrophotometry, Ultraviolet , StereoisomerismABSTRACT
The chemical properties of probes that improve amyloid detection by non-invasive (19)F magnetic resonance imaging (MRI) are of interest. We synthesized benzoxazole compounds with trifluoromethoxy groups, and found that these compounds displayed sharp (19)F nuclear magnetic resonance (NMR) signals in an assay buffer. However, the intensities of the (19)F NMR signals were dramatically reduced in mouse brain lysates. Our results indicate that the inhibitory effect of brain tissue on the (19)F NMR signals from these probes can be attributed to the hydrophobicity of the tissue. These results highlight the importance of using hydrophilic (19)F-MRI agents to avoid the inhibitory effects of brain tissues on (19)F NMR signals.
