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Discovery of New Benzohydrazide Derivatives Containing 4-Aminoquinazoline as Effective Agricultural Fungicides, the Related Mechanistic Study, and Safety Assessment.
J Agric Food Chem
January 2025
State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
A total of 38 new benzohydrazide derivatives bearing the 4-aminoquinazoline moiety were designed and synthesized based on the active subunit combination approach and tested in detail for their inhibition activities against eight agricultural phytopathogenic fungi. The bioassay results indicated that many of the synthesized compounds exhibited extraordinary fungicidal activities in vitro against the tested fungi. For example, compounds , , , and had EC (half-maximal effective concentration) values of 0.
View Article and Find Full Text PDFTransit of NEAT1 and MTP11 to the plasma membrane and co-localization to vesicles support a role for exocytosis-mediated export in metal homeostasis.
Physiol Plant
January 2025
Department of Plant Molecular Biology, Biophore Building, University of Lausanne, Lausanne, Switzerland.
Understanding the role and mode of action of nutrient transporters requires information about their dynamic associations with plant membranes. Historically, apoplastic nutrient export has been associated with proteins localized at the plasma membrane (PM), while the role of endomembrane localization has been less explored. However, recent work on the PHOSPHATE 1 (PHO1) inorganic phosphate (Pi) exporter demonstrated that, although primarily localized at the Golgi and trans-Golgi network (TGN) vesicles, PHO1 does associate with the PM when clathrin-mediated endocytosis (CME) was inhibited, supporting a mechanism for Pi homeostasis involving exocytosis.
View Article and Find Full Text PDFMITOCDNB DECREASES PLATELET ACTIVATION THROUGH ITS SELECTIVE ACTION ON MITOCHONDRIAL THIOREDOXIN REDUCTASE.
Biomed Pharmacother
January 2025
Thrombosis and Healthy Aging Research Center, MIBI: Interdisciplinary Group on Mitochondrial Targeting and Bioenergetics, Medical Technology School, Department of Clinical Biochemistry and Immunohematology, Faculty of Health Sciences, Universidad de Talca, Talca, Chile. Electronic address:
Platelet inhibition is a fundamental objective to prevent and treat thrombus formation. Platelet activation depends on mitochondrial function. This study aims to identify a new mitochondria-targeting compound with antiplatelet activity at safe concentrations in vitro.
View Article and Find Full Text PDFProximal tubule-on-chip as a model for predicting cation transport and drug transporter dynamics.
Sci Rep
January 2025
U1248 Pharmacology & Transplantation, Inserm, Univ. Limoges, Limoges, France.
Deciphering the sources of variability in drug responses requires to understand the processes modulating drug pharmacokinetics. However, pharmacological research suffers from poor reproducibility across clinical, animal, and experimental models. Predictivity can be improved by using Organs-on-Chips, which are more physiological, human-oriented, micro-engineered devices that include microfluidics.
View Article and Find Full Text PDFDevelopment of novel broad-spectrum amphipathic antimicrobial peptides against multidrug-resistant bacteria through a rational combination strategy.
J Adv Res
January 2025
State Key Laboratory of National Security Specially Needed Medicines, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China. Electronic address:
Introduction: In recent years, cationic amphipathic antimicrobial peptides (AMPs) have shown great promise in combating antibiotic resistance on account of their distinctive membrane-disruptive mechanism. However, the clinical application of AMPs is restricted by their unsatisfactory stability and safety. Although attempts have been made to improve the stability and safety of AMPs, many of them are accompanied by a decline in their antimicrobial activity and bacterial selectivity.
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