Synthesis and Antifungal Activity of Fmoc-Protected 1,2,4-Triazolyl-α-Amino Acids and Their Dipeptides Against Aspergillus Species

Biomolecules, Journal Year: 2025, Volume and Issue: 15(1), P. 61 - 61

Published: Jan. 4, 2025

In recent years, fungal infections have emerged as a significant health concern across veterinary species, especially in livestock such cattle, where diseases can result considerable economic losses, well humans. particular, Aspergillus notably flavus and versicolor, are opportunistic pathogens that pose threat to both animals This study focuses on the synthesis antifungal evaluation of novel 9-fluorenylmethoxycarbonyl (Fmoc)-protected 1,2,4-triazolyl-α-amino acids their dipeptides, designed combat pathogens. More detail, we evaluated activity against various including versicolor (ATCC 12134) 10567). The results indicated dipeptide 7a exhibited promising with an IC50 value 169.94 µM, demonstrating greater potency than fluconazole, standard treatment for infections, which showed 254.01 µM. Notably, slightly enhanced efficacy compared fluconazole also (IC50 176.69 µM vs. 184.64 µM), suggesting this might be more potent even strain. Remarkably, 3a A. candidus 10711. On other hand, protected amino acid demonstrated consistent inhibition all tested strains, but 267.86 flavus, it was less still showing some potential good molecule. Overall, our findings indicate synthesized 1,2,4-triazolyl derivatives hold promise agents treating Aspergillus-induced broader applications human health. Our mechanistic studies based molecular docking revealed compounds bind same region sterol 14-α demethylase fluconazole. Given rising concerns about resistance, these derivatives, unique bioactive structures, could serve class therapeutic agents. Further research into vivo safety profiles is warranted fully realize drugs clinical agricultural settings.

Language: Английский

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Oxidative Processes and Xenobiotic Metabolism in Plants: Mechanisms of Defense and Potential Therapeutic Implications

Journal of Xenobiotics, Journal Year: 2024, Volume and Issue: 14(4), P. 1541 - 1569

Published: Oct. 18, 2024

Plants are continuously exposed to environmental challenges, including pollutants, pesticides, and heavy metals, collectively termed xenobiotics. These substances induce oxidative stress by generating reactive oxygen species (ROS), which can damage cellular components such as lipids, proteins, nucleic acids. To counteract this, plants have evolved complex metabolic pathways detoxify process these harmful compounds. Oxidative in primarily arises from the overproduction of hydrogen peroxide (H2O2), superoxide anions (O2•−), singlet (1O2), hydroxyl radicals (•OH), by-products activities photosynthesis respiration. The presence xenobiotics leads a notable increase ROS, result disruption. combat developed strong antioxidant defense mechanism that includes enzymatic antioxidants work together eliminate thereby reducing their effects. In addition defenses, also synthesize various non-enzymatic antioxidants, flavonoids, phenolic acids, vitamins. compounds effectively neutralize ROS help regenerate other offering extensive protection against stress. metabolism xenobiotic occurs three stages: first involves modification, refers chemical alteration make them less harmful. second conjugation, where modified combined with solubility, facilitating elimination plant. third stage compartmentalization, is storage or isolation conjugated specific parts plant, helping prevent vital functions. Secondary metabolites found plants, alkaloids, terpenoids, play role detoxification Gaining deeper understanding mechanisms essential, this knowledge lead formulation plant-derived strategies aimed at alleviating effects pollution enhancing human health improving capabilities, discussed review.

Language: Английский

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Unveiling the Ocean's Arsenal: Successful Integration of Marine Metabolites into Disease Management

UTTAR PRADESH JOURNAL OF ZOOLOGY, Journal Year: 2024, Volume and Issue: 45(13), P. 170 - 188

Published: June 10, 2024

The growing problem of antibiotic resistance calls for a paradigm shift in medication discovery. Fortunately, the enormous oceans, home to an incredible diversity life, provide viable solution: marine metabolites. These unusual chemicals have potential treating wide range diseases. This present study investigates great using these marine-derived gems disease management techniques. Despite difficulty procuring and isolating organisms, discovering most effective metabolites, traversing lengthy research pipelines, rewards are apparent. To demonstrate power resources, paper examines successful case studies. Each delves deeply into single metabolite, including its source organism, it targets, precise mechanism by which metabolite disrupts process. We'll look at results clinical trials that examined efficacy safety medications, eventually exposing real-world influence on patient outcomes after incorporating them treatment plans. Examining cases provides useful insights resources producing novel opening path further discovery innovation battle against

Language: Английский

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Tick-Borne Encephalitis Virus (TBEV): Epidemiology, Diagnosis, Therapeutic Approaches and Some Molecular Aspects—An Updated Review

Microbiology Research, Journal Year: 2024, Volume and Issue: 15(4), P. 2619 - 2649

Published: Dec. 10, 2024

Tick-borne encephalitis virus (TBEV) is a significant public health concern, particularly in rural regions, like the Caucasus, where tick-borne diseases are prevalent. The review contains comprehensive data on TBEV circulation Caucasus region, demonstrating TBE cases North and Georgia, as well identification of new endemic foci Armenia Azerbaijan, highlighting need for further epidemiological studies surveillance region. This provides an updated overview TBEV, encompassing its status, subtypes, life cycle nature, epidemiology, approaches to treatment diagnostics, recent insights into molecular aspects. Understanding complexities transmission, clinical manifestations, advancements diagnostic techniques crucial effective management control strategies. Furthermore, exploring mechanisms underlying pathogenesis host interactions can offer valuable developing novel therapeutics preventive measures. aims consolidate research findings enhance our understanding ultimately contributing improved interventions patient outcomes.

Language: Английский

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Oceanic Breakthroughs: Marine-Derived Innovations in Vaccination, Therapy, and Immune Health

Vaccines, Journal Year: 2024, Volume and Issue: 12(11), P. 1263 - 1263

Published: Nov. 8, 2024

The vast, untapped potential of the world's oceans is revealing groundbreaking advancements in human health and vaccination. Microalgae such as

Language: Английский

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