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1.
J Environ Sci Health B ; 59(8): 521-539, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39001801

RESUMEN

Two years of monthly sampling and hydrological monitoring were performed at the outlet of a Mediterranean watershed in northern Tunisia to determine the contents of 469 pesticide active ingredients and metabolites in water and evaluate their behavior. Wadi Guenniche is a tributary of the Bizerte coastal lagoon, with a watershed area of 86 km2, which exhibits pluvial cereal, legume, and orchid cultivation and irrigated market gardening. Twenty-nine pesticide active ingredients and 2 metabolites were detected in water. Twenty-four pesticide active ingredients were authorized for use in Tunisia. Among them, 14 had never been mentioned in previous farmer surveys. Five herbicides and their metabolites were the most frequently detected: aminomethylphosphonic acid (AMPA) (100%), glyphosate (94%), simazine (94%), 2,4-D (70%), and deisopropylatrazine (DIA) (47%). The detection frequency and concentration range suggested that the phytosanitary pressure and resulting water contamination are close to those on the northern Mediterranean shore. These results, in addition to characterizing the pollution state, emphasized the need for additional studies on the use and fate of pesticides on the southern shore of the Mediterranean Sea, particularly in Tunisia.


Asunto(s)
Monitoreo del Ambiente , Plaguicidas , Contaminantes Químicos del Agua , Túnez , Contaminantes Químicos del Agua/análisis , Plaguicidas/análisis , Agricultura , Ciudades
2.
Environ Sci Pollut Res Int ; 30(40): 92182-92192, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37486469

RESUMEN

Mitigation of pesticide dispersion in soil and water is required to protect ecosystem health and the anthropic uses of water bodies. Biochar amendments have been suggested to reduce pesticide dispersion due to their high sorption potentials. Nevertheless, appraisals at different scales have been limited by the costs of pesticide analyses. The aim of this study was to evaluate the potential of two fluorescent tracers, uranine (UR) and sulforhodamine B (SRB), for use as pesticide proxies in the context of biochar amendments used for mitigation purposes. Therefore, we compared the sorption processes of both fluorescent tracers and those of three pesticides, glyphosate, 2,4-D, and difenoconazole for soils; three wood biochars (pine, oak, and beech/charm blend); and soil/biochar mixtures representing agricultural usages. The results showed that the sorption of glyphosate by soil was unaffected by amendment with the tested pine, oak, and wood blend biochars. In contrast, the sorption coefficients of UR, SRB, 2,4-D, and difenoconazole were significantly increased with these biochar amendments. SRB, in particular, exhibited sorption behavior similar to that of the hydrophobic fungicide difenoconazole. This indicates promise for the use of SRB as a proxy for hydrophobic pesticides, in testing biochar amendments.


Asunto(s)
Plaguicidas , Contaminantes del Suelo , Plaguicidas/química , Ecosistema , Adsorción , Carbón Orgánico/química , Suelo/química , Fluoresceína , Agua , Colorantes , Ácido 2,4-Diclorofenoxiacético , Contaminantes del Suelo/análisis
3.
J Med Chem ; 63(15): 8069-8087, 2020 08 13.
Artículo en Inglés | MEDLINE | ID: mdl-32687714

RESUMEN

Malaria is an infectious disease caused by a parasite of the genus Plasmodium, and the emergence of parasites resistant to all current antimalarial drugs highlights the urgency of having new classes of molecules. We developed an effective method for the synthesis of a series of ß-modified acyclonucleoside phosphonate (ANP) derivatives, using commercially available and inexpensive materials (i.e., aspartic acid and purine heterocycles). Their biological evaluation in cell culture experiments and SAR revealed that the compounds' effectiveness depends on the presence of a hydroxyl group, the chain length (four carbons), and the nature of the nucleobase (guanine). The most active derivative inhibits the growth of Plasmodium falciparum in vitro in the nanomolar range (IC50 = 74 nM) with high selectivity index (SI > 1350). This compound also showed remarkable in vivo activity in P. berghei-infected mice (ED50 ∼ 0.5 mg/kg) when administered by the ip route and is, although less efficient, still active via the oral route. It is the first ANP derivative with such potent antimalarial activity and therefore has considerable potential for development as a new antimalarial drug.


Asunto(s)
Antimaláricos/química , Antimaláricos/farmacología , Malaria Falciparum/tratamiento farmacológico , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/uso terapéutico , Femenino , Humanos , Células K562 , Ratones , Nucleósidos/química , Nucleósidos/farmacología , Nucleósidos/uso terapéutico , Organofosfonatos/química , Organofosfonatos/farmacología , Organofosfonatos/uso terapéutico , Plasmodium falciparum/fisiología
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