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1.
J Fungi (Basel) ; 9(9)2023 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-37755039

RESUMO

Date palm, an important crop in Morocco and many other arid regions around the world, faces significant challenges from wind, water shortages, and salinization, which contribute to vegetation loss and soil degradation in the harsh environmental conditions of oasis ecosystems with low soil fertility. Protecting and regenerating these degraded lands is crucial for sustainable agriculture and improving the dryland ecosystem. Arbuscular mycorrhizal fungi (AMF) comprise a vital element in this dynamic within the microflora of the soil rhizosphere. This study evaluated the potential in mycorrhizal soil and identified AMF in date palm rhizospheres in eight locations within the Figuig oasis (southeastern Morocco). This study found that Extension and Zenaga had more mycorrhizal propagules than other locations. Replanted maize (Zea mays L.) in these soils exhibited higher mycorrhization rates (91-93%) compared to that in other locations, with the Lamaiz site registering the lowest rate (39%). The phosphorus content was negatively correlated with the AMF spore frequency, intensity, and density, while a positive correlation was detected between the soil pH and the AMF spore frequency and density. The morphological identification of spores revealed Glomus as the predominant species, along with Acaulospora and Sclerocystis. This study represents an initial step toward the potential application of these fungi in environmental conservation and sustainable agriculture in arid regions.

2.
J Pharm Pharmacol ; 65(3): 402-10, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23356849

RESUMO

OBJECTIVES: The plasma pharmacokinetic profile in CD-1 mice of a novel 18ß-glycyrrhetinic acid (GA) derivative, which displays in vitro anti-cancer activity, was assessed. METHODS: This study involved an original one-step synthesis of N-(2-{3-[3,5-bis(trifluoromethyl)phenyl]ureido}ethyl)-glycyrrhetinamide, (2) a compound that displays marked anti-proteasome and anti-kinase activity. The bioselectivity profile of 2 on human normal NHDF fibroblasts vs human U373 glioblastoma cells was assessed. Maximal tolerated dose (MTD) profiling of 2 was carried out in CD1 mice, and its serum pharmacokinetics were profiled using an acute intravenous administration of 40 mg/kg body weight. KEY FINDINGS: Compound 2 displayed IC(50) in vitro growth inhibitory concentrations of 29 and 8 µm on NHDF fibroblasts and U373 glioblastoma cells, respectively, thus a bioselectivity index of ∼4. The intravenous pharmacokinetic parameters revealed that 2 was rapidly distributed (t(1/2dist) of ∼3 min) but slowly eliminated (t(1/2elim) = ∼77 min). CONCLUSIONS: This study describes an original and reliable nanoemulsion of a GA derivative with both anti-proteasome and anti-kinase properties and that should be further tested in vivo using various human xenograft or murine syngeneic tumour models with both single and chronic intravenous administration.


Assuntos
Antineoplásicos/farmacologia , Ácido Glicirretínico/análogos & derivados , Animais , Antineoplásicos/sangue , Antineoplásicos/química , Antineoplásicos/farmacocinética , Linhagem Celular Tumoral , Química Farmacêutica/métodos , Relação Dose-Resposta a Droga , Emulsões/química , Emulsões/farmacocinética , Emulsões/farmacologia , Feminino , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Glioblastoma/tratamento farmacológico , Glioblastoma/metabolismo , Ácido Glicirretínico/sangue , Ácido Glicirretínico/química , Ácido Glicirretínico/farmacocinética , Ácido Glicirretínico/farmacologia , Humanos , Camundongos , Tamanho da Partícula , Complexo de Endopeptidases do Proteassoma/efeitos dos fármacos , Complexo de Endopeptidases do Proteassoma/metabolismo
3.
Int J Oncol ; 38(3): 833-42, 2011 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21206969

RESUMO

Flavonoids are polyphenolic secondary metabolites from plants that possess a common phenylbenzopyrone structure (C6-C3-C6). Depending upon variations in their heterocyclic C-ring, flavonoids are categorised into one of the following groups: flavones, flavonols, flavanones, flavanols, anthocyanidins, isoflavones or chalcones. Flavonols include, among others, the molecules quercetin, myricetin and kaempferol. The anticancer activity of flavonols was first attributed to their electron-donating ability, which comes from the presence of phenolic hydroxyl groups. However, an emerging view is that flavonoids, including quercetin, may also exert modulatory actions in cells by acting through the protein kinase and lipid kinase signalling pathways. Data from the current study showed that 2 µM quercetin, a low concentration that represents less than 10% of its IC50 growth-inhibitory concentration as calculated from the average of eight distinct cancer cell lines, decreased the activity of 16 kinases by more than 80%, including ABL1, Aurora-A, -B, -C, CLK1, FLT3, JAK3, MET, NEK4, NEK9, PAK3, PIM1, RET, FGF-R2, PDGF-Rα and -Rß. Many of these kinases are involved in the control of mitotic processes. Quantitative video microscopy analyses revealed that quercetin displayed strong anti-mitotic activity, leading to cell death. In conclusion, quercetin partly exerts its anticancer activity through the inhibition of the activity of a large set of kinases. Quercetin could be an interesting chemical scaffold from which to generate novel derivatives possessing various types of anti-kinase activities.


Assuntos
Neoplasias/enzimologia , Neoplasias/patologia , Fosfotransferases/antagonistas & inibidores , Quercetina/farmacologia , Animais , Biologia Celular , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/farmacologia , Humanos , Concentração Inibidora 50 , Loranthaceae/química , Neoplasias/metabolismo , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Spodoptera
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