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1.
Microbiologyopen ; 10(2): e1183, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33970536

RESUMO

In recent years, the fermented milk product kefir has been intensively studied because of its health benefits. Here, we evaluated the microbial consortia of two kefir samples, from Escarcega, Campeche, and Campeche (México). We considered a functional comparison between both samples, including fungal and bacterial inhibition; second, we applied shotgun metagenomics to assess the structure and functional diversity of the communities of microorganisms. These two samples exhibited antagonisms against bacterial and fungal pathogens. Bioactive polyketides and nonribosomal peptides were identified by LC-HRMS analysis. We also observed a high bacterial diversity and an abundance of Actinobacteria in both kefir samples, and a greater abundance of Saccharomyces species in kefir of Escarcega than in the Campeche kefir. When the prophage compositions were evaluated, the Campeche sample showed a higher diversity of prophage sequences. In Escarcega, we observed a prevalence of prophage families that infect Enterobacteria and Lactobacillus. The sequences associated with secondary metabolites, such as plipastatin, fengycin, and bacillaene, and also bacteriocins like helveticin and zoocin, were also found in different proportions, with greater diversity in the Escarcega sample. The analyses described in this work open the opportunity to understand the microbial diversity in kefir samples from two distant localities.


Assuntos
Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Kefir/microbiologia , Metagenoma , Animais , Bactérias/classificação , Biodiversidade , Produtos Fermentados do Leite/microbiologia , DNA Bacteriano , DNA Fúngico , Fermentação , Microbiologia de Alimentos , Fungos/classificação , Metagenômica/métodos , México , Microbiota , Leite/microbiologia , Peptídeos/farmacologia , Policetídeos/farmacologia , Prófagos/genética , Metabolismo Secundário
2.
Chem Pharm Bull (Tokyo) ; 67(12): 1293-1300, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31787656

RESUMO

Based on our previous research on cysticidal drugs, we report the synthesis and evaluation of three new benzimidazole derivatives. In these compounds, the amido group was used as a bioisosteric replacement of the ester group. The molecular docking on ß-tubulin revealed that the derivatives interacted through hydrogen bonding with N165, E198 and V236. All compounds showed in vitro activity against Taenia crassiceps cysts. Among them, benzimidazole 3 was found to be the most potent of the series (EC50 0.86 µM). This compound also exhibited the highest probability of binding and the lowest binding free energy score and was therefore selected for in vivo evaluation. Results indicated that the efficacy of compound 3 was comparable to that of the reference drug, albendazole (50.39 vs. 47.16% parasite reduction). Animals treated with compound 3 seemed to tolerate this benzimidazole well, with no changes in behavior, or food and water consumption. These findings are consistent with the in silico prediction results, which indicated low toxicity risks. The pharmacokinetic study showed that the half-life and mean residence time (6.06 and 11.9 h, respectively) were long after oral administration. Together, these results indicate that this new benzimidazole derivative represents a promising structure with cysticidal activity.


Assuntos
Amebicidas/farmacologia , Benzimidazóis/farmacologia , Cisticercose/tratamento farmacológico , Simulação de Acoplamento Molecular , Taenia/efeitos dos fármacos , Amebicidas/síntese química , Amebicidas/química , Animais , Benzimidazóis/síntese química , Benzimidazóis/química , Relação Dose-Resposta a Droga , Feminino , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Relação Estrutura-Atividade
3.
Eur J Med Chem ; 44(4): 1794-800, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18582991

RESUMO

Despite albendazole being the drug of choice in neurocysticercosis treatment, its low solubility limits its bioavailability; therefore, more research is required in order to find new molecules with cestocidal activity and adequate aqueous solubility. A set of 13 benzimidazole derivatives were synthesized and their in vitro activities were evaluated against Taenia crassiceps cysts, using albendazole sulfoxide as reference molecule, showing that two of them exhibited good activity. Molecular modelling revealed that the cysticidal efficacy depends on the presence on the molecule of an H in the 1-position, a planar carbamate group at 2-position, and if the substituent in 5-position is voluminous, it should be orthogonal to the benzimidazole ring.


Assuntos
Anti-Helmínticos/química , Anti-Helmínticos/farmacologia , Benzimidazóis/química , Benzimidazóis/farmacologia , Desenho de Fármacos , Taenia/efeitos dos fármacos , Albendazol/análogos & derivados , Albendazol/farmacologia , Animais , Anti-Helmínticos/síntese química , Benzimidazóis/síntese química , Modelos Moleculares , Padrões de Referência
4.
Rev. colomb. biotecnol ; 10(2): 97-103, dic. 2008. tab, graf
Artigo em Espanhol | LILACS | ID: lil-505456

RESUMO

Con el empleo del sistema de inmersión temporal fue posible incrementar la multiplicación in vitro de los segmentos nodales en el clon de ñame Blanco de Guinea. Con este tipo de sistema de cultivo se obtuvieron los más altos valores para la altura de la planta, número de entrenudos por planta, así como para la masa fresca y seca de las mismas. Las condiciones de cultivo creadas en el sistema de inmersión temporal para la multiplicación in vitro de los segmentos nodales lograron el más alto coeficiente de multiplicación (8,50), así como redujeron el número de plantas con síntomas de vitrificación (3,30). Las plantas cultivadas en este tipo de sistema de cultivo se caracterizaron por el mayor crecimiento de los segmentos nodales, coloración verde y hojas más desarrolladas. La utilización de este tipo de sistema de cultivo en la fase de multiplicación in vitro de los segmentos nodales posibilitará incrementar el empleo de la micropropagación para la producción de semilla en el complejo Dioscorea cayenensis - D. rotundata


Assuntos
Dioscorea/crescimento & desenvolvimento
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