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1.
ScientificWorldJournal ; 2012: 374091, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22666113

RESUMO

The aim of this paper was to test the use of dual microbial inoculation with mycorrhizal and saprotrophic fungi in onion cultivation to enhance yield while maintaining or improving the nutritional quality of onion bulbs. Treatments were two-factorial: (1) arbuscular mycorrhizal fungi (AMF): the mix corresponding to fungal part of commercial product Symbivit (Glomus etunicatum, G. microaggregatum, G. intraradices, G. claroideum, G. mosseae, and G. geosporum) (M1) or the single-fungus inoculum of G. intraradices BEG140 (M2) and (2) bark chips preinoculated with saprotrophic fungi (mix of Gymnopilus sp., Agrocybe praecox, and Marasmius androsaceus) (S). The growth response of onion was the highest for the M1 mix treatment, reaching nearly 100% increase in bulb fresh weight. The effectiveness of dual inoculation was proved by more than 50% increase. We observed a strong correlation (r = 0.83) between the growth response of onion bulbs and AM colonization. All inoculation treatments but the single-fungus one enhanced significantly the total antioxidant capacity of bulb biomass, was the highest values being found for M1, S + M1, and S + M2. We observed some induced enhancement of the contents of mineral elements in bulb tissue (Mg and K contents for the M2 and M2, S, and S + M2 treatments, resp.).


Assuntos
Fungos/fisiologia , Valor Nutritivo , Cebolas
2.
J Med Chem ; 49(22): 6500-9, 2006 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-17064068

RESUMO

In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR study based on 35 analogues suggests ways in which the pharmacophore could be further optimized, for example, via substitutions in the 4-aryl ring. Enzyme kinetics studies with the lead compound and X-ray crystallography of an inhibitor-CDK2 complex demonstrated that its mode of inhibition is competitive. Functional kinase assays confirmed the selectivity toward CDKs, with a preference for CDK9-cyclin T1. The most potent inhibitor, 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol 31b (CAN508), reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays. Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9.


Assuntos
Compostos Azo/síntese química , Compostos Azo/farmacologia , Quinases Ciclina-Dependentes/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Pirazóis/síntese química , Pirazóis/farmacologia , Antimetabólitos , Bromodesoxiuridina , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Quinase 2 Dependente de Ciclina/antagonistas & inibidores , Humanos , Immunoblotting , Modelos Moleculares , RNA/biossíntese , RNA/isolamento & purificação , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Transcrição Reversa/efeitos dos fármacos , Relação Estrutura-Atividade , Especificidade por Substrato
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