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1.
J Appl Microbiol ; 113(4): 779-89, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22762374

RESUMO

AIMS: To investigate the phenanthrene-degrading abilities of the halophilic Martelella species AD-3 under different conditions and to propose a possible metabolic pathway. METHODS AND RESULTS: Using HPLC and GC-MS analyses, the phenanthrene-degrading properties of the halophilic strain AD-3 and its metabolites were analysed. This isolate efficiently degraded phenanthrene under multiple conditions characterized by different concentrations of phenanthrene (100-400 mg l(-1) ), a broad range of salinities (0·1-15%) and varying pHs (6·0-10·0). Phenanthrene (200 mg l(-1) ) was completely depleted under 3% salinity and a pH of 9·0 within 6 days. The potential toxicity of phenanthrene and its generated metabolites towards the bacterium Vibrio fischeri was significantly reduced 10 days after the bioassay. On the basis of the identified metabolites, enzyme activities and the utilization of probable intermediates, phenanthrene degradation by strain AD-3 was proposed in two distinct routes. In route I, metabolism of phenanthrene was initiated by the dioxygenation at C-3,4 via 1-hydroxy-2-naphthoic acid, 1-naphthol, salicylic acid and gentisic acid. In route II, phenanthrene was metabolized to 9-phenanthrol and 9,10-phenanthrenequinone. Further study indicated that strain AD-3 exhibited a wide spectrum of substrate utilization including other polycyclic aromatic hydrocarbons (PAHs). CONCLUSIONS: The results suggest that strain AD-3 possesses a high phenanthrene biodegradability and that the degradation occurs via two routes that remarkably reduce toxicity. SIGNIFICANCE AND IMPACT OF THE STUDY: To the best of our knowledge, this work presents the first report of phenanthrene degradation by a halophilic PAH-degrading strain via two routes. In the future, the use of halophilic strain AD-3 provides a potential application for efficient PAH-contaminated hypersaline field remediation.


Assuntos
Alphaproteobacteria/metabolismo , Redes e Vias Metabólicas , Fenantrenos/metabolismo , Alphaproteobacteria/enzimologia , Biodegradação Ambiental , Cromatografia Líquida de Alta Pressão , Cromatografia Gasosa-Espectrometria de Massas , Concentração de Íons de Hidrogênio , Salinidade
2.
Drug Discov Ther ; 6(1): 9-17, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22460423

RESUMO

Solasodine glycosides, such as solamargine, have been proved to be very important anti-cancer agents. In order to discover more potent cytotoxic agents and explore the preliminary structure activity relationship, a new series of solasodine glycosides 2-9 were synthesized via a transglycosylation strategy, and their cytotoxic activity against a panel of human cancer cell lines (MCF-7, KB, K562, and PC3 cells) were evaluated by MTT assays. The results indicated that compounds 2, 8, and 9 with the substitute moiety of rhamnose, 2-hydroxyethoxymethyl, and 1,3-dihydroxypropan-2-yloxy-methyl, respectively, exhibited quite strong anticancer activity. The underlying mechanism tests demonstrated that these compounds could induce apoptosis detected by DAPI staining, and Annexin V and propidium iodide binding. Cell cycle analysis indicated that the cancer cells were predominantly arrested at the G2/M phase when exposure to these compounds was examined by flow cytometry. These compounds may serve as lead candidates in the development of novel chemotherapeutics for cancer treatment.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Glicosídeos/farmacologia , Neoplasias/tratamento farmacológico , Alcaloides de Solanáceas/farmacologia , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Citometria de Fluxo , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Glicosídeos/síntese química , Glicosídeos/química , Humanos , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Neoplasias/patologia , Alcaloides de Solanáceas/síntese química , Alcaloides de Solanáceas/química , Relação Estrutura-Atividade
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