The treatment of cystic fibrosis (CF) patients chronically infected with Burkholderia cepacia complex (Bcc) bacteria requires extensive and aggressive antibiotics therapy, exposing these bacteria to prolonged antibiotics-selective pressure. In the present study, we have compared the susceptibility patterns to 13 antimicrobials of 94 Bcc isolates obtained from 15 Portuguese CF patients in the course of chronic infection during a five-year survey. These isolates were previously genotyped and represent 11 different strains of the species B. cenocepacia (subgroups A and B), B. cepacia, B. multivorans, and B. stabilis. The results are consistent with the notion that CF Bcc isolates are resistant to the most clinically relevant antimicrobials and suggest an uneven distribution of resistance rates among the different species, with B. cenocepacia subgroup A isolates being the most resistant. Phenotypic variants exhibiting differences in the antimicrobial susceptibility patterns were obtained from the sputum samples of clinically deteriorated CF patients during chronic lung infection. The isolation of resistant variants coincided with periods of pulmonary exacerbation and antibiotics therapy.
Acetylcholinesterase inhibition, antioxidant and cytotoxic activities of Hedychium gardnerianum leaf essential oils from S. Miguel Island were determined. All the oils inhibited acetylcholinesterase, with IC 50 values of approximately 1 mg/mL, showing no statistical differences between collection sites. Three oils presented mixed inhibition, whilst one was almost truly competitive. This activity can be attributed to the presence of sesquiterpenes, which constituted more than 60% of the composition of the oils. Regarding the antioxidant activity as measured by the DPPH method, all the oils presented activities similar to reference compounds, although with statistical differences between collection sites. Cytotoxicity measured using Artemia salina classified these oils as moderately toxic, with LC 50 values ranging from 300 to 500 µg/mL. These results indicate a possible application of these oils in aromatherapy as coadjuvants in the treatment of cognitive diseases such as Alzheimer, since they may contribute to increase acetylcholine in cholinergic neurons and simultaneously fight deleterious oxidations responsible by neurological degeneration.
Natural products have been the single most productive source of leads for the development of drugs, because of the great variety of their chemical structures. Previous chemical investigation of members of the genus Cystoseira resulted in the discovery of various bioactive secondary metabolites. The secondary metabolites isolated and characterized are very interesting, both from the biological activity and structural complexity points of view, which make this genus an attractive target for further investigations. The present review covers the research progress on natural products isolated from this genus since January 1995 until now, concerning the isolation and structural elucidation of the secondary metabolites from Cystoseira species. In this contribution significant biological properties are briefly discussed. Simultaneously, we gradually construct an intra-molecular pathway that logically interrelates the isolated compounds.
15The alkaloids from Chelidonium majus L. which had a significant inhibitory effect in mitochondrial respiration were those which contain a positive charge due to a quaternary nitrogen atom, i.e., chelerythrine, sanguinarine, berberine and coptisine, both with malate + glutamate or with succinate as substrates. When malate + glutamate was used as substrate, chelerythrine and berberine, which contain methoxy groups, were particularly more active, since they had a strong effect even at low concentrations. In submitochondrial particles, berberine and coptisine had a marked inhibitory effect on NADH dehydrogenase activity but practically no effect on succinate dehydrogenase activity, whereas chelerythrine and sanguinarine inhibited more strongly succinate dehydrogenase than NADH dehydrogenase, which is in agreement with the results found for mitochondrial respiration. Protopine and allocryptopine, which did not inhibit mitochondrial respiration, strongly inhibited NADH dehydrogenase in submitochondrial particles, but had no effect on succinate dehydrogenase activity.
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