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One of the pathological hallmarks of Alzheimer's disease (AD) is the formation of amyloid-β plaques. Since acetylcholinesterase (AChE) promotes the formation of such plaques, the inhibition of this enzyme could slow down the progression of amyloid-β aggregation, hence being complementary to the palliative treatment of cholinergic decline. Antiaggregation assays performed for apigenin and quercetin, which are polyphenolic compounds that exhibit inhibitory properties against the formation of amyloid plaques, reveal distinct inhibitory effects of these compounds on Aβ40 aggregation in the presence and absence of AChE. Furthermore, the analysis of the amyloid fibers formed in the presence of these flavonoids suggests that the Aβ40 aggregates present different quaternary structures, viz., smaller molecular assemblies are generated. In agreement with a noncompetitive inhibition of AChE, molecular modeling studies indicate that these effects may be due to the binding of apigenin and quercetin at the peripheral binding site of AChE. Since apigenin and quercetin can also reduce the generation of reactive oxygen species, the data achieved suggest that multitarget catechol-type compounds may be used for the simultaneous treatment of various biological hallmarks of AD. [ABSTRACT FROM AUTHOR]

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Uncertainty in thematic maps has been tested mainly in maps with discrete or fuzzy classifications based on spectral data. However, many ecosystem maps in tropical countries consist of discrete polygons containing information on various ecosystem properties such as vegetation cover, soil, climate, geomorphology and biodiversity. The combination of these properties into one class leads to error. We propose a probability-based sampling design with two domains, multiple stages, and stratification with selection of primary sampling units (PSUs) proportional to the richness of strata present. Validation is undertaken through field visits and fine resolution remote sensing data. A pilot site in the center of the Colombian Andes was chosen to validate a government official ecosystem map. Twenty primary sampling units (PSUs) of 10 × 15 km were selected, and the final numbers of final sampling units (FSUs) were 76 for the terrestrial domain and 46 for the aquatic domain. Our results showed a confidence level of 95%, with the accuracy in the terrestrial domain varying between 51.8% and 64.3% and in the aquatic domain varying between 75% and 92%. Governments need to account for uncertainty since they rely on the quality of these maps to make decisions and guide policies. [ABSTRACT FROM AUTHOR]

Two domino Diels-Alder adducts were obtained from 3,7-bis(cyclopenta-2,4-dien-1-ylidene)- cis-bicyclo[3.3.0]octane and dimethyl acetylenedicarboxylate or N-methylmaleimide under microwave irradiation. From the first adduct, a C20H24 diene with C2 v symmetry was obtained by Zn/AcOH reduction, hydrolysis, oxidative decarboxylation, and selective hydrogenation. Photochemical [2+2] cycloaddition of this diene gave a thermally unstable cyclobutane derivative, which reverts to the diene. However, both the diene and the cyclobutane derivatives could be identified by X-ray diffraction analysis upon irradiation of the diene crystal. New six-membered rings are formed upon the transannular addition of bromine or iodine to the diene. The N-type selectivity of the addition was examined by theoretical calculations, which revealed the distinct susceptibility of the doubly bonded carbon atoms to the bromine attack. [ABSTRACT FROM AUTHOR]

Nonsymbiotic hemoglobins AHb1 and AHb2 discovered in Arabidopsis thaliana are likely to carry out distinct physiological roles, in consideration of their differences in sequence, structure, expression pattern, and tissue localization. Despite a relatively fast autoxidation in the presence of O, we were able to collect O-binding curves for AHb2 in the presence of a reduction enzymatic system. AHb2 binds O noncooperatively with a p50 of 0.021 ± 0.003 Torr, a value consistent with a recently proposed role in O transport. The analysis of the internal cavities derived from the structures sampled in molecular dynamics simulations confirms strong differences with AHb1, proposed to work as a NO deoxygenase in vivo. Overall, our results are consistent with a role for AHb2 as an oxygen carrier, as recently proposed on the basis of experiments on AHb2-overexpressing mutants of A. thaliana. © 2011 IUBMB IUBMB Life, 63(5): 363-362, 2011. [ABSTRACT FROM AUTHOR]

The interaction between drugs and transport proteins, such as albumins, is a key factor in drug bioavailability. One of the techniques commonly used for the evaluation of the drug-protein complex formation is fluorescence. This work studies the interaction of human serum albumin (HSA) with four non-steroidal anti-inflammatory drugs (NSAIDs)—ibuprofen, flurbiprofen, naproxen, and diflunisal—by monitoring the fluorescence quenching when the drug-albumin complex is formed. Two approaches—the double logarithm Stern-Volmer equation and the STAR program—are used to evaluate the binding parameters. The results are analyzed considering the binding properties, determined by using other complementary techniques and the available structural information of albumin complexes with NSAID-related compounds. Finally, this combined analysis has been synergistically used to interpret the binding of flurbiprofen to HSA. [ABSTRACT FROM AUTHOR]