Radioiodination of p-hydroxyphenylisopropyladenosine: development of a new ligand for adenosine receptors

dl-p-Hydroxyphenylisopropyladenosine has been iodinated with 125I and tested as a ligand of adenosine receptors in membranes from rat brain using a filtration assay. Binding studies using l-[3H]phenylisopropyladenosine as a ligand were carried out in parallel, and the binding of both ligands could be displaced by dl-p-hydroxyphenylisopropyladenosine and l-phenylisopropyladenosine in a similar fashion. These data establish the feasibility of using radioiodinated derivatives of adenosine as ligands of suitable types of adenosine receptors.     

The cyclization of 3-O-benzyl-6-deoxy-6-nitro-D-glucose and -L-idose to O-benzyldeoxynitroinositols,and epimerizations related thereto

3-O-Benzyl-1,2-O-isopropylidene-α-D-xylo-pentodialdo-1,4-furanose (1) was found to give, with nitromethane under catalysis by sodium methoxide, 3-O-benzyl-6-deoxy-1,2-O-isopropylidene-6-nitro- α-D-glucofuranose (2) as the kinetically favored product. Subsequent, spontaneous epimerization led to a 2:1 mixture of 2 and its β-L-ido isomer (3), from which crystalline 3 was isolated. The free nitro hexoses (4 and 5) obtained by deacetonation of 2 and 3 were subjected to barium hydroxide-catalyzed cyclization (internal Henry reaction) to give mixtures of O-benzyldeoxynitroinositols. Under conditions of kinetic control, the α-D-gluco derivative 4 furnished 6-O-benzyl-3-deoxy-3-nitro-muco-inositol (6) and optically active 4-O-benzyl-1-deoxy-1-nitro-L-myo-inositol (L-7) in a ratio of 3:1. The β-L-ido derivative 5 gave the enantiomer (D-7) of the myo compound and 4-O-benzyl-1-deoxy-1-nitro-scyllo-inositol (8) in a similar ratio. Slow, thermodynamically controlled epimerization led from each individual nitro inositol to mixtures of the same composition, with 17–18% of 6, 68–69% of DL-7, and 11–12% of 8. All of the nitroinositol benzyl ethers were isolated crystalline and characterized further as crystalline tetraacetates (6a–8a). The muco isomer 6 gave a di-O-isopropylidene derivative (6b).     

In vitro binding of estrogens by dietary fiber and the in vivo apparent digestibility tested in pigs.

Within the framework of experiments related to the association between dietary fiber and breast cancer an in vitro test system was used to study the binding of estrogens to various fibers (e.g. cholestyramin, lignin and cellulose) and fiber sources (e.g. wheat bran, cereals, seeds and legumes). Furthermore, the in vivo apparent digestibility of the different fiber sources was tested using a mobile nylon bag technique in intestine-cannulated pigs. Estradiol-17 beta (E2) bound more strongly to the various fibers than did estrone (E1), estriol or estrone-3-glucuronide. At increasing pH (greater than 7) binding of both E1 and E2 to wheat bran decreased significantly. Cholestyramine and lignin bound almost all estrogens present in the medium. Linseed (91%), oats (83%), barley chaff (88%) and wheat bran (82%) are other excellent binders of E2. Corn, rye and white wheat flour showed lower binding capacity with a relatively low affinity. Cereals with the highest percentage of lignin in the fiber (greater than 3%) were also the fiber sources with the lowest apparent digestibility. Estrogens bound with the highest affinity (relative to bovine serum albumin) to these fiber sources. Together with wheat bran and lignin, oats, linseed and soybean seem to be products with good perspectives for in vivo evaluation of the lowering effect of dietary fiber on estrogen exposure of estrogen-sensitive tissues.     

Exploring the cellular network of metabolic flexibility in the adipose tissue

Background

Metabolic flexibility is the ability of cells to change substrates for energy production based on the nutrient availability and energy requirement. It has been shown that metabolic flexibility is impaired in obesity and chronic diseases such as type 2 diabetes mellitus, cardiovascular diseases, and metabolic syndrome, although, whether it is a cause or an effect of these conditions remains to be elucidated.

Main body

In this paper, we have reviewed the literature on metabolic flexibility and curated pathways and processes resulting in a network resource to investigate the interplay between these processes in the subcutaneous adipose tissue. The adipose tissue has been shown to be responsible, not only for energy storage but also for maintaining energy homeostasis through oxidation of glucose and fatty acids. We highlight the role of pyruvate dehydrogenase complex–pyruvate dehydrogenase kinase (PDC-PDK) interaction as a regulatory switch which is primarily responsible for changing substrates in energy metabolism from glucose to fatty acids and back. Baseline gene expression of the subcutaneous adipose tissue, along with a publicly available obesity data set, are visualised on the cellular network of metabolic flexibility to highlight the genes that are expressed and which are differentially affected in obesity.

Conclusion

We have constructed an abstracted network covering glucose and fatty acid oxidation, as well as the PDC-PDK regulatory switch. In addition, we have shown how the network can be used for data visualisation and as a resource for follow-up studies.

     

The Relative Importance of Habitat Structure and of Prey Characteristics for the Foraging Success of Water Pipits (Anthus spinoletta)*

While many studies on foraging have related energy gain to the density and the size of prey, only few have investigated whether and how habitat structure modifies the gain through affecting foraging success. In this study, the influences of habitat structure and prey characteristics on the foraging success of water pipits, Anthus spinoletta, were investigated experimentally. The birds take longer to find prey in tall than in short vegetation. The effects of vegetation on searching times differ between prey types. These differences are probably caused by variation in prey behaviour and in cryptic colouration, but not by prey size. Searching times increase with decreasing density for mealworms and tipulids, but not for caterpillars. Handling large prey items requires more time than handling smaller prey. Tipulids and caterpillars, which were offered alive, are handled for a longer time than dead mealworms of corresponding size. The success of attacks on flying insects is probably influenced by the prey's flight speed: fast houseflies are missed more often than slow tipulids. Overall, the results show that the time costs of foraging water pipits are influenced to a comparable degree by vegetation structure, by prey density and by other specific prey characteristics such as camouflage, hiding behaviour or agility. The amount of food gathered per unit time is determined primarily by factors that affect searching times, and less by handling and travelling times. Insertion of our data into an optimal diet model leads to the prediction that water pipits should be generalist foragers, which agrees with the observed behaviour.     

Fraud worries insurance companies but should concern physicians too,industry says

The amount of insurance fraud is increasing in Canada. This should worry physicians, because all personal-injury claims must be substantiated by a medical certificate. The vast majority of physicians are honest and ethical, fraud investigators say, but some are being duped as patients scheme to cheat the insurance industry. In one sensational auto-insurance-fraud case, some Ontario physicians are being investigated about possible involvement in a self-referral scheme. Nicole Baer looks at insurance fraud and the challenges it poses for doctors.     

Disability payments continue to climb: "Tell us what you see,not what you think," CPP tells MDs

Growing concern about the sustainability of the Canada Pension Plan has led to a closer look at the disability benefits it provides. The federal auditor general reported recently that the number of recipients has almost doubled in the past 10 years, and disability payments have more than tripled, to $3 billion annually. This article looks at the role physicians play in determining whether an applicant is disabled.     

Reproduction of the owl monkey (Aotus spp.) in captivity

Abstract: The reproduction performance of captive owl monkeys, a breed used extensively in biomedical research, was observed at the Battelle Primate Facility (BPF). The colony grew through captive breeding, imports from the Peruvian Primatological Project, and others to a peak size of 730. It included seven karyotypes of Aotus sp. Results showed that owl monkeys can breed successfully in a laboratory in numbers sufficient to sustain modest research programs. Reproductive success increases when pairs are compatible, of the same karyotype, and stabilized; however, mated pairs of different karyotype are also productive. Under conditions of controlled lighting and heating, owl monkeys at BPF showed no birth peak nor birth season.