Synthesis and evaluation of the antidepressant activity of the enantiomers of bupropion

The synthesis of the enantiomers of bupropion, (rac)-2-tert-butylamino-3′-chloropropiophenone 1 (Wellbutrin®) is described. The enantiomers were compared with the racemate in both the tetrabenazine-induced sedation model and the inhibition of uptake of biogenic amine assay. No significant differences were found in their potencies to reverse tetrabenazine-induced sedation in mice or in their IC₅₀ values as inhibitors of biogenic amine uptake into nerve endings obtained from mouse brain. © 1993 Wiley-Liss, Inc.     

The speckled wood butterflies Pararge xiphia and P. aegeria (Satyridae) on Madeira: distribution, territorial behaviour and possible competition

Madeira is home to two species of speckled wood butterfly. Pararge xiphia is endemic and is common at mid to high altitudes, within and around the edges of the indigenous laurel forest. In 1976 P. aegeria colonized the island and anecdotal reports suggest that it may have been responsible for the loss of P. xiphia from some of its former haunts. The aims of this paper were (1) to provide comprehensive data on the distribution, habitat preferences and recent changes of range of the two species and (2) to examine territorial behaviour to see if inter-specific competition is taking place. Census results show that there are basic differences between the species in altitudinal range and habitat, but they are found together at high densities at habitat boundaries. Repetition of some of the census routes after a 4-year gap suggests that P. aegeria is expanding its range into the areas dominated by P. xiphia. Behavioural data demonstrate that the males may be competing by causing each other to expend more energy in defence of territories. Although competition may be present, it is not yet possible to establish which species is more affected and how competition may have contributed to the recent changes in the species' ranges.     

EFFECTS OF HELPER PROTEINS ENCODED BY p19 AND orf1-orf2 GENES ON Cyt1Aa PROTEIN EXPRESSION IN ACRYSTALLIFEROUS STRAIN OF BACILLUS THURINGIENSIS

A series of plasmids were constructed to examine the effects of p19 and orf1‐orf2 genes from Bacillus thuringiensis on Cyt1Aa synthesis and inclusion formation. The plasmids expressed the cyt1Aa gene along with either p19 or orf1‐orf2, or each of them coordinatively with p20 in the acrystalliferous strain of B. thuringiensis subsp. israelensis 4Q7. No effect on the expression of Cyt1Aa protein was found when P19 or Orf1‐Orf2 co‐expressed with Cyt1Aa. However, when including p20 gene, the constructs with p19 or orf1‐orf2 gene produced lower yield of Cyt1Aa proteins than without p19 or orf1‐orf2 gene. Electron microscopy observation and bioassay showed that P19 and Orf1‐Orf2 have no influence on the crystal size and toxicity of Cyt1Aa protein. It is presumed that P19 and Orf1‐Orf2 might have negative effects on Cyt1Aa synthesis in B. thuringiensis.     

Property rights and the marginal wildebeest: an economic analysis of wildlife conservation options in Kenya

This paper discusses policy responses to the potential loss of biodiversity in the Mara Area of Kenya from the conversion of essentially wild and undeveloped rangeland to developed agriculture. Property rights are central to the debate, and raise two fundamental issues. First, to what extent do the Maasai, the traditional users and owners of the land, have the right to benefit from the development potential of their land to further their economic, social and political standing, even if by so doing they create domestic and global externalities through the loss of biodiversity. Second, if the state alienates their development rights in the name of conservation, then to what extent should the state compensate the Maasai for their lost economic opportunities. To the Maasai, conservation as implemented through Government policy is a publicc bad: they are denied access to resources, their costs of production are significantly increased, and development is slowed down or actively discouraged. A cost:benefit analysis suggests that it is neither supportable nor sustainable to condemn the Maasai to a poverty trap on behalf of conservation, and that it is instead socially prolitable for the Kenyan Government to meet in full their opportunity costs of forgone economic benefits.     

Transpiration and drought resistance of Douglas-fir seedlings exposed to excess ammonium

 In a pot trial growth and transpiration of 3-year-old Douglas-fir seedlings on an acid, sandy soil was examined at a deficient (30 kg N ha^{–  1} year^{–  1}) and an excessive level (120 kg N ha^{–  1} year^{–  1}) of NH₄ application. Dissolved ammonium sulphate was applied to the pots weekly for two growing seasons. In half of the pots a complete set of other nutrients was applied in optimal proportions to the applied nitrogen. Water supply was optimal and transpiration was recorded. At the end of the second treatment season irrigation was stopped for 2 weeks during dry and sunny weather. Both high application of NH₄ and additional nutrients increased shoot growth and transpiration demand in the first treatment year. The root system was smaller at higher N level and this reduced water uptake accordingly. In the second year the combination of high NH₄ ⁺ and additional nutrients affected root functioning predominantly due to salinity effects and this seriously decreased water uptake capacity and shoot water potentials, finally resulting in tree death. Without addition of other nutrients the high NH₄ ⁺ application resulted in a high degree of soil acidification, which damaged the roots, that showed a decrease in water uptake capacity. At the low NH₄ supply level soil acidification was lower, and root functioning was not affected, and the trees recovered quickly from the imposed drought. Higher needle K and P status depressed transpiration rates at the low NH₄ application rate. Received: 9 January 1995 / Accepted: 18 September 1995     

History of sedentary farming in Ångermanland, northern Sweden, during the Iron Age and Medieval period based on pollen analytical investigations

Compared with most parts of Europe, northern Sweden is essentially a sparsely populated wilderness. There is, however, an ever increasing body of archaeological and palaeoecological information that shows that the region has a long cultural history. In this paper, results of pollen analytical investigations from four lakes with varved lake sediments, in the province of Ångermanland, are presented. These investigations have yielded evidence of continuous and sedentary agriculture from the 6th century in the region close to the Bothnian coast and near the mouth of the large river Ångermanälven. This early agriculture appears to have been based on animal husbandry and cereal, mainly barley, cultivation. During a second farming expansion phase at ca. A.D. 1200, rye cultivation became more important. The increased farming activity during this period was most pronounced at the coast and in the river valley, but more peripheral regions away from the river valley were also exploited. During the period A.D. 1600–1800, arable farming assumed greater importance. In the first decades of the 20th century, the area under cultivation declined, cereal cultivation mostly ceased and the fields were used for pasture.     

Cloning single-stranded DNA

DNA sequence and expression analyses have greatly benefited from using M13 and pUC derived cloning vectors and their polycloning sites. A chronology of the original concepts and experiments is reviewed.     

Multiple xenobiotic-inducible P450s are involved in alkoxycoumarin and alkoxyresorufin metabolism in higher plants

O-Dealkylation of two series of fluorescent 7-alkoxy-coumarins and 7-alkoxyphenoxazones by plant cytochrome P450s was investigated in Helianthus tuberosus tuber tissues treated with prototype P450 inducers, environmental pollutants or agrochemicals. Methoxy-, ethoxy-, propoxy-and butoxycoumarins and methoxy- and ethoxyresorufins were metabolized by fplant microsomes. Dealkylation of pentoxy- and benzyloxyresorufins was not detected. All dealkylating activities were enhanced by aging plant tissues in the presence of xenobiotics, in some cases up to 20-fold relative to the activities detected in control tissues. Increases in total P450 in the same tissues never exceeded 3-fold. The isozymes induced by prototype P450 inducers clearly differed from those in mammalian liver. That multiple P450s with overlapping substrate specificities were involved in the metabolism of both alkoxycoumarins and alkoxyresorufins was demonstrated by (1) the differential induction of the activities in response to exposure to xenobiotics, (2) the differential inhibition of the activities by clotrimazole, paclobutrazole and tetcyclacis in aminopyrine and benzo(a)pyrene-treated tissues, and(3) the selective inhibition observed with antibodies raised against purified ethoxycoumarin deethylase fractions. Our results suggest that the measurement of the dealkylation of such fluorescent substrates in plants might be useful to monitor environmental pollution.     

Cellular responses to enteropathogenicEscherichia coli infection

EnteropathogenicEscherichia coli (EPEC), first described in the 1940's and 1950's, remain an important cause of severe infantile diarrhoea in many parts of the developing world. EPEC do not produce enterotoxins and are not invasive; instead their virulence depends upon exploitation of host cell signalling pathways and the host cell cytoskeleton both as a means of colonizing mucosal surfaces of the small intestine and causing diarrhoea. Following initial mucosal attachment, EPEC secrete signalling proteins and expresss a surface adhesin, intimin, to produce attaching & effacing lesions in the enterocyte brush border membrane characterised by localised destruction of brush border microvilli, intimate bacterial adhesion and cytoskeletal reorganisation and accretion beneath attached bacteria. The pathophysiology of EPEC diarrhoea is also complex and probably results from a combination of epithelial cell responses including both electrolyte secretion and structural damage.