Eel acetylcholinesterase inhibition studies with heteroarylphosphinates

The inhibition of eel acetylcholinesterase by the 4-nitrophenyl esters of 2-furyl(methyl)-, methyl(2-thienyl)-, di-2-furyl-, and di-2-thienylphosphinic acid (I, II, III, and IV, respectively) was investigated at pH 6.90 in 0.067 M phosphate buffer (25.0°C) using stopped-flow instrumentation and automated data processing. Our evaluation of the dissociation constant, K_d, the unimolecular bonding rate constant, k₂, and the bimolecular reaction constant, k_i, are the first reported values for these constants for alkyl/heteroaryl and diheteroaryl esters of phosphinic acids. The largest k_i value (19,330 M^?1 sec^?1) was observed for the reaction of I with the enzyme. The order for the remaining three is II > IV > III. There is no direct relationship between the hydrolysis rates of the esters and their anticholinesterase activities on eel acetylcholinesterase. Likewise, there is no direct relationship between their anticholinesterase activities and the LD₅₀ values in rats.     

Host plant stimulation of detoxifying enzymes in a phytophagous insect

The midgut microsomal aldrin epoxidase of variegated cutworm larvae (Peridroma saucia, Hübner) fed bean or peppermint leaves was up to 10 and 45 times more active, respectively, than that of larvae fed a basic control diet. Large increases in oxidase activity and cytochrome P-450 levels also occurred in larvae fed mint plant constituents such as menthol menthone, α-pinene, and β-pinene. Mint-fed larvae were more tolerant of the insecticide, carbaryl, than bean-fed larvae.     

Phenobarbital induction of detoxifying enzymes in resistant and susceptible houseflies

Houseflies, Musca domestica, L., were treated with the drugs phenobarbital and 3-methylcholanthrene to study the effects of these compounds as inducing agents of the microsomal oxidases, heptachlor epoxidase, and p-nitroanisole O-demethylase, and of DDT-dehydrochlorinase. Phenobarbital was active when applied by injection or as part of the diet but inactive when topically applied. The resulting increases in heptachlor epoxidase activity were as much as 25-fold that of the untreated controls. The net increase in enzyme activity after phenobarbital treatment was greater in an insecticide-susceptible strain, WHO-SRS strain, than in a carbamate-resistant strain. However, the phenobarbital induced increases in DDT-dehydrochlorinase were greater, about 2-fold, in the resistant strains than in the susceptible strain.The optimum dose for phenobarbital was 1% in the diet for a period of 3 days. None of the treatments with 3-MC, feeding, injection, exposure to residues, or topical, were effective in induction.     

Dose-titration studies of ivermectin against experimental Ancylostoma caninum and Uncinaria stenocephala infections

Dose-titration trials of ivermectin were conducted on pups with dual experimental infections of 4th-stage larvae or adult Ancylostoma caninum and Uncinaria stenocephala. Ivermectin was administered orally or subcutaneously at dosages of 0.006, 0.012, or 0.024 mg/kg of body weight. Maximal or near maximal (greater than or equal to 96% to 100%) anthelmintic effect was observed for both stages of development for each hookworm species by either route of administration at a dosage of 0.024 mg/kg. Responses for all of the aforementioned categories were linearly related to increasing log dosage of ivermectin, with common slopes (regression coefficients). Regression analysis also provided estimates of the minimal dosages required to produce maximal reduction in worm burden for each stage, species, and route of administration. The estimated ivermectin dosages for maximal efficacy ranged from a low of 0.014 mg/kg for adult A caninum by oral treatment to 0.044 mg/kg for 4th-stage larvae of U stenocephala by oral treatment.     

Persistence and colonization of gaps in sown swards of grass and clover under different sward managements

The effects of extensive sward management and patch size on the persistence and colonization of gaps in sown swards was examined by creating gaps of five different sizes (2·3, 7, 10, 14 and 19 cm in diameter) in four different sward treatments: a fertilized sward grazed to 4 cm, i.e. relatively intensive management, and three extensively managed unfertilized swards, which were not grazed or grazed to 4 cm or 8 cm. The swards were originally sown with ryegrass (Lolium perenne L.) and white clover (Trifolium repens L.), but had developed differences in species composition as a result of the management treatments imposed 2 years before and during the experiment. Light quality measurements, i.e. red-far red (R/FR) ratio, were used to determine when the light environment in the gaps no longer differed from that in control, uncut patches and this was used as an estimate of gap persistence. Persistence of gaps depended on both sward management and gap size. Gaps disappeared most rapidly in the ungrazed sward and fertilized 4-cm sward, and most slowly in the unfertilized 8-cm sward. Small gaps persisted for up to 2 weeks in all but 8-cm swards, whereas larger gaps were estimated to persist for up to 20–25 weeks in unfertilized, grazed swards. There was no evidence that the number of grass or dicotyledonous species increased in the gaps compared with the control areas. There were significant positive linear relationships between the vegetation that developed in gaps and that in the control, uncut patches, reflecting the different species composition of the established sward of the grazed (grass-dominant) and ungrazed (Ranunculus repens-dominant) treatments. For total grass dry matter and tiller numbers, as well as L. perenne tiller numbers, there was a small, but significant, effect of both patch size and sward management on the slopes of the regressions between the controls and gaps. The results are discussed in relation to the potential for species composition of sown swards to change as a result of gap creation.     

Genetic improvement of the Pacific oyster Crassostrea gigas (Thunberg) in Australia

The Pacific oyster industry in Australia is derived from importations from Japan in the late 1940s and early 1950s to Tasmania and is almost completely hatchery based. This makes it a good target for developing and deploying genetically improved strains. An allozyme survey comparing hatchery stocks with self‐recruiting Tasmanian stocks and with two collections from Japan found abundant variation and no significant evidence of allele loss. The subsequent selection programme (initiated in the summer of 1996/97) had several strands. We wanted to take advantage of the increased power that marker‐assisted selection could bring and, therefore, needed to develop a linkage map and isolate flanking markers around quantitative trait loci (QTLs). Several types of markers (allozymes, microsatellites and AFLPs) were used, and single‐pair crosses were set up; QTLs have been detected. Conventional selection programmes, one based on mass selection and one on family selection, have been established. Triploid Pacific oysters produced via chemical means have been available for several years, but rates of triploidy achieved by such means are usually less than 100%. In 1999, we will assess whether our tetraploid 2‐year‐old broodstock can be crossed with diploids to give 100% triploid offspring.     

A comparative study on Striga hermonthica interaction with a sensitive and a tolerant sorghum cultivar

In this study, the effects of Striga hermonthica (Del.) Benth. on a sensitive and a tolerant sorghum genotype were investigated, and the underlying tolerance mechanisms were distinguished. The sensitive sorghum cv. CK60-B and the tolerant sorghum landrace Tiemarifing were grown in pots with and without seed infestation. Both sorghum genotypes responded to infection by the parasite, but it was evident that CK60-B was more strongly affected than Tiemarifing. Sorghum plant height, final leaf number, green leaf area, kernel yield, number of kernels and 1000-kernel weight were significantly reduced by infection, which also had a marked effect on the phenological development of CK60-B; the majority of the plants remained vegetative and, in the remaining plants, flowering was delayed by about 2 weeks. No effect on the phenological development of Tiemarifing was observed. The tolerant landrace showed significantly lower and delayed emergence of S. hermonthica than the sensitive cultivar, and this could be explained by a delay in the onset of attachment. Significantly higher numbers of reproductive parasitic plants were found in the pots with the sensitive sorghum plants. It is concluded that differences in root architecture and the resulting early infection and higher S. hermonthica numbers are partly responsible for the stronger effects of the parasite on the sensitive cultivar.