Assessment of novel inhibitors of Helicoverpa aminopeptidases as anti-insect agents

Helicoverpa species present problems worldwide as pests on a variety of agricultural crops. In Australia, the costs of controlling H. armigera (Hübn.) and H. punctigera (Wall.) are a major burden on the cotton industry, and novel mechanisms are continually sought to combat these pests. Potential new targets for insecticides are the digestive proteases of the insect, including the aminopeptidases (APs). A variety of compounds, designed to be similar in structure to known AP inhibitors, were synthesized and screened for activity in inhibiting H. armigera larval growth and AP activity. The most effective compounds in both assays proved to be hydroxamic acids and methylphosphonic acids. Compounds that incorporated both of these groups were also found to have significant potential as control agents. The most inhibitory compounds included valine methylphosphonic acid and a leucine methylphosphonic acid/hydroxamic acid derivative. The valine methylphosphonic acid compound was tested further in vitro, with the aim of producing a new active capable of restricting the viability of Helicoverpa populations on commercial crops.     

Experimental bovine respiratory syncytial virus infection in conventional calves: ultrastructural respiratory lesions

The morphogenesis and repair of airway and alveolar injury induced by bovine respiratory syncytial virus (BRSV) was studied ultrastructurally in conventional calves to characterize pulmonary cell types susceptible to viral infection and cytopathologic changes associated with infection. Viral nucleocapsids and budding virions were present in tracheal and bronchial ciliated and nonciliated epithelial cells and mucous cells 3, 5, and 7 days after inoculation and in bronchiolar ciliated and nonciliated epithelial cells 5 days after inoculation. Mild interstitial pneumonia was observed 5 days after inoculation and was characterized by swelling of type 1 and type 2 alveolar epithelial cells, interstitial edema, and infiltration by lymphocytes and macrophages. Viral assembly and release in tracheal and bronchial epithelial cells was associated with loss of cilia from ciliated cells, formation of syncytial epithelial cells, swelling of mitochondria and endoplasmic reticulum, and cell necrosis. Neutrophils, lymphocytes, and macrophages were present in close association with the viral-infected and damaged epithelial cells. There was intercurrent hyperplasia of basal epithelial cells that, in association with other epithelial lesions, resulted in the loss of normal ciliated epithelium in these airways 5 and 7 days after inoculation. Regeneration of airway epithelium was largely completed by 10 days after inoculation, except in 1 of 4 calves that had failure of epithelial repair and that developed secondary bacterial pneumonia. Pulmonary ultrastructure in BRSV-inoculated calves 30 days after inoculation was indistinguishable from that in controls. The results demonstrated that BRSV can induce reversible alterations in airway epithelium, which may cause depression of mucociliary clearance and thereby enhance susceptibility to bacterial infection.     

Mycotic keratitis in a dog: concurrent Aspergillus sp and Curvularia sp infections

A dog with exposure keratopathy developed secondary bilateral keratitis from which Aspergillus sp and Curvularia sp were identified. Mycotic keratitis, while rare in the dog, should be considered in the differential diagnosis of keratitis.     

Mechanism of action of the 1,2,4-triazolo[1,5-a] pyrimidines

The substituted 1,2,4-triazolo[1,5-a]pyrimidines are a new class of highly active herbicides. Protection of Arabidopsis thaliana seedlings from triazolopyrimidine-induced injury by the branched-chain amino acids was observed. Acetolactate synthase (EC 4.1.3.18) was isolated and found to be quite sensitive to inhibition. I₅₀ values for inhibition of the enzyme from a number of plant sources show little variation and no correlation to whole-plant response, suggesting uptake, translocation and metabolism play key roles in modulating herbicidal activity. Further studies indicate that these chemicals are slow, tight-binding inhibitors that are readily dissociated by gel filtration. Some correlations between in-vitro activity and in-vivo activity were observed for ortho-substituted analogs on selected broadleaf species.     

The potential of entomopathogenic fungi to control the lettuce root aphid,<Emphasis Type="Italic">pemphigus bursarius</Emphasis>

The lettuce root aphid,Pemphigus bursarius, is a commercially important pest of lettuce and occupies a niche amenable to the action of entomopathogenic fungi. As the first stage of a biological control programme, a bioassay was developed against adult apterousP. bursarius. An isolate ofMetarhizium flavoviride was pathogenic toP. bursarius and sporulated abundantly upon aphid cadavers. However, two isolates ofVerticillium lecanii, pathogenic against glasshouse whitefly and aphids, were only weakly pathogenic toP. bursarius.