Areawide mating disruption treatments have been effective in controlling infestation of oriental fruit moth, Grapholita molesta (Busck) (Lepidoptera: Tortricidae), in Australian pome and stone fruit ...orchards. Although successful, the areawide mating disruption program has been an expensive approach by using hand-applied Isomate dispensers. Sprayable microencapsulated (MEC) pheromone formulations that can be applied with standard spray equipment could substantially reduce the cost of application. Field trials conducted during two consecutive seasons (2002–2004) demonstrated that monthly applications of MEC-OFM phase V (3M Canada, London, Ontario, Canada) at a rate of 125 ml/ha (37.1 g AI/ha) in replicated 2-ha blocks of both peaches and pears reduced oriental fruit moth shoot tip and fruit damage as effectively as a single application of Isomate OFM Rosso hand-applied dispensers (500 dispensers per ha) and as or more effectively than standard broad-spectrum insecticide sprays. Fruit protection was achieved despite high oriental fruit moth population densities in both crops as measured by moth catches in terpinyl acetate food and pheromone traps. Similar numbers of oriental fruit moths were captured among all treatments in food traps but captures of males in pheromone traps were disrupted (96–99%) in pheromone-treated blocks relative to controls. The results of this study suggest that microencapsulated formulations of pheromone could be effectively used in areawide mating disruption programs for oriental fruit moth in Australia as a cost-saving alternative to reservoir-style dispensers requiring labor-intensive hand application.
Five formulations of controlled release, polyethylene tube dispensers of pheromone were evaluated during three field seasons for disruption of codling moth, Cydia pomonella (L.) (Lepidoptera: ...Tortricidae), and the oriental fruit moth, Grapholita molesta (Busck) (Lepidoptera: Tortricidae). Evaluations were conducted in replicated 4-ha plots of commercial apple in Michigan. Disruption of both C. pomonella and G. molesta male orientation to pheromone traps in plots treated with a dual-species formulation (Isomate CM/OFM TT), simultaneously releasing the pheromone components of both C. pomonella and G. molesta, was equivalent to that obtained by treating plots with separate formulations for each species (Isomate C Plus or Isomate C TT for C. pomonella and Isomate M Rosso for G. molesta) through mid-season. However, disruption efficacy of the dual-species formulation was significantly lower near the end of the season for G. molesta compared with the Isomate M Rosso formulation because of depletion of active ingredients and coincided with a slight increase in fruit injury. Effective disruption of C. pomonella and G. molesta also was obtained with a multispecies formulation (Isomate CM/OFM/LR) that releases the main pheromone components of C. pomonella, G. molesta, and several leafroller species. Each formulation type releasing (E,E)-8,10-dodecadien-1-ol (codlemone) also was found to release the E,Z- and Z,E-isomers of codlemone. Our data provide further evidence that simultaneous disruption of C. pomonella and G. molesta with dispensers releasing both species'pheromone components is possible; however, the controlled release formulations tested here require modification or postponed deployment coupled with early season control by other means to achieve season-long efficacy. Simultaneous disruption of several species with a single formulation will be economically advantageous in regions where control of multiple pests is needed given the need for hand application of this technology.
The performance of polyvinyl chloride polymer (PVC) dispensers loaded with two rates of ethyl (E,Z)‐2,4‐decadienoate (pear ester) plus the sex pheromone, (E,E)‐8,10‐dodecadien‐1‐ol (codlemone) of ...codling moth, Cydia pomonella (L.), was compared with similar dispensers and two commercial dispensers (Isomate® and CheckMate®) loaded only with codlemone. Dispenser evaluations were conducted in replicated small (0.1 ha) and large (2 ha) field trials in apple, Malus domestica (Borkhausen), during 2006 (Washington) and 2007 (Michigan, large plot study only). Data recorded included male captures in traps baited with virgin female moths and codlemone lures and direct observations of moth behaviour in treated plots. Volatile air collections of field‐aged dispensers were conducted under laboratory conditions. Disruption of male catch in codlemone‐baited traps was generally similar among dispenser treatments, except for two instances: lower moth catches with the single and dual‐component PVC dispensers, compared with Isomate®, during the first flight in the large plots in Michigan in 2007 and for the dual‐component PVC dispenser compared with the CheckMate® dispenser during the second flight in small plots in Washington in 2006. Levels of fruit injury were similar in large plots treated with all dispensers. Male moth catches in virgin female‐baited traps did not differ among dispenser treatments and were significantly lower than the untreated control. Behavioural observations of adult moths in the field verified anemotactic approaches within 20 cm of pheromone dispensers loaded with and without pear ester that lasted ca. 15 s on average. Field‐aged dual‐component dispensers released pear ester at a >5‐fold higher rate than codlemone over the first 8 weeks and this ratio declined to near unity by 18 weeks.
Electroantennogram (EAG) and behavioral responses of female oriental fruit moth, Grapholita molesta (Busck) (Lepidoptera: Tortricidae), were studied using the synthetic major component, ...(Z)-8-dodecenyl acetate, and partial three-component blend, (Z)-8-dodecenyl-acetate:(E)-8-dodecenyl-acetate:(Z)-8-dodecenol (in a 93:6:1 ratio), of the sex pheromone. EAGs elicited by both the single and three-component pheromone were significantly greater compared with hexane solvent controls. In 1-liter plastic chambers with constant throughput of air (50 ml/min) over rubber septa loaded with 0.01 or 0.1 mg of the three-component pheromone blend, onset of female calling was advanced by ≈2 h compared with solvent controls. However, the total number of females calling at peak time and the time of calling termination did not differ between pheromone-exposed and control moths. Oviposition rates of pheromone-exposed and clean air-exposed mated female moths did not differ in similar 1-liter flow-through chambers lined with wax paper over 24-h intervals. In a separate experiment, male and female oriental fruit moth, caged in perforated 1-liter containers allowing air ventilation, were placed for 1-wk intervals in replicated glasshouses that were either treated with Isomate dispensers hung 0.5 m from chambers or left untreated. Oviposition rates between Isomate dispenser-exposed and control moths were similar. Female sensitivity to sex pheromone, termed “autodetection,” has been observed previously and is thought to function either as a mechanism to 1) advance female calling periodicity under high population densities to increase the probability of attracting males, 2) induce dispersal under high population densities to reduce competition for males or food resources, or 3) aggregate females to increase local probability of mating success. Autodetection also may affect the efficacy of mating disruption for oriental fruit moth depending on whether pheromone exposure affects the diel periodicity of male sexual response.
Single nucleotide polymorphisms (SNPs) at chromosome 17q21 confer an increased risk of early-onset asthma. The objective was to study whether 17q21 SNPs modify associations between early respiratory ...infections and asthma. Association analysis was conducted in 499 children (268 with asthma, median age 11 yrs) from the Epidemiological Study on the Genetics and Environment of Asthma (EGEA). The 12-yr follow-up data were used to assess persistent or remittent asthma in young adulthood. Respiratory infection before 2 yrs of age was assessed retrospectively. For the 12 17q21 SNPs studied, the odds ratios (OR) for association between infection and early-onset asthma (age at onset <or=4 yrs) were higher in carriers of risk genotypes (OR 3.42-6.36) than in noncarriers (OR 1.84-2.44; p-value for interaction 0.02-0.04 for five SNPs). Risk genotypes also increased the association between infection and childhood asthma that remits in adulthood (OR 4.84-7.16 in carriers and 1.74-2.25 in noncarriers; p-value for interaction 0.008-0.05 for 10 SNPs). In children with 17q21 risk genotypes and early-life environmental tobacco smoke (ETS) exposure, associations between infection and asthma were further enhanced. 17q21 genetic variants and early ETS exposure enhance the association between early respiratory infections and early-onset asthma and childhood asthma that remits in adulthood.
To address challenges in the preparation of a key building block containing a difluorocyclopropane moiety, we have developed a new protocol for difluorocarbene generation that relies on a ...Krapcho-type dealkylation of ethyl bromodifluoroacetate (EBDFA), an inexpensive and readily available fluorinated feedstock. Application of DoE and kinetic modeling was used to understand key reaction parameters and identify an optimal process. We report two variants of this procedure that offer different processing advantages and that have both been scaled successfully multiple times to deliver hundreds of kilograms of the resulting difluorocyclopropane. To access a single enantiomer of the target compound, we have also developed a classical resolution strategy and recycling protocol for the undesired enantiomer to replace previous chromatographic methods for separation.
Malaria continues to be a major cause of morbidity and mortality to this day, and resistance to drugs like chloroquine has led to an urgent need to discover novel chemical entities aimed at new ...targets. Here, we report the discovery of a novel class of potential antimalarial compounds containing an indolizinoindolone scaffold. These novel enantiopure indolizinoindolones were synthesized, in good‐to‐excellent yields and excellent diastereoselectivities, by cyclocondensation reaction of (S)‐ or (R)‐tryptophanol and 2‐acyl benzoic acids, followed by intramolecular α‐amidoalkylation. Interestingly, we were able to synthesize for the first time 7,13b‐cis indolizinoindolones in a two‐step route. The novel compounds showed promising activity against erythrocytic stages of the human malaria parasite, Plasmodium falciparum, and liver stages of the rodent parasite Plasmodium berghei. In particular, an (S)‐tryptophanol‐derived isoindolinone was identified as a promising starting scaffold to search for novel antimalarials, combining excellent activity against both stages of the parasite′s life cycle with low cytotoxicity and excellent metabolic and chemical stability in vitro.
All about antimalarials: A novel class of potential antimalarial compounds containing an indolizinoindolone scaffold showed promising activity against erythrocytic stages of the human malaria parasite, Plasmodium falciparum, and liver stages of the rodent parasite Plasmodium berghei. The most promising compound exhibited IC50 values of 1.2 and 0.6 μm for the erythrocytic and liver stages, respectively, with excellent metabolic and chemical stability.
Codling moth (CM) and oriental fruit moth (OFM) are very important orchard pests worldwide, and particularly in Victoria, Australia, where both species damage pome fruit. Individually CM and OFM have ...been controlled successfully by pheromone-mediated mating disruption, but treatment of pome fruit with full registered rates of two individual hand-applied dispensers for CM and OFM could be uneconomical for growers. Field trials conducted over three seasons in plots sprayed with insecticides consistently demonstrated that dual Isomate C/OFM TT dispensers, designed to disrupt both CM and OFM, were as effective as Isomate CTT and Isomate OFM Rosso dispensers applied individually in pears for control of CM and OFM respectively. The dual- and individual-species dispensers reduced moth catches and fruit damage to a similar degree. The results suggest that combined control of CM and OFM in pears by applying dual Isomate C/OFM TT dispensers at the full-recommended rate of 500 dispensers per hectare will be more economical than use of individual species dispensers, because the price and application cost of dual dispenser is about half that for individual dispensers.
We describe a series of improvements to the synthesis of a 3,8-diazabicyclo3.2.1octane derivative that result in a reduced step count and higher overall efficiency compared to previously published ...syntheses. Our method includes optimization and mechanistic understanding of a key diastereoselective cyclization to achieve a >95:5 diastereomeric ratio, as well as demonstration of a unique enzyme-catalyzed amidation reaction using hexamethyldisilazane as both an ammonia source and scavenger. Finally, we identify a novel cocrystal solid form of the target compound that provides improved purity and material properties. Demonstration of the new chemistry to prepare >100 kg of the target compound serves to illustrate the robustness of the new process.
Objectives
To assess if baseline iron deficiency, with or without anemia, is associated with incident infections over 3 years among community-dwelling older adults.
Design
Prospective secondary ...analysis of DO-HEALTH, a 3-year randomized, double-blind controlled trial.
Setting And Participants
2157 community-dwelling adults age 70+ from 5 European countries with good cognitive function and mobility and no major health events in the 5 years prior to enrollment Measurements: Incident infections, their severity and type were recorded every 3 months throughout the 3-year follow-up. Iron deficiency was defined as soluble transferrin receptor (sTfR) levels > 28.1 nmol/l and anemia as hemoglobin levels < 120 g/l for women and 130 g/l for men. We applied negative binomial mixed effects regression models with random effects for countries, and controlling for treatment allocation, age, sex, body mass index, polypharmacy, number of comorbidities, smoking status, living situation, alcohol intake, frailty status, and physical activity levels. A pre-defined stratified analysis was performed to explore if the associations between iron deficiency and infections were consistent by baseline anemia status.
Results
In total, 2141 participants were included in the analyses (mean age 74.9 years, 61.5% of women, 26.8% with iron deficiency). Across all participants, baseline iron deficiency was not associated with incident overall infections, but was associated with a 63% greater rate of incident severe infections requiring hospitalization (incidence rate ratio IRR 1.63, 95% Confidence Interval CI 1.11–2.41, p=0.01). This association was more pronounced among the 2000 participants who did not have anemia at baseline (IRR=1.80, 95% CI 1.20–2.69, p=0.005).
Conclusion
Based on this prospective study among generally healthy European community-dwelling older adults, iron deficiency was not associated with the incidence rate of overall infections but may increase the incidence of severe infections. Intervention studies are needed to prove the causality of this observation.
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