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Chemistry and biology of thiamethoxam: a second generation neonicotinoid.

Thiamethoxam is the first commercial neonicotinoid insecticide from the thianicotinyl subclass. It was discovered in the course of our optimisation program on neonicotinoids started in 1985. Novel variations of the nitroimino-heterocycle of imidacloprid led to 4-nitroimino-1,3,5-oxadiazinanes exhibiting high insecticidal activity. Among these, thiamethoxam (CGA 293433) was identified as the best compound and selected for worldwide development. The compound can be synthesised in only a few steps and high yield from easily accessible starting materials. Thiamethoxam acts by binding to nicotinic acetylcholine receptors. It exhibits exceptional systemic characteristics and provides excellent control of a broad range of commercially important pests, such as aphids, jassids, whiteflies, thrips, rice hoppers, Colorado potato beetle, flea beetles and wireworms, as well as some lepidopteran species. In addition, a strong preventative effect on some virus transmissions has been demonstrated. Thiamethoxam is developed both for foliar/soil applications and as a seed treatment for use in most agricultural crops all over the world. Low use rates, flexible application methods, excellent efficacy, long-lasting residual activity and favourable safety profile make this new insecticide well-suited for modern integrated pest management programmes in many cropping systems.

Animals↗

Persistence and performance of esfenvalerate residues on broccoli.

The efficacy of esfenvalerate (84 g litre-1 EC; Asana XL) at 7.0 g AI ha-1 on broccoli was tested against the flea beetle, Phyllotreta cruciferae Goeze (Chrysomelidae: Coleoptera) and the imported cabbage worm, Pieris rapae L (Pieridae: Lepidoptera) under field conditions. Insect populations were monitored before and after treatment. Periodic sweep-net collections and examination of the leaves in treated and untreated broccoli plots revealed mean reductions of P cruciferae levels of nearly 98% 1 week post-application compared with untreated plots. The residual toxicity of esfenvalerate was also effective for 2 weeks in reducing population density of P rapae by 69% on broccoli leaves. The impact of esfenvalerate on feeding damage to broccoli leaves was established by counting the number of feeding holes made by P cruciferae on spring broccoli and P rapae on fall broccoli. As the leaf area ingested increased, a linear relationship was seen between the number of holes and number of insects. Results indicated that forage destruction by the two pests was significantly reduced by esfenvalerate application. Esfenvalerate was extracted from broccoli at 1 h and 1, 3, 7, 10, and 14 days post-application for residue analysis. Residues on spring broccoli were 12.2, 5.2 and 2.9 micrograms cm-2 on the leaves and 0.13, 0.05 and 0.02 microgram g-1 on the heads at 1 h, 1 and 3 days, respectively. Only trace levels (0.001 microgram g-1) were detected in/on the heads 14 days after spraying. On the basis of half-life (T1/2) values, persistence of esfenvalerate on spring broccoli leaves (T1/2 = 1 day) was shorter than on fall broccoli (T1/2 = 1.6 days). T1/2 values were 2.1 and 3.6 days on spring and fall broccoli heads, respectively. The implications of these residue levels on re-entry times into treated fields are discussed.

Animals↗

Synthetic examination of incorrectly proposed structures of biomolecules.

Many incorrect structures of biomolecules have been proposed for natural products. Synthesis of compounds having the proposed structures often enabled us to judge the correctness of the proposals. In some cases, we were able to revise the structures by synthesizing the biomolecules themselves. In other cases, we were able to definitely disprove the proposed structures. Some examples treated in this review include: auxin-a and b; the sex pheromone of Chlamydomonas; sex pheromones of the gypsy moth, the American cockroach, and the pink bollworm moth; Persoons' periplanone-A; orobanchol; naurol A; bifurcarenone; koninginin A; alpha-acoradiene; himachalene-type pheromones of the flea beetle; differolide; blattellastanoside A and B; etc.

Animals↗

Green plants in starling nests: effects on nestlings.

European starlings, Sturnus vulgaris, intermingle fresh herbs, especially species rich in volatile compounds, with their otherwise dry nest material. In this field study we investigated whether these herbs reduce ectoparasites and thereby protect nestlings (the nest protection hypothesis). We also considered whether volatile compounds in herbs improve the condition of nestlings (the drug hypothesis). As measures of condition we used body mass, haematocrit levels and immunological parameters. We replaced 148 natural starling nests with artificial ones: half contained herbs and half (controls) contained grass. The ectoparasite loads (mites, lice, fleas) in herb and control nests were indistinguishable. However, nestlings in herb nests weighed more and had higher haematocrit levels at fledging than nestlings in control nests. Fledging success was similar in herb and control nests, but more yearlings from herb nests were identified in the colony the year after hatching. The response of the immune system when challenged with phytohaemagglutinin did not differ in nestlings from herb and control nests. Nestlings from herb nests had more basophils and fewer lymphocytes in their blood than those from control nests, while the eosinophil and heterophil counts did not differ. We conclude that herbs do not reduce the number of ectoparasites, but they improve the condition of nestlings, perhaps by stimulating elements of the immune system that help them to cope better with the harmful activities of ectoparasites. Copyright 2000 The Association for the Study of Animal Behaviour.

Journal Article↗

A review of the effects of bromate on aquatic organisms and toxicity of bromate to oyster (Crassostrea gigas) embryos.

A critical literature review has been undertaken of the effects that bromate (BrO3-) has on aquatic organisms. Chronic (multigeneration) studies using four marine phytoplankton species indicate a stimulation of cell division at concentrations up to 13.6 mg BrO3- liter-1, such that the EC50 is > 13.6 mg BrO3- liter-1 (exposure period unspecified). No published data were available for any freshwater algal or phytoplankton species. For freshwater invertebrates, the available data are limited to acute studies using two species: the water flea, Daphnia magna, with a 48-h LC50 of 179 mg BrO3- liter-1; and the planarian ("flatworm"), Polycelis nigra, with a 48-h LC50 of 2258 mg BrO3- liter-1. For saltwater invertebrates, there is a greater variety in the spread of species sensitivity to bromate. For crustaceans, the lowest reported acute value is a 24-h LC50 of 176 mg BrO3- liter-1 for mysid shrimp. For molluscs, the published data are somewhat contradictory, with different workers reporting EC50 values to oyster embryo-larvae of either 0.05-0.1 or 30 mg BrO3- liter-1. Following repeated attempts to resolve these differences using the Pacific oyster (Crassostrea gigas) embryo development assay, a 24-h EC50 of 170 mg BrO3- liter-1 was observed. Reported 96-h LC50 values for juvenile saltwater fish range from 427 to 512 mg BrO3- liter-1, while a 10-day LC50 of 279 mg BrO3- liter-1 is also reported. For fish early lifestages, newly hatched larvae are more sensitive than embryo hatching, with a larval 96-h LC50 of 31 mg BrO3- liter-1 being observed. Less severe effects have been reported for older larvae (pro-larvae), for which a 96-h LC50 of 404 mg BrO3- liter-1 is reported. In conclusion, a number of studies provide evidence for the acute toxicity of bromate to invertebrates and fish in the lowest region of 30 mg BrO3- liter-1. Applying the factor of 10 used to extrapolate from acute to potential chronic toxicity, the available data suggest that to protect aquatic organisms from long-term adverse effects, concentrations should not exceed approximately 3.0 mg BrO3- liter-1.

Animals↗

Screening of organophosphate insecticide pollution in water by using Daphnia magna.

A simple and rapid screening method using Daphnia magna Straus (water fleas) on the basis of their immobilization was developed for detecting pesticide pollution. The laboratory testing of the toxicity of 11 organophosphate insecticides to D. magna determined 50% inhibition concentration of mobility at 48 h of exposure (48-h EC50) of 0.19 to 2.6 microg/L. The mobility of D. magna was inhibited in several river and stream waters sampled from May 1995 to February 1998 in Tokyo. Chemical analysis of the waters revealed that they were polluted by sub-ppb or ppb level of organophosphate insecticides. A significant relationship was observed between the immobilization of D. magna and the pollution level of the river and stream waters. The D. magna test could be used as a low-cost preliminary screening method for insecticide pollution.

Animals↗

A hierarchical molecular phylogeny within the genus Daphnia.

The nucleotide sequences of two mitochondrial DNA regions were used to determine phylogenetic relationships in the genus Daphnia (water fleas), a group for which systematics are historically unstable. A portion of the small ribosomal RNA was used to reconstruct higher-level relationships among species, while a portion of the more rapidly evolving control region was used to reconstruct lower-level relationships among populations. Two unexpected results were obtained. First, the subgeneric status of Ctenodaphnia falls into uncertainty on the basis of the failure of the 12S rRNA sequences to support these species as comprising an outgroup to the remainder of Daphnia species. Second, the high similarity of 12S rRNA sequences of Daphnia pulex and Daphnia pulicaria samples, coupled with the dual paraphyly of these samples as reconstructed from control-region analysis, suggests that they are two clonotype constellations within the same species complex. A combination of a variety of ecological influences has apparently resulted in the evolution of sets of Daphnia genotypes that are genetically cohesive despite their phenotypic divergence.

Alleles↗

Imidacloprid, thiacloprid, and their imine derivatives up-regulate the alpha 4 beta 2 nicotinic acetylcholine receptor in M10 cells.

Neonicotinoids are the most important new class of insecticides of the last decade. They act as nicotinic acetylcholine receptor (AChR) agonists. This investigation tests the hypothesis for the first time that neonicotinoid insecticides and their imine derivatives up-regulate the alpha 4 beta 2 nicotinic AChR subtype, which represents >90% of the high-affinity [(3)H]nicotine binding sites in mammalian brain. The alpha 4 beta 2 receptor stably expressed in mouse fibroblast M10 cells was assayed after 3 days' exposure to the test compound, as [(3)H]nicotine binding following immunoisolation by monoclonal antibody (mAb 299) or as [(125)I]mAb 299 labeling for cell surface receptors. We found that imidacloprid (IMI) (one of the most important insecticides) and thiacloprid (THIA) increased [(3)H]nicotine binding levels (up-regulation of the alpha 4 beta 2 AChRs) by five- to eightfold with EC50s of approximately 70,000 and 19,000 nM, respectively, compared with 760 nM for (-)-nicotine. In contrast, two imine analogs [the desnitro metabolite of IMI (DNIMI) and the descyano derivative of THIA] gave up-regulation by eightfold and EC50s of 870 and 500 nM, respectively. The potency order for up-regulation by the five aforementioned compounds was correlated with their in vitro IC50s for inhibiting [(3)H]nicotine binding (r(2) = 0.99, n = 5), indicating that binding to the alpha 4 beta 2 receptor initiates the up-regulation. A potent olefin derivative of the THIA imine up-regulated with an EC50 of 22 nM. DNIMI-induced up-regulation mainly occurred intracellularly rather than at the cell surface. These findings in alpha 4 beta 2-expressing M10 cells indicate the possibility that some neonicotinoid insecticides or their metabolites, on accidental human exposure or when used for flea control on dogs, may also up-regulate the receptor in mammals.

Animals↗

West Nile virus and other zoonotic viruses in Russia: examples of emerging-reemerging situations.

Studies of the interactions of vertebrates, viruses and arthropod vectors of these viruses were monitored in terms of different ecological groups of viruses transmitted by mosquitoes and ticks in Northern Eurasia in an area encompassing more than 15 million km2. About 90 viruses were isolated, including 24 new to science. Newly recognized infections of vertebrates, including humans, were described. Many unusual epidemic situations were analysed. Permanent efforts were established to prevent bioterrorist activities and their consequences. Extensive epidemic outbreaks of West Nile fever (WNF; i.e., fever caused by West Nile virus) and Crimean-Congo hemorrhagic fever (CCHF) with unusual high mortality appeared in the last four years in southern Russia. We determined infection rates in humans, domestic and wild animals, mosquitoes and ticks from natural and synanthropic biocenoses [Editorial note: "synanthropic" means, roughly, all species living with (c.f. lice, fleas) or near people, such as in houses (c.f. house mice), parks (c.f. Rattus spp.), and the like, rather like "peridomestic", but not strictly so; "biocenosis" is the biome, the "totality of living populations in a particular habitat, which itself is only a part of the ecosystem".]. CCHF virus strains were phylogenetically similar to strains isolated in this area 35 years ago but different from Central-South-Asian and African strains. Before the outset of the current emergence of epidemic WNF, three genetic variants of this virus had been isolated in USSR, two African and one Indian. Phylogenetic analysis of complete genome sequences of epidemic strains demonstrated considerable similarity to strains from USA and Israel and differences from strains isolated in the same USSR areas 20-30 years before. In addition to strains of genotype 1, we isolated strains of second and third lineages and a strain of a fourth genetic variant. Nucleotide differences of these strains from all three genotypes was about 30%. The emerging WNF situation in Russia for the last 4 years probably has been the result of not only natural and social factors, but also to introduction of more virulent strains or by evolution of the virus.

Animals↗

Ectoparasites of guinea fowl (Numida meleagris galeata Pallas) and local domestic chicken (Gallus gallus) in southern Guinea Savanna, Nigeria.

The ectoparasites of poultry in a southern guinea savanna zone were investigated by the examination of guinea fowl and local domestic chickens in the range and guinea fowl under intensive management. The prevalent ectoparasites of range guinea fowl and local chickens include seven species of lice Menacanthus stramineus, Menopon gallinae, Goniodes gigas, Goniocotes gallinae, Lipeurus caponis, Numidilipeurus tropicalis, Damalinia bovis; three mites Bdellonyssus bursa, Megninia cubitalis, Dermanyssus gallinae; two fleas Echidnophaga gallinacea, Ctenocephalides felis and two ticks Argas persicus and Ambylomma variegatum. Under intensive management, infestation by G. gigas, L. caponis and M. gallinae led to clinical signs, feather damage, reduced food intake and death.

Animals↗

A survey of helminths in stray cats from Copenhagen with ecological aspects.

At autopsy of 230 adult stray cats, 120 from backyards and 110 from gardens, the intestinal tract was scrutinized for helminths. The prevalence of Toxocara cati, Taenia taeniaeformis and Dipylidium caninum was found to be 79%, 11% and 14%, respectively. Comparisons were made with the results of previous Danish investigations. The prevalence of Toxocara cati was found to be independent of time of collection and the sex and habitat of the cats and identical in cats with or without Taenia. This indicates that paratenic hosts do not play an important epizootiological role in the transmission of T. cati. The intensity of Toxocara per cat followed a negative binomial pattern. The high prevalence of T. cati combined with most cats having a low wormload shows that the cat population generally possesses a high degree of resistance against superimposed infections. The intensity of male Toxocara increases with the size of the worm population. This we consider to be an expression of increasing susceptibility of the cats. The prevalence of T. taeniaeformis was significantly higher in garden cats, due to their greater opportunity for catching mice. D. caninum, however, was significantly more frequent in backyard cats, probably owing to better living condition for the flea larvae in backyards. For both T. taeniaeformis and D. caninum a higher frequency was found in female cats, which is thought to be associated with their care for the kittens.

Animals↗

Current knowledge of Bartonella species.

Bartonella species are now considered emerging pathogens. Of the 11 currently recognized species, four have been implicated in human disease, although only two have been encountered in Europe. Bartonella quintana infections are now being diagnosed among the urban homeless and deprived, manifesting as trench fever, and Bartonella henselae has been shown to be the causative agent of cat scratch disease. Both species also cause a variety of HIV-associated infections, including bacillary anglomatosis. However, perhaps the most significant presentation of bartonellae infection is culture-negative endocarditis. The epidemiologies of Bartonella infections are poorly understood; most Bartonella henselae infections are probably acquired from infected cats, either directly by contact with a cat or indirectly via fleas. No animal reservoir has been implicated for Bartonella quintana; however, infection can be transmitted via the human body louse. Diagnosis of Bartonella infections can be made using histological or microbiological methods. The demonstration of specific antibodies may be useful in some instances, although certainly not in all. Cultivation of Bartonella is difficult, as the bacteria are extremely fastidious. Polymerase chain reaction-based or immunological methods for the detection of bartonella in infected tissues have proven useful. Clinical relapse is often associated with Bartonella infections despite a wide range of prescribed regimens. Only aminoglycosides display in vitro bactericidal activity against intracellular Bartonella species; therefore, they are recommended for treatment of Bartonella infections.

AIDS-Related Opportunistic Infections↗

Metazoan parasites of dogs in Sabah, Malaysia.

The parasites which occurred most frequently in 175 owned or stray dogs in Sabah were Ancylostoma spp. present in 68% of the animals. Dirofilaria immitis occurred in 70% of the adult dogs but neither D. immitis nor Spirocerca lupi were present in puppies under four months of age. The latter attained a prevalence of 30% in the adults. In contrast Toxocara canis occurred in 81% of the puppies but infrequently in older dogs. Dipylidium caninum was moderately prevalent (15 to 25%) in dogs of all ages. Ticks were the most common arthropod parasite being present on 26% of the dogs and were mainly Rhipicephalus sanguineus. Demodectic and sarcoptic mange were confirmed and fleas and lice were also recovered.

Animals↗

Interaction of lectins with Yersinia pestis strains.

The ability of lectins to interact with Yersinia pestis strains isolated from rodent fleas and human biological fluids, obtained from different geographic areas, was examined. Lectins of Canavalia ensiformis, Ulex europaeus, Phaseolus vulgaris, and Triticum vulgaris, as well as a new autochthonous lectin of Swartzia pickellii of undefined specificity, were used. Most of the Y. pestis strains did not agglutinate with U. europaeus or C. ensiformis lectin. However, P. vulgaris lectin agglutinated suspensions of all the bacillus strains used. Fifteen of the 19 strains tested positive for assays using S. pickellii lectin. It is believed this is the first report of Y. pestis strain agglutination by lectins. A similar agglutination pattern was obtained for lectins with specificity for oligosaccharides containing N-acetylglucosamine and S. pickellii lectin, which did bind to the affinity matrix chitin, a polysaccharide of N-acetylglucosamine. The use of bacterial strains and commercial lectins of defined specificity may be an approach to providing evidence about the lectin binding sites of undefined monosaccharide specificity.

Agglutination↗

Epipodite and fat cells as sites of hemoglobin synthesis in the branchiopod crustacean Daphnia magna.

In contrast to the malacostracan crustaceans that use hemocyanin as the oxygen carrier, a number of branchiopod crustaceans, such as the water flea Daphnia magna, utilize hemoglobin (Hb) as the respiratory protein. By means of in situ hybridization (ISH) techniques with subsequent signal amplification using catalyzed reporter deposition, sites of Hb synthesis were localized in Daphnia magna. Based on a previously reported Hb-cDNA sequence, a specific ISH probe was designed and hybridized with the Hb-mRNA in histological sections of adult D. magna. The detection of Hb-mRNA was tissue specific and revealed that Hb is synthesized in fat cells, which play a role in fat and glycogen metabolism, and in epithelial cells of the epipodites, which are involved in osmoregulation. Sites of Hb synthesis have been identified in several invertebrate phyla, including Annelida and Nematoda. However, this is the first example in the class Crustacea, and only the second in the phylum Arthropoda.

Adipocytes↗

[Farm animals as disease vectors of parasitic epizoonoses and zoophilic dermatophytes and their importance in dermatology].

Different pest arthropods and dermatophytes occurring primarily in farm animals may be transmissible to man and produce human dermatoses. The movement and cutaneous penetration habits of external parasites often cause crusted papules, severe itching and dermatitis or may damage their hosts by blood-sucking or by sensitizing them to their saliva. Furthermore different dermatophytes should be considered a possible cause of human skin lesions. Farm animals (cattle, pig, poultry, and rabbit) can transmit external parasites (ticks: Ixodes ricinus, Argas reflexus; fleas: Ceratophyllus gallinae, Spilopsyllus cuniculi, and mites: Sarcoptes scabiei var. bovis, Sarcoptes scabiei var. suis, Dermanyssus gallinae, Cheyletiella parasitovorax), and dermatophytes (Trichophyton sp., and Microsporum sp.). People who have close contact to infested farm animals are more often exposed to epizoonotic infections. Certain professions, such as farmers, and veterinarians, are especially vulnerable.

Agricultural Workers' Diseases↗

Distribution of pesticide residues within homes in central New York State.

Residues for 17 pesticides were analyzed in 41 households in central New York State that represented farm, rural, and urban houses. Samples were taken in both summer and winter of 2000-2001 from the same households from four locations; family room carpet; adjacent smooth floor; flat tabletop surface; and settled dust collected in a Petri dish on a tabletop. Pesticide residues were analyzed to identity factors that influence both the transport into and the redistribution of pesticides in the indoor environment. Differences were observed between the various pesticides and pesticide classifications relative to location within and between households as well as by season. Variations in the pesticide residues were related to a number of factors. Higher residues were observed in the farm households, particularly in summer, with the highest amount observed for chloropyrifos in carpet (33 microg/m2). For many pesticides, the frequency of detection and the amount of residues were higher in summer, which relates to usage patterns in agriculture and horticulture; however, larger amounts of insecticides such as mecoprop, resmethrin, and tetramethrin were found on flat surfaces in winter, indicating household use and possible redistribution within the home. Distribution patterns suggest that routines within a household may cause high variation in residues; these practices include indoor pets and treatment for fleas and ticks, use of termiticides, and fastidiousness of occupants. Frequency of pesticide detection was highest in carpet for both summer and winter for all households, indicating that carpets hold pesticides over time. Adsorbent fibrous materials such as textiles hold pesticides by macro- and micro-occlusion in their complex structures. Amounts of pesticide residue were higher in carpets than on smooth floors, particularly for rural farm households where the farmer was a certified pesticide applicator. The maximum amount of pesticide residue on a smooth floor surface was 13.6 microg/m2 malathion while the maxima on wiped surfaces and in settled dust were 1.8 microg/m2 2, 4 D and 3 microg/m2 pendimethalin, respectively. Physical properties of individual pesticides such as vapor pressure influenced the distribution of the pesticide within the households. Evidence of volatilization of pesticides and redeposition on surfaces was observed, indicating that this is a mechanism for contamination of surfaces in addition to adsorption on airborne particles and tracking. High residues in winter are evidence that closure of households in winter that reduces ventilation results in redistribution of pesticides within households.

Dust↗