The uptake of phorate, a systemic insecticide, applied as a slurry to wheat and mustard seeds

The absorption by plants of wheat and mustard of a systemic organophosphorus insecticide (phorate), applied as a slurry seed dressing, was studied by caging the aphid Rhopalosiphum padi (L.) on the foliage of wheat, and the aphid Brevicoryne brassicae (L.) and the Chrysomelid beetle Phaedon cochleariae (F.) on white mustard, grown from phorate-treated seed.
Wheat and mustard plants quickly lost their toxicity to insects when they were transplanted, suggesting that most of the insecticide from a slurry seed treatment passes into the soil and is picked up by the roots. That phorate or its derivatives occur in the soil was shown by tests of anticholinesterase activity. Insecticide can also pass into the seed of wheat and move to the growing embryo. Phorate becomes closely bound to the testa of mustard, but does not penetrate it to reach the cotyledons or other parts of the embryo. Mustard cotyledons can become contaminated by insecticide as they emerge through the soil.
Young and old leaves of both wheat and mustard depend on continued absorption of insecticide from the soil to maintain their toxicity. No insecticide moves from old to young leaves. Old leaves lose their toxicity to insects more slowly than young ones. When treated seeds are sown close together, the overlapping zones of insecticide round each seed can increase strength and persistence of insecticidal effect. This happens more with dimethoate, which readily dissolves in water, than with phorate, which is almost insoluble. At normal sowing rates the zones of insecticide round each seed would rarely overlap.
Roots of wheat and mustard from treated seed did not excrete insecticide, and the roots did not carry insecticide through the soil.     

Palatability and toxicity of fipronil as a systemic insecticide in a bromadiolone rodenticide bait for rat and flea control

Vector control in plague-infested areas requires a simultaneous killing of rodents and their fleas. We investigated the efficacy of a combination of a systemic insecticide, fipronil, in a rodenticide bait formulation under laboratory conditions. Four different concentrations of fipronil (0.05%, 0.005%, 0.0005% with acetone as a solvent, and 0.05% with propylene glycol as a solvent) and two controls (solvents only) were combined with the rodenticide bait (crushed organically grown wheat with 0.005% bromadiolone). Each concentration was offered together with an untreated non-poisonous challenge bait to 10 singly caged Rattus rattus L., each with 100 rat fleas Xenopsylla cheopis Rothschild (Siphonaptera: Pulicidae) in the nest. Treated bait consumption was relatively low and an unsatisfactory rat mortality of around 50% only was obtained in all tests. The palatability of the bait, however, was not affected by the fipronil concentration. Even at the lowest fipronil concentration, average flea mortality was still above 95%, and doses of more than I mg fipronil per kg rat body weight gave a nearly complete kill of fleas. Fipronil can be highly effective as a systemic insecticide to for flea control, provided that a more attractive bait base for roof rats is used.     

Transposition-mediated transcriptional overexpression as a mechanism of insecticide resistance

It has been proposed that amplification of genes for esterase that provide resistance to insecticides may originate from transposition events. To test this hypothesis, we have constructed a minigene coding for a soluble acetylcholinesterase under the control of a nontissue-specific promoter (hsp70). When introduced into Drosophila, the gene is expressed in all tissues and the extra acetylcholinesterase produced confers a low level of insecticide resistance (twofold). The minigene was mobilized by crossing the initial transformant with a strain providing a source of P-element transposase. After 34 generations of exposure to the organophosphate parathion, we obtained a strain with a higher resistance (fivefold). This strain had only one extra Ace gene, which overexpressed acetylcholinesterase. Thus, following transposition, resistance resulted from the overexpression of a single copy of the gene and not from gene amplification. Received: 9 August 1996 / Accepted: 27 May 1997     

Allergy as a systemic disease

The prevalence of allergic diseases has shown an increase in the last few years. Allergic diseases develop in persons with a genetic background, this genetic trait being known as atopy. The main pathophysiological characteristic of allergy is inflammation. The inflammatory process may explain the diversity of symptoms and signs of allergy. The early sensitization increases the risk of developing different symptomatic forms of allergy, and one person may present different symptoms and signs of allergy. But some persons can become allergic without atopy trait in conditions of a higher and longer exposure to allergens (e.g. occupational allergy). In the last years new allergens have induced symptoms, sometimes with a life-threatening evolution. The load of allergen in public areas is also increasing. In this context, allergy must be understood as a unique systemic disease with various forms of presentation.     

Ivermectin resistance

In this review of ivermectin resistance, Wesley Shoop discusses the definition of resistance, catalogs all known cases of ivermectin resistance, argues that overmectins and milbemycins belong in the same action family, discusses the possibility of resistance in the filariae, and suggests that detection of ivermectin resistance is the area where future research is most needed.     

Syphilis as a chronic systemic infection

During the last STDs'epidemic in Russia (1994 - 2004) over 2.7 min people have been infected with syphilis. At present the structure of syphilis morbidity is characterized by 37% of latent forms, including 1.5% late latency. The increased level of late latency may result from: an ever-growing number of those with asymptomatic syphilis; disorderly and self-dependent usage of antibacterial preparations; spread of the virus chronic infections (herpes, hepatitis B, C) altering the macroorganism immune response; alcohol and drug abuse which decreases the efficacy of specific therapy. In general, chronization of the syphilitic infection may be caused by antigenically inert treponemal cell surface; paucity of outer membrane protein; residence of treponemas within an immunoprotective niche; uncompleted phagocytosis of treponemes with macrophages. Syphilis remains an "infectio magna" and demands thorough attention to all diagnostic and therapeutic procedures on every stage of the disease.     

Ivermectin as a possible control agent for the tsetse fly,Glossina morsitans

Ivermectin produced 100% mortality in adult teneral males, mature males and fertile females ofGlossina morsitans morsitans following a single meal of defibrinated pig blood containing concentrations of 0.1, 1.6 or >1.6 g ml^–1 respectively. The lethal concentration was reduced to <0.04 g ml^–1 for teneral males when fed repeatedly on treated blood. When pregnant females were fed a single blood meal containing ivermectin (0.08 g ml^–1) on the day after their first larviposition, followed by normal blood meals, no offspring were produced in the subsequent reproductive cycle but full recovery occurred thereafter. A dose dependent decline in fecundity was measured and data were subjected to Probit analysis. Thus estimates were made of ivermectin concentrations in the peripheral blood of treated animals by measuring the reduction in fecundity induced in flies fed on such blood. Indications are that with subcutaneous injections at least, amounts greatly in excess of the recommended clinical dose would be required to achieve levels lethal to feeding flies following a single blood meal. Oral treatment of a horse with twice the anthelmintic dose of ivermectin (0.4 mg kg^–1) produced a maximum concentration in the blood of about 0.14 g ml^–1 within 24 h and this was adequate to reduce tsetse fecundity to zero following a single meal. Such levels in a single blood meal were also sufficient to shorten the life expectancy of teneral male flies. The half-life of ivermectin in the horse was approximately 5–6 days with a maximum of 2.4% of ingested material entering the peripheral circulation. A cow treated with injectable ivermectin (0.2 mg kg^–1) produced maximum blood levels of about 0.005 g ml^–1 after one week; this was only 0.17% of the administered dose and sufficient to reduce fecundity in female flies to 50% of normal following a single blood meal. Such levels in a single blood meal had no effect on the longevity of flies. However, at least half the maximum activity was present in the circulation between 3 and 14 days following injection. Repeated feeding on the blood of a treated animal reduced considerably the dose of ivermectin required to produce a given effect. The fecundity of female flies was reduced to zero by repeated feeding on blood taken from the horse 8 days after treatment, and even after 15 days the blood of the horse contained sufficient drug to reduce fly fecundity to 50% of normal. Thus where domestic animals constitute major hosts of tsetse, treatment with ivermectin can be expected to achieve some measure of fly population reduction.

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L'invermectine comme moyen de lutte utilisable contre la mouche tsé-tsé,Glossina morsitans

Résumé Après un repas unique de sang de porc défibrillé contenant 0,1; 1,6 ou plus de 1,6 g ml^–1 d'ivermectine, tous les mâles jeunes non encore alimentes, tous les mâles adultes et toutes les femelles fécondes deGlossina morsitans morsitans sont tués. Les concentrations léthales ont été réduites à moins de 0,04 g ml^–1 pour les jeunes mâles quand on les a alimentés régulièrement sur du sang traité. Quand des femelles en gestation ont été alimentées, le jour après leur première parturition, avec un seul repas de sang contenant 0,08 g ml^–1 d'ivermectine, et ensuite avec des repas de sang normal, il n'y a pas eu production de descendants pendant le cycle suivant, bien qu'une restauration totale ait eu lieu par la suite. Une diminution de la fécondité en relation avec la dose a été enregistrée, et les données soumisses à un test Probit. Ainsi des estimations de la concentration en ivermectine du sang périphérique des animaux traités ont été obtenues en mesurant la réduction de la fécondité induite chez les mouches ayant consommé ce sang. Ceci montre qu'une dose absorbée de 4 mg kg^–1, ou une injection souscutanée de 16 mg kg^–1, seraient nécessaires pour obtenir le seuil létal chez des mouches alimentées après un repas de sang unique, c'est-à-dire 20 fois la dose absorbée et 80 fois la dose subcutanée nécessaires contre les nématodes gastrointestinaux. Le traitement par voie buccale d'un cheval avec 2 fois la dose vermifuge d'ivermectine (0,4 mg kg^–1) provoque dans les 24 heures des taux sanguins suffisants pour réduire la fécondité jusqu'à zéro après un seul repas de sang. La demi-vie dans le cheval a été approximativement de 5 à 6 jours avec une pénétration dans la circulation périphérique d'une quantité maximale de 2,4% de l'ivermectine absorbée. Une vache traitée avec de l'ivermectine injectable (0,2 mg kg^–1) atteint la teneur sanguine maximale au bout d'une semain; celle-ci, correspondant seulement à 0,17% de la quantité administrée, était suffisante pour réduire de 50% la fécondité des mouches après un repas unique de sang. Cependant, entre les 3ème et 14ème jours suivant l'injection, la circulation sanguine présente au moins la moitié de l'activité maximale. Des repas répétés sur le sang des animaux traités réduisent considérablement la dose d'ivermectine nécessaire pour produire un effet donné. La fécondité des mouches devient nulle après des repas répétés sur le sang d'un cheval 8 jours après le traitement; et même après 15 jours, le sang de ce cheval contient suffisamment de produits pour abaisser la fécondité des mouches de 50%. Ainsi, à où les animaux domestiques constituent les principaux hôtes de la mouche tsé-tsé, avec le traitement à l'ivermectine, on peut espérer réduire d'une façon efficace la population de mouches.

     

Ivermectin: an update

Ivermecan was introduced as an antiparasitic agent in 1981. It is now registered for animal-health use in 35 countries and is being evaluated for possible use in man. This review summarises its antiparasitic efficacy and apparent mode of action. Additional information is given in previous review articles.     

Membrane fluidity as affected by the insecticide lindane

Fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH) was used to study the interaction of lindane with model and native membranes. Lindane disorders the gel phase of liposomes reconstituted with dimyristoyl-, dipalmitoyl- and distearoylphosphatidylcholines (DMPC, DPPC and DSPC), since it broadens and shifts the main phase transition, but no apparent effect is detected in the fluid phase. These effects of lindane are more pronounced in bilayers of short-chain lipids, e.g., DMPC. In equimolar mixtures containing DMPC and DSPC, lindane preferentially interacts with the more fluid lipid species inducing lateral phase separations. However, in mixtures of DMPC and DPPC, the insecticide only broadens and shifts the main phase transition, i.e., an effect similar to that observed in bilayers of pure lipids. Lindane has no apparent effect in DMPC bilayers enriched with high cholesterol content (greater than or equal to 30 mol%), whereas disordering effects can still be detected in bilayers with low cholesterol (less than 30 mol%). Apparently, lindane does not perturb the fluid phase of representative native membranes, namely, mitochondria, sarcoplasmic reticulum, myelin, brain microsomes and erythrocytes in agreement with the results obtained in fluid phospholipid bilayers, despite the reasonable incorporation of the insecticide in these membranes, as previously reported (Antunes-Madeira, M.C. and Madeira, V.M.C. (1985) Biochim. Biophys. Acta 820, 165-172).     

A biological assay technique for the assessment and comparison of systemic insecticide residues

A technique is described using mortality of aphids on excised leaf samples to assess residual systemic insecticides within the leaf or on its surface. Residues in crops or soil can also be assessed by keeping aphids on leaf samples treated with solvent extracts of contaminated material. Little or no pre-treatment for the removal of potentially interfering materials co-extracted from the crop is required. Comparison of mortalities caused by unknown residues with mortalities caused by known amounts of insecticide enables the technique to be used quantitatively. The sensitivity of the technique varies with the toxicity of the compound being assayed. With most of the insecticides tested, extract solutions down to about 10 ppm may be assessed directly; weaker solutions must first be concentrated.     

Use of systemic insecticide to measure antixenosis to aphids in plant choice experiments

Antixenosis in three wheat varieties (Timmo, Moghan 2 and Ommid) toRhopalosiphum padi (L.) was measured by pairing plants of any two varieties with one plant of each pair treated with a soil drench of the systemic insecticide pirimicarb. Aphids were then allowed access to equivalent leaf areas from the two plants in a leaf cage. The results were compared with similar choice experiments without insecticide. By either technique, the two Iranian varieties (Moghan 2 and Ommid) showed antixenosis in comparison with Timmo. The statistical analysis of the data, using a heterogeneity ² test, is described.

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Zusammenfassung Die Antixenose gegenüberRhopalosiphum padi (L.) in den drei Weizensorten Timmo, Moghan 2 und Ommid, von denen die zwei letzteren Sorten aus dem Iran stammen, wurde unter Verwendung des systemischen Insektizids Pirimicarb gemessen. Jeweils zwei Pflanzen aus verschiedenen Sorten wurden als Paar verwendet (in allen Kombinationen der drei Sorten), pro Paar ein Topf mit Pirimicarb gegossen, und zwanzig Blattlaüse über Blattflächen von beiden Sorten gekäfigt. Ähnliche Versuche wurden auch ohne Insektizid ausgeführt. Beide Methoden zeigten deutliche Antixenose von Moghan 2 und Ommid in Vergleich mit Timmo. Die Insektizidmethode zeigte auch eine Bevorzugung von Moghan 2 gegenüber Ommid, ein Resultat, das mit der schon bekannten relativen Antibiose dieser zwei Sorten übereinstimmte, während sich ohne Insektizid kein solcher Unterschied erwies. Die statistische Analyse solcher Versuche mit einem Insektizid, die eine Modifikation der Berechnung des erwarteten Werts mit dem ² Test enthält, ist beschrieben.

     

微囊藻藻胆蛋白光敏杀虫剂毒杀机制研究

用果蝇（Drosophila melanogaster）和草地夜蛾卵巢细胞Spodoptea Frugiperda 21（SF21）来探讨微囊藻藻胆蛋白（MC-PBP）作为光敏杀虫剂的作用和机理。实验结果表明：MC-PBP对果蝇的LC50为750μg/mL,致死剂量为4000μg/mL;血卟啉甲醚（HMME）对果蝇的LC50为1000μg/mL。MC-PBP浓度4000μg/mL时,果蝇的死亡率是93.33%,而相同浓度下,HMME光敏剂的致死率是66.66%;在细胞水平研究中发现：MC-PBP光照处理SF21细胞48 h之后,400μg/mL的MC-PBP对细胞的抑制率达到65%;MC-PBP处理SF21细胞后,其细胞内丙二醛（MDA）含量明显升高,而细胞内还原型GSH相对含量随MC-PBP浓度升高而显著降低。结果表明MC-PBP光敏杀虫剂毒杀机制与细胞内脂质过氧化和细胞抗氧化损伤能力减弱相关。     

Spiroindolines identify the vesicular acetylcholine transporter as a novel target for insecticide action

The efficacy of all major insecticide classes continues to be eroded by the development of resistance mediated, in part, by selection of alleles encoding insecticide insensitive target proteins. The discovery of new insecticide classes acting at novel protein binding sites is therefore important for the continued protection of the food supply from insect predators, and of human and animal health from insect borne disease. Here we describe a novel class of insecticides (Spiroindolines) encompassing molecules that combine excellent activity against major agricultural pest species with low mammalian toxicity. We confidently assign the vesicular acetylcholine transporter as the molecular target of Spiroindolines through the combination of molecular genetics in model organisms with a pharmacological approach in insect tissues. The vesicular acetylcholine transporter can now be added to the list of validated insecticide targets in the acetylcholine signalling pathway and we anticipate that this will lead to the discovery of novel molecules useful in sustaining agriculture. In addition to their potential as insecticides and nematocides, Spiroindolines represent the only other class of chemical ligands for the vesicular acetylcholine transporter since those based on the discovery of vesamicol over 40 years ago, and as such, have potential to provide more selective tools for PET imaging in the diagnosis of neurodegenerative disease. They also provide novel biochemical tools for studies of the function of this protein family.     

Selective effect of the systemic insecticide Phosphamidon on soil,root-surface and leaf-surface fungi

Results of the effect of Phosphamidon on soil, root- and leaf-surface fungi of Vigna sinensis var. azmerly were generally inconsistent. However, there were some consistent ones. Its effect on soil, root- and leaf-surface fungi persisted till after 40 days. In soil the total count was regularly increased after 20 days by the low and medium doses and after 40 days by the high dose. In the rhizosphere, Fusarium was almost consistently activated by the three doses after 5 days of treatment and by the low dose after 20 days. In the rhizoplane, the total count of fungi was lowered by the three doses after 40 days in the two sowings. Alternaria alternata was toxicated by the three doses after several experimental periods of the two sowings in the phyllosphere and phylloplane. When this insecticide was incorporated with the agar medium, it was of no significant effect on the total count of fungi at the low and medium doses but abnormally increased the total count at the high dose. In the liquid medium, the mycelia of the test fungi were not significantly affected except that of Penicillium corylophilum which was significantly retarded by the three doses and Rhizopus stolonifer which was significantly activated by the high dose.     

Membrane fluidity as affected by the organochlorine insecticide DDT

Fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH) was used to study the interaction of DDT with model and native membranes. DDT decreases the phase transition midpoint temperature (Tm) of liposomes reconstituted with dimyristoyl-, dipalmitoyl- and distearoylphosphatidylcholines (DMPC, DPPC and DSPC), and broadens the thermotropic profile of the transition. The effects of DDT are concentration dependent and are more pronounced in bilayers of short-chain lipids, e.g., DMPC. The insecticide fails to alter DPH polarization in the fluid phase of the above lipids. Similar effects were observed in binary mixtures of DMPC plus DPPC. Furthermore, DDT alters the single broad transition of the equimolar mixture of DMPC plus DSPC into a biphasic transition. The lower temperature component has a midpoint at 25 degrees C, i.e., a value close to the Tm of DMPC. DDT inhibits to some extent the cholesterol-induced ordering in DMPC bilayers and high cholesterol concentrations (greater than or equal to 30 mol%) do not prevent insecticide interaction, conversely to the effect observed for lindane (Antunes-Madeira, M.C. and Madeira, V.M.C. (1989) Biochim. Biophys. Acta 982, 161-166). Apparently, the bilayer order is not disturbed by DDT in fluid native membranes of mitochondria and sarcoplasmic reticulum, but moderate disordering effects are noticed in membranes enriched in cholesterol, namely, brain microsomes and erythrocytes.     

伊维菌素搽剂的毒理学研究

目的　研究放线菌属产生的阿凡曼菌素 Ｂ１ 的衍生物伊维菌素（ Ｉｖｅｒｍ ｅｃｔｉｎ） 搽剂皮肤用药的急性和长期毒性作用。方法　观察给予正常皮肤和破损皮肤动物一次性或长期经皮给药产生的毒性反应。结果　以２６７ｍ ｇ／ｋｇ 大剂量的伊维菌素经皮给药 ２４ｈ 后出现震颤、运动失调等中毒症状, ７２ｈ 后症状消失; 以１００ｍ ｇ／ｋｇ 经皮给药 ４５ 天后无明显的毒性。结论　大剂量 （２６７ ｍ ｇ／ｋｇ） 的伊维菌素经破损皮肤给药可致动物急性中毒, 较大剂量 （１００ ｍ ｇ／ｋｇ） 长期皮肤用药无明显的毒性作用。