Biochemical evidence that an S431F mutation in acetylcholinesterase-1 of Aphis gossypii mediates resistance to pirimicarb and omethoate

Molecular changes in acetylcholinesterase (AChE) leading to target-site resistance to carbamate and organophosphate insecticides have recently been identified. Of particular interest is the S431F mutation in ace2 and its orthologue ace1 of Myzus persicae Sulzer and Aphis gossypii Glover, respectively. This mutation has been correlated with resistance to pirimicarb, but biochemical evidence has not yet been provided. Here, we describe for the first time that recombinantly expressed AChE1 from A gossypii carrying the S431F mutation is insensitive to pirimicarb and omethoate, but sensitive to demeton-S-methyl and hypersensitive to carbofuran. Furthermore, site-directed mutagenesis of the serine residue at position 431 in ace1 from a pirimicarb-susceptible clone of A gossypii conferred insensitivity to pirimicarb. We conclude that AChE1 of A gossypii is the target of toxicological relevance of carbamates and organophosphates.     

Monitoring of spirodiclofen susceptibility in field populations of European red mites, Panonychus ulmi (Koch) (Acari: Tetranychidae), and the cross-resistance pattern of a laboratory-selected strain

BACKGROUND: Phytophagous mites such as the European red mite, Panonychus ulmi (Koch), are serious pests in European fruit tree orchards, and a number of acaricides are frequently used to control them. Spirodiclofen (Envidor^®) has been a commonly used acaricide for several years. In the present study, European field populations collected in 2009 and 2010 were checked for their susceptibility to spirodiclofen by using discriminating dose and full dose response bioassays. RESULTS: In 2009 and 2010, a total of 63 field populations (including winter eggs) of European red mites were collected in different European countries, and in several populations from south‐western Germany a shifting in susceptibility against spirodiclofen was observed. Full dose response bioassays on different developmental stages of field‐collected strains suggested an age‐dependent expression of resistance because eggs remain fully susceptible to spirodiclofen. Artificial selection with spirodiclofen of one of the field strains resulted in resistance ratios of > 7000. Synergism studies suggest a possible role of cytochrome‐P450‐dependent monooxygenases in spirodiclofen detoxification. Most of the other acaricides from different chemical classes displayed no or low cross‐resistance in a spirodiclofen‐selected strain. CONCLUSION: In order to preserve spirodiclofen as an important tool in spider mite resistance management, the efficacy situation should be continuously monitored, and it is suggested that spirodiclofen be alternated with acaricides coming from different mode‐of‐action classes. An observed age‐specific expression of resistance revealed full susceptibility of eggs, so targeting spirodiclofen particularly against eggs is likely to reduce the selection pressures imposed on other life stages. Copyright © 2011 Society of Chemical Industry     

Mode of action of etoxazole

The mode of action of the 2,4-diphenyl-1,3-oxazoline acaricide/insecticide etoxazole has been argued to be moulting inhibition, but experimental results supporting this hypothesis are lacking. This study investigated the effect of etoxazole on chitin biosynthesis in the fall armyworm, Spodoptera frugiperda (Smith) (Lepidoptera: Noctuidae). Etoxazole induced moulting defects in fall armyworm larvae similar, if not identical, to those caused by benzoylphenylureas, a well-known class of insecticidal chitin biosynthesis inhibitors. Furthermore, in contrast to untreated larvae, the chitin content in the integuments of larvae several days after treatment did not differ from that in freshly ecdysed individuals, thus suggesting strong chitin biosynthesis inhibition in vivo. A more detailed investigation of the inhibitory potential by incubating cultured integument pieces from larvae of S. frugiperda with [14C]N-acetyl-D-glucosamine, a radiolabelled chitin precursor, revealed I50 values of 2.95 and 0.071 microM for etoxazole and triflumuron respectively. The incorporation of radiolabel into potassium hydroxide-resistant material was inhibited by etoxazole in a dose-dependent manner. Based on these results, it is concluded that the acaricidal and insecticidal mode of action of etoxazole is chitin biosynthesis inhibition.     

Untersuchungen zur Akarizidresistenz an Populationen der Obstbaumspinnmilbe, Panonychus ulmi KOCH (Acari: Tetranychidae) aus dem Bodenseegebiet

One of the major acarine pest species of deciduous fruit trees like apple and plum is the European red mite, Panonychus ulmi KOCH (Acari: Tetranychidae). Feeding damage by P. ulmi results in leaf bronzing followed by an early defoliation and a reduction in yield, which is usually prevented by the application of acaricides. A problem often associated with mite control is the (sometimes rapid) development of resistance due to their high reproductive potential, a short life cycle allowing numerous generations per season and frequent applications of acaricides. Therefore a resistance monitoring is considered to be an essential part within resistance management strategies where only compounds providing full efficacy at recommended rates should be used. Once a new acaricide is considered for market introduction a so-called baseline susceptibility study is requested by the European authorities. Such a baseline study was also conducted for the new acaricidal compound spirodiclofen (Envidor^®), which is known to inhibit lipid biosynthesis and particularly active against juvenile stages of tetranychid mite pests such as P. ulmi. However, a strong reduction of female adult fecundity results in excellent residual efficacy. Here we report on the baseline susceptibility of 15 European red mite populations against spirodiclofen, which were collected in 2005 in apple orchards at Lake Constance, Germany. The baseline data were combined because of a low population-to-population variation in response to spirodiclofen and a composite dose effect calculation revealed a diagnostic concentration (LC₉₅) of 5?mg/liter (ppm) for future monitoring purposes in P. ulmi larvae. Furthermore we checked the susceptibility of the very same field populations against pyridaben, hexythiazox and abamectin. This helps to identify candidates for a balanced resistance management strategy avoiding the implication of cross-resistance issues.     

Antifeedant effect,biological efficacy and high affinity binding of imidacloprid to acetylcholine receptors in Myzus persicae and Myzus nicotianae

It is known from laboratory studies that tobacco-associated forms of Myzus persicae (Sulzer) and the closely related tobacco aphid Myzus nicotianae (Blackman) are often somewhat less susceptible to imidacloprid than non-tobacco strains of M. persicae. Choice tests (floating leaf technique) showed that tobacco aphids were also less susceptible to the antifeedant potential of imidacloprid in contact bioassays. Synergists like piperonyl butoxide or DEF did not enhance the susceptibility of tobacco-associated morphs of Myzus ssp. to imidacloprid, thus providing evidence that neither oxidative detoxication nor hydrolytic metabolization took place. However, in an attempt to study the influence of endosymbiotic bacteria on the efficacy of imidacloprid, we allowed small populations of tobacco aphids to feed on diets containing the antibiotic chlortetracycline prior to imidacloprid treatment. While the effectiveness of imidacloprid, i.e. lower LC₅₀ values, could be improved in all strains, including the susceptible reference strain, there was no change in overall tolerance factors. In order to investigate any possible alteration of the target site, the affinity of imidacloprid and nicotine to nicotinic acetylcholine receptors in whole-aphid homogenates was measured. All strains (and clones) showed the same high-affinity binding sites and no detectable difference. Studies using the FAO dip method revealed that the lower susceptibility of M. nicotianae is not restricted to chloronicotinyls like imidacloprid or acetamiprid, because other insecticides with different modes of action such as pymetrozine and fipronil were also affected in laboratory studies. It is considered that the observed tolerance to chloronicotinyls in certain strains of Myzus ssp. is a natural variation in response, probably not coupled with any known mechanism of resistance in this species complex. © 1998 SCI     

Movento, an innovative ambimobile insecticide for sucking insect pest control in agriculture: Biological profile and field performance

The tetramic acid derivative spirotetramat (brand name Movento^®), has shown an outstanding performance against sucking insect pests in laboratory and greenhouse assays as well as in semi-field and field trials. The product acts as an inhibitor of lipid biosynthesis and affects juvenile stages with additional effects on adult fecundity. There is no cross-resistance to any other insecticide. After foliar application spirotetramat penetrates through the leaf cuticle and is translocated as spirotetramat-enol via xylem and phloem, up to growing shoots and down to roots. This full ambimobility or two-way systemicity (phloem and xylem transport) ensures the control of hidden and soil living sucking pests after foliar application and protects new shoots. The worldwide field development of spirotetramat in Bayer CropScience AG resulted in numerous uses against many species of whiteflies, aphids, scales (soft and armoured scales), mealy bugs, psyllids and selected thrips species in vegetables, cotton, soybean, pome and stone fruit, grapes, hop, citrus, nut trees and banana. The new mode of action renders spirotetramat as an excellent rotation partner with existing products for the management of aphid, whitefly and psyllid populations, which are frequently resistant to conventional insecticides. Moreover, only low adverse effects have been found on beneficial arthropods, which make the product suitable for modern integrated pest management (IPM) systems. These unique properties contribute to safeguarding the crop yield potential both in quality and quantity. In this paper, the new chemistry is presented, compared with standard insecticides and novel applications in IPM systems are discussed.     

Organophosphate insecticides and acaricides antagonise bifenazate toxicity through esterase inhibition in Tetranychus urticae

BACKGROUND: Bifenazate is a carbazate acaricide known for its potency, particularly against tetranychid mite species such as the two-spotted spider mite, Tetranychus urticae Koch (Acari: Tetranychidae). It was recently shown that the compound needs to be activated by an S,S,S-tributyl-phosphorotrithioate (DEF)-sensitive mechanism in spider mites to display full acaricidal efficacy. The ability of well-known organophosphates and carbamates to inhibit the activation of bifenazate and thus compromise its acaricidal potential was tested.RESULTS: Esterase activity determined in vivo after pre-exposure of mites with organophosphates and carbamates revealed--depending on the compound--varying esterase inhibition nicely correlated with the ability of the individual compound to antagonise bifenazate action on mites.CONCLUSIONS: The findings illustrate that organophosphates and carbamates interfere with bifenazate efficacy, most probably by inhibiting carboxylesterases responsible for the activation of the pro-drug. As a result of the strong antagonism, mixtures of bifenazate with carbamates or organophosphates should not be used under field conditions. Moreover, there exists a real threat in repeatedly applying organophosphates and bifenazate. The present study again illustrates how important mode of action information is for the proper planning of resistance management strategies.     

Effect of imidacloprid on the reproduction of acaricide-resistant and susceptible strains of Tetranychus urticae Koch (Acari: Tetranychidae)

Occasional reports linking neonicotinoid insecticide applications to field population outbreaks of the two-spotted spider mite, Tetranychus urticae Koch, have been a topic of concern for integrated pest management (IPM) programmes, particularly in apples. In order to shed light on the factors which may contribute to the occasional field population increase of T. urticae following the application of neonicotinoid insecticides, greenhouse experiments have been set up. Four different T. urticae strains, namely GSS (acaricide-susceptible), WI (organophosphate-selected), USA (a largely uncharacterised strain) and Akita (METI (mitochondrial electron transport inhibitor) acaricide-resistant and cross-resistant to dicofol), were compared for their fecundity without insecticide treatment and for their ovipositional response to foliar and drench applications of the field-relevant dose of imidacloprid (100 mg litre(-1)). Without insecticide treatment, strain GSS laid significantly more eggs (162.50 (+/- 5.43)) than the multiple resistant strain Akita (139.90 (+/- 5.54)) during a 16 day oviposition period. With imidacloprid treatment the highest effect was observed with GSS, with a significantly reduced number of eggs in drench (143.40 (+/- 4.22)) and foliar (144.60 (+/- 5.85)) applications. For strains Akita and USA, no significant differences were observed in oviposition between imidacloprid treatments and controls. The proportion of F1 female offspring decreased significantly with drench application for GSS and WI, while no differences were observed among strains in the survival of F1 immature stages, except for strain USA. The viability of eggs was relatively high (from 82.9 (+/- 4.5)% for USA to 95.2 (+/- 1.2)% for GSS) and not affected by imidacloprid treatments.     

Applied aspects of neonicotinoid uses in crop protection

Neonicotinoid insecticides comprise seven commercially marketed active ingredients: imidacloprid, acetamiprid, nitenpyram, thiamethoxam, thiacloprid, clothianidin and dinotefuran. The technical profiles and main differences between neonicotinoid insecticides, including their spectrum of efficacy, are described: use for vector control, systemic properties and versatile application forms, especially seed treatment. New formulations have been developed to optimize the bioavailability of neonicotinoids through improved rain fastness, better retention and spreading of the spray deposit on the leaf surface, combined with higher leaf penetration. Combined formulations with pyrethroids and other insecticides are also being developed with the aim of broadening the insecticidal spectrum of neonicotinoids and to replace WHO Class I products from older chemical classes. These innovative developments for life-cycle management, jointly with the introduction of generic products, will, within the next few years, turn neonicotinoids into the most important chemical class in crop protection.