Similar mode of action of pyrethroids and DDT on sodium channel gating in myelinated nerves

Vijverberg, Henk P.M.; Zalm, J.M. van der; Bercken, Joep van den

doi:10.1038/295601a0

Cited by 200 publications

(71 citation statements)

References 20 publications

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“…The hooked tail currents induced by deltamethrin in this study have been observed in mammalian neurons and sodium channels expressed in oocytes (such as Lund and Narahashi, 1982;Vijverberg et al, 1982;Song et al, 1996;Vais et al, 2000). The initial increasing phase of the tail current is the result of the delayed closing of the inactivation gate upon termination of depolarization.…”

Section: Discussionmentioning

confidence: 89%

“…Specifically, the sodium current during depolarization is prolonged, and the tail current associated with repolarization is greatly augmented. The pyrethroid-induced tail current has been used to quantify pyrethroid modification of the sodium channel (Lund and Narahashi, 1982;Vijverberg et al, 1982;Song et al, 1996;Lee et al, 1999c;Vais et al, 2000). Cohen and colleagues (Vais et al, 2000) compared two tail current recording protocols, one with a 500 ms depolarization from −100 to 0 mV and the other with a 100-pulse train of 5 ms depolarization from −100 to 0 mV.…”

Section: Kdr-type Mutations Altered the Para Csma Channel Sensitivitymentioning

confidence: 99%

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Novel sodium channel gene mutations in Blattella germanica reduce the sensitivity of expressed channels to deltamethrin

Tan

Liu

Tsai³

et al. 2002

Insect Biochemistry and Molecular Biology

104

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Pyrethroid insecticides alter the normal gating of voltage-gated sodium channels in the nervous system. Three sodium channel mutations (E434K, C764R, L993F) were recently identified in pyrethroid resistant German cockroach populations. In this report, we show that the L993F mutation decreased sodium channel sensitivity to the pyrethroid, deltamethrin, by five-fold in Xenopus oocytes. In contrast, neither E434K nor C764R alone decreased channel sensitivity to deltamethrin. However, E434K or C764R combined with L993F reduced deltamethrin sensitivity by 100-fold. Furthermore, concomitant presence of all three mutations (KRF) reduced channel sensitivity to deltamethrin by 500-fold. None of the mutations significantly affected channel gating. However, sodium current amplitudes from the mutant sodium channel carrying either E434K or C764R alone were much reduced compared to those of the wild-type channel or the channel carrying the double or triple mutations (KF, RF and KRF). These results indicated that evolution of sodium channel insensitivity in the German cockroach is achieved by sequential selection of a primary mutation L993F and two secondary mutations E434K and C764R, and concomitant presence of all three mutations dramatically reduced sodium channel sensitivity to deltamethrin.

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Section: Discussionmentioning

confidence: 89%

Section: Kdr-type Mutations Altered the Para Csma Channel Sensitivitymentioning

confidence: 99%

Novel sodium channel gene mutations in Blattella germanica reduce the sensitivity of expressed channels to deltamethrin

Tan

Liu

Tsai³

et al. 2002

Insect Biochemistry and Molecular Biology

104

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“…They are also potent inhibitors of the mitochondria complex I (Gassner et al, 1997), oxygen consumption (Gosh 1989, Reddy andPhilip, 1992), hence they inhibit the production of adenine triphosphate (ATP) in the mitochondria of cells. This leads to the alteration of the Na + /K + pump kinetics, a principal molecular mode of action of synthetic pyrethroids (Vijverberg et al, 1982;Vijverberg and van den Bercken, 1990;Tatebayashi and Narahashi, 1994). There is sodium and water transport into the cell cytosol, cellular water overload, deranged protein synthesis and mechanical function (Guyton and Hall, 2000).…”

Section: Figmentioning

confidence: 99%

Clinical signs and organ pathology in rats exposed to graded doses of pyrethroids- containing mosquito coil smoke and aerosolized insecticidal sprays

Taiwo¹,

Nwagbara²,

Suleiman³

et al. 2010

African Journal of Biomedical Research

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Morphological changes in tissues/organs of weanling Albino rats exposed to graded doses of popular brands of pyrethroids-containing insecticidesmosquito coil and aerosolized spray were studied over a period of 18 days. Rats were exposed to 0.4, 0.8, 1.2 and 1.6mg/kg BW of active ingredients in aerosolized insecticidal spray for 15, 30, 45 and 60 seconds, in two divided doses daily for 18 days. Control rats were not exposed. Early clinical signs include irritability, head shaking and scratching of nostrils; these later gave way to sneezing, gurgling, fine muscular tremors, ruffled fur, lethargy and depression. No self-death was recorded in all the exposed and control groups. Gross changes were not apparent in most organs, but for pulmonary oedema and slight hepatomegaly and palor of kidneys in rats exposed to high doses of the fumes sacrificed on days 12, 15 and 18 post-exposure. Histopathology revealed varying degrees of vacuolar degeneration and necrosis of hepatocyctes, myocardiac degeneration, glomerular and tubular degeneration and necrosis, meningitis, neuronophagia, demyelination of neuronal axons and exudative pnuemonia. Others include blood vascular damage, haemorrhages, vasculitis and thrombosis in many organs, and Kuppfer and intestinal goblet cells hyperplasia. The severity of the lesions was dose and time dependent. The lesions observed suggest interference with tissue energy metabolism and widespread vascular damage and multi-organ degeneration and necrosis. The implications of the consistent and uncontrolled use of pyrethroids-containing insecticides on farm and market produce and in human inhabitants and their effects on public health and biodiversity conservation are discussed.(Afr. J. Biomed. Res. 11: 97 -104)

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“…Type I pyrethroids (e.g., permethrin, allethrin, and tetramethrin), do not have a-cyano group whereas Type II pyrethroids (e.g., cypermethrin, a-cypermethrin, deltamethrin, and fenvalerate), possess an a-cyano group, which has been related to mammalian toxicity. In addition, Type II pyrethroids are more potent insecticides because of the a-cyano group in their structure [Vijverberg et al, 1982;Tabarean and Narahashi, 1998]. …”

Section: Introductionmentioning

confidence: 99%

The in vitro genotoxic effects of a commercial formulation of α‐cypermethrin in human peripheral blood lymphocytes

Kocaman

Topaktaş

2008

Environ and Mol Mutagen

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a-Cypermethrin, a highly active pyrethroid insecticide, is effective against a wide range of insects encountered in agriculture and animal husbandry. The potential genotoxicity of a commercial formulation of a-cypermethrin (Fastac 100 EC, containing 10% a-cypermethrin as the active ingredient) on human peripheral lymphocytes was examined in vitro by sister chromatid exchange (SCE), chromosomal aberrations (CAs), and micronucleus (MN) tests. The human lymphocytes were treated with 5, 10, 15, and 20 lg/ml of a-cypermethrin for 24-and 48-hr. a-Cypermethrin induced SCEs and CAs significantly at all concentrations and treatment times and MN formation was significantly induced at 5 and 10 lg/ml of a-cypermethrin when compared with both the control and solvent control. Binuclear cells could not be detected sufficiently in the highest two concentration of a-cypermethrin (15 and 20 lg/ml) for both the 24-and 48-hr treatment times. a-Cypermethrin decreased the proliferation index (PI) at three high concentrations (10, 15, and 20 lg/ml) for both treatment periods as compared with the control groups. In addition, acypermethrin reduced both the mitotic index (MI) and nuclear division index (NDI) significantly at all concentrations for two treatment periods. The PI and MI were reduced by a-cypermethrin in a concentration-dependent manner during both treatment times. In general, a-cypermethrin showed higher cytotoxic and cytostatic effects than positive control (MMC) at the two highest concentrations for the 24-and 48-hr treatment periods. The present study is the first to report the genotoxic and cytotoxic effects of commercial formulation of a-cypermethrin in peripheral blood lymphocytes. Environ. Mol. Mutagen. 50:27-36, 2009. V V C 2008 Wiley-Liss, Inc.

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Similar mode of action of pyrethroids and DDT on sodium channel gating in myelinated nerves

Cited by 200 publications

References 20 publications

Novel sodium channel gene mutations in Blattella germanica reduce the sensitivity of expressed channels to deltamethrin

Novel sodium channel gene mutations in Blattella germanica reduce the sensitivity of expressed channels to deltamethrin

Clinical signs and organ pathology in rats exposed to graded doses of pyrethroids- containing mosquito coil smoke and aerosolized insecticidal sprays

The in vitro genotoxic effects of a commercial formulation of α‐cypermethrin in human peripheral blood lymphocytes

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