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1.
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2.
Insecticidal activity against the Colorado potato beetle, Leptinotarsa decemlineata, was measured for a series of substituted N-tert-butyl-dibenzoylhydrazines, in which one of the benzoyl moieties closer to the tert-butyl group was fixed as being 2-chloro-substitued and the other variously substituted singly or doubly. The effects of substituents on the activity were quantitatively analysed using the classical quantitative structure–activity relationship (QSAR) procedure. The activity against the Colorado potato beetle increases with the molecular hydrophobicity. In addition, various types of steric effect are at work, depending upon the positions. Hydrogen-bonding acceptor substituents at the para position enhance the activity. There seem to be threshold (or optimum) values, albeit position-dependent, in the molecular hydrophobicity, above which the activity starts to decrease. This biphasic contribution of the molecular hydrophobicity to activity against coleopterous larvae is the most conspicuous difference in substituent effects from those found for similar compounds against lepidopterous pest insects, and may be the basis of the variations in the activity spectrum for certain compounds in this series. The introduction of bulkier substituents into the meta- and para-positions of the benzene ring, apart from the tert-butyl group, is unfavorable to activity. LD50 values against Colorado potato beetle larvae of methoxyfenozide (RH-2485) and tebufenozide (RH-5992) were in the order of 10−7 mol per insect, whereas those of RH-5849, and halofenozide (RH-0345) were very low, 10−9–10−10 mol per insect being selective to the coleopterous larvae. © 1999 Society of Chemical Industry  相似文献   

3.
The activity profile of the most recent commercial non-steroidal ecdysteroid agonist chromafenozide (ANS-118), was evaluated on a comparative basis to methoxyfenozide (RH-2485) that is to date the most potent commercial agonist against Lepidoptera. This was done first at the molecular and cellular level regarding its induction activity of an ecdysteroid-responsive reporter gene and its cell proliferation inhibition activity, and subsequently at the level of larvicidal toxicity. For in vitro experiments three ecdysteroid-responsive insect cell lines were used: Drosophila melanogaster (Diptera) S2 cells, Bombyx mori (Lepidoptera) Bm5 cells and Spodoptera exigua (Lepidoptera) Se4 cells. The in vivo toxicity was scored against two major lepidopteran pests in the world, the beet armyworm S. exigua and the cotton leafworm Spodoptera littoralis. In vitro results revealed that chromafenozide and methoxyfenozide are highly potent against lepidopteran cells compared to dipteran cells, supporting the lepidopteran-specificity of these compounds. Interestingly, in the reporter gene induction experiments and proliferation inhibition experiments, a slightly higher efficacy was observed in S2 compared to Bm5 cells at high concentrations of chromafenozide and methoxyfenozide. Our analysis shows the high potency and efficacy of the chromafenozide compound as an ecdysteroid agonist towards lepidopteran insects at a level that is similar to methoxyfenozide.  相似文献   

4.
The comparative toxicity of two non-steroidal ecdysteroid agonists, RH-2485 and RH-5992 (tebufenozide), on development stages, fecundity and egg viability of a susceptible laboratory strain and a pyrethroid-resistant field strain ofSpodoptera littoralis (Boisduval) was evaluated. Taking the LC50s as the criterion, RH-2485 was 3–7-fold more potent than RH-5992 against the susceptible and 7–14-fold more against the field strain. The LC50 of RH-2485 in the 1st and 6th instars of the susceptible strain was 0.32 and 0.57 mg a.i./l, respectively. The field strain showed a mild cross-resistance of about threefold to both compounds in 1st instars and to a lesser extent in 6th instars. A considerable increase in fecundity (~3-fold) and no effect on egg viability was observed when 6th instars were fed on cotton leaves treated with 0.25 mg a.i./l RH-2485 (~LC40). Our results indicate that both compounds are potentially potent insecticides for controllingS. littoralis larvae, being 10-60-fold more potent than a previous ecdysteroid agonist, RH-5849.  相似文献   

5.
BACKGROUND: Diacylhydrazine (DAH) analogues have been developed successfully as a new group of insect growth regulators, called ecdysone agonists or moulting accelerating compounds. These DAHs have been shown to manifest their toxicity via interaction with the ecdysone receptor (EcR) in susceptible insects, as does the natural insect moulting hormone 20‐hydroxyecdysone (20E). A notable feature is their high activity and specificity, particularly against lepidopteran insects, raising the question as to whether non‐lepidopteran‐specific analogues can be isolated. However, for the discovery of ecdysone agonists that target other important insect groups such as Diptera, efficient screening systems that are based on the activation of the EcR are needed. RESULTS: In this study, a dipteran‐specific reporter‐based screening system with transfected S2 cells of Drosophila melanogaster Meig. was developed in order to discover and evaluate compounds that have ecdysone agonistic or antagonistic activity. A library of non‐steroidal ecdysone agonists containing different mother structures with DAH and other related analogues such as acylaminoketone (AAK) and tetrahydroquinoline (THQ) was tested. None of the compounds tested was as active as 20E. This is in contrast to the very high activity of several DAH and AAK congeners in lepidopteran cells (Bombyx mori L.‐derived Bm5 cells). The latter agrees with a successful docking of a DAH, tebufenozide, in the binding pocket of the lepidopteran EcR (B. mori), while this was not the case with the dipteran EcR (D. melanogaster). Of note was the identification of two THQ compounds with activity in S2 but not in Bm5 cells. Although marked differences in activity exist with respect to the activation of EcR between dipterans and lepidopterans, there exists a positive correlation (R = 0.724) between the pLC50 values in S2 and Bm5 cells. In addition, it was found through protein modelling that a second lobe was present in the ligand‐binding pocket of lepidopteran BmEcR but was lacking in the dipteran DmEcR protein, suggesting that this difference in structure of the binding pocket is a major factor for preferential activation of the lepidopteran over the dipteran receptors by DAH ligands. CONCLUSIONS: The present study confirmed the marked specificity of DAH and AAK analogues towards EcRs from lepidopteran insects. THQ compounds did not show this specificity, indicating that dipteran‐specific ecdysone‐agonist‐based insecticides based on the THQ mother structure can be developed. The differences in activity of ecdysone agonists in dipteran and lepidopteran ecdysone‐reporter‐based screening systems are discussed. Copyright © 2010 Society of Chemical Industry  相似文献   

6.
The calcium channel and the ‘calcium release channel’ of muscle membrane of the cockroach Periplaneta americana have been characterized. Biological assays with calcium channel blockers and ryanodine on different insects and acari revealed pronounced insecticidal effects with ryanodine, but not with calcium channel blockers, at concentrations between 0·1 and 300 μg ml−1. Skeletal muscle membranes derived either from the tubular network or from the sarcoplasmatic reticulum of P. americana were characterized with respect to the binding of the dihydropyridine (DHP) [3H]isradipine (PN 200-110), the phenyl-alkylamine [3H]verapamil and the alkaloid [3H]ryanodine. Preliminary binding studies with the benzothiazepine [3H]diltiazem suggest a low-affinity binding site with a IC50 value of 3·3 μM . All binding sites tested were sensitive to treatment with proteinase K. Optimal conditions for binding of the radioligand ryanodine revealed the highest specific binding at pH 8 and at calcium chloride concentrations between 100 and 500 μM . EGTA at 10 μM abolished 95% of the ryanodine binding. Binding studies with calcium channel binding sites revealed a pronounced effect of low Ca2+ concentrations on specific isradipine binding, whereas verapamil and diltiazem binding were only reduced by the presence of 200 μM EGTA. With respect to high Ca2+ concentrations, specific binding of diltiazem, isradipine and verapamil was reduced by 73, 40 and 20%, respectively, at 5 mM Ca2+. Radioligand binding experiments showed high-affinity binding sites for ryanodine and isradipine. KD values of 0·95 nM (Bmax=550 fmol mg−1 protein) and 0·75 nM (Bmax=213 fmol mg−1 protein) were determined respectively. A lower-affinity binding site was identified in binding studies with verapamil (KD=7·4 nM and Bmax=27 fmol mg−1 protein). [3H]isradipine displacement studies with several dihydropyridines revealed the following ranking of affinity: nitrendipine>isradipine>Bay K8664≪nicardipine. Displacement of [3H]verapamil binding by effectors of the phenylalkylamine binding site showed that bepridil and S(-)verapamil had the highest affinities of the compounds tested followed by (±)verapamil, nor-methylverapamil and R(+)verapamil.  相似文献   

7.
Ecdysteroid signal transduction is a key process in insect development and therefore an important target for insecticide development. We employed an in vitro cell-based reporter bioassay for the screening of potential ecdysone receptor (EcR) agonistic and antagonistic compounds. Natural ecdysteroids were assayed with ecdysteroid-responsive cell line cultures that were transiently transfected with the reporter plasmid ERE-b.act.luc. We used the dipteran Schneider S2 cells of Drosophila melanogaster and the lepidopteran Bm5 cells of Bombyx mori, representing important pest insects in medicine and agriculture. Measurements showed an EcR agonistic activity only for cyasterone both in S2 (EC50 = 3.3 μM) and Bm5 cells (EC50 = 5.3 μM), which was low compared to that of the commercial dibenzoylhydrazine-based insecticide tebufenozide (EC50 = 0.71 μM and 0.00089 μM, respectively). Interestingly, a strong antagonistic activity was found for castasterone in S2 cells with an IC50 of 0.039 μM; in Bm5 cells this effect only became visible at much higher concentrations (IC50 = 18 μM). To gain more insight in the EcR interaction, three-dimensional modeling of dipteran and lepidopteran EcR-LBD was performed. In conclusion, we showed that the EcR cell-based reporter bioassay tested here is a useful and practical tool for the screening of candidate EcR agonists and antagonists. The docking experiments as well as the normal mode analysis provided evidence that the antagonist activity of castasterone may be through direct binding with the receptor with specific changes in protein flexibility. The search for new ecdysteroid-like compounds may be particularly relevant for dipterans because the activity of dibenzoylhydrazines appears to be correlated with an extension of the EcR-LBD binding pocket that is prominent in lepidopteran receptors but less so in the modeled dipteran structure.  相似文献   

8.
Fourth-instar Bombyx mori (silkworm) was used as a model insect to study the effects of Bacillus thuringiensis (Bt) on ion homeostasis in the larval lepidopteran midgut. The K+ chemical gradient across the midgut of B. mori larvae is quite small, sustained by a lumen/haemolymph activity ratio of only 1.6. More than 95% of the driving force causing K+ flux from lumen to haemolymph is electrical. In contrast to K+, the H+ chemical gradient is exceedingly large, with luminal pH values of 11–12 and haemolymph/lumen H+ ratios as high as 105. At equilibrium, the steep proton gradient is consistent with a passive distribution of H+ across the midgut epithelium as predicted from the Nernst equation. In B mori larvae, ingestion of a lethal dose of Bt δ-endotoxin produces an increase in K+ conductance in the midgut apical epithelium, causing a decrease in the electrical gradient and dissipation of the pH gradient. Larval morbidity can be correlated with a rise in haemolymph K+ and pH and a decline in luminal pH. Midgut K+ activity, however, remains unchanged. An important factor in the pathogenesis of Bt is irreversible alkalization of the epithelial cells as H+ is redistributed across the midgut to reach a new Nernst equilibrium.  相似文献   

9.
The effect of the ecdysone agonists RH-2485 (proposed name methoxyfenozide) and tebufenozide (RH-5992), was examined on eggs and larvae of the southwestern corn borer, Diatraea grandiosella Dyar. Both compounds exhibited a concentration-dependent ovicidal activity. More than 95% of eggs died when egg masses were dipped in solutions of 100 or 200 mg liter-1 of either compound in acetone+distilled water (1+1 by volume). Although some eggs treated with 1 or 10 mg liter-1 of the compounds hatched, the survival rate was low. Newly hatched larvae were fed for seven days on an artificial diet containing RH-2485 or tebufenozide. The LC50 values were 0·049 mg kg-1 for RH-2485 and 0·185 mg kg-1 for tebufenozide, showing that RH-2485 was about four times more active than was tebufenozide. Although increasing the time of exposure to either compound decreased the LC50 value significantly, the relative potency of RH-2485 versus tebufenozide was not changed. Newly ecdysed 4th-instar larvae fed with diets containing 0·125, 0·25 or 0·5 mg kg-1 RH-2485 or tebufenozide ceased feeding approximately 8 h after exposure, indicating that larvae had prematurely entered a molting cycle. Larvae treated with RH-2485 ecdysed earlier and died more quickly than those treated with tebufenozide. Ingestion of sublethal concentrations of RH-2485 (0·005 and 0·01 mg kg-1) or tebufenozide (0·03 and 0·06 mg kg-1) retarded larval growth, and decreased pupal weight and adult emergence. Increasing exposure time to tebufenozide tended to increase the larval mortality, significantly retarded larval growth, and decreased the mean weights of male and female pupae and adult emergence. RH-2485 (0·125 and 0·25 mg kg-1) and tebufenozide (0·25 and 0·5 mg kg-1) were lethal to newly hatched larvae, even after diets containing these compounds were held for 20 days at 30°C under long days (16 h light: 8 h dark). Our results suggest that field trials to assess the potential of RH-2485 and tebufenozide to control D. grandiosella are warranted. © 1998 SCI  相似文献   

10.
BACKGROUND: The toxicity of a fusion protein, ButalT/GNA, comprising a venom toxin (ButaIT) derived from the red scorpion, Mesobuthus tamulus (F.), and Galanthus nivalis agglutinin (GNA), was evaluated under laboratory conditions against several pest insects. Insecticidal activity was compared with SFI1/GNA, a fusion comprising a venom toxin (SFI1) derived from the European spider Segestria florentina (Rossi) and GNA, which has been previously demonstrated to be effective against lepidopteran and hemipteran pests, and to GNA itself. RESULTS: Injection assays demonstrated that both fusion proteins were toxic to lepidopteran larvae, dipteran adults, coleopteran adults and larvae and dictyopteran nymphs. ButalT/GNA was more toxic than SFI1/GNA in all cases. GNA itself made a minor contribution to toxicity. Oral toxicity of ButalT/GNA towards lepidopteran pests was confirmed against neonate Spodoptera littoralis (Boisd.), where incorporation at 2% dietary protein resulted in 50% mortality and > 85% reduction in growth compared with controls. ButaIT/GNA was orally toxic to Musca domestica L. adults, causing 75% mortality at 1 mg mL?1 in aqueous diets and, at 2 mg g?1 it was orally toxic to Tribolium castaneum (Herbst.), causing 60% mortality and a 90% reduction in growth. CONCLUSIONS: Toxicity of the ButaIT/GNA recombinant fusion protein towards a range of insect pests from different orders was demonstrated by injection bioassays. Feeding bioassays demonstrated the potential use of the ButaIT/GNA fusion protein as an orally active insecticide against lepidopteran, dipteran and coleopteran pests. These experiments provide further evidence that the development of fusion protein technology for the generation of new, biorational, anti‐insect molecules holds significant promise. © Crown Copyright 2009. Reproduced with permission of Her Majesty's Stationery Office. Published by John Wiley & Sons, Ltd.  相似文献   

11.
A field study was conducted to investigate the persistence of tebufenozide in white spruce foliage. An aqueous suspension concentrate formulation, RH-5992 2F, was sprayed over single trees at three dosage rates, 35, 70 and 140 g of the active ingredient (AI), in 2·0 litre ha−1, using ground application equipment. Foliage was collected at different intervals of time up to 64 days after treatment and tebufenozide residues were measured by high-performance liquid chromatography. Foliage was also fed to laboratory-reared 4th- and 6th-instar spruce budworm (Choristoneura fumiferana Clemens). The data indicated that tebufenozide residues in foliage declined with time according to first-order kinetics. The average rate-constant and half-life of disappearance (DT50) were 0·0340 and 20·45 days, respectively. Larval mortality declined gradually, corresponding to the residues, but was still appreciable (49 to 70%) when the larvae were fed with foliage collected 64 days after treatment. The amount of foliage consumed by the larvae decreased when foliar residues of tebufenozide increased, thus indicating anti-feedant activity of the chemical. The LD50 values for both instars were similar and averagedc.25 ng per insect, but the LD90 values were significantly lower for 4th-instar than for 6th-instar, at 63·6 and 96·1 ng per insect respectively. This implies that, theoretically, at a foliar concentration of 1·0 μg tebufenozide g−1 foliage (fresh wt), the spruce budworm larva needs to consume 65 to 100 mg of foliage in 10 days to cause mortality in about 90% of a population of the insect.  相似文献   

12.
BACKGROUND: In this study, the effects of three saponins and one sapogenin with a triterpenoid or steroid structure in two lepidopteran insect cell lines, ovarian Bm5 and midgut CF‐203 cells, were analysed with regard to cell viability, cell membrane permeation, EcR responsiveness and DNA fragmentation. In addition, the entomotoxic action of Q. saponaria saponin with primary midgut cell cultures and larval stages of the cotton leafworm Spodoptera littoralis was tested. RESULTS: Both lepidopteran cell lines show a high sensitivity to all four sapo(ge)nins, with a concentration‐dependent viability loss and EC50 values of 25–100 µM in MTT bioassays. A trypan blue assay with Q. saponaria saponin confirmed rapid cell membrane permeation to be a cause of cytotoxicity. Saponins caused no EcR activation in Bm5 cells, but a loss of ecdysteroid signalling was observed with IC50 values of 5–10 µM . Lower saponin concentrations induced DNA fragmentation, confirming their potential to induce apoptosis. Finally, Q. saponaria saponin caused cytotoxicity in primary midgut cell cultures of S. littoralis (EC50 = 4.7 µM ) and killed 70–84% of S. littoralis larvae at pupation at 30‐70 mg g?1, while lower concentrations retarded larval weight gain and development. CONCLUSIONS: The data obtained provide evidence that saponins exert a strong activity on lepidopteran cells, presumably based on a cytotoxic action due to permeation of the cell membrane. Primary midgut cell cultures and larvae of S. littoralis showed high sensitivity to Q. saponaria saponin, indicating the insect midgut as a primary target for entomotoxicity and the potential use of saponins in the control of pest Lepidoptera. Copyright © 2012 Society of Chemical Industry  相似文献   

13.
Over a concentration range of 5.0 × 10?6?7.5 × 10?4M, the selective herbicide difenzoquat (1,2-dimethyl-3,5-diphenyl-1H-pyrazolium) caused more pronounced inhibition of potassium ion (K+) absorption by excised seedling roots of susceptible wild oat (Avena fatua L.) compared to those of tolerant barley (Hordeum vulgare L. cv. Bonanza) or wheat (Triticum aestivum L. cv. Neepawa). At 2.5 × 10?5M difenzoquat, the relative inhibition of K+ (86Rb) absorption by wild oat root segments inceased from 30% with a 10-min uptake period to 75% with an uptake period of 90 min, whereas no inhibition at all was evident for wheat root segments even after a 90-min exposure to the herbicide. An ion efflux compartmental analysis procedure demonstrated that difenzoquat did not affect the passive permeability properties of the plasma membrane of wild oat root cells. The experimental findings indicated that difenzoquat interfered directly with the process of active ion transport across the plasma membrane of root cells.  相似文献   

14.
The effects of abamectin (AVMB1) on intracellular potassium ion activity (aKi) and resting membrane potential (Em) of the skeletal muscle cells of final instar larvae of Phormia terraenovae (Diptera) were investigated using K+-selective micro-electrodes. Bathing the preparation in 10? M AVMB1(+ 1 ml litre?1 dimethylsulfoxide) for 60 min caused a significant (31%) decrease in aKi, whilst Em depolarized on average by 19 mV (nearly 50% of the original control value). The difference EK-Em increased by 9 mV, although EK (potassium equilibrium potential) remained more negative than Em. These results could be due to a cationic effect of AVMB1 possibly involving an increase in K+ and Na+ conductances of the muscle plasma membrane.  相似文献   

15.
Three 2,4‐diaminopyrimidines were tested against several insect species. They were active against lepidopteran pests with LC50 values <3 mg liter−1 for most species tested. They were also active against two‐spotted spider mite, Tetranychus urticae, (LC50 10–40 mg liter−1). Folinate, but not hypoxanthine or thymidine was found to be an effective rescue agent, requiring a concentration of 100 mg liter−1 diet to rescue half of the intoxicated larvae. The results confirm dihydrofolate reductase to be the site of action for these insecticides and are consistent with the mode of action of folinate rescue in mammals. © 2000 Society of Chemical Industry  相似文献   

16.
The results showed that the essential oil from Piper sarmentosum has strong antifeedant and toxicity effects on Brontispa longissima. The best antifeedant and contact toxicity effects were observed in the 1st-2nd instar larvae. The essential oil also displayed a notable fumigation effect on the eggs and pupae of B. longissima. It took the control-treated insects 43.34 d to complete one generation, while the insects treated with 2000 mg/L essential oil needed 73.58 d. The essential oil was analyzed by gas chromatography/mass spectrometry and 41 components were identified. Myristicin (65.22%) and trans-caryophyllene (13.89%) were the major components. Myristicin exhibited strong antifeedant and contact toxicity effects on both the 3rd instar larvae and the imagoes of B. longissima, when it showed a significant fumigation effect on the eggs and pupae of B. longissima. Another P. sarmentosum essential oil and myristicin all showed a strong inhibiting effect on the growth and development of B. longissima along with the activity of AChE, CarE, GSTs and Na+, K+-ATPase in B. longissima larvae.  相似文献   

17.
When an elicitor is applied to plants to induce resistance, one of the first detectable events is the efflux of ions from the treated tissue. Here we are the first to demonstrate that an elicitor from Mycosphaerella pinodes evokes leakage of Na+ and K+ ions from isolated cell walls of pea and cowpea in vitro, as observed for epicotyl tissues. Pharmacological experiments showed that this elicitor-stimulated leakage was sensitive to vanadate and N-(3-methylphenyl)biphenyl-4-sulfonamide (NGXT-191), that inhibit a cell wall-associated ATPase (apyrase). Vanadate or NGXT-191 suppressed elicitor-induced superoxide generation and expression of defense genes in vivo. On the basis of these results, we assume that the leakage of these ions, probably associated with an ATP-dependent process(es) in the cell wall, is likely associated with induced defenses of pea and cowpea.  相似文献   

18.
The effects of chlordimeform on rectus abdominis muscle of frog were investigated. Chlordimeform (10?3M) caused a slow contraction, and at lower concentration (10?5–10?3M) it inhibited the acetylcholine-induced contraction in noncompetitive manner. When chlordimeform was applied to the muscle of Rana catesbiana, K+-induced contraction was also inhibited in noncompetitive manner. Whereas it had no effect on caffeine-induced contraction.Chlordimeform-induced contraction was not affected by respective addition of d-tubocurarine (10?4M), procaine (10?3M), or eserine (0.3 mM), which results were same as that of K+-induced contraction. Chlordimeform, at lower concentration (10?5–10?3M), inhibits the acetylcholine- and K+-induced contractions probably owing to depression of not only the sensitivity of endplate but also the excitability of cell membrane.  相似文献   

19.
A muscarinic acetylcholine receptor (mAChR) has been demonstrated and partially characterized in larvae of the cattle tick Boophilus microplus. Its properties are compared with mAChR from an epithelial cell line from the dipteran insect Chironomus tentans. Competition studies with cholinergic ligands of different specificity revealed the muscarinic nature of the cholinergic receptors investigated in both species. In homogenates from tick larvae, specific binding sites for [3H]quinuclidinyl benzilate (QNB) with high affinity (1·2±(0·13) nM ; Bmax 22·5 pmol mg protein−1) were detected that do not bind nicotinic compounds specifically. The estimated IC50 values for nicotine, imidacloprid and α-bungarotoxin were all in the mM range. Additionally, with tick larvae, high-affinity nicotinic binding sites were detected with [3H]nicotine which could be displaced by high concentrations of imidacloprid or QNB. The estimated IC50 values for nicotine, α-bungarotoxin, imidacloprid and QNB were 43(±8) nM , 0·8(±0·2) μM , 2·8(±0·6) μM and 78(±1·9) μM , respectively. With homogenates of the non-neuronal insect cell line from C. tentans, only high-affinity binding sites for [3H]QNB were found. Muscarinic antagonists selectively displaced [3H]quinuclidinyl benzilate (QNB) binding to tick larvae homogenates. The mAChR of B. microplus preferred pirenzepine (IC50 2·13(±1·02) μM ) among different subtype-specific mAChR antagonists (4-DAMP had IC50 49·9(±9·13) μM and methoctramine had IC50 121(±14·2) μM ) indicating a type of binding site similar to the vertebrate M1 mAChR subtype. The tick muscarinic receptor seems to be a G-protein-coupled receptor, as concluded from the 4·8-fold reduction in receptor affinity for binding of the muscarinic agonist oxotremorine M upon treatment with the non-hydrolysable GTP-analogue γ-S-GTP. Binding data for the agonists oxotremorine M (IC50 71·3(±19·6) μM ) and carbachol (IC50 253(±87·1) μM ) parallel the biological efficacy of these compounds, in that, while oxotremorine M showed some activity against ticks, carbachol was ineffective.  相似文献   

20.
In vitro effects of methylene bisthiocyanate (MBT) on hyphal morphology and ultra-structure of Ophiostoma floccosum were examined using differential interference contrast, epifluorescence and transmission electron microscopy (TEM). To understand the mode of action of MBT, experiments were undertaken to measure potassium ion (K+) leakage from cells, oxygen consumption, glucose and ATP levels. Differential interference contrast microscopy indicated that MBT caused rapid changes in O. floccosum hyphae resulting in extensive vaculoation and accumulation of granular materials within the cytoplasm. Epifluorescence microscopy provided evidence that MBT treatment causes a loss in the permeability properties of the plasma membrane. TEM showed retraction of the plasma membrane from the cell wall, aggregation of cytoplasmic contents, vesiculation of membranous components, a dramatic increase in vacuolation, and eventually a complete loss in the integrity of organelles. There was a rapid efflux of intracellular K+ ions from cells, a substantial loss in K+ ions occurring within the first 5 min of MBT treatment. The rate of K+ leakage was MBT concentration treatment-time dependent. The study also showed that the effect of lower concentrations of MBT (0.01 and 0.1 mM) on respiratory activity was negligible. However, at the same concentrations, glucose consumption and ATP production were affected. Taken together, these observations suggest that the target site of MBT in O. floccosum alters membrane properties and uncouples oxidative phosphorylation from the respiratory chain.  相似文献   

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