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1.
Inhibition of ATPase from aphid plasma membrane, sarcoplasmic reticulum (SR), and brain synaptosomal plasma membrane of locust, by 1,5-diphenyl-2-penten-1-one (dp-B), was studied. Results demonstrated that dp-B exhibited the similar effects on ATPase found in the three membranes amongst which the plasma membrane Ca2+–Mg2+-ATPase is the primary target. The effects of dp-B on Ca2+–Mg2+-ATPase activity were bi-directional: the enzyme enhanced hydrolyzation when dp-B or Ca2+ concentrations were low but inhibited significantly when at high concentrations. The inhibition of Ca2+–Mg2+-ATPase by dp-B from brain synaptosomal plasma membrane of insect is higher than that from other organizational plasma membranes of the insect. Dp-B inhibiting Ca2+- and CaM-requiring ATPase activity may be an important mechanism by which the insect gets poisoned (for example aphid).  相似文献   

2.
In rice seedlings, the organochlorine insecticide hexachlorocyclohexane (HCH) and its four major isomers—α,β, γ, and δ—have been shown to elicit their phytotoxic action by interacting with indol-3-ylacetic acid (IAA)-regulated growth and Ca2+-ATPase activity. When rice seedlings were grown in the presence of 0.34 mM HCH, seedling vigour was reduced to 33% of the control. A similar effect was observed when seedlings were grown in the presence of the γ and δ isomers, but not with the α and δ isomers of HCH. This reduced vigour could be restored by treating the seedlings with 100 nM IAA, suggesting that HCH and its isomers (γ and δ) limit either IAA synthesis or action or both. In a microsomal fraction from rice seedlings grown in the presence of either HCH or its isomers, the calmodulin-regulated Ca2+-ATPase activity was inhibited as follows: technical HCH = 46%, α isomer = 80%, β isomer = 72%, γ isomer = 65% and δ isomer = 62% of the control value, respectively. TLC analysis suggested that the various isomers of HCH are metabolised by the plant, except for the δ isotner, which accumulated. This isomer, along with the degraded products of other isomers, may be responsible for the phytotoxic action of HCH.  相似文献   

3.
A series of 25 pyrethroids were assessed for their effects on Na+-dependent norepinephrine release and on Ca2+ uptake in vitro using a crude rat brain synaptosomal preparation. The most effective pyrethroids required a concentration of 3–10 μM to promote norepinephrine release. Plotting release data versus lipophilicity (as log P) for each compound resulted in a parabolic curve with log Popt being 5.4 for maximal release. The release promoted by most of the compounds assessed at 30 μM could not be or was only partially reversed by either tetrodotoxin or substituting choline for Na+ conditions which readily reversed the release promoting effects of veratridine. Thus, many pyrethroids, particularly those without the α-cyano group, did not display their expected effects on the Na+ channel in rat brain. When assessed at 5 μM, pyrethroids inhibited, had no effect, or caused increases in the amount of Ca2+ incorporated in the presence of ATP. The effectiveness of the various pyrethroids to inhibit Ca2+ uptake again displayed a parabolic relationship with log Popt being 6.4. It was concluded that the variations in pyrethroid effects on norepinephrine release and Ca2+ uptake are not solely related to their particular chemical structures, but to lipophilicity. The effects of many pyrethroids on Ca2+ metabolism, particularly displacement of bound Ca2+, better explain the transmitter release promoting properties in vitro rather than a direct effect on the Na+ channel. No direct relationship between known toxicity to mammals and Ca2+ inhibition by pyrethroids was established.  相似文献   

4.
Two types of Ca2+/calmodulin-dependent protein kinase (CaMK) were found in Magnaporthe oryzae. MgCaMK1 and MgCaMK2 were both cloned and sequenced. High similarities in amino acid sequence to other reported CaMKs in fungi suggested that CaMKs were relatively conserved. Both MgCaMK1 and MgCaMK2 have a serine/threonine protein kinase active site and a calmodulin (CaM)-binding domain. Southern blot analysis showed that MgCaMK1 or MgCaMK2 existed as a single copy in the M. oryzae genome. Subsequently, MgCaMK1 or MgCaMK2 was expressed in Escherichia coli BL21 via a pET-32a (+) plasmid. The purified proteins exhibited protein kinase activity. The autophosphorylation and substrate phosphorylation of MgCaMK1 exhibited a Ca2+/calmodulin-dependent manner, and suggested that it belonged to the group of Ca2+/calmodulin-dependent protein kinases. However, the autophosphorylation and substrate phosphorylation of MgCaMK2 exhibited a Ca2+-dependent manner and suggested that it belonged to the group of Ca2+-dependent protein kinases.  相似文献   

5.
为了明确钙离子与东莨菪内酯联合作用的杀螨效果,进而为东莨菪内酯的开发利用提供参考,采用玻片浸渍法测定了钙离子(Ca2+)与东莨菪内酯混用对朱砂叶螨Tetranychus cinnabarinus雌成螨的杀螨毒力,并测定了活体和离体条件下对螨体内Ca2+-ATP酶活性的影响,对Ca2+的增效作用机理进行了初步分析。结果表明:Ca2+与东莨菪内酯联合使用能显著增强东莨菪内酯的杀螨效果,其中联合作用24和48 h的LC50值分别比东莨菪内酯单独处理降低20%和45%;对朱砂叶螨Ca2+-ATP酶活性的测定结果表明,无论在活体还是离体条件下,Ca2+与东莨菪内酯联用均能显著增强对Ca2+-ATP酶的抑制作用,而相同浓度的Ca2+单独作用则对Ca2+-ATP酶活性无影响,这也在一定程度上证明了Ca2+-ATP酶是东莨菪内酯的重要作用靶标之一。  相似文献   

6.
The enzymatic hydrolysis of 32P-labeled diazoxon was studied using tissue homogenates of rat and American cockroach. The order of the hydrolytic activities of rat tissues for diazoxon was as follows: liver > blood > lung > heart > kidney > brain. A liver enzyme hydrolyzing diazoxon to diethyl phosphoric acid and 2-isopropyl-4-methyl-6-hydroxypyrimidine was located in the microsomes. The activity of the microsomal enzyme was inhibited by EDTA, heavy and rare earth metal ions, and SH reagents. Ca2+ activated the enzyme and protected it from inactivation. Mitochondrial and soluble enzymes from liver and a serum enzyme also hydrolyzed diazoxon and they were also activated by Ca2+. The removal of calcium bound to the microsomal enzyme protein by dialysis against EDTA led to a partially irreversible change of the enzyme. The hydrolysis of diazoxon by the Ca2+-requiring microsomal and serum enzymes was more rapid than that of paraoxon. Hydrolysis of diazoxon did not occur in American cockroach homogenates. This difference in the capacity to hydrolyze diazoxon between mammals and insects is discussed in relation to the selective toxicity of diazinon.  相似文献   

7.
为寻找防治枸杞蚜虫的适用药剂,采用玻璃管药膜法,测定了4种拟除虫菊酯类杀虫剂对枸杞蚜虫的毒力及对其三磷酸腺苷酶(ATPase)和谷胱甘肽S-转移酶(GSTs)活性的影响。结果表明:枸杞蚜虫对联苯菊酯最敏感,LC50值为4.34 mg/L;氯菊酯、高效氯氰菊酯和甲氰菊酯的LC50值分别为17.08、40.50和184.84 mg/L。4种杀虫剂对枸杞蚜虫两种ATPase活性均有抑制作用,药剂浓度为1×10-4mol/L时,4种药剂对Na+-K+-ATPase活性的抑制率均高于对Ca2+-M g2+-ATPase的抑制率,其中对Na+-K+-ATPase活性的抑制率从高到低依次为:联苯菊酯高效氯氰菊酯氯菊酯甲氰菊酯,而对Ca2+-M g2+-ATPase的抑制率则是联苯菊酯最高(46.41%),高效氯氰菊酯最低(33.04%)。4种药剂对枸杞蚜虫GSTs活性的影响差异较大:联苯菊酯在低浓度时对GSTs具有诱导作用,高浓度时则表现为一定的抑制作用;不同浓度高效氯氰菊酯和氯菊酯对GSTs活性均表现为抑制作用,抑制率最高达85.02%;而甲氰菊酯处理后GSTs的活性则升高了193.07%~249.96%。  相似文献   

8.
N-Arylcarbamoylpyrazolines with various substituents at the para position of the carbamoyl benzene ring inhibited ATP-dependent Ca2+-uptake in synaptosomes prepared from the rat brain. The activity of these compounds was evaluated as log(1/I50), the reciprocal logarithm of half inhibitory concentration, I50 (m ), from the concentration–response curve for the inhibition of Ca2+-uptake. Among the compounds tested, methyl 3-(4-chlorophenyl)-4-methyl-1-[N-(4-trifluoromethylphenyl)carbamoyl]-2-pyrazoline-4-carboxylate was the most potent, the I50 value of which as 9·12×10−7 m . Variations in the activity in terms of log(1/I50) were quantitatively analysed using a substituent parameter, showing that the higher the electron-withdrawing effect of the substituent, the higher was the activity. The substituent effects were similar to those on insecticidal activity against the Americal cockroach. The higher the inhibitory activity against Ca2+ uptake, the higher seemed to be the insecticidal activity. Methyl(4S) - 3 - (4 - chlorophenyl) - 4 - methyl - 1 - [N - (4 - chlorophenyl)carbamoyl] - 2 - pyrazoline -4-carboxylate had higher inhibitory activity against Ca2+-uptake and higher in-secticidal activity than the R-isomer, but the difference was greater in theCa2+-uptake system.  相似文献   

9.
The action of deltamethrin on the calcium/calmodulin-dependent protein kinase (CaM-Kinase II) and phosphatase system in the rat brain synapse was studied under various experimental conditions to optimize these enzyme activities and to facilitate the studies of the mechanism of interaction of this pesticide with several components of this enzyme system. To obtain a clear-cut inhibition of this enzyme by deltamethrin the following conditions must be met: (a) the enzyme system should be purified by precipitation with ammonium sulfate (450 g litre?1) prior to the addition of deltamethrin, (b) both Ca2+ and calmodulin (CaM) should be added to the incubated media before the addition of [y-32P]ATP, (c) deltamethrin should be incubated at least 10 min (but less than 30 min) with the enzyme system before [y-32P]ATP addition, (d) the incubation temperature should be above 20°C (optimum 30°C), (e) [y-32P]ATP concentration should be in the order of 10? M (concentration adjusted using cold ATP), and (f) the incubation time with [y?P]ATP for incorporation of 32P into the protein should be in the neighborhood of 60 s. Under these conditions, the inhibitory potency of various active and inactive isomers or analogs of pyrethroids and DDT was tested. The order of the inhibitory power of these active forms of pesticides was 1 R-deltamethrin > (S)(RS) fenvalerate ≥ p,p′-DDT. Other compounds were not active at the concentration tested, indicating the differential sensitivity of this enzyme and the existence of a correlation of inhibitory power to insecticidal activity.  相似文献   

10.
Cochliobolus miyabeanus forms a specialized infection structure, an appressorium, to infect rice. Contacting a hard surface induces appressorium formation in C. miyabeanus, while the hydrophobicity of the substratum does not affect this morphogenic infection event. To determine whether the calcium/calmodulin-dependent signaling system is involved in prepenetration morphogenesis in C. miyabeanus, the effects of a calcium chelator (ethylene glycol tetraacetic acid; EGTA), phospholipase C inhibitor (neomycin), intracellular calcium channel blocker (TMB-8), calmodulin antagonists (chlorpromazine, phenoxybenzamine, and W-7), and calcineurin inhibitor (cyclosporin A) on morphogenesis and infection were examined. Addition of Ca2+ and the calcium ionophore A23187 did not affect conidial germination, while the number of appressoria decreased with higher concentrations. EGTA inhibited conidial germination and appressorium formation. The calcium channel blocker did not affect appressorium formation at any concentration; however, calmodulin antagonists and the calcineurin inhibitor specifically reduced appressorium formation at the micromolar level. One of the calmodulin antagonists, W-7, also inhibited accumulation of mRNA of the calmodulin gene within germinating conidia and/or appressorium-forming germ tubes. Thus, biochemical processes controlled by the calcium/calmodulin signaling system seem to be involved in the induction of prepenetration morphogenesis on rice.  相似文献   

11.
Isolated rat brain synaptosomes were used to evaluate the action of pyrethroid mixtures on Ca2+ influx and subsequent glutamate release under depolarizing conditions. In equipotent binary mixtures at their respective and/or estimated EC50s with deltamethrin always as one of the two components, cismethrin, λ-cyhalothrin, cypermethrin, esfenvalerate and permethrin were additive and S-bioallethrin, fenpropathrin and tefluthrin were less-than-additive on Ca2+ influx. In binary mixtures with deltamethrin always as one of the two components, esfenvalerate, permethrin and tefluthrin were additive and λ-cyhalothrin was less-than-additive on glutamate release. Binary mixture of S-bioallethrin and cismethrin was additive for both Ca2+ influx and glutamate release. Only a subset of pyrethroids (S-bioallethrin, cismethrin, cypermethrin, and fenpropathrin) in binary mixtures with deltamethrin caused a more-than-additive effect on glutamate release. These binary mixtures were, however, only additive (cismethrin and cypermethrin) or less-than-additive (S-bioallethrin and fenpropathrin) on Ca2+ influx. Therefore, increased glutamate release evoked by this subset of pyrethroids in binary mixture with deltamethrin is not entirely occurring by Ca2+-dependent mechanisms via their action at voltage-sensitive calcium channels. These results suggest that pyrethroids do not share a common mode of toxicity at presynaptic nerve terminals from rat brain and appear to affect multiple target sites, including voltage-sensitive calcium, chloride and sodium channels.  相似文献   

12.
双氧木脂素E（haedoxane E）是从杀虫植物透骨草Phryma leptostachya L.中分离出的一种对多种农林害虫和卫生害虫具有杀虫活性的化合物。本研究以东方粘虫Mythimna separata为供试昆虫,对双氧木脂素E对其幼虫杀虫作用部位进行了初步研究。电镜观察表明,双氧木脂素E对东方粘虫幼虫体壁肌具有致毒作用,能使肌细胞发生明显病变,细胞核皱缩变形,染色质浓缩,线粒体肿胀、大面积空泡化,肌质网扩张,肌原纤维排列紊乱,胞质内出现大量多泡体。酶活力测定结果也显示,双氧木脂素E能不同程度抑制Na+-K+-ATPase和Ca2+-ATPase活力。因此推测双氧木脂素E是一种作用于东方粘虫肌肉组织的肌肉毒剂。  相似文献   

13.
The toxicity of deltamethrin, bifenthrin, and endosulfan to the fourth-instar larvae of rice stem borer, Chilo suppressalis (Walker), was measured at 17, 27, and 37 °C. The three insecticides all displayed a positive temperature coefficient between 17 and 37 °C. The temperature coefficients of deltamethrin, bifenthrin, and endosulfan were 5.59, 1.68, and 2.85, respectively. However, temperature coefficients of deltamethrin and bifenthrin between 17 and 27 °C and between 27 and 37 °C varied. The inhibition of the above three insecticides to mitochondrial Na+-K+-ATPase and Ca2+-Mg2+-ATPase from the fourth-instar larvae of rice stem borer was determined at 17, 27, and 37 °C. The inhibition of deltamethrin to the specific activities of Na+-K+-ATPase and Ca2+-Mg2+-ATPase showed a negative temperature coefficient, but endosulfan exhibited a positive temperature coefficient. Inhibition of bifenthrin exhibited the contrary temperature coefficients between Na+-K+-ATPase and Ca2+-Mg2+-ATPase and a negative temperature coefficient for the former and a positive temperature coefficient for the later.  相似文献   

14.
A Ca-ATPase highly sensitive to DDT has been found in peripheral nerves of lobster, Homarus americanus. The observed I50 for this Ca-ATPase toward DDT is on the order of 10?9M and has a low temperature quotien. The ATPase seems to work over a wide range of ATP concentrations. It is stimulated by Ca2+ (optimum 0.1 mM) and shows sensitivity to Na+ (optimum 20 mM) and K+ (optimum 20 mM) ions. The fact that it is highly sensitive to ruthenium red (I50 = 10 μM) suggests that the enzyme is a Ca-ATPase and not a Mg-ATPase. Furthermore the enzyme is not a CaMg-ATPase, since the presence of Mg2+ along with Ca2+ ion is not required for its activity. DDT is found to inhibit the process of Ca2+ binding in the axonic membrane only in the presence of ATP. The evidence suggests the important role of the Ca-ATPase in regulating Ca2+ concentrations in the membrane. The possible significance of DDT inhibition of the ATPase is discussed.  相似文献   

15.
Isolated presynaptic nerve terminals prepared from whole rat brain were used to evaluate the action of deltamethrin on voltage-sensitive calcium channels by measuring calcium influx and endogenous glutamate release. Deltamethrin-enhanced K+-stimulated calcium influx and subsequent Ca2+-dependent glutamate release. The effect of deltamethrin was concentration-dependent, stereospecific, blocked by ω-conotoxin MVIIC but unaltered in the presence of tetrodotoxin. These results suggest that N-type voltage-sensitive calcium channels are a site of action at the presynaptic nerve terminal. Electrophysiological studies were carried out using rat brain Cav2.2 and β3 subunits coexpressed in Xenopus oocytes to validate such action. Deltamethrin reduced barium peak current in a concentraion-dependent and stereospecific manner, increased the rate of activation, and prolonged the inactivation rate of this channel. These experiments support the conclusion that N-type voltage-sensitive calcium channel operation is altered by deltamethrin.  相似文献   

16.
No correlation was found between the chitosan or Fusarium solani-induced disease resistance responses in pea pod tissue and fluctuations in [Ca2+], inhibition of calmodulin, blockage of Ca2+ channels or host membrane leakage. Addition of exogenous Ca2+ 3 h before or after chitosan or F. solani treatments of pea pod tissue failed to alter the host response within 6 h, the time when the host actively resists both the compatible (F. solani f. sp. pisi) and incompatible (F. solani f. sp. phaseoli) macroconidia. Additionally, Ca2+ applied exogenously 3 h before or after chitosan significantly altered the level of UV-absorbing material released from the host tissue; however, it failed to affect the chitosan's ability to elicit phytoalexin formation by 24 h. Addition of exogenous Ca2+ 3 h before or after inoculation with either the compatible (f. sp. pisi) or incompatible (f. sp. phaseoli) fungi did not significantly change the host response by 24 h. The addition of EGTA or Ca2+ channel antagonists with the chitosan treatments also failed to significantly alter the chitosan-induced host response, thereby suggesting that chitosan probably does not function in the pea system by causing a Ca2+ influx into the host tissue which might then activate the host's resistance response. Inhibition of calmodulin related activities by calmidazolium failed to inhibit the chitosan or fungal induced host response. These results suggest that the response(s) induced in pea pod tissue by chitosan treatment or fungal inoculation may not be mediated by Ca2+, calmodulin or membrane leakage.  相似文献   

17.
To determine whether Ca2+ promotes powdery mildew penetration, Ca2+-treated barley coleoptiles were inoculated with conidia of pathogenic and nonpathogenic fungi. Penetration efficiency of the pathogenic powdery mildew Blumeria graminis was enhanced by Ca2+ treatment, but that of the necrotrophic pathogen Helminthosporium sp. remained unaffected. Similarly, when actin-dependent penetration resistance is suppressed with cytochalasin A, Ca2+ treatment specifically enhanced penetration of the nonpathogenic powdery mildew Erysiphe pisi but not that of other nonpathogens. Calmodulin inhibitors suppressed the promotive effect of Ca2+ on B. graminis penetration. These results suggest that barley powdery mildew specifically requires Ca2+ and calmodulin for penetration.  相似文献   

18.
In order to develop an effective trunk‐injection agent against pine wood nematode, Bursaphelenchus xylophilus, an in vitro assay was used to examine the antinematodal activity of 58 commercially available compounds with known modes of action. Among compounds tested, the GABA receptor agonists had better anti‐nematodal activity than compounds influencing glutamate, N‐methyl‐D ‐aspartate, β‐adrenergic, dopamine, muscarinic acetylcholine and nicotinic acetylcholine receptors, as well as those inhibiting acetylcholinesterase, monoamine oxidase, 5‐hydroxytryptamine uptake and Ca2+, K+, Na+ and Cl− channels. Avermectins and milbemycins strongly inhibited propagation of the nematode. Emamectin benzoate proved to be the most active (IC95 0.050 µM ) being over 140 times more active than the active ingredient of conventional trunk‐injection agents. It is concluded that emamectin benzoate is a strong candidate for an anti‐nematodal trunk injection agent. © 2000 Society of Chemical Industry  相似文献   

19.
Signals mediating phytoalexin (PA) production were analyzed in primary leaves of oats cv. Iowa X469 treated with an elicitor victorin. Production of the PA avenanthramide A was inhibited by DPI, an inhibitor of NADPH oxidase/nitric oxide synthase (NOS) and the NOS inhibitors l-NMMA and 1,3-PBIT. However, catalase and superoxide dismutase (SOD) hardly suppressed it. From the data, NO functions as a major reactive oxygen species in signal transduction leading to PA production in the defense response of oats. EGTA, verapamil and ruthenium red inhibited PA production, suggesting that Ca2+ influx into the cytoplasm and intracellular Ca2+ movement are involved in the defense response. Trifluoperazine, a calmodulin function inhibitor, and K-252a, a serine/threonine kinase inhibitor, also suppressed the accumulation, whereas okadaic acid, a serine/threonine phosphatase inhibitor, did not suppress it, suggesting the involvement of calmodulin and protein kinase, but not of phosphatase in PA production. Received 24 December 1999/ Accepted in revised form 4 February 2000  相似文献   

20.
Recent evidence suggests that nitric oxide (NO) signaling plays an important role in plant–pathogen interactions and that aconitase is a major target of NO. In the present study on the signaling role of NO in the elicitation of defense responses in peach fruit against Monilinia fructicola and subsequent effect on brown rot disease, 15 μM NO solution induced disease resistance in harvested peaches. As a potentiated elicitor, NO induced high levels of endogenous NO and superoxide (O2 ?), hydrogen peroxide (H2O2), and NADPH oxidase and Ca2+-ATPase activity in the fruit. Aconitase activity in peach fruit was inhibited by NO. Activity of partially purified aconitase was inhibited in vitro by sodium nitroprusside (SNP) and H2O2; however, the inhibition could be relieved by carboxy-2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl 3-oxide (cPTIO) or catalase (CAT), indicating that the defense response and signals induced by NO transduction depend on aconitase and conditions leading to elevated levels of NO; otherwise, H2O2 would inactivate aconitase directly in fruit. Treatment with NO resulted in salicylic acid (SA) accumulating during storage. Higher levels of jasmonic acid (JA) were detected in NO-treated fruit 48 h after the treatment. But after NO was removed, the level of SA and JA were lower than in the control. The results suggest that exogenous NO enhances resistance of harvested peach fruit against the fungus by inducing signals such as endogenous NO, reactive oxygen species (ROS), SA and JA and by inhibiting aconitase activity.  相似文献   

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