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棉蚜对有机磷杀虫剂抗性的生化机理 总被引:31,自引:8,他引:31
本文对有机磷抗性和感性棉蚜Aphis gossypii三个种群抗性生化机制进行了讲究.首先用解毒酶的抑制剂测定药剂的解毒途径.进一步测定乙酰胆碱酯酶活力及其敏感性和多功能氧化酶、谷胱甘肽s-转移酶、α-乙酸萘酯酶和α-乙酸萘酯羧酸酯酶等解毒酶的活力.结果表明,体内条件下,多功能氧化酶与抗性有关,但在离体条件下,在棉蚜匀浆液中有内源抑制剂存在.α-乙酸萘酯酶和α-乙酸萘酯羧酸酯酶活力的增加,乙酰胆碱酯酶对杀虫剂敏感性的降低也是造成棉蚜对有机磷产生抗性的原因. 相似文献
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N-甲基取代苯基氨基甲酸酯的系列合成及其对家蝇的生物活性 总被引:6,自引:1,他引:5
利用酰氯水相简易工艺合成了52个N-甲基取代苯基氨基甲酸酯类化合物, 并测定了它们对家蝇Musca domestica的室内毒力。结果表明:烷基单取代化合物中,间位取代物的活性大于邻、对位;单卤素取代物中,邻位取代活性大于间位和对位,邻溴代物大于邻氯代物;对位硫甲基和邻位硫乙基取代物的活性均较高。对于烷基间位苯环取代化合物,在一定限度内随烷基分子量增大,化合物对家蝇的毒力增高,其次序为异丙基>乙基>甲基>未取代基。 相似文献
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寄主植物对棉蚜羧酸酯酶活性的影响 总被引:31,自引:2,他引:31
不同棉花品种对棉蚜Aphis gossypii Glov.羧酸酯酶活性具有明显的影响,在试验的7个棉花品种中,取食中棉12叶片的棉蚜α-乙酸萘酯(α-NA)羧酸酯酶活性最高(2.47微摩尔/毫克蛋白质分钟),是取食泾阳鸡脚棉种群的5.74倍.β-乙酸萘酯(β-NA)羧酸酯酶的活性以取食方渑双无的棉蚜最高(3.41微摩尔/毫克蛋白质分钟),是取食BR-S-10棉蚜的4.49倍.在取食方渑双无叶片的棉蚜中,羧酸酯酶活性大于2.5(微摩尔/毫克蛋白质分钟)的个体占28.3%(α-NA)和67.1%(β-NA),而在取食BR-S-10的种群中仅占2.6%(α-NA)和1.3%(β-NA).取食中棉12的棉蚜对β-NA与α-NA活性的比值为0.79,而取食其它棉花品种的种群β-NA与α-NA活性比值均大于1.用中棉12饲养的棉蚜对α-NA和β-NA活性均低于种群平均值的个体(CE1型)占26%;均高于平均值的个体(CE2型)占19%;对α-NA活性高于平均值,对β-NA活性低于平均值的个体(CE3型)占31%;对α-NA活性低于平均值,对β-NA活性高于平均值的个体(CE4型)占24%.取食其它6个棉花品种的棉蚜中,CE1和CE2型的比例分别为49.4—64.0%和23.4—47.2%,明显高于取食中棉12的种群,而CE3和CE4型个体仅占0—7.6%和3.4—10.4%,明显低于取食中棉12的种群.说明寄主植物对棉蚜羧酸酯酶的量和质均有影响. 相似文献
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本文研究了一系列阿赛硫磷(Acethion)类化合物对家蝇头部胆碱酯酶的抑制作用、被鼠肝羧酸酯酶的水解作用以及对家蝇(Musca domestica vicina Macq.)和小白鼠的毒性。化合物的羧酸酯酶水解速度(CO2微升)的对数值和抗胆碱酯酶活性的负对数(pI50)与烷基诱导效应指数(I)之间都存在直线关系。化合物对家蝇毒性(LD50)的对数值与抗胆碱酯酶活性的负对数(pI50)之间大致有直线关系,但有些化合物距离直线较远,这可能由于在体内易于进行活化作用使毒性增高。化合物对小白鼠毒性(LD50)的对数值与羧酸酯酶水解速度(CO2微升)对数值之间,没有直线关系。说明羧酸酯酶的水解作用不是此类化合物解毒作用的唯一因素,可能包括磷酸酶的水解作用。所合成的化合物大部分部有选择毒性,其中APd的选择比率(LD50)小白鼠/LD50家蝇)最高,为221。 相似文献
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光活化多炔类化合物对蚊幼虫的毒力 总被引:21,自引:2,他引:19
采用自制的光活化实验装置,测定了11个合成的多炔类化合物对致倦库蚊Culex quinquefasciatus 4龄幼虫的光活化毒力,发现部分化合物在近紫外光照射条件下,能明显地提高光活化毒杀效应,测得化合物5(1-苯基-4-(3,4-亚甲基二氧)苯基-丁二炔)光照与未光照处理LC50分别是0.35 μg/mL和8.89 μg/mL。实验中发现蚊虫先接触药后,再进行光照处理,才能较好地发挥毒效,而且毒杀效应与光照时间呈正相关。模拟田间试验表明,太阳光能显著提高化合物5毒杀蚊幼虫的药效。利用抗氧化剂进行猝灭作用试验,间接地证明化合物5的光活毒杀机理是与过氧化作用有关。分析结构与活性关系,发现二苯基-丁二炔衍生物比二烷基取代丁二炔活性高,苯基上不同取代基也影响光活毒杀效果,它们的活性顺序是:亚甲基二氧基>甲氧基>邻硝基>间硝基>甲基酯。 相似文献
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采用体外α-葡萄糖苷酶抑制模型对一株球毛壳菌H6的发酵液和菌丝体两种乙酸乙酯提取物进行活性评价,结果表明,发酵液乙酸乙酯提取物对α-葡萄糖苷酶具有较强的抑制活性,其IC50值为(510.76±23.46)μg/mL。采用硅胶、Sephadex LH-20、半制备高效液相等色谱技术从其发酵液乙酸乙酯提取物中分离得到12个化合物。通过各种光谱分析,依次鉴定为chaetoviridins A-B(1-2),chaetoglobosins A-D(3-6),chaetoglobosin J(7),chaetoglobosin Q(8),prochaetogobosinsⅠ-Ⅲ(9-11),vibratilicin(12),其中化合物12为首次从毛壳属中分离得到。对化合物进行α-葡萄糖苷酶抑制活性测定发现,化合物12显示弱的抑制活性,其IC50为(1 182.75±19.14)μg/mL。 相似文献
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《Bioorganic & medicinal chemistry》2014,22(17):4637-4645
γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xenopus oocytes. Thio-4-PIOL showed weak antagonism of three insect GABA receptors. The antagonistic activity of Thio-4-PIOL was enhanced by introducing bicyclic aromatic substituents into the 4-position of the isothiazole ring. The 2-naphthyl and the 3-biphenylyl analogs displayed antagonist potencies with half maximal inhibitory concentrations in the low micromolar range. The 2-naphthyl analog induced a parallel rightward shift of the GABA concentration–response curve, suggesting competitive antagonism by these analogs. Both compounds exhibited weak insecticidal activities against houseflies. Thus, the orthosteric site of insect GABA receptors might be a potential target site of insecticides. 相似文献
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1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (DDPH) is a potent α?-adrenoceptor antagonist that is currently under Phase II clinic trials. However, the fast metabolism has restricted its further use. In this paper, 11 DDPH analogs were designed according to the probable metabolism pathways of DDPH, and featured the structures of halogen, methyl, and cyano groups at the 3-, or 4-position of aromatic ring A to block the hydroxylation, and one hydroxyl group at the 3-, or 4-position of aromatic ring B to extend the duration time. These compounds were synthesized in moderate to good yields from the reductive amination of substituted phenoxyacetones with substituted phenylethylamines, and fully characterized with 1H NMR, IR, and HRMS. Biological evaluation indicated that most of the compounds exhibited strong blocking and moderate to good antihypertensive activities. It is clear that the compounds having 4-OH/3-OMe on group B exhibited higher blocking activities and longer duration time than their corresponding analogs having 4-OMe/3-OMe (and also 3-OH/4-OMe). Among them, compound 13 having bromo group at the 4-position of ring A and 4-OH/3-OMe on group B, exhibited the highest blocking activity, whereas compound 17 that had a methyl group at the 4-position of ring A and a hydroxyl group at the 4-position of ring B, was more active than potent DDPH in terms of both blocking and antihypertensive activities. In addition, the possible correlations between the blocking and antihypertensive activities are also briefly discussed. 相似文献
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Zhao G Liu C Wang R Song D Wang X Lou H Jing Y 《Bioorganic & medicinal chemistry》2007,15(7):2701-2707
Ethacrynic acid (EA), an alpha,beta-unsaturated carbonyl compound, is a glutathione S-transferase P1-1 (GSTP1-1) inhibitor. Twenty-one novel EA derivatives have been synthesized. The effects of these compounds on GSTP1-1 activity and on the proliferation of human leukemia HL-60 cells have been determined. Compounds with a halogen substitution at the 3'-position of the aromatic ring have greater inhibitory effects on GSTP1-1 activity than those of compounds with a methyl substitution there. Compounds with substitutions at both the 2'- and 3'-positions of the aromatic ring have more antiproliferative ability than those with one substitution at 3'-position. Esterification of the carboxyl group appears to increase the antiproliferative ability. 相似文献
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《Bioorganic & medicinal chemistry》2016,24(3):391-402
A series of new pymetrozine analogues containing both methyl on the imine carbon and phenoxy group at the pyridine ring were designed and synthesized. Their insecticidal activities against bean aphid (Aphis craccivora), mosquito larvae (Culex pipiens pallens), cotton bollworm (Helicoverpa armigera), corn borer (Ostrinia nubilalis) and oriental armyworm (Mythimna separata) were evaluated. The results of bioassays indicated that most of the target compounds showed good insecticidal activity against bean aphid; especially, IIIf (80%) and IIIl (80%) exhibited higher aphicidal activity than pymetrozine (30%) at 5 mg/kg, and the two compounds still showed 20% and 30% mortality at 2.5 mg/kg, respectively, whereas pymetrozine displayed no activity at the same concentration. These compounds exhibited a completely different structure–activity relationship to that of known pymetrozine derivatives, in which it is thought introducing alkyl group on the imine carbon could be detrimental to the activities. Our new result suggested that the methyl on the imine carbon and phenoxy group at the pyridine ring of phenoxy group may play additive effects on the improvement of aphicidal activity. Besides this, compound IIIs, containing an allyl at the para position of phenoxy group, exhibited excellent insecticidal activity against mosquito larvae, lepidoptera pests cotton bollworm, corn borer and oriental armyworm. 相似文献
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Kaoru Sota Takehiro Amano Makoto Aida Akifumi Hayashi Ichiro Tanaka 《Bioscience, biotechnology, and biochemistry》2013,77(5):1019-1025
As a simplified model of natural pyrethrins, trans-2,5-hexadien-l-yl chrysanthemate (V), and its 2- or 3-methyl substituted homologues (III and IV), were prepared and tested for insecticidal activities against houseflies. All these compounds retained sufficient insect toxicity to illustrate an interesting relationships between chemical structure and insecticidal activity.The cis isomer (XII) of compound V and two positional isomers, 2-methylene-4-penten-l-yl and 1,5-hexadien-3-yl chrysanthemates (XIII and XIV), were also synthesized. Of these isomers, XIII was very slightly active, but the other isomers (XII and XIV) were completely ineffective.On the other hand, the insecticidal activity of 5-hexen-2-yn-l-yl ester (XV), en-yne analogue of V, was almost the same as that of V. 相似文献
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Venkatasamy R Faas L Young AR Raman A Hider RC 《Bioorganic & medicinal chemistry》2004,12(8):1905-1920
A wide range of piperine analogues has been synthesised in order to undertake a structure-activity study of their ability to stimulate melanocyte proliferation. Results demonstrate that an aromatic ring containing at least one ether function and a carbonyl group containing side chain is essential for this activity. A number of highly active piperine analogues have been identified, for instance 1-(3,4-methylenedioxyphenyl)-penta-2E,4E-dienoic acid methyl ester (5a), 1-E,E-piperinoyl-isobutylamine (4f) and 1-(3,4-methylenedioxyphenyl)-pentanoic acid cyclohexyl amide (20). A selection of analogues has also been evaluated for their effect on melanocyte morphology and melanogenesis. The piperine analogues altered cell morphology by increasing dendrite formation leading to bi-, tri- and quadripolar cells. These same analogues were found to increase total melanin in cell cultures, although melanin content per cell was not significantly altered from control in the presence of these compounds. 相似文献
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Design, synthesis, and biological activity of novel 4-(3,4-dimethoxyphenyl)-2-methylthiazole-5-carboxylic acid derivatives 总被引:2,自引:0,他引:2
Novel 4-(3,4-dimethoxyphenyl)-2-methylthiazole-5-carboxylic acid derivatives (11-23) were synthesized from 3,4-dimethoxyacetophenone (5) in six-step procedure. Their biological activities were evaluated in the greenhouse. Some of the compounds had shown fungicidal and insecticidal activities at 375 g ai/ha and 600 g ai/ha, respectively. 相似文献
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Kaoru Sota Makoto Aida Katsumi Noda Akifumi Hayashi 《Bioscience, biotechnology, and biochemistry》2013,77(13):2287-2296
From a consideration of the structure-activity relationships, nineteen 2- or 4-thiazolylmethyl cyclopropanecarboxylates, including three benzyl-thiazolylmethyl chrysanthemates (IVf, Xb and Xc), were prepared from thioamides and α-haloketones or α-haloaldehydes and examined for insecticidal activity against houseflies. All those with benzyl substitutions on the thiazole ring were ineffective, as were the other substituents. Only 4,5,6,7-tetrahydrobenzothiazolylmethyl chrysanthemate and 2,2,3,3-tetramethylcyclopropanecarboxylate (Xf and Xlf) possessed about the same order of activity as allethrin, and their activities were 0.61 and 1.56 μg/fly respectively. 相似文献
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Expression of an aromatic-dependent decarboxylase which provides growth-essential CO2 equivalents for the acetogenic (Wood) pathway of Clostridium thermoaceticum. 总被引:8,自引:3,他引:5
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The acetogen Clostridium thermoaceticum generates growth-essential CO2 equivalents from carboxylated aromatic compounds (e.g., 4-hydroxybenzoate), and these CO2 equivalents are likely integrated into the acetogenic pathway (T. Hsu, S. L. Daniel, M. F. Lux, and H. L. Drake, J. Bacteriol. 172:212-217, 1990). By using 4-hydroxybenzoate as a model substrate, an assay was developed to study the expression and activity of the decarboxylase involved in the activation of aromatic carboxyl groups. The aromatic-dependent decarboxylase was induced by carboxylated aromatic compounds in the early stages of growth and was not repressed by glucose or other acetogenic substrates; nonutilizable carboxylated aromatic compounds did not induce the decarboxylase. The decarboxylase activity displayed saturation kinetics at both whole-cell and cell extract levels, was sensitive to oxidation, and was not affected by exogenous energy sources. However, at the whole-cell level, metabolic inhibitors decreased the decarboxylase activity. Supplemental biotin or avidin did not significantly affect decarboxylation. The aromatic-dependent decarboxylase was specific for benzoates with a hydroxyl group in the para position of the aromatic ring; the meta position could be occupied by various substituent groups (-H, -OH, -OCH3, -Cl, or -F). The carboxyl carbon from [carboxyl-14C] vanillate went primarily to 14CO2 in short-term decarboxylase assays. During growth, the aromatic carboxyl group went primarily to CO2 under CO2-enriched conditions. However, under CO2-limited conditions, the aromatic carboxyl carbon went nearly totally to acetate, with equal distribution between the carboxyl and methyl carbons, thus demonstrating that acetate could be totally synthesized from aromatic carboxyl groups. In contrast, when cocultivated (i.e., supplemented) with CO under CO2-limited conditions, the aromatic carboxyl group went primarily to the methyl carbon of acetate. 相似文献
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Sawao Murao Yasuhiro Shimizu Masaru Kameda Toyokazu Nishino 《Bioscience, biotechnology, and biochemistry》2013,77(12):3075-3077
Several analogs modifying the 6-methoxy-2-methoxymethyl-3-(3,4-methyienedioxyphenyl)-1,4-benzodioxan-7-yl group of haedoxans were synthesized and their insecticidal activity was examined. 2-(2,6-Dimethoxyphenoxy)-1-hydroxy-6-(2-methoxy-5-methoxyethoxyphenyl)-3,7-dioxabicyclo-[3.3.0]octane, which lacked the 3-(3,4-methylenedioxybenzyloxy) moiety of the benzodioxanyl group, was not insecticidal, but caused prolonged paralysis of the housefly. A compound replacing the 6-(2-methoxy-5-methoxyethoxyphenyl) by 6-(5-butoxy-2-methoxyphenyl) exhibited insecticidal activity comparable to one thirty-thousandth of that of haedosan A. It became evident that the 1,4-benzodioxane framework charging the 3-(3,4-methylenedioxy)phenyl group is important for the insecticidal activity of haedoxans. 相似文献