Endosulfan-induced neurotoxicity and serum acetylcholinesterase inhibition in rabbits: The protective effect of Vit C

The neurotoxic effects and acetylcholinesterase inhibition induced by endosulfan, and the amelioration of these effects by Vitamin C (Vit C), were studied in the brains of New Zealand white rabbits. The cerebrum and cerebellum of each rabbit was examined grossly and histopathologically, and caspase-3 activity was determined by immunohistochemical methods. Twenty-four rabbits were divided into four groups (n = 6). Rabbits in Group I (END) were given a sublethal dose of endosulfan (1 mg/kg bw) in corn oil daily by oral gavage for 6 weeks. Group II (END + C) received the same dose of endosulfan and also Vit C (20 mg/kg bw) every second day during the 6 week period. Group III (OIL + C) received oral corn oil daily and Vit C every second day for 6 weeks. Group IV (OIL) received corn oil daily by oral gavage throughout the experiment. A significant reduction in acetylcholinesterase activity was observed in the END group, which was ameliorated in the END + C group. Hyperemia and slight hemorrhages in brains and cerebellums were seen in some rabbits in the END group. There were no gross cerebral or cerebellar lesions in the other groups. Hemorrhages, degenerations and slight gliosis were the marked histopathological findings of some rabbits belonging to the END group. A positive caspase-3 reaction was more severe in the END group than in the others. An ameliorating effect of Vit C on gross, histopathological, and immunohistochemical findings was observed in the END + C group. Thus, although endosulfan could cause neurotoxic effects in rabbits, this toxicity was decreased by Vit C treatment, which increased serum acetylcholinesterase activity.     

Bt与硫丹、氟铃脲对棉铃虫的联合作用

通过室内和田间试验，研究了Bt与硫丹、氟铃脲对棉铃虫的联合作用。结果表明：(1)Bt与硫丹无论以何种比例相混，对敏感品系和氰戌菊脂中抗品系均增效。(2)Bt与氟铃脲只有以1:60相混才明显增效；Bt中加入少量氟铃脲和氟铃脲中加入少量Bt则明显拮抗。（3）Bt与硫丹和氟铃脲混用，明显加快了2龄幼虫的死亡速度，混剂在处理后第3d，死亡率便明显高于Bt，而与硫丹或氟铃脲单用接近。（4）田间试验中，Bt和硫丹的混剂显著增效，Bt与氟铃脲的混剂在药后4d表现出一定的增效作用，但药后7d明显拮抗。     

Toxicity of Mixtures of Bacillus thuringiensis with Endosulfan and Other Insecticides to the Cotton Boll Worm Helicoverpa armigera

In the laboratory, low concentrations of Bacillus thuringiensis Berliner (B.t.), as ‘Dipel’ 2X applied (at about the LC₅) to cotton leaves enhanced the activity of endosulfan and reduced resistance to endosulfan from approximately seven fold to two fold in neonate larvae of Helicoverpa armigera (Hubner). Low (LC₅) concentrations of endosulfan also increased the toxicity of B.t. Both endo-sulfan and B.t. increased the toxicity of the stomach poison cryolite to H. armigera. This increased toxicity was not observed where B.t./endosulfan combinations were applied topically to larvae or where B.t. was combined with organophosphorus or pyrethroid insecticides which are considered primarily to be contact toxicants. Mixtures of B.t. and endosulfan applied at equitoxic concentrations were less toxic than similar concentrations applied alone.     

Toxicity and metabolism of endosulfan and its effect on oxygen consumption and total nitrogen excretion of the fish Macrognathus aculeatum

Experiments were conducted with the freshwater fish Macrognathus aculeatum to study the toxicity and metabolism of endosulfan and the effect of the pesticide on the oxygen consumption and total nitrogen excretion. The 96-hr LC₅₀ value was 3.5 ± 0.2 ppb. In brain, gills, gut, liver, and kidney, endosulfan was metabolized to endosulfan sulfate, but this appears to be only an intermediary step as the nontoxic endosulfan ether was found only in the liver and kidney, the principal organs of elimination of toxicants in fish. The pesticide, both at sublethal and lethal concentrations, decreased oxygen consumption and total nitrogen excretion.     

The toxicities of some analogues of dieldrin,endosulfan and isobenzan to bloodsucking diptera,especially tsetse flies

The dieldrin analogue, 1, 8, 9, 10, 11, 11-hexachloro-4, 5-exo-epoxy-2, 3-7, 6-endo-tricyclo-[6.2.1.0^{2, 7}]undec-9-ene (HEOM), and the isomeric 3, 4-exo-epoxy-and 3, 6-endo-epoxy compounds (HCE and ODA, respectively), incorporating structural modifications of the non-chlorinated ring system, were tested against adult mosquitoes (mainly Anopheles stephensi List.), tsetse flies (mainly Glossina austeni Newst.) and stable flies, Stomoxys calcitrans (L.). The order of toxicity was ODA > HCE > HEOM. In further tests of residual activity against A. stephensi, ODA was better than HCE but neither was sufficiently persistent to be a promising mosquito toxicant. Analogues of dieldrin (HEOD), endosulfan and isobenzan with reduced numbers of chlorine atoms were tested against G. austeni. In the pentachloro-analogues of dieldrin and α-endosulfan, the anti-bridge chlorine was more important than the syn-chlorine for toxicity. The general effect of reductive dechlorination was to reduce toxicity, but the effect was small for some endosulfan analogues and in one case there was an increase in toxicity. In the main, toxicities of the endosulfan analogues compared favourably with those of the dieldrin analogues. However, toxicity fell drastically following replacement of the second ethylenic chlorine in isobenzan. The effect of these structural changes on toxicity evidently varied from one series to another and was influenced in an unpredictable manner by the rest of the molecule.     

毒死蜱对子代雄鼠性激素相关基因mRNA表达的影响

有机磷类农药毒死蜱 (chlorpyrifos,CPF) 可影响雄性动物生殖系统功能。为探究胚胎早期毒死蜱暴露对雄性小鼠生殖功能的影响,于母鼠妊娠后第7天 (gestational day, GD7) 至分娩前1 d每天给予母鼠灌胃染毒10 mg/kg (b.w.) 剂量的毒死蜱,于子代雄鼠出生后第42 天处死,取血液及睾丸,测定睾丸质量,通过酶联免疫法检测血液中睾酮 (testosterone,T) 及促黄体生成素 (luteinizing hormone,LH) 含量,同时采用RT-qPCR方法检测睾丸中与胆固醇及睾酮合成相关的5个基因mRNA表达的变化。结果显示:与对照组相比,毒死蜱染毒组子代鼠睾丸质量增加了16.5%,差异极显著 (P < 0.01);血清中睾酮及促黄体生成素含量分别增加了9.9%和6.2%,但与对照差异不显著 (P > 0.05)。睾丸中胆固醇合成基因HMG-CoA synthase的mRNA表达量升高了72.9%,运输基因StAR的mRNA表达量升高了45.3%;此外,睾丸中睾酮合成基因P450scc、P450-17α和3β-HSD的mRNA表达量分别升高了95.5%、68.9%和112.0%。各基因mRNA的表达量在染毒组与对照组间均差异极显著 (P < 0.01)。研究表明,毒死蜱暴露可影响子代雄鼠睾酮合成相关基因mRNA的表达,推测毒死蜱可能是通过该途径发挥其毒性作用。     

Acute toxicity of organochlorine insecticide endosulfan and its effect on behaviour and some hematological parameters of Asian swamp eel (Monopterus albus, Zuiew)

In Asia, Monopterus albus (Asian swamp eel) is commonly found in rice fields, muddy ponds and swamp areas. Because of its habitat, it is exposed to toxic pesticides used in rice fields, especially endosulfan, which is one of the most widely used insecticides. This study aims to determine the acute toxicity of endosulfan and its effect on the behaviour and some hematological parameters of the fish. The 96 h-LC₅₀ (with 95% confidence limits) obtained in this study for M. albus was 0.42 (0.35-0.50) μg L⁻¹. After 96 h exposure to endosulfan, the fish exhibited a series of abnormal behavioural responses; these included imbalanced position, restlessness of movement, erratic swimming, tremor, flashing and lethargy. When the swamp eels were exhausted, they were laterally recumbent on the bottom and had no opercula movement. Endosulfan toxicity also caused a significant lower (p < 0.05) value of erythrocyte count, leukocyte count, hemoglobin and hematocrit as compared to the control experiment. Nevertheless, the erythrocyte cell showed an increasing trend in size. The swollen erythrocyte cells may be impaired in their oxygen-carrying capacity. Severe blood loss through the gill capillary and hematemesis of the fish may be the main reasons for the hematological changes in the test organisms. Despite its relatively bigger size (30-40 cm in length) as compared to most of the other test organisms (<5 cm in length) for endosulfan toxicity, it is interesting to find that this fish is one of the most sensitive freshwater fishes to endosulfan.     

Toxico-pathological effects of cypermethrin upon male reproductive system in rabbits

The objective of this work was to identify the reproductive toxico-pathological effects of cypermethrin (CY) in mature male rabbits. Apparently healthy adult age- and weight-matched rabbits (n = 40) were procured from the local market, kept under similar management conditions and divided into four equal groups. Different doses of CY (50, 100 and 150 mg kg⁻¹ body mass) mixed in mustard oil were injected intraperitonealy at weekly intervals in male rabbits (groups B-D) prior to mating. Group A served as control and each animal in this group received equivalent volume of mustard oil. Treatment was continued for 71 days. Decreased testicular and epididymal sperm counts were recorded mostly in dose and time dependent manner in CY-treated rabbits. The serum testosterone concentrations in CY-treated rabbits were significantly lower than those of control group. Degeneration, arrested spermatogenesis and connective tissue (CT) proliferation in testes, while sperm-less seminal plasma and tailless spermatozoa in epididymis of CY-treated rabbits were observed. It was inferred that CY-induced defects in sperms and pathological alterations in testes and epididymis.     

Chronic chlorpyrifos-induced oxidative changes in the testes and pituitary gland of Wistar rats: Ameliorative effects of vitamin C

Chlorpyrifos (CPF), a chlorinated organophosphate insecticide that is widely used in agriculture and public health, has been implicated in male reproductive toxicity. Apart from acetylcholinesterase inhibition, CPF has been shown to induce changes characteristic of oxidative stress. Therefore, the aim of the present study was to evaluate the effects of vitamin C on oxidative changes in the testes and pituitary gland of rats chronically exposed to CPF. Twenty adult male Wistar rats were divided into four groups of five animals each: Group I (S/oil) received soya oil (2 ml/kg); Group II (VC) was administered with vitamin C (100 mg/kg); Group III (CPF) was given CPF (10.6 mg/kg; ∼1/8th LD₅₀); Group IV (VC + CPF) was pretreated with vitamin C (100 mg/kg) and then given CPF (10.6 mg/kg), 30 min later. The regimens were administered orally by gavage once daily for 15 weeks. Thereafter, the rats were sacrificed and the testes and pituitary glands were evaluated for the concentration of malonaldehyde (MDA) and activities of superoxide dismutase (SOD) and catalase (CAT). The result shows that CPF increased MDA concentration and reduced activities of SOD and CAT, which were ameliorated by pretreatment with vitamin C.     

杀虫剂对中华草蛉幼虫的毒力及其选择性研究

用点滴法测定了 13种杀虫剂对中华草蛉 (Chrysopa sinia (Jieder) )幼虫的毒力 ,按敏感性由高至低依次为 :久效磷、氯氟氰菊酯、灭多威、丙溴磷、辛硫磷 >氧乐果、甲基对硫磷、甲基毒死蜱 >硫丙磷 >抑太保 >氰戊菊酯 >阿维菌素及硫丹。同时测定了多种药剂对棉铃虫 (H elicoverp a armigera Hübner)、棉蚜 (Aphis gossyp ii Glover)的毒力 ,证明多数有机磷杀虫剂及灭多威为非选择性药剂 ;具有选择性的药剂中 ,硫丹选择性最高 ,其次为氰戊菊酯。氯氟氰菊酯对中华草蛉与棉铃虫表现出一定程度的选择性 ,但对中华草蛉与棉蚜则表现为非选择性 ;随棉蚜抗药性提高 ,各药剂选择性降低。     

Hormone profile of an edible, freshwater teleost, Sarotherodon mossambicus (Peters) under endosulfan toxicity

The hormone profile of Sarotherodon mossambicus (Peters) under endosulfan (an organochlorine pesticide) toxicity was investigated by estimating the serum levels of T₃ (triiodothyronine), T₄ (thyroxine), cortisol, prolactin and insulin in control and sub-lethal (0.001 mg L⁻¹) endosulfan-exposed fish for 1, 6, 12, 24 h and 5 days. Exposure of fish to sub-lethal concentration of endosulfan caused varying changes in the levels of serum hormones studied. Based on the results obtained, it was concluded that (i) the fish registered an increased metabolic activity during the initial period followed by an adaptive lowering of metabolic rate as indicated by changes in the serum T₃ and T₄ levels, (ii) the fish showed an adaptive stress response as indicated by the reduced cortisol level which could be probably due to severe interrenal exhaustion, (iii) the increased serum prolactin levels in the fish under endosulfan exposure is indicative of a possible action of prolactin on gills and kidney towards hydromineral regulation in the fish body under pesticide stress, (iv) the fish adaptively increases its serum insulin level thereby registering a possible adaptive hypoglycemic role of the hormone to favour the transport of glucose to different tissues besides a possible lipogenic activity of the higher insulin level in fish tissue under pesticide toxicity and (v) the fish appears to exhibit a possible adaptive recovery response in its hormone profile following prolonged exposure for 24 h and 5 days.     

Effect of temperature on toxicity of pyrethroids and endosulfan, activity of mitochondrial Na-K-ATPase and Ca-Mg-ATPase in Chilo suppressalis (Walker) (Lepidoptera: Pyralidae)

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.     

Topical and residual toxicity of six pesticides to <Emphasis Type="BoldItalic">Orius majusculus</Emphasis>

The toxicity of six pesticides (four insecticides and two fungicides) to Orius majusculus (Reuter) (Hemiptera: Anthocoridae) adults and nymphs was determined using different exposure methods. Mortality upon topical exposure to abamectin, endosulfan and spinosad at recommended field doses ranged from 56% to 100% after 24 h. However, in leaf residue tests, toxicity to both life stages decreased significantly, ranging from 0% to 33% mortality. Benomyl and copper salts + mancozeb (fungicides) were much less toxic to O. majusculus, with less than 15% mortality of either adults or nymphs in topical and residue bioassays. In persistent toxicity tests, insects were exposed to the same three insecticides for 4 days; mortality varied from 38% to 100%. Egg hatching was not significantly affected when abamectin, endosulfan and spinosad were topically applied. Number of eggs laid per female in choice and no-choice tests did not differ significantly from the control. The insecticides did not show considerable repellent effect in the choice tests. Topical, residue and systemic uptake methods were also compared to determine the differences in the toxicity levels of imidacloprid, a systemic insecticide. However, 100% mortality occurred with all methods.     

The impact of simultaneous intoxication with agrochemicals on the antioxidant defense system in rat

It is known that the presence of pesticides may alter the reproductive performance of animals. We studied the effect of chronic pesticide exposure in rats injected i.p. for 5 weeks with doses between 1/50 and 1/250 LD50 of dimethoate, glyphosate and zineb, either alone or in combination. All tested agrochemicals increased the oxidative stress status in the plasma, liver, and testes, and also modified hormonal parameters involved in reproductive function. The increase in oxidative stress and damage biomarker levels, as well as the alteration of the antioxidant defence system decreased testosterone, FSH and LH levels in the plasma of pesticide-treated rats. These effects were more pronounced when pesticides were administered in combination, and should be considered indicative of involuntary exposure to residual agrochemicals.     

13种杀虫剂对龟纹瓢虫及大草蛉的毒力研究

本实验采用玻瓶药膜法，测定了6种杀虫单剂及7种杀虫混剂对龟纹瓢虫及大草蛉成虫的室内毒力。结果表明：6种单剂对龟纹瓢虫及大草蛉的毒力顺序完全一致，即高效氯氟氰菊酯＞灭多威＞辛硫磷＞甲基对硫磷＞甲胺磷＞硫丹；7种混剂对龟纹瓢虫及大草蛉的毒力顺序有所差别，但其中均以甲胺磷＋硫丹表现最为完全，而以灭多威＋甲基对硫磷表现毒力最高；联合毒力以甲基对硫磷＋辛硫磷、高效氯氟氰菊酯＋辛硫磷对2种天敌一致表现为拮抗，甲胺磷＋硫丹、灭多威＋甲基对硫磷、高效氯氟氰菊酯＋硫丹一致表现为增毒。     

Toxicity of biorational insecticides to Helicoverpa spp. (Lepidoptera: Noctuidae) and predators in cotton field

Field trials on upland cotton (Gossypium hirstum L.) during its reproductive phase were used to assess the toxicity of several biorational pesticides and chemicals to Helicoverpa armigera (Hübner) and H. puntigera Wallengren, as well as major predators at Dalby, Queensland, Australia. Moderate rate-dependent control was obtained in plots treated with neem (Azadirachta indica A. Juss) seed extract-azadirachtin (Aza) at rates of 30, 60 and 90 g/ha. Plots treated with Talstar EC (bifenthrin) applications achieved the best results, followed by treatment with alternation of chemicals (methomyl, bifenthrin, thiodicarb and endosulfan) and biorational insecticides (neem oil, azadirachtin and Bacillus thuringiensis kurstaki var. Berliner). Predators, including lady beetles, lacewings, spiders and predatory bugs, were insensitive to Aza, tooseendanin (Tsdn) andBT applications. In contrast, chemicals were very destructive of predators. All treatments provided some protection from infestation of H. armigera and H. puntigera. The effect of Aza on Helicoverpa spp. was reflected in a relatively higher yield of seed cotton harvested from Aza-treated plots compared with the control, but chemical control achieved significantly higher yields than any other treatment.     

Protective role of propolis against reproductive toxicity of chlorpyrifos in male rats

Chlorpyrifos (CPF) is causing different toxicity and propolis has been reported to be an effective antioxidant. Therefore, the present study is aimed to elucidate the possible protective effects of propolis in alleviating the toxicity of chlorpyrifos on reproductive performance, testosterone levels, enzyme activities and lipids profile in serum of male rats. Animals were divided into four groups; one orally administered (o.d.) CPF at a dose of 9 mg/kg b.w. for consecutive 70-days, propolis group (50 mg/kg b.w.), propolis and chlorpyrifos group and a control group. Results showed that there was a correlation between CPF administration and the significant decrease of the sperm counts, spermatozoon survival and testosterone level as well as increase of sperm aberrations. CPF increased significantly the lipid profile and the levels of various serum liver marker enzymes. In contrast, co-administration of propolis to CPF-treated rats restored almost most of these biochemical parameters to normal levels. On the other hand, CPF resulted in histopathological alterations in testes of male rats. However, pre-administration of propolis to CPF-treated animals improved the testicular damage and alleviates the toxic effects of CPF on reproductive functions in male rats.     

18种杀虫剂对绿盲蝽蟓的击倒活性

药膜法表明,烯啶虫胺是试验杀虫剂中对绿盲蝽蟓击倒速度最快的,KD50为5.49 min;击倒速度最慢的是硫丹,在1 h之内不能击倒绿盲蝽蟓,但24 h后死亡率为100%;在有机磷杀虫剂中,丙溴磷对绿盲蝽蟓的击倒速度是最快的,KD50为11.74 min;在拟除虫菊酯杀虫剂中,氰戊菊酯和联苯菊酯也有较快的击倒活性。     

Effects of pyrethroids and endosulfan on fluidity of mitochondria membrane in Chilo suppressalis (Walker)

The effects of pyrethroids and endosulfan on fluidity of mitochondrial membranes from Chilo suppressalis were investigated at different temperatures by steady-state fluorescence polarization using 1,6-diphenyl-1,3,5-hexatriene (DPH) molecule as probe. The results showed that changes in DPH polarization caused by the pyrethroids tested were more at lower temperature than at higher temperature, which showed a negative temperature coefficient of the pyrethroids. On the contrary, change in DPH polarization caused by endosulfan was more at higher temperature than at lower temperature. Endosulfan displayed a positive temperature coefficient. Moreover, these effects of pyrethroids and endosulfan on changes of DPH polarization were dose-dependent in mitochondrial membranes of C. suppressalis. DPH polarization value increased in the mitochondrial membranes treated by all concentrations of pyrethroids and decreased by endosulfan, and changes caused by pyrethroids were more pronounced than by endosulfan.     

Determination of residues of endosulfan and endosulfan sulfate on eggplant,mustard and chickpea

Extractable residues of endosulfan stereoisomers and its toxic metabolite, endosulfan sulfate, on a vegetable, an oilseed and a pulse crop were determined by gas-liquid chromatography. The study revealed that the alpha isomer degraded faster than the beta isomer. Beta-endosulfan accumulated during the first three days following the treatment. Endosulfan sulfate residues appeared a few days after application and decreased with time. The total endosulfan residues in the seeds from treated mustard ranged from 0.08 to 0.12 mg kg^?1 and were at or below the limit of determination (0.02 mg kg^?1) in chickpea seeds following harvest.