Clinical effects and cholinesterase activity changes in workers exposed to Phorate (Thimet)

Phorate (Thimet), an aliphatic derivative of phosphorus is a highly toxic insecticide. In order to implement the safety measures, the clinical manifestations and cholinesterase (ChE) activity were evaluated before and after 2 weeks of exposure to this insecticide in 40 male formulators. The 2 week's exposure reveal signs and symptoms of toxicity in 60% of the formulators. Gastrointestinal symptoms and lowering of heart rate (bradycardia) were more prominent as compared to the neurological symptoms. A significant depression in plasma ChE activity was observed at the end of 1st week (55%) and 2nd week (71%) as compared to the respective pre-exposure values. A recovery up to 79% of the pre-exposure activity of this enzyme was noticed 10 days after cessation of the above exposure.     

Inhibition, recovery and oxime-induced reactivation of muscle esterases following chlorpyrifos exposure in the earthworm Lumbricus terrestris

Assessment of wildlife exposure to organophosphorus (OP) pesticides generally involves the measurement of cholinesterase (ChE) inhibition, and complementary biomarkers (or related endpoints) are rarely included. Herein, we investigated the time course inhibition and recovery of ChE and carboxylesterase (CE) activities in the earthworm Lumbricus terrestris exposed to chlorpyrifos, and the ability of oximes to reactivate the phosphorylated ChE activity. Results indicated that these esterase activities are a suitable multibiomarker scheme for monitoring OP exposure due to their high sensitivity to OP inhibition and slow recovery to full activity levels following pesticide exposure. Moreover, oximes reactivated the inhibited ChE activity of the earthworms exposed to 12 and 48 mg kg⁻¹ chlorpyrifos during the first week following pesticide exposure. This methodology is useful for providing evidence for OP-mediated ChE inhibition in individuals with a short history of OP exposure (≤1 week); resulting a valuable approach for assessing multiple OP exposure episodes in the field.     

Subacute effects of a phosphorothionate pesticide on mixed function oxidases of wistar rats

Abstract

Subacute oral toxicity of a newly developed phosphorothionate insecticide (2‐butenoic acid‐3‐(diethoxy‐phosphinothioyl) methyl ester), coded as RPR‐2, was studied in male rats by oral (multiple) intubation of low (0.014 mg kg^‐1 day^‐1), medium (0.028 mg kg^‐1 day^‐1), and high (0.042 mg kg^‐1 day^‐1) dose for 90 days. The medium and high dose produced toxic symptoms along‐with some mortality (20%) occurred in the high dose treated rats. The medium and high doses caused significant inhibition in cytochrome P‐450 activity in liver, lung, kidney and brain tissues at 45 and 90 days. The high dose caused significant decrease in cyt.b₅ activity of all the four tissues at 45 and 90 days. Whereas, medium dose brought such effect in liver and lung at 45 and 90 days. Kidney and brain cyt.b₅ activity decreased significantly at 90^th day due to medium dose. Low dose also caused inhibition in cyt.b₅ activity in brain at 90^th day. Cytochrome P‐450 reductase activity was decreased significantly in liver, lung, kidney and brain at 45 and 90^th by the medium and high dose. The results indicated that RPR‐2 had potential to modulate hepatic and extra‐hepatic cyt.P‐450 dependent monooxygenase system of rat due to subacute exposure. These metabolic alterations were quite reversible after 28 days withdrawal of treatment.     

Effects of the organophosphate insecticide azinphos-methyl on the reproduction and cholinesterase activity of Biomphalaria glabrata

Azinphos-methyl is an organophosphate insecticide used for pest control on a number of food crops in many parts of the world. The snail Biomphalaria glabrata is a freshwater gastropod widely distributed in South America, Central America and Africa. The aim of the present work was to investigate whether azinphos-methyl causes alterations in the reproduction of B. glabrata. To this end, gastropod pigmented specimens were exposed to various concentrations of the insecticide (0.021, 0.5, 2.5, and 5 mg L⁻¹) for either 2 or 14 d. Along 14 d, several reproduction parameters and cholinesterase (ChE) activity were evaluated. In each group, the number of egg masses, the number of eggs per mass, the number of hatchings, the time to hatching, and the survival of the offspring after one month of treatment was evaluated. The results showed that, depending on the concentration and time of exposure, azinphos-methyl induced alterations in the reproduction of B. glabrata. These alterations were mainly represented by a decrease in the number of egg masses, and, in some cases, by a lower number or even the total absence of hatchings. Thus, the gastropods exposed to 2.5 and 5 mg L⁻¹ of azinphos-methyl for 14 d showed ChE inhibitions higher than 35% along time and completely lost their ability to reproduce. On the other hand, exposure to high acute concentrations or exposure to low concentrations for 14 d resulted in ChE inhibition equal to or lower than 35% between 7 and 14 d of treatment and similar alterations in reproduction. These were represented by a decrease in the number of egg masses. At low pestice levels, the number of egg masses and the number of offspring resulted to be more sensitive biomarkers than ChE inhibition. It is concluded that the insecticide azinphos-methyl can cause a decline in the reproductive performance of B. glabrata.     

Effect of four experimental insecticides on enzyme activities and levels of adenosine triphosphate in mineral and organic soils

Abstract

A laboratory study was conducted to determine the effect of four experimental insecticides, DOWCO429X, DPX43898, tefluthrin and trimethacarb, on enzyme activities and levels of adenosine 5'‐triphosphate (ATP) in mineral and organic soils. DOWCO429X decreased urease activity in organic soil after 7 days while a stimulatory effect was observed with most treatments after 14 days. No inhibition on acetylene (C₂H₂) reduction by nitrogenase was evident with any of the insecticides in either soil. With the exception of DOWCO429X and tefluthrin at 7 days in organic soil, none of the insecticide treatments inhibited dehydrogenase activity in either soil. Dehydrogenase activity, measured by formazan formation, was greater in many samples in sandy loam than the control throughout the experiment. No inhibitory effect was observed on amylase activity after 2 or 3 days in sandy soil. A stimulatory effect was apparent in many samples after 2 days in organic soil. All insecticide treatments in sandy soil reduced invertase activity at 2 days. However, none of the experimental insecticides inhibited invertase activity after 3 days. A stimulatory effect in invertase activity was apparent in most cases at 2 days in organic soil and no difference was observed after 3 days. Phosphatase activity in insecticide treated samples was equal to or greater than that of control in sandy soil after 2 h. With the exception of DPX43898, the insecticides depressed phosphatase activity in most organic soil samples. The insecticides did not affect ATP levels in either soil. Results indicated that the chemical treatments at the levels tested did not significantly affect activities of enzymes or level of ATP in both soils.     

Genotoxicity of methyl parathion in short‐term bacterial test systems

Abstract

Genotoxicity of the insecticide methyl parathion was investigated in Salmonella typhimurium and Escherichia coli bacterial test systems for the detection of back mutations and DNA‐damage. Methyl parathion was mutagenic to S. typhimurium strain TA100 after activation with rat liver microsomal and cytosolic enzymes. In DNA repair tests, methyl parathion was effective in inducing damage to the S. typhimurium strain TA1538 which lack excision repair compared to the strain TA1978 which is proficient in excision repair mechanisms. Normal laboratory light conditions had no effect on the mutagenicity tests, however, exposure of methyl parathion in the petri dish containing the tester strain TA100 and rat liver microsomal and cytosolic enzymes reduced the mutagenic activity and increased the toxic effects of methyl parathion.     

Effects of deltamethrin on hepatic microsomal cytochrome p450‐dependent monooxygenases in carp

Abstract The in vivo effects of sublethal concentrations of deltamethrin (DM), a pyrethroid insecticide, on the hepatic microsomal cytochrome P450 (Cyt P450) content and the Cyt P450‐dependent monooxygenase activities (para‐nitrophenetole‐O‐deethylase, pNPOD; aminopyrene‐N‐demethylase, APND; ethylmorphine‐N‐demethylase, EMND; 7‐ethoxycoumarin‐O‐deethylase, ECOD; and ethoxyresorufin‐O‐deethylase, EROD) were examined in adult carp (Cyprinus carpió L.).

0.2 μg/1 DM treatment resulted in significant increases in APND, EMND and ECOD activities, whereas 2 μg/1 DM resulted in significant inhibitions of all studied isoenzyme activities with the exceptions of pNPOD and APND after 72 h. EROD was the only enzyme for which a slight increase in activity was observed. On repeated treatment, Cyt P450 could not be detected after 48 h, but the Cyt P420 level increased. All tested isoenzyme activities were inhibited, with the exception ofthat of EROD, which was enhanced.

All these changes in enzyme activities and Cyt P450 content demonstrate the effects of DM on fish. DM treatment at low concentration is presumed to cause induction of the Cyt P450‐dependent monooxygenases which may lead to faster metabolization of the insecticide. In contrast, DM at higher concentration strongly inhibited the activities of the studied enzymes. This finding may be due to the damaging effect of DM on the xenobiotic metabolizing enzyme systems offish.     

The aerobic soil degradation of spinosad ‐ a novel natural insect control agent

Abstract

Spinosad is a natural product with biological activity against a range of insects including lepidoptera. It is comprised of two major components namely spinosyns A and D. The degradation of spinosad in soil under aerobic conditions was investigated using two U.S. soils (a silt loam and a sandy loam) which were treated with either ¹⁴C‐spinosyn A or ‐spinosyn D at a 2X use rate of 0.4mg/kg soil for spinosyn A and 0.1mg/kg for spinosyn D. Further samples of soil were pre‐sterilised prior to treatment in order to establish whether spinosyns A and D degrade abiotically. Flasks of treated soil were incubated in the dark at 25°C for up to one year after treatment.

HPLC and LC‐MS of soil extracts confirmed that the major degradation product of spinosyn A was spinosyn B, resulting from demethylation on the forosamine sugar. Other dégradâtes were hydroxylation products of spinosyns A and B, with hydroxylation probably taking place on the aglycone portion of the molecule. Half lives were similar for both spinosyns and were in the range 9–17 days, with longer half lives in the pre‐sterilised soils (128–240 days) suggesting that degradation was largely microbial.     

Short communication

Abstract

The presence of the insecticide carbaryl (Sevin) and its decomposition product l‐napthol was confirmed in irrigation and drainage canal water. However, their residues disappeared from the water 6 days after application.     

Effects of sublethal exposure to a pesticide on levels of energetic compounds in Anguilla anguilla.

Abstract

The effect of two sublethal fenitrothion concentrations (0.02 and 0.04 mg/L) on the energy metabolism of the european eel Anguilla anguilla and its recovery from intoxication was investigated. Analysis of various parameters such as glycogen, proteins and total lipids was made on liver and muscle eel tissues after 2, 8, 12, 24, 32, 48, 56, 72 and 96 hr of fenitrothion (0,0‐dimethyl 0–3‐methyl‐4‐nitrophenyl phosphorothioate) exposure. Subsequently, the fish were allowed recovery periods of 8, 12, 24, 48, 72, 96, 144 and 192 hr in clean water, and the same parameters were again evaluated. The results obtained during the exposure to the pesticide as well as during the recovery phase were used to calculate the caloric content in both tissues of A. anguilla. A reduction in energy reserves in the selected tissues was observed after exposure to both fenitrothion concentrations and the caloric content in those animals was lower than in the controls. Most of the metabolic disorders did not persist after allowing recovery in clean water during a week.     

Fate of 14C‐lindane in a rice‐fish model ecosystem*

Abstract

A model ecosystem has been used to evaluate the impact of ¹⁴C‐lindane on rice‐fish agricultural system. The distribution of ¹⁴C‐residues among the constituents of the model ecosystem was studied over a period of 90 days. The insecticide was found to be readily absorbed by the roots and translocated to all parts of the rice plant. The peak level in the shoots (26 ppm) and roots (105 ppm) of plants was reached to within three weeks. Lindane was concentrated in fish and residues as high as 90 ppm could be detected after 30 days.

The major part of the residues present in the different constituents of the ecosystem could be extracted with hexane and proved to contain soley the parent compound. The data obtained show that lindane possesses a relatively low biodegradability in fish and in rice plant. The insecticide accumulates in fish and rice plant to considerable extent.     

Persistence of diflubenzuron and bay sir 8514 in natural and sterile sandy loam and organic soils

Abstract

Disappearance rates of 10 ppm technical diflubenzuron (N(((4‐chloro‐phenyl)amino)carbonyl)‐2,6‐diflurobenzamide, Dimilin^®) and BAY SIR 8514 (2‐chloro‐N(((4‐trifluoromethoxyphenyl)amino)carbonyl)benzamide) applied on quartz sand to natural sandy loam and muck soils were significantly greater than for the corresponding sterilized soils, e.g. 47–51% vs. 68–87% BAY SIR 8514 and 2–12% vs. 80–87% diflubenzuron remaining at 12 wk, indicating that soil microorganisms play a major role in their degradation. Kinetic analysis of the data based on a first order dependence on the insecticide concentration showed that the rate constants for these disappearance reactions decreased with time.     

Root uptake,translocation, accumulation and dissipation of the botanical insecticide,azadirachtin, in young spruce trees

Abstract

A formulation containing the biopesticide azadirachtin‐A (AZ‐A), extracted from the seeds of neem tree, Azadirachta indica A. Juss, was applied (10 μg/mL) in a nutrient solution (200 mL) to the roots of young spruce trees [Picea glauca (Moench) Voss]. The uptake, translocation, persistence and dissipation of AZ‐A in spruce were studied. The insecticide was taken up by the root system, translocated via xylem vessels and accumulated in the photosynthate sinks (areas of new growth, especially shoots), confirming that AZ‐A is systemic. The peak AZ‐A concentrations (μg/g, fresh weight) in the shoots (5.16 ± 0.73) and needles (2.56 ± 0.31) occurred at 8 and 15 d after treatment, respectively. The AZ‐A concentrations in bark and wood during this period were very low, however they were high in the root samples. The dissipation of AZ‐A from the shoots was rapid compared to other matrices. The initial (0‐d) and final (20‐d) AZ‐A concentrations (μg/mL) in the nutrient solution were 8.99 ± 1.24 and 3.24 + 0.55, respectively. The dissipation of AZ‐A in the nutrient solution followed first‐order kinetics. Dissipation half‐life (DT₅₀) and rate constant (C), calculated from the nonlinear regression equation (Y = 8.400 e^‐00544t), were 12.74 d and 0.0544, respectively. Usefulness of AZ‐A as a systemic insecticide in forest insect control programs is discussed.     

Dissipation of Phosalone and Diazinon in Fresh and Dried Alfalfa

The objectives of this study were to determine the persistence of phosalone (S-6-chloro-2,3-dihydro-2-oxobenzoxazol-3-ylmethyl O, O-diethyl phosphorodithioate) and diazinon (O,O-diethyl O-2-isopropyl-6-methylpyrimidin-4-yl phosphorothioate) residues in fresh and baled alfalfa under field conditions. Plots of alfalfa were sprayed with each insecticide. Fresh alfalfa was sampled up to 20 days after treatment, and dried alfalfa was sampled up to 25 weeks after baling. Samples were analyzed for residues using high performance liquid chromatography (HPLC) equipped with a UV detector. The half-lives of diazinon and phosalone in fresh alfalfa were 1.8 and 3.3 days, respectively. In baled alfalfa the half-life of diazinon and phosalone were 2.8 and 16.7 weeks, respectively. No diazinon residues were detected in baled alfalfa, sampled after week 9, although the concentration of phosalone found at week 25 was 5.51 mg/kg.     

Effects of DDT and piperonyl butoxide on the metabolic alterations in pigeon (columba livia)

Abstract

Effect of acute doses of technical grade of dichloro diphenyl trichloro ethane (DDT) and piperonyl butoxide (PB) on hepatic micro‐somal cytochrome P₄₅₀ (Cyt. P450) and cytosolic glutathione‐S‐transferase (GST) activity in pigeon were studied after 24 hours of treatment. A completely reverse trend of changes in Cyt. P450 and GST activity were found as increase in Cyt. ?450 paralleled with decrease in GST activity following exposure to DDT. However, intensity of changes in Cyt. P450 was greater than that of GST. A dose dependent decrease in Cyt. ?450 and GST activity was observed after PB treatment. The study may, therefore, throw some light on metabolic alterations in wild birds resulting from environmental pollution by DDT and allied chemicals.     

Biochemical effects of some organo‐phosphorus insecticides on new targets in white rats

Abstract

The three S‐n‐propyl phosphates and phosphothioates: RH 218, profenofos and prothiophos were compared with fenitrothion in their potential as inhibitors of rat liver and brain AChE. Fenitrothion was more potent as an inhibitor than the three S‐n‐propyl derivatives. Incubation of hepatic protein enhanced ChE inhibition in brain in the case of fenitrothion, while it reduced the inhibitory effect of the S‐n‐propyl derivatives. On the other hand, the four organophosphorus esters caused hypoglycemia in both male and female rats and also reduced their blood urea with different degrees.     

Dermal exposure to pesticides modifies antioxidant enzymes in tissues of rats

Abstract

Superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) activities were determined in rat tissues after dermal exposure to pesticides. Two experiments were conducted in male SD rats, 190–210 g body weight. Acephate (ACP), methamidophos (MAP) and nicotine (NIC) were dissolved either individually or together in 0.25 mL of 50% ethanol, which contained: AP=12.6 or MAP 1.3 or NIC= 9.6 mg; EXP 1 ‐ individual pesticide exposure; 64 rats, 16/group; EXP 2 ‐ mixture of AP+MAP+NIC at levels of IX, 2X, 3X; 48 rats, 12/group; 0.25 mL of solution or ethanol (Controls) was applied to 25 mm² area of shaved skin 3 times a week. Half the rats were terminated after 4 weeks and the rest after 4 weeks of stopping exposure. Single pesticides decreased erythrocyte (RBC) SOD by 17 % after exposure and in the NIC group after post exposure (P#0.05). Increasing concentrations of AP+MAP+NIC mixture elevated RBC SOD by 22 % in the 2X and 3X groups and CAT by 13 % in the 3X group (P#0.05); post exposure increased RBC SOD by 2–3 fold and CAT activity by 13 % in all 3 groups. Liver GPX increased by 30–40 % and CAT decreased by 12 % in all exposed and post exposed groups (P#0.05). The results suggest that dermal exposure to mixtures of pesticides can selectively induce SOD, CAT and GPX activities in RBC and liver.     

Enhanced degradation of carbofuran in pacific northwest soils

Abstract

Persistence of ¹⁴C‐carbonyl carbofuran was measured in Pacific Northwest soils that had received 1–14 applications of the insecticide for root weevil control on perennial crops. Insecticide decay curves were obtained in nonautoclaved soil and several autoclaved soil samples from previously‐treated fields and in nonautoclaved soils from paired control sites not previously treated with carbofuran. The insecticide usually degraded faster in soil from previously‐treated fields than in soil from corresponding control fields. Among 26 previously‐treated fields, the pseudo half‐life (time for 50% loss) of carbofuran was < one wk in 11 soils, 1–3 wks in 8 soils and > 4 wks in the remaining soils. Among the nontreated control fields the pseudo half‐life was > than 2 wks in all cases and > than 15 wks in 5 of the soils. The carbofuran decay curve always possessed an initial lag phase where soil mixing enhanced insecticide decline. Carbofuran degraded very slowly in autoclaved soil samples. The half‐life of carbofuran exceeded 16 wk in all autoclaved soils tested and in most instances 85–90% of the original dosage remained when the tests were terminated 112 days after treatment. These results provided evidence that many of the soils which received applications of carbofuran over the past several years have developed a capacity to degrade carbofuran very rapidly.     

Some toxicological aspects op methamidophos exposure in mice 1

Abstract

Cholinesterase activity in the brain, RBC and plasma of Swiss mice was determined following different routes of administration of methamidophos. Continuous feeding with the insecticide caused a progressive inhibition of both plasma‐ and erythrocyte enzymes. The effect of methamidophos was more pronounced when applied in diet than when administered dermally or intraperitoneally. Following a single injection (i.p.) of methamidophos, the brain enzyme showed maximum inhibition 24 hr following treatment. At the appearance of tremors, the plasma and RBC‐enzymes showed considerable inhibition, the former being more inhibited. The plasma enzyme appears to be the most sensitive enzyme and may be taken as a suitable index for exposure to methamidophos.     

Foliar washoff of pesticides (FWOP) model: Development and evaluation

Abstract

The Foliar Washoff of Pesticides (FWOP) Model was developed to provide an empirical simulation of pesticide washoff from plant leaf surfaces as influenced by rainfall amount. To evaluate the technique, simulations by the FWOP Model were compared to those by the foliar washoff algorithm of the Chemical, Runoff and Erosion from Agricultural Management Systems (CREAMS) Model. The two algorithms were linked individually to the Pesticide Runoff Simulator (PRS) for the comparison. Five years of test data from a Mississippi watershed were used to evaluate six insecticides (carbaryl, profenofos, methyl parathion, permethrin, phorate, and toxaphene).

Initially, the FWOP model was used to evaluate the relative impact of chemical distribution (foliage versus soil) on the subsequent foliar washoff and soil surface contributions to runoff losses. Results indicated that runoff losses were low If all of the insecticide was applied to the foliage whereas high losses occurred if applied only to the soil. When an assumed application was distributed between the plant and soil (i.e., 90% to foliage and 10% to soil), predicted runoff losses compared well with observed field data (<3% of the application rate).

Except for toxaphene, the FWOP model generally predicted less washoff and subsequent runoff losses than the CREAMS approach. Simulated toxaphene washoff losses were in good agreement with observed field data. Statistical comparisons of the two modeling approaches using the Kolmogorov‐Smirnov test showed differences in the two cumulative frequency distributions for washoff but smaller differences for runoff. Average 5‐year runoff losses, however, were greater using the CREAMS approach—by factors of 2, 3, and 3 for profenofos, methyl parathion and phorate, respectively.

Results from this study will be useful for upgrading current exposure assessment models to more accurately address foliar washoff losses of pesticides as well as for assessing the impact of foliar‐applied chemicals on environmental quality.