Comparative excretion of DDT analogues into milk of indian buffalo,Bubalus bubalis L. following oral administration

Four groups of Indian buffaloes were fed daily with 25 mg of p,p′-DDT p,p′-TDE p,p′-DDE or o,p′-DDT for 100 days. Milk was analysed for organochlorine residues during this period and also for 100 days after pesticide administration had been discontinued. For the period showing ‘plateau level’ residues, 17.2% of p,p′-DDE, 17% of p,p′-TDE, 14% of p,p′-DDT as p,p′-DDT (3.5%); p,p′-TDE (10.5%); 3.2% of p,p′-DDT as o,p′-DDT (1.3%) and o,p'-TDE (1.9%) of their administered amounts were excreted in the milk. Since these compounds were excreted at different rates, the residue levels in the milk expected from a given feed would depend on their concentration and proportional distribution in the feed. The maximum tolerable content of DDT analogues in feed was derived to be 0.1 mg kg^?1 (dry weight basis) by using the maximum accumulation coefficient and incorporation of the necessary safety margin. It is concluded that Indian buffaloes fed with rations contaminated with a total of DDT analogues below this limit will yield milk of acceptable quality. Following the termination of feeding with contaminated rations, the elimination of p,p′-DDE in the milk took the longest time and that of o,p′-DDT the shortest. These results suggest that the time required for the initial high residue concentration to decline to less than the legal limit would be determined by the relative amounts of DDE, TDE and DDT in the milk, after elimination of the potent source of contamination.     

Biota uptake of pesticides by selected plant species; the case study of Kilombero sugarcane plantations in Morogoro Region, Tanzania

This paper reports on biota uptake of pesticides by selected plant species from soil in which they are grown. The study was conducted at Kilombero sugarcane plantations and environs, Morogoro Region, Tanzania. Three species of the plant materials were collected namely sugarcane (Saccharum officinarum), guinea grass (Panicum maximum) and mango leaves (Mangifera indica). The sugarcane and guinea grass were used to reveal the plant uptake in the plantations whereas mango leaves were used to represent the environs. GPC cleaned sample extracts were analysed by GC-ECD and GC-NPD and the results confirmed using GC-MS. A total of 16 different pesticide residues were detected in soil samples and only 11 pesticide residues were detected in flora samples. o,p′-DDT had the highest concentration of all detected pesticides in soil samples with a mean concentration of 21.04 μg/kg d.w. whereas the highest concentrations of 17.16 μg/kg d.w. was recorded for p,p′-DDD in flora samples. The other DDT metabolites detected in soil samples were p,p′-DDT, p,p′-DDE, o,p′-DDE, p,p′-DDD and o,p′-DDD with concentration ranging from 2.00 to 18.30 μg/kg d.w. whereas the other pesticides detected in flora samples were p,p′-DDT α-endosulfan and γ-HCH with a mean concentration range of 3.21 to 13.54 μg/kg d.w. The paired sample t-test showed no significant difference between the concentrations of pesticides in flora and those found in soil.     

Residues of organochlorine pesticides in broilers from feed fortified with known levels of these compounds

p, p'-DDT, HEOD, endrin, heptachlor epoxide, hexachlorobenzene and lindane were fed in combination to day-old broiler chickens at levels of 0.05, 0.15 and 0.30 part/million in the feed, for a period of about 7 weeks. Birds were killed at regular intervals and samples of abdominal fat and other tissues examined for residues of the chlorinated pesticides by gas-liquid chromatography. The lipid content of each sample was determined and the residue levels calculated for the whole tissue and also for the fat contained in the sample. At the end of the 7 weeks (when in practice broilers are slaughtered) residues were highest for heptachlor epoxide, followed by hexachlorobenzene, HEOD, DDT (total), endrin, and lindane. Heptachlor epoxide residue levels in fat were 13 times the levels in the feed, for lindane the ratio was 3.3. Fat residues of each pesticide reached a plateau level relatively quickly, and these levels were proportional to the fortification rates in the feed. HEOD and p, p'-DDT alone were fed to separate groups of birds. No differences in residue build-up of these compounds were found between these groups and the groups that had received these compounds in combination with the other pesticides. The total amounts of each pesticide in the tissues were reduced when the meat was fried, probably by loss of fat during preparation and frying. For p, p'-DDT and heptachlor epoxide also smaller residue were observed in the remaining fat after frying.     

Inhibition of acetyl-coenzyme a carboxylase by coenzyme a conjugates of grass-selective herbicides

A total of 146 samples of different kinds of cheeses produced in Spain were analysed in order to ascertain the specific contamination pattern. The organochlorine compounds studied were those most commonly investigated in previous surveys: α-HCH, β-HCH, γ-HCH (lindane), γ-HCH, chlordane, aldrin, dieldrin, endrin, heptachlor, heptachlor epoxide, and the isomers and metabolites of DDT. α-HCH, β-HCH, γ-HCH, chlordane, p,p′, DDT, and p,p′-DDE were found in more than 76% of samples; p,p′-DDE and γ-HCH were the most frequently detected, with frequencies of 100 and 97.9% respectively. γ-HCH, aldrin, dieldrin, heptachlor, heptachlor epoxide, o,p′-DDT, p,p′-DDD and o,p′-DDD were observed at lower frequencies. No residues of endrin were detected in any sample. Insecticides exceeding the maximum residue limits (MRLs) were chlordane, β-HCH, α-HCH and γ-HCH, with 42, 20, eight and six samples respectively. Mean residues of organochlorines found were as follows (μ kg^?1 butterfat): α-HCH = 46.3; β-HCH = 46.5; γ-HCH = 54.2; δ-HCH = 16.9; aldrin = 16.7; dieldrin = 9.7; heptachlor = 15.9; heptachlor epoxide = 14.8; chlordane = 50.2; o,p′-DDT = 5.1; p,p′-DDT = 12.4; o,p′-DDT = 19.6; p,p′-DDD = 46.7; o,p′-DDE = 6.9; p,p′-DDE = 40.7 (.DDT = 55.0). Estimated dietary intakes (EDIs) from cheese consumption were compared to acceptable daily intakes (ADIs) for the pesticides where residues exceeded the MRL. EDIs calculated were in all cases below ADIs, and, therefore, based on the ADIs, there is no health risk involved in the consumption of cheese from Spain arising from organochlorine residues.     

Excretion of DDT residues into milk of the Indian buffalo,Bubalus bubalis (L.) after oral and dermal exposure

Three groups of buffaloes were fed with 20, 100 and 400 mg of p,p′-DDT in their daily rations. The DDT residues in the milk fat of the treated animals showed an initial rapid rise but soon attained a dose-dependent equilibrium. The transfer coefficient of DDT residues in milk at ‘plateau’ levels showed an average value of about 12%. Half-life values for the rate of decline of DDT residues during the post-dosing period were computed according to a two-open-compartment model. Dermal application of p,p′-DDT to buffaloes also resulted in excretion of a significant amount of its residues in milk. TDE was the predominant compound present in milk when buffaloes had ingested p,p′-DDT, whilst p,p′-DDT itself was present in greater quantity than its metabolites when animals were treated dermally.     

DDT and BHC residues in some body tissues of goats, buffalo, and chickens, Lucknow, India

Muscle, liver, brain, and abdominal body fat samples of goats, buffalo, and chickens, all common meat sources in India, were analyzed by gas-liquid chromatography (GLC) for residues of DDT and benzene hexachloride (BHC). A few samples of goat and buffalo bone marrow were also included. Relatively high residue levels were found in body fat and bone marrow compared with other tissues. DDT and BHC residue levels were highest in chicken body fat, averaging 4.157 ppm sigma DDT and 3.879 ppm BHC. DDT content was much higher in goat and buffalo bone marrow than in the corresponding body fat. DDT levels in brain samples were highest (0.138 ppm) in buffalo. p,p'-TDE levels were higher than p,p'-DDE levels in buffalo; overall DDT levels were lowest in goats. BHC residues were generally low in buffalo; alpha-BHC accounted for most BHC residues in brain tissues. Greater accumulations of DDT and BHC were found in leg muscles than in breast muscles of chickens.     

Studies on the induction of rat uterine ornithine decarboxylase by DDT analogs. I. Comparison with estradiol-17β activity

The effect of DDT analogs and estradiol-17β on uterine ornithine decarboxylase activity in the immature intact and ovariectomized rat was studied. Pretreatment with various doses of o,p′DDT [1-(o-chlorophenyl)-1-(p-chlorophenyl)-2,2,2-trichloroethane] or estradiol-17β caused a marked increase in the specific activity of ornithine decarboxylase in the 20,000g supernatant fraction of uterine homogenates but not in liver homogenates. Doses as low as 0.5 mg of o,p′DDT or 0.002 μg of estradiol-17β stimulated uterine ornithine decarboxylase activity in the ovariectomized rat. The peaks of activity after treatment with o,p′ DDT and estradiol-17β occurred at 6 and 5 hr, respectively. The level of ornithine decarboxylase activity in untreated groups was consistently lower in ovariectomized rats than in intact immature animals. Treatment with o,p′ DDT (10 mg/100 g body weight) of ovariectomized and intact immature rats demonstrated at 131-fold and an about 20-fold increase in uterine ornithine decarboxylase activity, respectively. Treatment of ovariectomized rats with cycloheximide or actinomycin D effectively blocked the increase in ornithine decarboxylase caused by o,p′ DDT. Similar results were obtained with cycloheximide in the intact immature rat. Animals subjected to both adrenalectomy and ovariectomy demonstrated an increase in ornithine decarboxylase activity when treated with either estradiol-17β or o,p′ DDT. Dose-response curves obtained for estradiol-17β and o,p′ DDT suggest a similar mechanism of action for the two compounds. Graphic analysis of the dose-response curves for estradiol-17β and o,p′ DDT demonstrated an ED₅₀ of 0.038 μg/100 g body weight and 1.8 mg/100 g body weight, respectively. The examination of various DDT analogs in intact and ovariectomized animals showed that o,p′ DDT was the most potent inducer of ornithine decarboxylase. The order of decreasing potency of DDT analogs was o,p′ DDT, o,p′ DDD. p,p′ DDT, p,p′ DDD, and p,p′ DDE.     

The metabolism of p,p′-DDT by the feral pigeon (Columba livia)

Male feral pigeons were dosed with ring-labeled $\text{[}{}^{14}\text{C}\text{]p,p′-}\text{DDT}$ and the tissues and droppings analyzed for total ¹⁴C, extractable ¹⁴C, and metabolites. Only 16% of an intraperitoneal dose of 1.5–2.2 mg kg^?1 was voided in the droppings over 28 days; the rate of loss reached a maximum on the 14th day and then fell quickly away. The rate of removal of ¹⁴C in droppings was low in comparison to that found in the rat and the Japanese quail. When pigeons were dosed with 32–38 mg kg^?1 DDT per bird, and killed after 77 days, 5.4% of the dose was eliminated in droppings and 87% was recovered in the body. The tissues and droppings from this experiment were analyzed for DDT and its metabolites. Of the ¹⁴C remaining in tissues 88% was accounted for as the apolar compounds DDE, DDT, and DDD. Approximately half of the ¹⁴C in droppings was present as DDE, DDT, and DDD, whereas 27–35% was apparently in conjugated form, extractable from aqueous solutions by ethyl acetate after prolonged acid hydrolysis. Two polar metabolites were isolated from the acid-released material. One was p,p′-DDA; the other was extractable from aqueous solution at pH 8 and was tentatively identified as a monohydroxy derivative of p,p′-DDT. DDE accounted for 93% of the ¹⁴C present as metabolites in tissues and droppings, clearly indicating the importance of this intermediate in this study. The metabolism of DDT in the feral pigeon is discussed in relation to its metabolism by other species.     

Species and sex differences in the reductive dechlorination of DDT by supplemented liver preparations

p,p′-DDT was converted to DDD, 1,1-dichloro-2,2-bis(p-chlorophenyl)ethane, by unheated 12,000g supernate supplemented with NADPH, made from liver of rat, mouse, hamster, quail, chicken and pigeon. The additional presence of exogenous riboflavin did not augment reduction. If, however, riboflavin was added to unheated microsomes supplemented with NADPH or NADH the rate of reduction was more than doubled.Heated 12,000g supernate, unsupplemented or containing only exogenous riboflavin, did not reduce DDT. When NAD(P)H was present, big species differences in activity occurred, the pigeon and cockerel scarcely reducing any DDT in 2 hr, the Wistar rat supernate being most active. Addition to heated 12,000g supernate of 30 μg riboflavin as well as NAD(P)H resulted in increased reductive activity for all six species. The species difference in effect of exogenous riboflavin between the pigeon and rat was also observed using four DDT analogs as substrates. A sex-related difference in activity of preheated, supplemented 12,000g supernate from livers of the chicken and Norwegian hooded rat was not found when unheated preparations were used. In contrast to the activity possessed by preheated 12,000g supernate of rat liver supplemented with NAD(P)H, similarly supplemented preheated microsomes did not reduce DDT. On adding riboflavin as well as NAD(P)H, however, preheated hepatic microsomes of both pigeon and rat produced DDD, and this activity was further increased by addition of unheated microsomal (105,000g) supernate. The biocatalytic system functioning in preheated preparations appears to need at least one component of heated microsomes, NAD(P)H and one or more water-soluble components.     

Residues of DDT in cottonseed after spraying with DDT and torbidan

DDT at 1.12 and 2.24 kg/ha a.i. and Torbidan at 5 and 10 litre formulation/ha (1 and 2 kg DDT/ha) were sprayed five times on cotton over a period of 15 weeks. Seeds from the first pick of the crop were found to contain as residues pp′-DDT and pp′-DDE [1,1-dichloro-2,2-di- (4-chlorophenyl)ethylene]. The highest residue level (0.783 parts/10⁶) was found in seeds from Torbidan 10 litre/ha treatment.     

Accumulation and distribution of pp′-DDT and related compounds in an apple orchard. II. Residues in trees and herbage

DDT residues in or on the roots and leaves of the herbage and the roots, bark, leaves and fruit of the trees are given for an apple orchard sprayed annually (1953–1969). The distribution of DDT in both the grass and the grass roots was in circular areas of residues, with maximum values at each trunk and decreasing radially to each alley. Of the spray applied at the green cluster stage 80% was deposited on the grass sward and very little, if any, directly on the soil surface. The pp′-DDT content of the grass fell rapidly with successive mowings (from which the cuttings remained in situ) from 400 μg/g at spraying to 2 μg/g after nine months. 33 g/ha pp′-DDT was found in the herbage roots (0.87% of the total residues in the soil). The residues in the bark (87.5 g/ha) were much lower than expected after 13 years spray application. There were increased amounts of pp′-DDE, pp′-TDE and pp′-TDEE relative to pp′-DDT, indicating some breakdown on the bark, but the chief losses were attributed to volatilisation and to removal by wind and rain. The residue content of root bark varied from 3 μg/g near the emerging trunk to 0.05 μg/g at a depth of 90 cm. The pp′-DDT content of leaves at leaf fall rose from <1 ng/g after a single spring spray to 8.33 μg/g following an additional spray in late June. There was a large loss of DDT from the canopy between the June spray and leaf fall (440–480 g/ha down to 25 g/ha), attributed to volatilisation. The amount of pp′-DDT on the fruit, after a single spray, was 3 ng/g fresh weight (80.9 mg/ha out of a total of 1.0–1.5 kg/ha used).     

Shell and operculum formation by immature roman snails Helix pomatia L. when treated with pp′-DDT

Roman snails (Helix pomatia) have been treated with pp′-DDT from 2 wk of age until hibernation. Taking snail size into account, relatively low doses of DDT significantly reduced shell and operculum weight whereas higher doses of DDT did not cause this response. After reemergence from hibernation, the incidence of operculum eating was significantly higher among snails hibernating late in the season, and as exposure to DDT increased so operculum eating became more prevalent.Shell thinning in snails due to pesticide is likely to have occurred in some heavily treated agricultural localities if the response of other species to DDT is similar to that of Helix pomatia.     

Effects of nereistoxin on the neuroexcitatory action of insecticides

Nereistoxin suppressed the excitatory actions of α- and γ-BHC and HEOD in the central nervous system of Periplaneta americana (L.). However, it did not affect the neurotoxic action of DDT and DBrDT. Since nereistoxin is an acetylcholine antagonist, it is postulated that BHC and HEOD act to produce high level of acetylcholine and the resulting after-discharges, while DDT and DBrDT seem to attack the noncholinergic region of insect nervous system.     

The effect of some DDT and methoxychlor analogs on temperature selection and lethality in brook trout fingerlings

The effects of several DDT and methoxychlor analogs on trout fingerling temperature selection and lethality were investigated. The molecular requirements for lethality and alteration of temperature selection were different. Only p, p′-DDT, p, p′-DDD, and p, p′-methoxychlor were toxic in the range 10–50 ppb used. All the compounds tested, except DDE-type analogs, altered temperature selection. The effect of p, p′-methoxychlor on temperature selection progressively decreased until normal values were obtained 5 days after exposure. The effect of p, p′-DDT was still pronounced 9 days after exposure.     

Distribution and breakdown of DDT in orchard soil

Amounts of DDT and its breakdown products were determined in soil in an apple orchard in Herefordshire. Samples were taken for a number of years (1972–79) after use of the insecticide in the orchard had ceased in 1969. The results were compared with those obtained in an investigation of the same orchard in 1968. From 1968 to 1979, soil residues of pp′-DDT, p′--DDT and pp′--TDE decreased gradually whereas those of pp′--DDE increased, and there were linear relationships between log (concentration) and time. The calculated time for 50% decrease in concentration (Dt₅₀) was 11.7 years for pp′--DDT, 3.3 years for pp′--TDE and 7.1 years for op′--DDT; the time for doubling the concentration for pp′--DDE was 9.1 years. Regression analysis on the two major components (pp′--DDT+pp′--DDE) indicated that the total amount (2.7 mg kg^?1) was not decreasing with time. It was concluded that during a post-spray era, the breakdown of pp′--DDT to pp′--DDE was a significant feature of the persistence of DDT, and that, in contrast to the findings of other workers who sampled when DDT was being used, there were no losses by volatilisation. There was an exponential decrease in the amount of DDT residues with increasing soil depth and approximately 90% was found in the top 10 cm of the undisturbed soil profile.     

Structural insights into the interaction between gabazine (SR-95531) and Laodelphax striatellus GABA receptors

γ-Aminobutyric acid receptors (GABARs) mediate fast inhibitory neurotransmission and are targets for insecticides. GABARs are composed of five subunits, the composition of which dictates the pharmacological characteristics of GABARs. Both competitive and noncompetitive GABAR antagonists can be used as insecticides. Gabazine is a potent competitive antagonist of mammalian α1β2γ2 GABARs; however, it is less potent against insect GABARs. To explore how gabazine interacts with GABARs, we examined whether the sensitivity of the small brown planthopper (Laodelphax striatellus) RDL GABAR (LsRDLR) to gabazine is increased when its amino acid residues are substituted with α1β2γ2 GABAR residues. In the results, two of the generated mutants showed enhanced gabazine sensitivity. Docking simulations of gabazine using LsRDLR homology models and an α1β2γ2 GABAR cryo-EM structure revealed that the accommodation of gabazine into the “aromatic box” in the orthosteric site lowered the binding energy. This information may help in designing GABAR-targeting insecticides with novel modes of action.     

Organochlorine pesticides and polycyclic aromatic hydrocarbons in water and sediment of the Bosten Lake,Northwest China

We evaluated organic pollution in Bosten Lake, Xinjiang, China, by measuring the concentrations and distributions of organochlorine pesticides(OCPs) and polycyclic aromatic hydrocarbons(PAHs). Water and sediment samples were collected from 19 sites(B1–B19) in the lake for analysis. Our analytical results show that the concentrations of total OCPs in water ranges from 30.3 to 91.6 ng/L and the concentrations of PAHs ranges from undetectable(ND) to 368.7 ng/L. The concentrations of total OCPs in surface(i.e., lake bottom) sediment ranges from 6.9 to 16.7 ng/g and the concentrations of PAHs ranges from 25.2 to 491.0 ng/g. Hexachlorocyclohexanes(HCHs) and dichlorodiphenyltrichloroethanes(DDTs) account for large proportions of the OCPs. Low α- to γ-HCH ratios in both water and sediment samples indicate possible contributions from both industrial products and lindane. DDTs in water are probably from historical input, whereas DDTs in sediments are from both historical and recent inputs. Moreover, DDT products in both water and sediments were from multiple sources in the northwestern part of the lake(B11, B12, B13, and B14). Fugacity ratios for DDT isomers(p,p′-DDE and p,p′-DDT) at these sites were generally higher than equilibrium values. These results suggest that the input from the Kaidu River and diffusion of DDTs from the sediment to the water are responsible for DDT pollution in the water. Lower-molecular-weight PAHs, which originate primarily from wood and coal combustion and petroleum sources, represent the major fraction of the PAHs in both water and sediment samples. Our findings indicate that OCPs and PAHs in Bosten Lake can be attributed primarily to human activities. A risk assessment of OCPs and PAHs in water and sediment from Bosten Lake, however, suggests that concentrations are not yet high enough to cause adverse biological effects on the aquatic ecosystem.     

几种有机氯杀虫剂防治小麦吸浆虫成虫研究

施用药剂杀灭小(?)吸浆虫成虫,是防治吸浆虫重要方法之一。以几种有机氯杀虫剂进行室内、田间杀虫作用和药效等研究,证明γ 666、艾氏剂、狄氏剂和DDT 均具有强大的触杀作用,其中以γ 666毒效最怏,DDT 最慢。γ 666及艾氏剂还具有相当强的熏蒸杀虫作用。田间试验结果也说明γ 666粉剂浓度虽低至0.1%,仍能杀虫95%以上。0.25% γ 666粉剂效果与0.5%的相若,试验也证明,不同浓度的γ 666粉剂兑土稀释为0.25%药粉,稀释土的种类,对杀虫效果均无影响,并在全国不少地区推广应用均证明效果显著,解决了药剂供应问题,扩大了防治面积。田间残效试验证明,不同浓度的666粉剂,在羽化盛期前2天施用,均能毒杀羽化盛期的成虫;但如在前5天施用,除1%粉剂效果较好外,0.25%及0.5%粉剂浓度的防治效果均不理想。     

Raf-1 is dually down regulated by p,p′-DDE via reduced thyroid hormone and activated ERK

Raf-1 is the best characterized member of the mammalian raf family. The raf-1 kinase has many important physiological functions but its regulation is complex. 1,1-Dichloro-2,2 bis(p-chlorophenyl) ethylene (p,p′-DDE), a major and important metabolite of organochlorine pesticide DDT, is a widespread environmental pollutant. Previous studies have reported that p,p′-DDE influences the MAPK pathway, but little details are known regarding how the raf-1 activity is influenced and regulated by p,p′-DDE in those events. And here, we used 20 male rats that received different doses of p,p′-DDE (0, 20, 60, 100 mg/kg b.wt) every other day by intraperitoneal injection for 10 days. Results showed that the raf-1 mRNA and protein expressions showed significant down-regulation. The thyroxine (T4) level and the protein kinase C alpha (PKCα) mRNA expression declined, but the raf kinase inhibitory protein (RKIP) up regulated. In addition, the p,p′-DDE-induced oxidative stress resulted in declines of glutathione peroxidase (GSH-PX) and superoxide dismutase (SOD) activities. The elevations of ERK mRNA level and phosphorylated ERK protein expression were also observed. Taken together, these results suggest that the raf-1 is dually down regulated by p,p′-DDE via two pathways. One pathway is that the p,p′-DDE exposure elevates RKIP level by decreasing T4 and PKCα level, and the increased RKIP eventually down regulates the raf-1. The other is that the p,p′-DDE exposure activates the ERK by oxidative stress, and the activated ERK down regulates the raf-1 through the negative feedback phosphorylation.     

Comparative metabolism of 1,1-Bis-(p-chlorophenyl)-2-nitropropane (Prolan) in mouse,insects, and in a model ecosystem

¹⁴C-labeled Prolan or 1,1-bis-(p-chlorophenyl)-2-nitropropane was found to be some-what more biodegradable than DDT. This insecticide, although highly resistant to microsomal metabolism, was degraded by elimination to 1,1-bis-(p-chlorophenyl)-1-propene, and by reduction to 1,1-bis-(p-chlorophenyl)-2-aminopropane. The major degradative pathway, however, was by oxidation to 1,1-bis-(p-chlorophenyl)-2-propanone, to 1,1-bis-(p-chlorophenyl)-pyruvic acid, to bis-(p-chlorophenyl)-acetic acid, and ultimately to p,p′-dichlorobenzophenone. Therefore the ultimate degradative products of Prolan are identical to those produced from DDT.