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Effect in vitro of propoxur on the specific activity of calcium stimulated ATPase and calcium uptake was studied in the rat brain synaptosomes. The data suggest that propoxur might disrupt the synaptic function by altering the calcium dependent ATP hydrolysis and calcium uptake in the central nervous system.
In southern Iran, adults of Anopheles stephensi, the main vector of malaria, are resistant to DDT, dieldrin and malathion. Susceptibility tests carried out with propoxur-impregnated papers during 1976-86 in 5 villages in Minab County, showed that, despite 10 years of propoxur application twice a year in dwellings, An. stephensi remained susceptible to this insecticide.
Propoxur applied aerially at 4.7 liters/ha was an effective adulticide against organophosphate resistant Culex tarsalis. Applications by fixed-wing and helicopter underslung spray systems equipped with hydraulic nozzles provided good coverage of test areas as indicated by the mortality patterns of sentinel mosquitoes. However, the propoxur wettable powder in larvicide oil formulation was dispersed in a very broad particle range. The fixed-wing (Ayres Thrush) aircraft treated 260 ha (640 acres) in 45 min and could carry a full load of 1500 liters (400 gal) at temperatures in excess of 38 degrees C. In contrast, the helicopter (Bell UH-1) with an underslung spray system (Simplex Model 6800) required over 2 hrs to treat the same area at lower temperatures and could not carry a full load of 570 liters (150 gal) at temperatures greater than 38 degrees C.
Ten dogs were fitted with 10% propoxur-(0-isopropoxyphenyl methylcarbamate) and 10 dogs were fitted with 16% carbaryl-(1-naphthyl-N-methylcarbamate) impregnated flea collars. Ten cats were fitted with carbaryl-impregnated flea collars. There were 5 control animal for each trial. Insecticidal activity against experimental infestations with the cat flea (Ctenocephalides felis) was evaluated. The propoxur collars on dogs reduced the flea populations by 90% within 2 days of infestation for at least 13 weeks. By the 16th week, the flea population was reduced 65% in 2 days and 87% in 7 days. In subsequent infestations, efficiency was less than 80% after 7 days. Carbaryl collars on dogs reduced the flea population by as much as 80% in 2 days for a period of 16 weeks. An efficiency of at least 80% at 7 days was maintaned for 17 weeks. Carbaryl collars on cats reduced the flea population within 2 days by 80% or more for a period of at least 19 weeks--the last experimental infestation.
The effect of the carbamate insecticide, propoxur, on yolk synthesis in the ovarioles of the blow fly, Chrysomyia albiceps (Wiedemann) was studied. Histochemical studies showed that DNA, RNA, protein and lipid synthesis in propoxur--treated ovarioles decreased as compared to that in non-treated ovarioles, with some deteriorations in the chromatin materials in the nuclei of some nurse cells. On the other hand, the synthesis of carbohydrate is more or less not affected.
Three carbamate insecticides (propoxur, methomyl, and aldicarb) were evaluated for their ability to induce micronuclei (MN) in vitro using cultured Chinese hamster ovary (CHO) cells, and in vivo in mouse bone marrow erythrocytes. In vitro, all three insecticides induced a significant increase in micronucleated binucleate cells, which was generally both dose and sample time dependent. The in vivo studies involved treating male BALB/c mice by different routes, either once or on 3 consecutive days, followed by multiple or single sampling. Treatment by intraperitoneal injection or oral gavage induced a significant increase in micronucleated reticulocytes (MNRETs) in peripheral blood. For all three chemicals, the MN response depended on sample time and the number of treatments, while for aldicarb, the response depended also on the route of exposure. These positive results demonstrate that propoxur, methomyl, and aldicarb are capable of inducing structural and/or numerical chromosomal aberrations in mammalian cells either in vitro or in vivo. Furthermore, based on the results obtained, on optimal in vivo MN protocol for carbamate insecticides is a single treatment followed by blood sampling at 24 and 48 hr after treatment.
To compare the toxicity of seven N-methyl carbamates, time course profiles for brain and red blood cell (RBC) cholinesterase (ChE) inhibition were established for each. Adult, male, Long Evans rats (n=4-5 dose group) were dosed orally with either carbaryl (30 mg/kg in corn oil); carbofuran (0.5 mg/kg in corn oil); formetanate HCl (10 mg/kg in water); methomyl (3 mg/kg in water); methiocarb (25 mg/kg in corn oil); oxamyl (1 mg/kg in water); or propoxur (20 mg/kg in corn oil). This level of dosing produced at least 40% brain ChE inhibition. Brain and blood were taken from 0.5 to 24 h after dosing for analysis of ChE activity using two different methods: (1) a radiometric method which limits the amount of reactivation of ChE activity, and (2) a spectrophotometric method (Ellman method using traditional, unmodified conditions) which may encourage reactivation. The time of peak ChE inhibition was similar for all seven N-methyl carbamate pesticides: 0.5-1.0 h after dosing. By 24 h, brain and RBC ChE activity in all animals returned to normal. The spectrophotometric method underestimated ChE inhibition. Moreover, there was a strong, direct correlation between brain and RBC ChE activity (radiometric assay) for all seven compounds combined (r(2)=0.73, slope 1.1), while the spectrophotometric analysis of the same samples showed a poor correlation (r(2)=0.09). For formetanate, propoxur, methomyl, and methiocarb, brain and RBC ChE inhibitions were not different over time, but for carbaryl, carbofuran and oxamyl, the RBC ChE was slightly more inhibited than brain ChE. These data indicate (1) the radiometric method is superior for analyses of ChE activity in tissues from carbamate-treated animals (2) that animals treated with these N-methyl carbamate pesticides are affected rapidly, and recover rapidly, and (3) generally, assessment of RBC ChE is an accurate predictor of brain ChE inhibition for these seven pesticides.
A 28-day oral exposure with 8.51, 3.40, and 0.851 mg/kg propoxur (PR) and 4.67, 1.87, and 0.467 mg/kg pirimicarb (PI) was performed in male Wistar rats, and the occurrence of numerical and structural chromosome aberrations and the changes in certain immune function parameters (plaque-forming cell (PFC) assay, delayed-type hypersensitivity reaction) and in some basic toxicological (body weight gain and weights of brain, thymus, lung, heart, liver, spleen, kidneys, adrenals, and popliteal lymph node) and hematological (white blood cells, red blood cells, hematocrit (Ht), mean cell volume of red blood cells (MCV) cell content of the femoral bone marrow) parameters were investigated. The high dose of PR increased the relative liver weight and the cell content of femoral bone marrow, and all three doses increased Ht and MCV. The applied doses of PI decreased the relative adrenal weight in a dose-dependent manner, and its highest dose increased the relative liver weight. Among the immune function parameters tested, PFC content of the spleen was decreased by high-dose PR and elevated by high-dose PI, whereas the maximum and the time course of the delayed-type hypersensitivity reaction showed no changes in this dose range. In the genotoxicological investigations only the high PR dose increased the number of numerical, but not the structural, chromosome aberrations. In addition to the changes in relative adrenal weight following PI treatment, the PFC assay showed the highest sensitivity for detection of the 4-week exposure with these carbamates. On the basis of our results, the immunotoxicological approach seems to have the same (PR) or higher (PI) sensitivity in early detection of the repeated low-dose exposure by these carbamates compared to the genotoxicological approach.
The N-nitroso derivative of an extensively used insecticide, propoxur, consistently induced dose-responsive chromosome aberrations and sister-chromatid exchanges (SCEs) in Chinese hamster ovary (CHO-W8) cells. Further investigations indicated that post-treatment incubation with a regular 1.5-cell-cycle period did not offer an unbiased estimation of the genotoxicity of N-nitroso carbamate insecticides. The scale of chromosome aberration induction increased with extension of the post-treatment incubation period. Comparable phenomena were not found in CHO-AGT cells proficient for O(6)-methylguanine-DNA-methyltransferase. In CHO-W8 cells, pulsed-treatment of the insecticide in the 1st replication cycle showed higher SCE induction than in the 2nd cycle. Similar phenomenon was also found in SCE induced by N-nitroso derivatives from other carbamate insecticides including aldicarb, carbofuran and methomyl. Treated cells did not show significantly perturbed cell cycle progression until 12 h after treatment removal. Based on the above observations, the O(6)-methylguanine-DNA adduct is suggested to be the major lesion caused by the delayed genotoxic effect of N-methyl carbamate insecticides as described in this report.
The effects of 6 weeks of oral exposure to propoxur (PR; at doses of 0.851 and 8.51 mg/kg body wt.), methylparathion (MP; at doses of 0.218 and 0.872 mg/kg body wt.), and their combinations were investigated in male Wistar rats. Measurement endpoints of the investigation were certain general toxicological parameters (body weight gain, organ weights), plaque-forming cell (PFC) count from the spleen, open field (OF) behavior, auditory startle response (ASR), prepulse inhibition (PPI), rotarod performance, somatosensory and auditory cortical evoked potentials, and peripheral nerve conduction velocity. The treated rats did not show any sign of acute intoxication during the 6 weeks of exposure. The higher dose of PR, but not of MP, significantly decreased the relative liver weight. Both agents produced a significant dose-dependent increase of OF activity, with larger expression after 2 weeks than after 6 weeks. The number of ASR responses and the ASR amplitude increased. The amplitude after PPI was increased by MP but only minimally altered by PR and the combinations. There was a small, but with high-dose PR significant, increase in the latency of the somatosensory evoked potentials. Neither of the two substances alone had any effect on the PFC response. The effect of the combination of high-dose PR and low-dose MP was significantly different from that of high-dose PR alone on the liver weight, on the ASR amplitude, and on the PFC/10(6) cell and PFC/spleen counts. With high-dose MP and low-dose PR, no such interaction was observed. According to the results, the noneffective dose of MP can influence the toxicity of the effective dose of PR in a combined exposure situation.
In the present study, the effects of subchronic per os exposures to cadmium chloride (CdCl(2)), and a carbamate insecticide, propoxur (Pr), were investigated in male Wistar rats on general toxicological (body weight gain, relative organ weights) haematological (RBC, WBC, Ht, MCV, cell content of the femoral bone marrow) immune function (plaque forming cell (PFC) assay, delayed type hypersensitivity (DTH) reaction) and neurotoxicological (spontaneous and stimulus-evoked cortical activity, nerve conduction velocity) parameters. The animals were treated for 4, 8 and 12 weeks with 6.43 mg/kg CdCl(2), 8.51 mg/kg Pr, or with a combination of 6.43 mg/kg CdCl(2)+0.851 mg/kg Pr or 8.51 mg/kg Pr+1.61 mg/kg CdCl(2). Cadmium exposure affected the relative thymus, liver, and adrenal weight, RBC count, haematocrit and MCV, and there was an increase in nerve conduction velocity and a decrease in the cortical evoked potential latency. Pr induced a decrease in thymus weight, had some effect on the liver weight but none on the electrophysiological parameters. A significant interaction between Cd and Pr was detected by the following parameters: RBC, Ht, PFC, and nerve conduction velocity. The results indicate that combined exposures in humans may result in a shift in the apparent detection limits and/or in the LOEL of the single substances. The latter raises the necessity to reconsider exposure limits in situations where the risk of combined exposure is high.
The efficacy of 2 sets of collars (Kiltix Collar, Bayer AG), containing different plasticisers and impregnated with the acaricides flumethrin (2.25%) and propoxur (10%), was compared against adult Rhipicephalus sanguineus on experimentally infested, kennelled dogs. Thirty individually penned dogs were infested with 25 male and 25 female, unfed R. sanguineus. On the following day they were allocated to 3 groups of 10 dogs each on the magnitude of their tick burdens. Two days after infestation, medicated collars containing 1 of the plasticisers were fitted to 10 of the dogs and similar collars containing the other plasticiser were fitted to 10 others. The remaining 10 dogs were the untreated controls. Seven and 28 days after having fitted the collars, all dogs were re-infested with 50 unfed adult ticks of both sexes, and again at approximately 28-day intervals up to the 5th month, and then at approximately 14-day intervals during the 6th month. Efficacy was determined by comparing the mean number of live, attached ticks on the untreated control group with those on the collared dogs 2 days after each re-infestation. Immediate efficacy of the collars (Day +2) was > 95%, and residual efficacy was > 98% up to and including Day +114, and > 93% up to Day +170 on both groups of collared dogs. The mean tick counts on the 2 groups of collared dogs did not differ significantly (P < 0.0001) for any of the assessment days.
A significant and stable difference in the residual night-biting collection (NBC, observed/expected) of A. gambiae s.l. was observed among different villages of the West African savannah when sprayed for 2 years with propoxur. The residual mosquito density of a given village was positively associated with some of its pre-spraying characteristics: the NBC/PSC (pyrethrum spray collections) ratio, the median biting hour, and possibly the proportion of species B. It was not significantly associated with several other pre-spraying characteristics (absolute mosquito density, the ratios between NBC indoors and NBC outdoors, between ETC (exit-trap collections) and PSC, between fed and gravid in the PSC or ETC, between males and females in the PSC), and was not associated with variations in recorded coverage, with latitude, or with distance from unsprayed villages.In a comparison between A. gambiae s.l., A. funestus, and A. pharoensis, the residual NBC (observed/expected) was positively associated with the pre-spraying NBC/PSC ratio, and was negatively associated with the median biting hour.The pre-spraying NBC/PSC ratio thus appears to be a predictor of the variation, between villages or species, in the reduction of the NBC by residual spraying, and may assist in forecasting the effect of a residual insecticide. The limitations of any absolute prediction must, however, be kept in mind.
The effect of repeated peroral introduction (4 times) of 1/4 and 1/20 LD50 of monomethylcarbamate insecticide Propoxur (Baygon) on the activity of two lysosomal enzymes (beta-N-acetylglucosaminidase and alpha-mannosidase) is studied in the serum of white male rats with starting weight 300 g. Upon using the higher dose, a statistically significant rise (p less than 0.02) of the activity of either of the enzymes is established. The results obtained are interpreted as a sign of impaired permeability of the lysosomal and cell membrane.
A low volume formulation of propoxur wettable powder suspended in larvicidal oil was evaluated on 4 occasions in Kern Co., California during 1983 using fixed and rotary wing aerial application systems. Culex tarsalis abundance was suppressed significantly by all sprays, although reduction below the virus maintenance threshold of 30 females per trap night was achieved only at one foothill site. Western equine encephalomyelitis virus minimum infection rates decreased significantly after serial applications on 2 occasions at a valley site. However, virus persisted in the spray zone at minimum infection rates of greater than 1 per 1000 Cx. tarsalis females tested and transmission of virus to sentinel chickens continued. The parity rates were reduced significantly at 2 semi-isolated foothill sites, but not at a valley site where elevated autogeny rates increased the reproductive age of the host-seeking population. Spraying during late afternoon by helicopter resulted in better control than early morning applications by fixed wing aircraft at a valley site.
A survey of resistance in larvae of Culex quinquefasciatus conducted at three widely separated geographical areas of California, namely Coachella Valley, southeast Los Angeles and northern San Joaquin Valley, revealed high resistance to temephos and lower resistance to chlorpyrifos, methyl parathion and malathion at all locations. Likewise resistance to DDT was high in all areas despite its withdrawal from use since 1970. There was no obvious tolerance to propoxur. Tests for the presence of esterase-2A have shown a close correlation between the frequency of this esterase and the level of organophosphate resistance.
A sensitive technique allowing to identify the three genotypes (AceSS, AceRR and AceRS) of the Ace gene existing in natural populations of Culex pipiens in southern France is described. The technique is based on the comparison of AChE (acetylcholinesterase) activity in 3 equal aliquots taken from the homogenate of a single mosquito (a) in absence of inhibitor (RA), (b) in presence of eserine that inhibits the AChE encoded by AceS and AceR alleles (RI) and (c) in presence of a concentration of propoxur inhibiting the AChE coded by the AceS allele but not by the AceR allele (RG). The mosquito tested is AceSS when RG = RI, AceRR when RG = RA and AceRS when RI less than RG less than RA.
Rats were exposed to propoxur-impregnated strips in a conventional laboratory animal room. The air in the room was monitored for the pesticide, and erythrocyte acetylcholinesterase activity was determined periodically. Air concentration of the pesticide never exceeded 0.8 microgram/m3, and no significant change in enzyme activity was observed.