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Resistance development and insecticide susceptibility in Culex quinquefasciatus against selection pressure of malathion and permethrin and its relationship to cross-resistance towards propoxur.

To determine resistance level and characterize malathion and permethrin resistance in Culex quinquefasciatus, two methods were used namely: WHO procedures of larval bioassay to determine the susceptibility of lethal concentration (LC) and adult bioassay to determine the lethal time (LT) which are resistant to malathion and permethrin. These mosquito strains were bred in the Insectarium, Division of Medical Entomology, IMR. Thousands of late fourth instar larvae which survived the selection pressure to yield 50% mortality of malathion and permethrin were reared and colonies were established from adults that emerged. Larvae from these colonies were then subjected to the subsequent 10 generations in the test undertaken for malathion resistant strain (F61 - F70) and permethrin resistant strain (F54 - F63). Selection pressure at 50% - 70% mortality level was applied to the larvae of each successive generation. The rate of resistance development and resistance ratio (RR) were calculated by LC5 0 for larval bioassay and LT50 value for adult bioassay. The lab bred Cx. quinquefasciatus was used as a susceptible strain for comparison purpose. The adult bioassay test was carried out by using diagnostic dosages of malathion 5.0%, permethrin 0.75% and with propoxur 0.1%. All bioassay results were subjected to probit analysis. The results showed that LC5 0 for both malathion (F61 - F70) and permethrin (F54 - F63) resistant Cx. quinquefasciatus increased steadily to the subsequent 10 generations indicating a marked development of resistance. The adult female malathion resistant strain have developed high resistance level to malathion diagnostic dosage with resistance ratio 9.3 to 9.6 folds of resistance. Permethrin resistance ratio remained as 1.0 folds of resistance at every generation. It was obvious that malathion resistance developing at a higher rate in adult females compared to permethrin. Female adults exposed to 2 hours of exposure period for propoxur 0.1% showed presence of cross-resistance among the both strains of mosquitoes towards propoxur and it was indicated by 70%-100% mortality at 24 hours post-recovery period.

Animals↗

Resistance of German cockroach (Blattella germanica) to DDT and Propoxur in some parts of Bulgaria.

Five field strains of Blattella germanica from different areas of Bulgaria were tested for resistance to DDT. The strain from Sofia-city after 24 hours of exposure was resistant to DDT in terms of mortality by resistant ratio of 3.76 at the LT50 level. Also 5 strains of B. germanica from 3 regions of Bulgaria have been tested to the carbamate insecticide--Propoxur. For the first time in Bulgaria, DDT- and Propoxur-resistant cockroach strains have been found. It is due to female and nymph resistance, while the males are highly susceptible to Propoxur.

Animals↗

A study of liver microsomal enzymes in rats following propoxur (Baygon) administration.

Groups of rats were given either propoxur, were left as untreated controls, or were given phenobarbital, DDT, chlordane or toxaphene which are known to induce liver microsomal detoxification enzymes. Microsomal enzyme activity was measured by testing the ability of liver homogenates to degrade EPN (O-ethyl O-(4-nitrophenyl) phenylphosphonothioate) to p-nitrophenol. The activity of aminopyrine-N-demethylase, cytochrome P-450 and p-nitroanisole-O-demethylase in liver homogenates of rats receiving propoxur was measured. Liver microsomal detoxification enzymes were not induced by propoxur exposure.

Aminopyrine N-Demethylase↗

Colorimetric determination of propoxur and its residues in vegetables.

A method has been developed for the determination of propoxur (o-isopropoxyphenyl N-methylcarbamate) based on the hydrolysis of propoxur with methanolic potassium hydroxide to its phenol and coupling with diazotized 4,4-diaminodiphenyl sulfone. The orange complex formed has an absorption maximum at 500 nm and obeys Beer's law in the range 0.25-5.0 micrograms/mL. The method can be applied to levels as low as 0.5 ppm propoxur from vegetables.

Colorimetry↗

[The effects of malathion, fenitrothion and propoxur on the house fly, Musca domestica I. (Diptera: Muscidae), populations].

The present work was carried out to determine the LD50 and LD90 of Malathion, Fenitrothion and Propoxur for the house fly, MUSCA DOMESTICA L., under laboratory conditions. The house fly populations were collected from the municipality garbage area of Ankara in September 1981, April and September, 1982. The resistance tests were applied on both sexes by means of Topical Application method. The highest resistance level for Malathion was observed in Ankara strains. The values of LD50 were 261.1, 302.1, 312,6 micrograms/female, respectively. The populations were not showed high resistance ratio to Fenitrothion (R/S 93.3, 126.6, 56.6 at LD50) and Propoxur (R/S 34.2, 31.4, 21.4 at LD50). It is clear that, Propoxur was more toxic to female and male flies than Fenitrothion. However the males were more susceptible to the applied insecticides than the females. It was concluded that susceptibility of houseflies to the insecticides varied widely by seasons in the same habitat. The results of the tests indicated that the resistance level of Malathion was very high. Therefore it should not be recommended for the control of houseflies in Ankara.

Animals↗

Sensitive determination of propoxur by spectrophotometry using 3-aminopyridine.

A simple spectrophotometric method for the determination of propoxur, a widely used insecticide, in various environmental samples and pesticide formulations is described. The method is based on the coupling of the hydrolysis product of propoxur with diazotized 3-aminopyridine in an alkaline medium, to form an azo-dye which has a maximum absorbance at 463 nm. Beer's law is obeyed over the concentration range of 0.05 to 1.2 microg ml(-1) of propoxur. The molar absorptivity and Sandell's sensitivity are found to be 3.10 x 10(4) l mol(-1) cm(-1) and 0.007 microg cm(-2), respectively. The important analytical parameters and optimum reaction conditions were evaluated. The method is free from the interference of other commonly used pesticides and inorganic metal ions.

Journal Article↗

Biodegradation of a carbamate pesticide, Propoxur, in rat tissues.

Propoxur (Baygon, 2-isopropoxyphenyl N-methylcarbamate) is a carbamate pesticide commonly used against house insects. When the insecticide was administered intramuscularly in rats it was converted to a new metabolite which was found to be present in the serum, liver, kidney and brain 6 h after the administration of the pesticide. The metabolite was purified by high performance liquid to chromatography and comparison of the infrared spectra of Propoxur and the metabolite showed that a deamination reaction was responsible for the formation of the metabolite from the parent pesticide. The pesticide also induced haematological changes such as an increased level of total bilubrin, amylase and glutamic-oxalacetic transaminase and decrease of cholinesterase activity, indicating damage of the liver and nervous system in rats.

Animals↗

Effects of humic acids, para-aminobenzoic acid and ascorbic acid on the N-nitrosation of the carbamate insecticide propoxur and on the mutagenicity of nitrosopropoxur.

Nitrosation of the carbamate insecticide propoxur at pH 3 and 37 degrees C was determined colorimetrically and found to be time- and sodium nitrite concentration-dependent. Nitrosated propoxur was mutagenic when exposed to the seeds of the higher plant Arabidopsis thaliana but the formation of nitrosopropoxur, the presumed mutagen, was inhibited by humic acids, para-aminobenzoic acid and ascorbic acid. These agents also reduced the mutagenicity of preformed nitrosopropoxur.

4-Aminobenzoic Acid↗

Acute toxicity of propoxur on carbohydrate metabolism of Indian catfish (Heteropneustes fossilis).

Exposure of Indian catfish (Heteropneustes fossilis) to 5.20 ppm propoxur for 3, 6, 12, 48 and 96 h caused muscle glycogen depletion at 12 h and hepatic glycogenolysis at 3, 12, 48 and 96 h; hyperglycemia developed at all time-intervals. Blood pyruvate levels increased significantly at 12 and 48 h. Hyperlacticemia was observed at 6 h but hypolacticemia resulted at 12, 48 and 96 h in pesticide-treated fish. The observed effects are explained in terms of acute stress syndrome; possible mechanisms underlying the effect of anticholinesterase action of propoxur on carbohydrate metabolism are also discussed.

Animals↗

The influence of skin moisture on the dermal absorption of propoxur in human volunteers: a consideration for biological monitoring practices.

A large number of workers in agriculture are exposed daily (through skin contact) to pesticides either directly during mixing and loading or indirectly due to contact. The aim of this study was to investigate the influence of skin moisture on the dermal uptake of the pesticide propoxur. The study was conducted in human volunteers under controlled temperature conditions (30 degrees C) and environmental relative humidities of either 50, 70 or 90%. The study was approved by the Medical Ethics Committee. In this study a linear relationship between the environmental relative humidity and the level of skin moisture was observed. The results indicate that the level of skin moisture influences the absorption of propoxur via the dermal route, dramatically ranging from, on average, 13, 33-63% of the potentially absorbed dose' which is excreted in urine as the primary metabolite 2-isopropoxyphenol (IPP) at relative humidity levels of, on average 50, 70 and 90%, respectively. The 'potentially absorbed dose' is defined as the difference between the applied dose and the dislodged dose after 4 h. It can be concluded that by assessing health risks of workers in agriculture exposed dermally to pesticides and e.g. in testing the efficiency of protective clothing under realistic conditions, the influence of the level of skin moisture on absorption of substances may be considerable and has to be taken into account.

Adult↗

Production of monoclonal antibodies to the N-methylcarbamate pesticide propoxur.

Monoclonal antibodies (MAbs) to the pesticide propoxur were produced from haptens with carboxylic spacer arms of different lengths introduced at the carbamate group of the analyte structure. MAbs were subsequently characterized in the conjugate-coated format using these immunizing haptens and newly synthesized compounds as homologous and heterologous assay conjugates, respectively. Appropriate combinations of immunoreagents resulted in competitive enzyme immunoassays (ELISA) with I(50) values in the low nanomolar range (6.5-17.9 nM). A modification of the conjugate-coated format consisting of the simultaneous incubation of the MAb and the peroxidase-labeled secondary antibody in the presence of the analyte resulted in an assay with an I(50) value of 4.4 nM. This one-step conjugate-coated ELISA format is as simple and fast as the antibody-coated format but without the need of synthesizing enzyme-hapten conjugates. Major N-methylcarbamate pesticides were not recognized by the MAb. This immunoassay should reasonably allow the rapid, low-cost, and sensitive determination of propoxur in food, soils, and the environment at levels of regulatory and practical importance.

Animals↗

Effect of sublethal propoxur exposure on male German cockroaches (Orthoptera: Blattellidae) and their feeding behavior.

Exposure of male German cockroaches, Blattella germanica L., to propoxur produced significant water loss at 2 and 24 h after treatment. This effect was dependent upon the state of hydration before insecticide exposure. Hydrated males lost as much as 10% of their total body mass in the form of water; dehydrated males lost about 4.3%; and untreated controls lost approximately 1.8% during the same time period. No significant compensatory feeding responses were observed 1-4 d after treatment. Water depletion associated with propoxur exposure resulted in increased water consumption for the first 2 d after treatment and then reached a plateau for the duration of the study. Males consumed water daily regardless of insecticide exposure.

Animals↗

Adaptive larval thermotolerance and induced cross-tolerance to propoxur insecticide in mosquitoes Anopheles stephensi and Aedes aegypti.

Fourth-instar larvae of mosquitoes Anopheles stephensi and Aedes aegypti normally died within 90 min at 43 degrees C. Pre-exposure to high but sublethal temperatures conferred adaptive thermotolerance, dependent on the temperature and the duration of pre-exposure. Adaptive cross-tolerance to propoxur (a carbamate insecticide) was also induced in larvae by pre-exposing them to sublethal temperatures. Pre-exposure to sublethal concentrations of propoxur was found to confer cross-thermotolerance to a lower extent. These results suggest that the shock proteins (e.g. heat shock proteins) induced by unrelated stress factors play an important role in the development of adaptive cross-protection (stress response) to other stress conditions.

Aedes↗

Effect of single or chronic injection with a carbamate, propoxur, on the brain cholinergic system and behavior of mice.

Propoxur, an anticholinesterase carbamate, was injected singly (10 mg/kg, s.c.) or chronically (5 mg/kg/day, s.c., for 10 days) into mice. Animals were examined for effects on the cholinergic system in brain tissue and on behavior. Single injection caused an increase in brain acetylcholine (ACh) content at 10 and 60 min; and it caused decreases in acetylcholinesterase (AChE) activity at 10, 60 and 180 min, high-affinity choline uptake into synaptosomes at 10 and 60 min, and [3H]quinuclidinyl benzilate (QNB) binding at 10 min without causing any change in choline acetyltransferase (ChAT) activity. Open-field behavior and rotarod performance were depressed at 10 min and rectal temperature was decreased at 10, 60 and 120 min after a single injection. Chronic treatment caused decreases in high-affinity choline uptake and [3H]QNB binding 24 hr after the final injection without any changes in ACh content, AChE activity or ChAT activity. In behavioral tests conducted 10 min prior to daily administration, rotarod performance was slightly suppressed only during the period of injection. Although propoxur is considered to have effects similar to those of organophosphorus compounds, the changes observed in the present experiments seemed to be reversible.

Animals↗

Toxicity of propoxur to rats by subacute inhalation.

Male and female rats were exposed to propoxur (2-isopropoxyphenyl-N-methyl-carbamate) aerosol, concentrations averaging 5.7, 18.7 and 31.7 mg/m3 air, for 6 hours daily on five days in a week over a period of 12 weeks. The effects were depressions of plasma by 20 to 30%, and of erythrocyte and brain cholinesterase activities which were caused by the highest air concentration of 31.7 mg/m3. On the basis of the physical, biochemical, phamacokinetic and metabolic behaviors of propoxur, a maximum allowable concentration of 2.5 mg/m3 air is suggested.

Aerosols↗

[Changes in the serum activity of lysosomal enzymes in rats after the use of propoxur (Baygon) insecticide. 2. The dynamics of beta-N-acetylglucosaminidase].

The influence of 1/50 and 1/10 LD50 of the monomethylcarbamate insecticide Propoxur (Baygon) on the lysosome enzyme beta-N-acetylglucose-aminidase serum activity is studied in white rats upon daily administration per os, over a period of 2, 4, 8, 15, 30, 60 and 90 days. A statistically significant increase of the enzyme activity is recorded at 15 days after introduction of 1/50 LD50, and at 15 and 30 days after 1/10 LD50 administration, followed by a reduction of the activity and returning to normal values. In all likelihood, the harmful effect of Propoxur on the lysosome and cellular membrane decreases after the 15th day because of activation of the microsome enzymes which, in turn, speed up the process of rendering innocuous the insecticide administered.

Acetylglucosaminidase↗

Effect in vitro of propoxur on kinetics of K+ stimulated PNPPase and protection by thiol reagents.

Kinetics analysis of K+ stimulated PNPPase was studied in the rat brain synaptosomes in the presence of propoxur. Non-competitive inhibition with respect to activation by PNPP was seen by the decreased maximal velocity (Vmax) without change in Michaelis-Menten Constant (Km). Activation energy values (delta E) were increased suggesting the decreased catalytic potential of the enzyme. It is also observed that dithiothrietol (DTT) (76 microM), cysteine (82 microM) and glutathione (120 microM) neutralized the inhibition of K(+)-PNPPase by propoxur to different extents.

4-Nitrophenylphosphatase↗

Modulations in ionic composition and ATPase system in the brain of albino rat under induced propoxur toxicity.

Modulations in ionic composition were seen in the rat brain during propoxur treatment indicating an impairment in the electric activity of neurons, oxygen consumption, ATPase system, disruption in the movement of ions across ionic pumps and synaptic transmission. The specific activity levels of ATPases were also altered confirming that the impairment in the ATPase system might be due to the ionic imbalances under propoxur stress.

Adenosine Triphosphatases↗