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At least 19 recordsLinked to original sources
PubMed1995

Enzymological differences of AChE and diazinon hepatic metabolism: correlation of in vitro data with the selective toxicity of diazinon to fish species.

The in vitro hepatic metabolism of diazinon, as well as the sensitivity of the brain acetylcholine esterase, to diazoxon inhibitory action have been studied in order to explain the different toxicity of diazinon to Oncorhynchus mykiss (rainbow trout), Poecilia reticulata (guppy), Brachydanio rerio (zebra fish) and Cyprinus carpio (carp). In spite of a very sensitive acetylcholine esterase the carp is very resistant to diazinon toxicity because of its very low rate of bioactivation and relatively high activity of detoxicating enzymes. The trout is very sensitive towards diazinon in spite of its low activity of bioactivation, because of its lack of detoxicating enzymes and a very sensitive acetylcholine esterase. Diazinon is very toxic for the guppy, because this fish combines a relatively sensitive acetylcholine esterase with a high rate of bioactivation. The zebra fish has the most insensitive acetylcholine esterase, associated with a limited activation rate, thus resulting a rather resistant species. The results obtained indicate that diazinon toxicity differences among the fish species studied can largely be explained in relation to metabolic balances in the liver and with the features of the target enzyme.

Acetylcholinesterase↗
PubMed1985

The tissue distribution of diazinon and the inhibition of blood cholinesterase activities in rats and mice receiving a single intraperitoneal dose of diazinon.

The tissue distribution of diazinon and the inhibition of cholinesterase (ChE) activities in plasma, erythrocyte and brain were investigated using male rats and mice which received a single intraperitoneal (i.p.) dose of diazinon (20 or 100 mg/kg body wt) in olive oil. The blood diazinon level was estimated to reach a maximum at 1-2 h after the i.p. administration. It was demonstrated that the diazinon residue levels are the highest in the kidney, when comparing the distribution of diazinon among liver, kidney and brain in the animals after dosing. It was indicated that the ChE inhibition by diazinon exposure is greater in the plasma than in the erythrocytes for male mice, while its inhibition is greater in the erythrocytes for male rats. Brain ChE activity was also inhibited markedly in the mice after dosing.

Animals↗
PubMed1985

Diazinon concentrations and blood cholinesterase activities in rats exposed to diazinon.

The tissue distribution of diazinon and the inhibition of blood cholinesterase (ChE) activity were investigated in male rats which received a single intraperitoneal (i.p.) dose of diazinon (100 mg/kg body wt) in olive oil. Diazinon concentration in the blood reached a maximum 1-2 h after dosing. Comparing the distribution of diazinon among liver, kidney and brain in treated rats, the diazinon residue was much greater in the kidney than in other organs, being 500 times that in the liver and 11 times that in the brain at 8 h after dosing. Erythrocyte and plasma ChE activities were inhibited rapidly, but ChE inhibition was greater in the erythrocytes than in plasma.

Animals↗
PubMed1996

The efficacy of diazinon impregnated ear tags against buffalo fly and resulting weight gains and diazinon residues in meat and milk.

Ear tags impregnated with 20% diazinon were evaluated for their efficacy against the buffalo fly (Haematobia irritans exigua) on beef cattle in southern Queensland. Buffalo fly numbers and weight changes were recorded and diazinon residues in tissues of beef cattle and milk from lactating dairy cattle were assayed at different time intervals after tagging. In 2-efficacy trials conducted over 19 and 20 weeks, the mean numbers of buffalo fly on cattle each fitted with ear tags were 1 to 9 and 0 to 16, respectively, in trials 1 and 2, compared with 44 to 345 and 26 to 306 per head on untreated herds, respectively, despite regular spraying of the untreated herd in trial 1 with cypermethrin to reduce fly burdens. Percentage buffalo fly control was 96.7 to 99.5% and 89.3 to 100% in the 2 trials. Cattle fitted with ear tags gained an average of 94 kg body weight after 5 months compared with 61 kg in the untreated herd, a net increase of 60% in treated animals compared with 28% in the untreated herd. Mean diazinon residue concentrations in the fat of perianal tissue biopsies were 0.02 to 0.03 mg/kg 1 to 8 weeks after tagging. Mean diazinon residue concentrations in the butterfat of milk from lactating dairy cattle were 0.01 to 0.04 mg/kg after tagging.

Animal Identification Systems↗
PubMed1994

Rapid gas chromatographic assay of diazinon: application to the study of diazinon kinetics in rats.

A rapid method was developed for the determination of diazinon in plasma using gas chromatography with electron-capture detection (GC-ECD). Following a single extraction with hexane from 100 microliters of plasma, diazinon was quantitated on a 3% OV-17 column. The detection limit was 10 ng/ml and linearity was obtained in the range of 25 ng/ml-2500 ng/ml. The applicability of the assay to single-dose kinetics in rats is illustrated.

Animals↗
PubMed2003

Biological monitoring of diazinon exposure using saliva in an animal model.

Alternative biological monitoring methods are currently being pursued to better quantify pesticide exposures. In this study, the feasibility of using saliva as a tool for measuring diazinon exposure was determined in an animal model. Male Spraque-Dawley rats were dosed with 1 or 10 mg/kg diazinon by bolus intravenous injection. Time-matched saliva and arterial blood samples were collected from 10 to 250 min post administration. Diazinon was distributed and eliminated rapidly in rats following intravenous (iv) bolus injection, according to a two-compartmental pharmacokinetic analysis. Salivary concentration of diazinon showed a strong correlation with plasma concentration of diazinon. The saliva/plasma (S/P) concentration ratio of diazinon was not affected by administered dose, sampling time, or salivary flow rate, suggesting that salivary excretion of diazinon in rats is fairly constant. Diazinon concentrations in saliva were consistently lower than those in arterial plasma. The mean S/P concentration ratios of diazinon were 0.16 and 0.13 for 1 and 10 mg/kg iv bolus doses, respectively. It is most likely that the incomplete transfer of diazinon from plasma to saliva is due to protein binding of diazinon in plasma. If the protein-unbound fraction of diazinon in plasma is used to calculate the S/P ratio, the S/P concentration ratio of diazinon is close to unity. The results from this study support the conclusion that diazinon salivary concentrations not only can be used to predict the plasma levels of diazinon in rats, but also reflect the unbound fraction of diazinon in plasma.

Animals↗
PubMed2001

Effects of field exposure to diazinon on small mammals inhabiting a semienclosed prairie grassland ecosystem. I. Ecological and reproductive effects.

The widespread use of cholinesterase-inhibiting pesticides in the environment presents increasing concerns about their effects on human, wildlife, and ecosystem health. As a group, these pesticides are generally highly toxic and have great potential for negatively affecting nontarget organisms. Small mammals have proven to be ideal biomonitors of environmental contaminants, and were used here to test for possible effects of a widely used cholinesterase-inhibiting insecticide, diazinon, in a natural field setting. Using 12 0.1-ha terrestrial mesocosms, we examined the effects of low-level diazinon exposure on the small mammal communities inhabiting semienclosed grassland ecosystems. Our primary objective was to test the hypothesis that diazinon, applied at two different recommended label application rates, would not cause any observable adverse ecological or reproductive effects on small mammal populations and communities. Experimental small mammal communities consisting of Sigmodon hispidus, Microtus ochrogaster, Reithrodontomys fulvescens, and Mus musculus were stocked at natural densities and sex ratios inside empty mesocosms. Diazinon 4E was applied at two different maximum recommended label application rates, 0.56 kg a.i./ha (1x) and 4.5 kg a.i./ha (8x), and controls remained unsprayed, with four enclosures (replicates) per treatment. Two 30-d trials were run during peak rodent breeding seasons and enclosures were sampled on days 2, 16, and 30 of each trial. Recovery of small mammals was not significantly different among treatments, although fewer animals were recovered from the diazinon-exposed enclosures in both trials. Analysis of trapping data suggested that the normally strong competitive relationship between Sigmodon and Microtus may be altered by the pesticide, favoring Microtus in the diazinon-exposed enclosures. Incidence of reproductive condition was found to be reduced 20 to 80% and 33 to 100% in diazinon-exposed males and females, respectively. Reproductive productivity, including percentage of pregnant females and of females giving birth, was significantly reduced in diazinon-exposed animals. Percentage of pregnant females ranged from 13.6 to 43.5% in diazinon-exposed animals compared to 40 to 80% for control animals, and percentage of females giving birth ranged from 0 to 17% in diazinon-exposed animals compared to 22 to 50% for control animals. Generally, the effects found in this study suggest that diazinon was relatively persistent in the sprayed enclosures and that oral routes of exposure (consumption of dead and dying arthropods, grooming) may have been important. Ecological relationships and reproduction in both herbivorous and omnivorous mammals were negatively impacted by diazinon exposure. Overall, ecological relationships in the enclosed prairie grassland ecosystem were disrupted by diazinon, probably through a combination of sublethal effects, particularly reproductive effects, impacting individuals and their populations. This suggests that negative impacts on populations and community structure and function may persist longer than diazinon persists in the environment.

Animals↗
PubMed2000

Electrophysiological and biochemical effects of single and multiple doses of the organophosphate diazinon in the mouse.

Diazinon is an organophosphorus compound (OP) widely used in pesticides. The relationship between dose of diazinon, inhibition of acetylcholinesterase, and effect on neuromuscular transmission has been studied in a mouse model. Inhibition of acetylcholinesterase activity occurred within 1 h, was maximal by 3 h and remained inhibited for at least 24 h. Blood, brain, diaphragm, and soleus acetylcholinesterase activities were differentially affected by diazinon. Brain and soleus activities were not affected by low doses. Multiple daily dosing of diazinon caused a cumulative decrease in acetylcholinesterase activity, although to a lesser extent in brain and soleus. Diazinon had no effect on the activity of neuropathy target esterase. Plasma and brain levels of diazinon peaked at 15 min after dosing and declined with a half-life of 2.5 h. Metabolic products of diazinon were cleared from the urine within 24 h. Increased miniature end-plate current half decay times occurred in a dose-dependent manner. Single doses of diazinon caused an increase in the jitter (variability of latencies) of evoked action potentials recorded in the diaphragm but did not affect end-plate potential (EPP) jitter. Multiple lower doses of diazinon caused an increase in EPP jitter after 28 days. This effect on nerve function was delayed and occurred when acetylcholinesterase activity had returned to control levels. The results indicate that diazinon produces long-term electrophysiological changes in neurotransmission following repeated dosing in the mouse. This has implications for the current use of diazinon; however, there is a need to further define the mechanism of this effect.

Acetylcholinesterase↗
PubMedDate not supplied

Inhibition and recovery of maternal and fetal cholinesterase enzyme activity following a single cutaneous dose of methyl parathion and diazinon, alone and in combination, in pregnant rats.

Pregnant Sprague-Dawley rats (14-18 days of gestation) were treated with a single cutaneous subclinical dose(s) of 10 mg kg(-1) (15% of LD(50)) of methyl parathion (O,O-dimethyl O-4-nitrophenyl phosphorothioate) and 65 mg kg(-1) (15% of LD(50)) of diazinon (O,O)-diethyl O-2-isopropyl-6-methylpyrimidinyl phosphorothioate, and their combination. Animals were sacrificed at 1, 2, 4, 12, 24, 48, 72, and 96 h after dosing. Inhibition of maternal and fetal cholinesterase enzyme activity has been determined. Methyl parathion significantly inhibited maternal and fetal brain acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BuChE) activity within 24 h after dosing. Diazinon and a mixture of methyl parathion and diazinon caused lesser inhibition compared with methyl parathion alone. Recovery of maternal and fetal brain AChE activity was in the order of diazinon > combination of diazinon and methyl parathion > methyl parathion 96 h after dosing. Although fetal plasma BuChE activity recovered to 100% of control within 96 h of application, maternal BuChE activity remained inhibited to 55% and 32% of control 96 h after application of methyl parathion and a mixture of methyl parathion and diazinon, respectively. Following a single dermal dose of methyl parathion, the activity of maternal liver BuChE was 63% of control 2 h after dosing, whereas inhibition of placental AChE or BuChE activity occurred 12 and 1 h following a single dose of methyl parathion, corresponding to activities of 63% and 54% of control, respectively. Diazinon, alone or in combination with methyl parathion, did not inhibit significantly the maternal liver BuChE or placental AChE and BuChE activity. The results suggest that dermal application of a single dose of methyl parathion and diazinon, alone or in combination, has an easy access into maternal and fetal tissues, resulting in inhibition of cholinesterase enzymes. The lower inhibitory effect of the combination of methyl parathion and diazinon might be due to competition of diazinon with methyl parathion for cytochrome P-450 enzymes, resulting in formation of the potent cholinesterase inhibitor methyl paraoxon. The faster recovery of fetal cholinesterase enzymes is attributed to the rapid de novo synthesis of cholinesterase fetal tissues compared with the mother.

Acetylcholinesterase↗
PubMed2005

Diazinon-induced hepatotoxicity and protective effect of vitamin E on some biochemical indices and ultrastructural changes.

Diazinon, an organophosphate insecticide has been used in agriculture and domestic for several years. The aim of present study was to analyze the hepatotoxic effect of diazinon which caused biochemical and ultrastructural changes in adult male Wistar rats and to evaluate the possible protective effect of vitamin E. Vitamin E (200 mg/kg, twice a week), diazinon (10 mg/kg per day, once a day in corn oil) and vitamin E (200 mg/kg, twice a week)+diazinon (10 mg/kg per day, once a day in corn oil) combination were given to rats (n=8) orally via gavage for 7 weeks. Biochemical indices in serum [total protein, albumin, alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST), total cholesterol, triglyceride and low density lipoprotein cholesterol (VLDL-cholesterol)] and ultrastructural changes were investigated at the end of the 1st, 4th and 7th weeks comparatively with control group (n=8). It was observed that; at the end of 1st week, there was a statistically significance in all parameters except total protein and albumin, and at the end of 4th and 7th weeks, there was a statistically significance in all parameters when diazinon-treated group compared to control group (P<0.01). At the end of 1st week, ALP, ALT, total cholesterol and triglyceride, at the end of 4th week, all parameters except VLDL-cholesterol, at the end of 7th week, all parameters were statistically significant when vitamin E+diazinon-treated group compared with diazinon-treated group (P<0.01). In our electron microscopic investigations, while swelling of mitochondria and breaking up of the mitochondrial cristae of hepatocytes in diazinon-treated groups were observing, no pathological findings were observed in vitamin E+diazinon-treated groups. We conclude that vitamin E decreases diazinon hepatotoxicity, but vitamin E does not protect completely.

Alanine Transaminase↗
PubMed2003

Influence of gender on thermoregulation and cholinesterase inhibition in the long-evans rat exposed to diazinon.

Diazinon is an organophosphate (OP)-based, anticholinesterase insecticide that irreversibly inhibits acetylcholinesterase activity and produces cholinergic stimulation in central nervous system (CNS) and peripheral tissues. Our laboratory has found that OPs administered orally in rats induce a transient period of hypothermia followed by a delayed fever that persists for several days after exposure. There is little information on the thermoregulatory effects of diazinon. Core temperature (Tc) and motor activity (MA) were monitored by radiotelemetry in male and female rats of the Long-Evans strain dosed orally with diazinon (0 [corn-oil vehicle], 100, 200, or 300 mg/kg in males and 0, 50, 100, or 200 mg/kg in females). There was a dose-dependent decrease in Tc during the first night after treatment, with females exhibiting slightly greater sensitivity than males. MA was unaffected in females exposed to diazinon at doses of 50 to 200 mg/kg; MA of males was reduced during the first night after dosing with 300 mg/kg. There was a delayed elevation in Tc of males dosed with 200 and 300 mg/kg and females dosed with 50, 100, and 200 mg/kg diazinon. The elevated Tc was only manifested during d 2 and 3 after diazinon. Administration of 200 mg/kg sodium salicylate to females 48 h after being treated with 200 mg/kg diazinon led to a rapid abatement of the fever. Diazinon doses of 50 to 300 mg/kg led to 40% to 50% inhibition in plasma cholinesterase (ChE) activity 4 h after dosing, and females displayed a significantly slower recovery of ChE activity compared to males. When compared on a molar basis, the hypothermic response to diazinon was relatively small compared to other OPs such as chlorpyrifos. The delayed fever and efficacy of sodium salicylate to block diazinon-induced fever are similar to the effects of OPs chlorpyrifos and diisopropyl fluoro-phosphate (DFP).

Analysis of Variance↗