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Chemosphere Mar 2022Benfuracarb (BEN), a broad-spectrum carbamate insecticide used for crop protection, is considered toxic to humans and aquatic organisms. However, the potential risk...
Benfuracarb (BEN), a broad-spectrum carbamate insecticide used for crop protection, is considered toxic to humans and aquatic organisms. However, the potential risk level of BEN to aquatic organisms is still unclear. In this study, we exposed zebrafish embryos to BEN (0.08, 0.49, and 0.90 mg/L) from 3 to 96 hours post-fertilization (hpf). The results showed that BEN caused shorter body length in zebrafish larvae. The activity of superoxide dismutase (SOD) was significantly increased after BEN exposure. Furthermore, the transcription levels of marker genes associated with early embryonic development (myoD, nkx2.4b, myh6, and gh) were disrupted after BEN treatment. Taken together, the data indicate that BEN possesses developmental toxicity to zebrafish. The results provide a valuable reference for assessing BEN's potentially harmful effects on aquatic ecosystems.
Topics: Animals; Benzofurans; Ecosystem; Embryo, Nonmammalian; Humans; Larva; Oxidative Stress; Water Pollutants, Chemical; Zebrafish; beta-Alanine
PubMed: 34801571
DOI: 10.1016/j.chemosphere.2021.132955 -
Cytotechnology Aug 2016Benfuracarb is a carbamate insecticide used to control insect pests in vegetables and it has anti-acetylcholinesterase activity lower than other carbamates. Cytotoxic...
Benfuracarb is a carbamate insecticide used to control insect pests in vegetables and it has anti-acetylcholinesterase activity lower than other carbamates. Cytotoxic effects of benfuracarb were evaluated by using root growth inhibition (EC50), mitotic index (MI), and mitotic phase determinations on the root meristem cells of Allium cepa and mutagenic effects were determined in Salmonella typhymurium Ames test by TA98 and TA100 strains with and without metabolic activation. In Allium test, 1 % DMSO was used as negative control group and 10 ppm MMS was used as positive control group. 75 ppm concentration of benfuracarb was found as EC50. In MI and mitotic phases determination study, 37.5, 75 and 150 ppm doses of benfuracarb were used. Dose-dependent cytotoxic activity was found by root growth inhibition and MI studies. It was identified that mitotic inhibition activity of benfuracarb was higher than 10 ppm MMS. In Ames test, mutagenic activity was not observed and over 200 µg/plate of benfuracarb was determined as cytotoxic to S. typhymurium strains. Benfuracarb can be called as "mitotic inhibitor" but not called as mutagen.
PubMed: 25381170
DOI: 10.1007/s10616-014-9811-3 -
Toxicology Letters Jan 2014In vitro metabolism of benfuracarb in liver microsomes from seven species was studied in order to quantitate species-specific metabolic profiles and enhance benfuracarb... (Comparative Study)
Comparative Study
In vitro metabolism of benfuracarb in liver microsomes from seven species was studied in order to quantitate species-specific metabolic profiles and enhance benfuracarb risk assessment by interspecies comparisons. Using LC-MS/MS, a total of seven phase-I-metabolites were detected from the extracted chromatograms and six of them were unequivocally identified. Benfuracarb was metabolized via two metabolic pathways, the sulfur oxidation pathway and nitrogen sulfur bond cleavage, yielding carbofuran, which metabolized further. Analysis of the metabolic profiles showed that benfuracarb was extensively metabolized with roughly similar profiles in different species in vitro. In vitro intrinsic clearance rates as well as calculated in vivo hepatic clearances indicated that all seven species metabolize benfuracarb via the carbofuran metabolic pathway more rapidly than the sulfoxidation pathway. The highest interspecies differences in hepatic clearance rate values were for mouse and rat liver microsomes compared to human, i.e. 4.8 and 4.1-fold higher, as illustrated by in vivo hepatic clearance of carbofuran. Overall, there are quantitative interspecies differences in the metabolic profiles and kinetics of benfuracarb biotransformation. These findings illustrate that in vitro studies of benfuracarb metabolite profiles and toxicokinetics are helpful for the proper selection and interpretation of animal models for toxicological evaluation and chemical risk assessment.
Topics: Adult; Animals; Benzofurans; Dogs; Female; Humans; Insecticides; Macaca fascicularis; Male; Mice; Mice, Inbred DBA; Microsomes, Liver; Middle Aged; Rabbits; Rats; Risk Assessment; Species Specificity; beta-Alanine
PubMed: 23958702
DOI: 10.1016/j.toxlet.2013.08.009 -
Bulletin of Environmental Contamination... Sep 2009The fate of benfuracarb was studied under field conditions in brinjal fruits and soil following foliar spray application at 0.25 and 0.50 microg g(-1) by HPLC. At 0.25...
The fate of benfuracarb was studied under field conditions in brinjal fruits and soil following foliar spray application at 0.25 and 0.50 microg g(-1) by HPLC. At 0.25 microg g(-1), benfuracarb persisted up to 7 days both in soil and brinjal but at 0.50 microg g(-1), benfuracarb residues persisted up to 10 and 12 days in soil and brinjal fruits, respectively. The persistence of benfuracarb residues, both in soil and brinjal, followed first-order kinetics. The half-life values of benfuracarb in soil and brinjal fruit were found to be 3.54 and 3.90 days at 0.25 microg g(-1) and 3.75 and 4.73 days at 0.50 microg g(-1), respectively.
Topics: Benzofurans; Biodegradation, Environmental; Fruit; Half-Life; Insecticides; Kinetics; Pesticide Residues; Soil; Soil Pollutants; Solanum melongena; Spectrophotometry, Ultraviolet; Weather; beta-Alanine
PubMed: 19333533
DOI: 10.1007/s00128-009-9710-z -
Toxicology Letters Jan 2014Human responses to the toxicological effects of chemicals are often complicated by a substantial interindividual variability in toxicokinetics, of which metabolism is...
Human responses to the toxicological effects of chemicals are often complicated by a substantial interindividual variability in toxicokinetics, of which metabolism is often the most important factor. Therefore, we investigated human variation and the contributions of human-CYP isoforms to in vitro metabolism of benfuracarb. The primary metabolic pathways were the initial sulfur oxidation to benfuracarb-sulfoxide and the nitrogen-sulfur bond cleavage to carbofuran (activation). The Km, Vmax, and CL(int) values of carbofuran production in ten individual hepatic samples varied 7.3-, 3.4-, and 5.4-fold, respectively. CYP2C9 and CYP2C19 catalyzed benfuracarb sulphur oxidation. Carbofuran formation, representing from 79% to 98% of the total metabolism, was catalyzed predominantly by CYP3A4. The calculated relative contribution of CYP3A4 to carbofuran formation was 93%, while it was 4.4% for CYP2C9. The major contribution of CYP3A4 in benfuracarb metabolism was further substantiated by showing a strong correlation with CYP3A4-selective markers midazolam-1'-hydroxylation and omeprazole-sulfoxidation (r=0.885 and 0.772, respectively). Carbofuran formation was highly inhibited by the CYP3A inhibitor ketoconazole. Moreover, CYP3A4 marker activities were relatively inhibited by benfuracarb. These results confirm that human CYP3A4 is the major enzyme involved in the in vitro activation of benfuracarb and that CYP3A4-catalyzed metabolism is the primary source of interindividual differences.
Topics: Adult; Benzofurans; Biotransformation; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Female; Humans; Insecticides; Isoenzymes; Ketoconazole; Male; Metabolic Networks and Pathways; Microsomes, Liver; Middle Aged; beta-Alanine
PubMed: 24016712
DOI: 10.1016/j.toxlet.2013.08.023 -
The Journal of Toxicological Sciences May 1995The antidotal action of atropine sulfate and 2-pyridine aldoxime methiodide (2-PAM) against poisoning attributable to the new procarbamate insecticide benfuracarb...
The antidotal action of atropine sulfate and 2-pyridine aldoxime methiodide (2-PAM) against poisoning attributable to the new procarbamate insecticide benfuracarb [(ethyl N-[2,3-dihydro-2,2-dimethylbenzofuran-7-yloxycarbonyl (methyl) aminothio]-N-isopropyl-beta-alaninate] was compared utilizing rats as our experimental model. Both the intraperitoneal and oral administrations of these antidotes were examined after five, ten, fifteen and thirty minutes exposure periods, following treatment with benfuracarb at dose levels approximating LD50 and LD100. The results obtained demonstrate that both the intraperitoneal and oral administrations of atropine sulfate blocked or significantly reduced the toxic effects of benfuracarb and protected the animals from death. The intraperitoneal administration route appears to be more effective than was the oral route. In addition, the administration of atropine sulfate after the shorter period (up to 15 minutes), following exposure to benfuracarb, improved antidotal action, particularly with the LD100 dose of benfuracarb. It is suggested that atropine sulfate antagonizes benfuracarb poisoning by blocking acetylcholine (ACh) receptors, as many other carbamate insecticides, since benfuracarb was an in vivo cholinesterase (ChE) inhibitor and the toxic effect of benfuracarb was reduced by atropine sulfate. 2-PAM, however, did not significantly block or reduce the toxic effects of benfuracarb.
Topics: Administration, Oral; Animals; Antidotes; Atropine; Benzofurans; Carbamates; Cholinesterase Reactivators; Injections, Intraperitoneal; Insecticides; Male; Pralidoxime Compounds; Rats; Rats, Sprague-Dawley; beta-Alanine
PubMed: 7473892
DOI: 10.2131/jts.20.143 -
Bulletin of Environmental Contamination... Apr 2006
Comparative Study
Topics: Adsorption; Benzofurans; Carbofuran; China; Insecticides; Soil Microbiology; Soil Pollutants; beta-Alanine
PubMed: 16688558
DOI: 10.1007/s00128-006-0979-x -
Pest Management Science Feb 2011Sorption-desorption processes govern the movement of pesticides in soil. These processes determine the potential hazard of the pesticide in a given environment for...
BACKGROUND
Sorption-desorption processes govern the movement of pesticides in soil. These processes determine the potential hazard of the pesticide in a given environment for groundwater contamination and need to be investigated.
RESULTS
In the present study, sorption-desorption processes of benfuracarb were investigated using a batch method in two mollisols. The kinetics of benfuracarb sorption in mollisols conformed to two-compartment (1 + 1) first-order kinetics. The fast sorption rate constant was about 3 times higher for silt loam than for loam soil. However, the slow sorption rate constants were statistically similar for both soils. The concentration-dependent sorption-desorption isotherms of benfuracarb could not closely conform to the Freundlich isotherm in mollisols of high organic C content. The computed values of both the sorption (log K) and desorption (log K') capacities were higher for silt loam than for loam soil. The desorption index (n'/n) values in the range 30.0-41.3 indicated poor reversibility of sorbed benfuracarb in mollisols.
CONCLUSION
In view of the strong sorption of benfuracarb in mollisols with only partial desorption, the possibility of the leaching of soil-applied benfuracarb to contaminate groundwaters appears to be low.
Topics: Adsorption; Benzofurans; Insecticides; Kinetics; Soil; Soil Pollutants; beta-Alanine
PubMed: 21072780
DOI: 10.1002/ps.2053 -
Communications in Agricultural and... 2004Blatta germanica is the more prevalent cockroach species in Algeria. In the present study, we tested the effect on reproduction in B. germanica of two insect growth...
Blatta germanica is the more prevalent cockroach species in Algeria. In the present study, we tested the effect on reproduction in B. germanica of two insect growth regulators, RH-0345, a benzoylhydrazine analogue that mimics the action of 20-hydroxyecdysone, and methoprene, one of the most commercially important juvenile hormone analogues, and a novel carbamate insecticide, benfuracarb. The compounds were applied topically (10 and 20 microg/insect for RH-0345, and 1 and 10 microg/insect for methoprene) or orally administrated (at 2% for benfuracarb) on newly emerged females and evaluated on reproductive events during the adult life (2, 4 and 6 days). Treatment with RH-0345 and benfuracarb reduced significantly the number of oocytes, the size and the volume of the basal oocyte during the experimental period. Methoprene distorted the ovarian development since it caused a significant reduction in the number of oocytes at 2, 4 and 6 days for the two tested doses, and an increase in oocyte size at 2, 4 and 6 days with 1 microg and a decrease with 10 microg. In a second series of experiments, the effects of these compounds were assayed on the ovarian proteins. Data from biochemical analysis revealed that RH-0345 and benfuracarb reduced the ovarian amounts of proteins, while treatment with methoprene increased it during the sexual maturation.
Topics: Administration, Topical; Animals; Benzoates; Benzofurans; Blattellidae; Female; Hydrazines; Insecticides; Juvenile Hormones; Methoprene; Oocytes; Ovary; Reproduction; beta-Alanine
PubMed: 15759422
DOI: No ID Found -
Environmental Science and Pollution... Mar 2006N-methylcarbamate insecticides are widely used chemicals for crop protection. This study examines the hydrolytic and photolytic cleavage of benfuracarb, carbosulfan and...
BACKGROUND
N-methylcarbamate insecticides are widely used chemicals for crop protection. This study examines the hydrolytic and photolytic cleavage of benfuracarb, carbosulfan and carbofuran under natural conditions. Their toxicity and that of the corresponding main degradation products toward aquatic organisms were evaluated.
METHODS
Suspensions of benfuracarb, carbosulfan and carbofuran in water were exposed to sunlight, with one set of dark controls, for 6 days, and analyzed by 1H-NMR and HPLC. Acute toxicity tests were performed on Brachionus calyciflorus, Daphnia magna, and Thamnocefalus platyurus. Chronic tests were performed on Pseudokirchneriella subcapitata, and Ceriodaphnia dubia.
RESULTS AND DISCUSSION
Under sunlight irradiation, benfuracarb and carbosulfan gave off carbofuran and carbofuran-phenol, while only carbofuran was detected in the dark experiments. The latter was degraded to phenol by exposure to sunlight. Effects of pH, humic acid and KNO3 were evaluated by kinetics on dilute solutions in the dark and by UV irradiation, which evidenced the lability of the pesticide at pH 9. All three pesticides and phenol exhibited acute and higher chronic toxicity towards the aquatic organisms tested.
CONCLUSION
Investigation on the hydrolysis and photolysis of benfuracarb and carbosulfan under natural conditions provides evidence concerning the selective decay to carbofuran and/or phenol. Carbofuran is found to be more persistent and toxic.
RECOMMENDATIONS AND OUTLOOK
The decay of benfuracarb and carbosulfan to carbofuran and the relative stability of this latter pesticide account for many papers that report the detection of carbofuran in water, fruits and vegetables.
Topics: Animals; Benzofurans; Carbamates; Carbofuran; Daphnia; Insecticides; Lethal Dose 50; Rotifera; Water Pollutants, Chemical; beta-Alanine
PubMed: 16612899
DOI: 10.1065/espr2005.10.285