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Activity: Herbicide (dinitroaniline)
Structure:

Adverse Effects:
Blood
Brain
CNS
Cytotoxic, genotoxic, and induces apoptosis
Endocrine: Testicular - spermatogenesis
Genotoxic
Liver
Environmental

Blood (click on for all fluorinated pesticides)

PubMed Abstract: Basalin, a herbicide, was administered orally to male rats at doses ranging from 60 mg to 1.92 g/kg for 13 weeks. Oral LD50 of the compound was 1.65 g/kg. Toxic effects included hyperexcitability and tremors. The cumulative lethal dose (CLD50) at the end of week 13 was 135 mg/kg with a cumulative toxicity factor (CTF) of 12.22. At 1.92 g/kg, no animals survived to 13 weeks. At 60 and 120 mg/kg, there were no significant changes in body weight gain compared with the controls and a significant decrease in total leukocyte count (TLC), erythrocyte sedimentation rate (ESR) and Hb was observed. There was a decrease in spermatogenesis and infiltration of mononucleated cells in the liver.
Ref: Toxicol Lett 1983 Aug;18(1-2):13-8. Subacute toxicity of Basalin in rats. Gupta PK, Singh YP, Parihar NS.
http://www.fluoridealert.org/pesticides/Fluchloralin.PubMebAbstract.htm

Brain (click on for all fluorinated pesticides)

Abstract. Basalin, a formulation of fluchloralin (N-(2-chloroethyl)-2-6-dinitro-N-propyl-4-(trifluoromethyl)-aniline), is being very widely used as herbicide in large number of important crops. But very limited data on its toxicological profile is available. Its adverse effects on central nervous system and locomotor alterations in sheep given 5 mg/kg orally have been reported. Preliminary studies in our laboratory indicated alteration in gait in chicken given Basalin orally @ 200-500 mg/kg followed by ataxia at higher doses. Since chicken is a suitable model for neurotoxicity assay, present studies were conducted on one week old broiler chicks given Basalin daily for four weeks through feed at different dose levels of 50 mg/kg (Gr I), 100 mg/kg (Gr II) and 150 mg/kg (Gr III). Each group contained ten chicks. The control chicks (Gr C) were given equal amount of normal feed. Activities of brain, liver and plasma acetylcholinesterase (ACHE), carboxylesterase (CE) and brain neurotoxicesterase (NTE) were estimated, the tissue esterases after four weeks treatment and plasma esterases at weekly intervals. The locomoter activity was determined using inclined plane at alternate days. Histopathological examinations of brains and spinal cords of four birds from each group were conducted after four weeks treatment. The data on all these experiments indicated inhibition of all tissue and plasma esterases in a dose dependent manner, which were significant in chicks of Gr III receiving maximum dose for four weeks. (Brain NTE 70%, brain and liver ACHE 85.71 and 85.45% respectively and liver CE 85.58% of control activity). The plasma ACHE and CE activities were significantly inhibited in this group after two weeks onwards (ACHE90.8-90.3%, CE 84.9-84.5% of control). Alteration in gait in Gr III chicks was observed after three weeks treatment and was correlated with NTE inhibition. Histopathological examinations of brain and spinal cords of chicks receiving maximum dose revealed increased number of Schwann cells in brain and small numbers of myelinated nerve fibers in spinal cord. The studies thus indicated possibility of neuropathic effects of Basalin on prolonged exposure or at higher doses.
Ref: Basalin induced neurotoxic effects in broiler chicks; by Sushma Rishi and Uma Arora. Toxicology Letters; Volume 95, Supplement 1 , July 1998, Pages 144-145.

CNS (click on for all fluorinated pesticides)

Human Toxicity Excerpts: SYMPTOMATOLOGY INDICATES OVERDOSING MAY PRODUCE /CNS DEPRESSION/ AND OTHER GENERAL CNS INVOLVEMENT. [Weed Science Society of America. Herbicide Handbook. 5th ed. Champaign, Illinois: Weed Science Society of America, 1983. 238]
Ref: Hazardous Substance Data Bank for FLUCHLORALIN CASRN: 33245-39-5 from Toxnet.

Abstract. Male Swiss mice, 25-30 g, were utilized to define some of the behavioral effects of the herbicides Lasso [alachlor 43%; (A)], Basalin [fluchloralin 45%; (F)], Premerge 3 [dinoseb 51%; (D)], and the fungicide Maneb-80 [maneb 80%; (M)]. These compounds were tested for their effects on locomotor activity and for their ability to establish a conditioned taste aversion following oral or dermal exposure. Individual and grouped (N = 5) activity measures were assessed immediately following the dermal administration of the commercially available pesticide formulations. Grouped activity measures were also assessed following the oral administration of the compounds. Total activity was significantly (p less than 0.05) increased over vehicle controls in both grouped and individual subjects by A, F, and D following dermal administration. Grouped activity measures were also increased by A, F, D, and M following the oral administration of the compounds...
Ref: The behavioral effects of pesticides in male mice; by Mitchell JA, Long SF, Wilson MC, Kallman MJ. Neurotoxicol Teratol 1989 Jan-Feb;11(1):45-50.

Abstract. Basalin, a formulation of fluchloralin (N-(2-chloroethyl)-2-6-dinitro-N-propyl-4-(trifluoromethyl)-aniline), is being very widely used as herbicide in large number of important crops. But very limited data on its toxicological profile is available. Its adverse effects on central nervous system and locomotor alterations in sheep given 5 mg/kg orally have been reported. Preliminary studies in our laboratory indicated alteration in gait in chicken given Basalin orally @ 200-500 mg/kg followed by ataxia at higher doses. Since chicken is a suitable model for neurotoxicity assay, present studies were conducted on one week old broiler chicks given Basalin daily for four weeks through feed at different dose levels of 50 mg/kg (Gr I), 100 mg/kg (Gr II) and 150 mg/kg (Gr III). Each group contained ten chicks. The control chicks (Gr C) were given equal amount of normal feed. Activities of brain, liver and plasma acetylcholinesterase (ACHE), carboxylesterase (CE) and brain neurotoxicesterase (NTE) were estimated, the tissue esterases after four weeks treatment and plasma esterases at weekly intervals. The locomoter activity was determined using inclined plane at alternate days. Histopathological examinations of brains and spinal cords of four birds from each group were conducted after four weeks treatment. The data on all these experiments indicated inhibition of all tissue and plasma esterases in a dose dependent manner, which were significant in chicks of Gr III receiving maximum dose for four weeks. (Brain NTE 70%, brain and liver ACHE 85.71 and 85.45% respectively and liver CE 85.58% of control activity). The plasma ACHE and CE activities were significantly inhibited in this group after two weeks onwards (ACHE90.8-90.3%, CE 84.9-84.5% of control). Alteration in gait in Gr III chicks was observed after three weeks treatment and was correlated with NTE inhibition. Histopathological examinations of brain and spinal cords of chicks receiving maximum dose revealed increased number of Schwann cells in brain and small numbers of myelinated nerve fibers in spinal cord. The studies thus indicated possibility of neuropathic effects of Basalin on prolonged exposure or at higher doses.
Ref: Basalin induced neurotoxic effects in broiler chicks; by Sushma Rishi and Uma Arora. Toxicology Letters; Volume 95, Supplement 1 , July 1998, Pages 144-145.

Cytotoxic, genotoxic, and induces apoptosis (click on for all fluorinated pesticides)

Pub Med Abstract: Fluchloralin is cytotoxic and genotoxic and induces apoptosis in mammalian cells.
The genotoxic and cytotoxic effects of a widely used herbicide, fluchloralin, were assessed using cultured mammalian cells. Treatment of cells for 8-12 hr with fluchloralin resulted in a significant increase in the frequency of metaphase cells with chromosomal damage. At higher concentrations, the herbicide also induced an increase in the frequency of sister chromatid exchange. A 50% loss in viability was observed when cells were exposed to the herbicide for 72 hr. To understand the mechanism of cell death caused by fluchloralin, its effect on DNA synthesis and its ability to induce apoptosis were investigated. Even short (6 hr) treatment of cells with fluchloralin resulted in a 30-50% inhibition of DNA synthesis. Agarose gel electrophoresis of DNA from herbicide-treated cells and cytochemical staining indicate the induction of apoptosis by fluchloralin.
Ref: Environ Mol Mutagen 1998;31(3):257-62. Fluchloralin is cytotoxic and genotoxic and induces apoptosis in mammalian cells. Sinha S, Panneerselvam N, Shanmugam G.
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9585264&dopt=Abstract

Abstract: The genotoxic effect of fluchloralin (33245-39-5) in cultured human blood lymphocytes was investigated. Venous blood samples were obtained from healthy donors and lymphocyte cultures were established. Cell cultures were treated with 2.5, 5.0, or 10 micrograms/milliliter (microg/ml) fluchloralin for 24 or 48 hours. Following treatment, slides were prepared and cells were scored for chromatid aberrations. In a micronuclei (MN) test, cell were exposed up to 50microg/ml fluchloralin for up to 48 hours. Cell microslides were prepared and scored for MN frequency. Treatment of the lymphocytes for 24 to 48 hours resulted in a significant dose dependent increase in the total number of chromatid type aberrations. The frequency of chromatid aberrations was high compared to isochromatid breaks at all dose levels. The increase in the frequency of isochromatid breaks was notable after 48 hours of treatment. Gap formation was high at all concentrations. Multiple aberrated cells showed a dose dependent increase at both time points. The frequency of occurrence of MN in cultured human blood lymphocytes following fluchloralin treatment was noted. The induction of MN formation was similar and significant at 24 and 48 hours of treatment at 2.5 to 10microg/ml. At the higher concentrations there was a statistically dose related increase in the frequency of micronucleated binucleate cells. The authors conclude that fluchloralin at higher concentrations have the ability to damage the human genome.
Ref: Genotoxicity of the herbicide fluchloralin on human lymphocytes in vitro: chromosomal aberration and micronucleus tests; by Panneerselvam N, Sinha S, Shanmugam G. Mutat Res 1995 Aug;344(1-2):69-72

Endocrine: Testicular (click on for all fluorinated pesticides)

Abstract. Subacute and acute toxicity of the herbicide N-propyl-N-(2-chloroethyl)-2,6-dinitro-4-trifluromethyl-aniline (33245-39-5) (Basalin) was investigated. Some male albino-rats received graded doses from 0.5 to 4 grams per kilogram (g/kg) of the compound, orally administered as a single dose. Median lethal doses (LD50) were calculated. Other rats received 60, 120, 240, 480, or 960 milligrams (mg)/kg or 1.92g/kg Basalin, orally administered 6 days a week for 13 weeks, and cumulative LD50 were determined. Animals receiving 60 and 120mg/kg Basalin were killed; liver, kidney, heart, spleen, brain, lung, testes, and adrenal glands were weighed, sectioned, and examined for structural changes. Blood total leukocyte count, erythrocyte sedimentation rate, packed cell volume, and blood glucose were measured. The oral LD50 for Basalin in male rats was 1.65g/kg. No animals receiving Basalin at a dose of 1.92g/kg or more daily for 1 week survived. Animals developed hyperexcitability and tremors; these were followed by convulsions and death. The cumulative LD50 after 13 weeks was 135mg/kg. Basalin had a slow and steady cumulative effect, reaching a maximum after 10 weeks. In animals receiving 60 or 120mg/kg of the herbicide for 13 weeks, liver weight was significantly increased whereas that of spleen, heart, testes, and adrenal glands was significantly decreased. Total leukocytes, hemoglobin, and erythrocyte sedimentation rate were increased in a dose dependent manner. Blood glucose showed a 10 percent decrease at 120mg/kg Basalin. The 60mg/kg dose did not produce significant pathological change in the organs examined. However, 120mg/kg provoked infiltration of mononuclear cells in liver tissue. Spermatids in seminiferous tubules were reduced at this dose; a few tubules were coalescing and filled with binucleate spermatogonial cells. The authors conclude that oral administration of Basalin as a single dose or with repeated administration produces a dose dependent toxicity.
Ref: Toxicol Lett 1983 Aug;18(1-2):13-8. Subacute toxicity of Basalin in rats. Gupta PK, Singh YP, Parihar NS.
http://www.fluoridealert.org/pesticides/Fluchloralin.PubMebAbstract.htm

Genotoxic (click on for all fluorinated pesticides)

Pub Med Abstract: Fluchloralin is cytotoxic and genotoxic and induces apoptosis in mammalian cells.
The genotoxic and cytotoxic effects of a widely used herbicide, fluchloralin, were assessed using cultured mammalian cells. Treatment of cells for 8-12 hr with fluchloralin resulted in a significant increase in the frequency of metaphase cells with chromosomal damage. At higher concentrations, the herbicide also induced an increase in the frequency of sister chromatid exchange. A 50% loss in viability was observed when cells were exposed to the herbicide for 72 hr. To understand the mechanism of cell death caused by fluchloralin, its effect on DNA synthesis and its ability to induce apoptosis were investigated. Even short (6 hr) treatment of cells with fluchloralin resulted in a 30-50% inhibition of DNA synthesis. Agarose gel electrophoresis of DNA from herbicide-treated cells and cytochemical staining indicate the induction of apoptosis by fluchloralin.
Ref: Environ Mol Mutagen 1998;31(3):257-62. Fluchloralin is cytotoxic and genotoxic and induces apoptosis in mammalian cells. Sinha S, Panneerselvam N, Shanmugam G.
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9585264&dopt=Abstract

Liver (click on for all fluorinated pesticides)

PubMed Abstract: Basalin [Fluchloralin], a herbicide, was administered orally to male rats at doses ranging from 60 mg to 1.92 g/kg for 13 weeks. Oral LD50 of the compound was 1.65 g/kg. Toxic effects included hyperexcitability and tremors. The cumulative lethal dose (CLD50) at the end of week 13 was 135 mg/kg with a cumulative toxicity factor (CTF) of 12.22. At 1.92 g/kg, no animals survived to 13 weeks. At 60 and 120 mg/kg, there were no significant changes in body weight gain compared with the controls and a significant decrease in total leukocyte count (TLC), erythrocyte sedimentation rate (ESR) and Hb was observed. There was a decrease in spermatogenesis and infiltration of mononucleated cells in the liver.
Ref: Toxicol Lett 1983 Aug;18(1-2):13-8. Subacute toxicity of Basalin in rats by Gupta PK, Singh YP, and Parihar NS.
http://www.fluoridealert.org/pesticides/Fluchloralin.PubMebAbstract.htm