Inhibitor Report for: Fosthiazate

BACKGROUND: The potential for enhanced degradation of the carbamoyloxime nematicides aldicarb and oxamyl and the organophosphate fosthiazate was investigated in 35 UK agricultural soils. Under laboratory conditions, soil samples received three successive applications of nematicide at 25 day intervals.
RESULTS: The second and third applications of aldicarb were degraded at a faster rate than the first application in six of the 15 aldicarb-treated soils, and a further three soils demonstrated rapid degradation of all three applications. High organic matter content and low pH had an inhibitory effect on the rate of aldicarb degradation. Rapid degradation was observed in nine out of the ten soils treated with oxamyl. In contrast, none of the fosthiazate-treated soils demonstrated enhanced degradation. CONCLUSION: The potential for enhanced degradation of aldicarb and oxamyl was demonstrated in nine out of 15 and nine out of ten soils respectively that had previously been treated with these active substances. Degradation of fosthiazate occurred at a much slower rate, with no evidence of enhanced degradation. Fosthiazate may provide a useful alternative in cases where the efficacy of aldicarb and oxamyl has been reduced as a result of enhanced degradation.

Considerable attention has been paid to the enantiomeric resolution and toxicity of some chiral organophosphorous pesticides (OPs) with one asymmetric center, but research concerning chiral OPs with two asymmetric centers is still limited. In the present study, the stereoisomeric separation and toxicity of fosthiazate, a chiral OP with two asymmetric centers on phosphorus and carbon atoms, was investigated. All four stereoisomers of fosthiazate were separated successfully with a Chiralpak(R) AD [amylase tris(3,5-dimethyl-phenyl carbamate)] column on high-performance liquid chromatography. The resolved isomers and the pairs of enantiomers were further distinguished using a circular dichroism detector and an optical rotation detector, designating the first (pk1) and third (pk3) eluted peaks as one pair of enantiomers and the second (pk2) and fourth (pk4) peaks as the other pair. The developed method was used to prepare microquantities of individual stereoisomers that were used for in vitro and in vivo bioassays. The inhibition potencies of the stereoisomers against acetylcholinesterase of Electrophorus electricus were slightly stereoselective, with a maximum difference of 1.4-fold among the isomers. A 3.1-fold difference, however, was observed in the acute toxicity of isomers to Daphnia magna. The 48-h toxicity of isomers to D. magna followed the order pk1 > pk2 > pk4 > racemate approximately pk3. The stereoselective toxicity to D. magna found in fosthiazate suggests that the environmental safety of fosthiazate should be evaluated on the basis of its individual isomers.

Adsorption and degradation behavior of a pesticide in soil has a strong effect on its environmental fate as well as efficacy for pest control. Fosthiazate is an organophosphate compound that is currently under development as a nonfumigant nematicide. In this study, we evaluated adsorption and degradation kinetics of fosthiazate in three U.S. soils with different properties. Adsorption of fosthiazate in mineral soil was negligibly weak but appeared to increase with soil organic matter (OM) content. The half-life (T(1/2)) of fosthiazate ranged from 0.5 to 1.5 months in nonsterile soils but was prolonged to 1-3 months after sterilization. Degradation of fosthiazate in soil appeared to be caused by both chemical and microbial transformations. The persistence of fosthiazate generally decreased with increasing soil pH, but increased with increasing soil OM and clay contents. This results suggest that fosthiazate may have an enhanced leaching potential in acidic soils with low OM content, and its efficacy in high pH soils may not last as long as in neutral soils because of faster degradation.

The root-knot nematode Meloidogyne incognita causes severe damage to continuously cropping vegetables. The control of this nematode relies heavily on organophosphate nematicides in China. Here, we described resistance to the organophosphate nematicide fosthiazate in a greenhouse-collected resistant population (RP) and a laboratory susceptible population (SP) of M. incognita. Fosthiazate was 2.74-fold less toxic to nematodes from RP than that from SP. Quantitative real-time PCR revealed that the acetylcholinesterase2 (ace2) transcription level in the RP was significantly higher than that in the SP. Eighteen nonsynonymous amino acid differences in ace2 were observed between the cDNA fragments of the RP and SP. The acetylcholinesterase (AChE) protein activity in the RP was significantly reduced compared with that in the SP. After knocking down the ace2 gene, the ace2 transcription level was significantly decreased, but no negative impact on the infection of juveniles was observed. The 50% lethal concentration of the RNAi RP population decreased 40%, but the inhibition rate of fosthiazate against AChE activity was significantly increased in RP population. Thus, the increased fosthiazate insensitivity in the M. incognita resistant population was strongly associated with mutations in ace2. These results provide valuable insights into the resistance mechanism of root-knot nematode to organophosphate nematicides.

BACKGROUND: The potential for enhanced degradation of the carbamoyloxime nematicides aldicarb and oxamyl and the organophosphate fosthiazate was investigated in 35 UK agricultural soils. Under laboratory conditions, soil samples received three successive applications of nematicide at 25 day intervals.
RESULTS: The second and third applications of aldicarb were degraded at a faster rate than the first application in six of the 15 aldicarb-treated soils, and a further three soils demonstrated rapid degradation of all three applications. High organic matter content and low pH had an inhibitory effect on the rate of aldicarb degradation. Rapid degradation was observed in nine out of the ten soils treated with oxamyl. In contrast, none of the fosthiazate-treated soils demonstrated enhanced degradation. CONCLUSION: The potential for enhanced degradation of aldicarb and oxamyl was demonstrated in nine out of 15 and nine out of ten soils respectively that had previously been treated with these active substances. Degradation of fosthiazate occurred at a much slower rate, with no evidence of enhanced degradation. Fosthiazate may provide a useful alternative in cases where the efficacy of aldicarb and oxamyl has been reduced as a result of enhanced degradation.

BACKGROUND: In intensive agriculture, the use of pesticides and soil fumigants is necessary to produce economically viable crops worldwide. However, this practice may involve undesirable effects on human health and the environment. In 1995, methyl bromide was restricted by the Montreal Protocol because of possible ozone depletion. The objective of this study was to compare intrinsic environmental and toxicological properties of 11 active substances with nematicidal properties, some of them recognized as methyl bromide alternatives. RESULTS: Four groups of active substances were discriminated by a series of principal component analyses (PCAs): (a) high toxicity to non-target fauna, humans and animals and medium persistence in the environment (cadusafos, ethoprophos and fenamiphos); (b) high toxicity to humans, animals and non-target fauna and high persistence (carbofuran and fosthiazate); (c) low toxicity to non-target fauna, humans and animals and low persistence (carbosulfan, benfuracarb and oxamyl); (d) low toxicity to humans, animals and non-target fauna and medium persistence in the environment (1,3-dichloropropene, chloropicrin and methyl bromide). CONCLUSION: Evaluating the multiple aspects of toxicological and environmental properties of active substances through PCA is proposed as a helpful tool for initially comparing the complex toxicological behaviour of active substances as plant protection products.

Fosthiazate is an organophosphorus nematicide which was recently included in Annex I of the Directive 91/414/EEC under the clause that it should be used with special care in soils vulnerable to leaching. Thus, the leaching of fosthiazate was investigated in columns packed with three different soils which represented situations of high (site 2), intermediate (site 1) and low (site 3) leaching potential. The recommended dose of fosthiazate was applied at the surface of the soil columns and fosthiazate fate and transport was investigated for the next two months. Fosthiazate concentrations in the leachate collected from the bottom of the columns packed with soil from site 2 exceeded 0.1 microgl(-1) in most cases. This soil was characterized as acidic, indicating longer fosthiazate persistence, with low organic matter content, indicating weak adsorption, thus representing a situation vulnerable to leaching. In contrast, the lowest concentrations of fosthiazate in the leachate were evident in the columns packed with soil from site 3. This soil was characterized as alkaline, indicating faster degradation, with higher organic matter content, indicating stronger adsorption, thus representing a situation not favoring leaching of fosthiazate. The highest concentration of fosthiazate in the leachate from the columns packed with soil from site 2 was 3.44 microgl(-1) compared to 1.17 and 0.16 microgl(-1), which were the corresponding maximum values measured in columns packed with soil from sites 1 and 3, respectively. The results of the current study further suggest that fosthiazate is mobile in soil and can leach under conducive soil conditions like acidic soils with low organic matter content.

Considerable attention has been paid to the enantiomeric resolution and toxicity of some chiral organophosphorous pesticides (OPs) with one asymmetric center, but research concerning chiral OPs with two asymmetric centers is still limited. In the present study, the stereoisomeric separation and toxicity of fosthiazate, a chiral OP with two asymmetric centers on phosphorus and carbon atoms, was investigated. All four stereoisomers of fosthiazate were separated successfully with a Chiralpak(R) AD [amylase tris(3,5-dimethyl-phenyl carbamate)] column on high-performance liquid chromatography. The resolved isomers and the pairs of enantiomers were further distinguished using a circular dichroism detector and an optical rotation detector, designating the first (pk1) and third (pk3) eluted peaks as one pair of enantiomers and the second (pk2) and fourth (pk4) peaks as the other pair. The developed method was used to prepare microquantities of individual stereoisomers that were used for in vitro and in vivo bioassays. The inhibition potencies of the stereoisomers against acetylcholinesterase of Electrophorus electricus were slightly stereoselective, with a maximum difference of 1.4-fold among the isomers. A 3.1-fold difference, however, was observed in the acute toxicity of isomers to Daphnia magna. The 48-h toxicity of isomers to D. magna followed the order pk1 > pk2 > pk4 > racemate approximately pk3. The stereoselective toxicity to D. magna found in fosthiazate suggests that the environmental safety of fosthiazate should be evaluated on the basis of its individual isomers.

Adsorption and degradation behavior of a pesticide in soil has a strong effect on its environmental fate as well as efficacy for pest control. Fosthiazate is an organophosphate compound that is currently under development as a nonfumigant nematicide. In this study, we evaluated adsorption and degradation kinetics of fosthiazate in three U.S. soils with different properties. Adsorption of fosthiazate in mineral soil was negligibly weak but appeared to increase with soil organic matter (OM) content. The half-life (T(1/2)) of fosthiazate ranged from 0.5 to 1.5 months in nonsterile soils but was prolonged to 1-3 months after sterilization. Degradation of fosthiazate in soil appeared to be caused by both chemical and microbial transformations. The persistence of fosthiazate generally decreased with increasing soil pH, but increased with increasing soil OM and clay contents. This results suggest that fosthiazate may have an enhanced leaching potential in acidic soils with low OM content, and its efficacy in high pH soils may not last as long as in neutral soils because of faster degradation.

The nematicide fosthiazate was evaluated over a 3-year period for management of Meloidogyne incognita race 3 (site 1) and M. arenaria race 2 (site 2) in flue-cured tobacco. Fosthiazate was applied broadcast and incorporated at rates ranging from 22 to 88 g a.i./100 m(2), and compared with the nematicides fenamiphos (67 g a.i./100 m(2)), 1,3-D (56.1 L/ha, 670 ml/100-m row), and an untreated control. Root-gall indices and leaf yields were averaged over the 3-year period. Root galling was negatively correlated in a linear relationship with fosthiazate application rate at sites 1 and 2. Leaf yields were positively correlated with fosthiazate application rate at site 1 and could be described by a quadratic equation. Leaf yields were greater at 33 and 88 g a.i./100 m(2) application rates (site 2) than the untreated control. Leaf yields in fosthiazate (88 g a.i./100 m(2))-treated plots infested with M. incognita or M. arenaria were not different from plots fumigated with 1,3-D. Plants in plots with fosthiazate applied in a row band (1993) had a lower root-gall index than those in plots with the same rate of fosthiazate applied broadcast. Fosthiazate may provide an alternative to fumigation for control of M. incognita and M. arenaria.

The impacts of fosthiazate on potato (Solanum tuberosum) tuber yields and populations of root lesion nematodes (primarily Pratylenchus penetrans) were studied during 1991-1994 in experimental plots on Prince Edward Island. Tuber yields were greater in treated plots when compared to untreated plots by 8% and 30% during 1991 and 1993, respectively. Numbers of nematodes in roots were reduced by the treatments in every year, and nematode populations in soil were suppressed in 1991, 1993, and 1994. Tuber yields in 1993 and 1994 were higher, and nematode counts in soil and roots in 1991, 1993, and 1994 were lower in plots treated with the emulsifiable concentrate formulations of fosthiazate than in plots treated with the granular formulations. Yields of plots treated with fosthiazate did not differ consistently from yields of plots treated with aldicarb. The results indicated that fosthiazate should be useful for potato production in the Maritime region of Canada.

One grower trial and two experiment station tests were conducted to evaluate a new nematicide, fosthiazate, for management of Meloidogyne javanica in Florida flue-cured tobacco. Fosthiazate was applied broadcast and incorporated at rates ranging from 21 to 84 g/100 m(2) and compared with 1,3-dichloropropene at 240 and 460 ml/100 m(2) and fenamiphos at 67 g/100 m(2). All fosthiazate treatments increased tobacco yields and reduced root galling. Application of 1,3-D provided the highest tobacco yields and greatest reductions in root galling. The fenamiphos treatment outperformed all fosthiazate treatments in tobacco yield and root gall reduction. Fosthiazate may therefore have limited utility compared with 1,3-D and fenamiphos as a nematicide for tobacco in peninsular Florida.