Design, Synthesis, and Nematocidal Evaluation of Waltherione A Derivatives: Leveraging a Structural Simplification Strategy.

Southern root-knot nematodes are among the most pernicious phytoparasites; they are responsible for substantial yield losses in agricultural crops worldwide. The limited availability of nematicides for the prevention and control of plant-parasitic nematodes necessitates the urgent development of novel nematicides. Natural products have always been a key source for the discovery of pesticides. Waltherione A, an alkaloid, exhibits potent nematocidal activity. In this study, we designed and synthesized a series of quinoline and quinolone derivatives from Waltherione A, leveraging a strategy of structural simplification. Bioassays have revealed that the quinoline derivatives exhibit better activity than quinolone derivatives in terms of both nematocidal and fungicidal activities. Notably, compound D1 demonstrated strong nematocidal activity, with a 72 h LC50 of 23.06 µg/mL, and it effectively controlled the infection of root-knot nematodes on cucumbers. The structure-activity relationship suggests that the quinoline moiety is essential for the nematocidal efficacy of Waltherione A. Additionally, compound D1 exhibited broad-spectrum fungicidal activity, with an EC50 of 2.98 µg/mL against Botrytis cinerea. At a concentration of 200 µg/mL, it significantly inhibited the occurrence of B. cinerea on tomato fruits, with an inhibitory effect of 96.65%, which is slightly better than the positive control (90.30%).

Biocontrol of plant parasitic nematodes by bacteria and fungi: a multi-omics approach for the exploration of novel nematicides in sustainable agriculture.

Plant parasitic nematodes (PPNs) pose a significant threat to global crop productivity, causing an estimated annual loss of US $157 billion in the agriculture industry. While synthetic chemical nematicides can effectively control PPNs, their overuse has detrimental effects on human health and the environment. Biocontrol agents (BCAs), such as bacteria and fungi in the rhizosphere, are safe and promising alternatives for PPNs control. These BCAs interact with plant roots and produce extracellular enzymes, secondary metabolites, toxins, and volatile organic compounds (VOCs) to suppress nematodes. Plant root exudates also play a crucial role in attracting beneficial microbes toward infested roots. The complex interaction between plants and microbes in the rhizosphere against PPNs is mostly untapped which opens new avenues for discovering novel nematicides through multi-omics techniques. Advanced omics approaches, including metagenomics, transcriptomics, proteomics, and metabolomics, have led to the discovery of nematicidal compounds. This review summarizes the status of bacterial and fungal biocontrol strategies and their mechanisms for PPNs control. The importance of omics-based approaches for the exploration of novel nematicides and future directions in the biocontrol of PPNs are also addressed. The review highlighted the potential significance of multi-omics techniques in biocontrol of PPNs to ensure sustainable agriculture.

Simulation and application assessment of the efficacy of fosthiazate-loaded microcapsules against root-knot nematode.

BACKGROUND: Although microencapsulation technology is an effective pesticide formulation method, the correlation between the release properties of microcapsules and pesticide concentrations in soil and their efficacy has not been thoroughly investigated. Here, the effects of the release properties of the nematicide Fosthiazate (FTZ) from microcapsules on their efficacy against the nematode Meloidogyne incognita were examined using experimental and mathematical approaches. RESULTS: Gradual release of FTZ from both polyurea microcapsules (PU-MC) and melamine-formaldehyde microcapsules (MF-MC) was observed over 30 days in the release test, and each release curve was completely distinct. In the biological test, the efficacy of both microcapsules against M. incognita 42 days after the application was 8-15% higher than that of the non-encapsulated FTZ at a concentration of 2.0 mg FTZ kg-1 soil. Soil degradation experiments suggested that the microcapsules worked effectively to protect the FTZ from degradation, which resulted in higher efficacy at a later stage. A simulation study to predict the concentration of FTZ outside the microcapsule found that the timing of supplying FTZ was important and suggested that the mixture of non-encapsulated FTZ (non-MC) and MF-MC showed enhanced efficiency for the entire cultivation period in the biological test; the efficacy against nematodes was also confirmed by the measurement of nematode density using the Bearman funnel method. CONCLUSION: The release properties of FTZ from microcapsules are critical for their effective application against M. incognita, and the established simulation study is a useful step in designing suitable release properties under complex soil conditions. © 2024 Society of Chemical Industry.

Unraveling the enigma of root-knot nematodes: from origins to advanced management strategies in agriculture.

MAIN CONCLUSION: Integrated management strategies, including novel nematicides and resilient cultivars, offer sustainable solutions to combat root-knot nematodes, crucial for safeguarding global agriculture against persistent threats. Root-knot nematodes (RKN) pose a significant threat to a diverse range of host plants, with their obligatory endoparasitic nature leading to substantial agricultural losses. RKN spend much of their lives inside or in contact by secreting plant cell wall-modifying enzymes resulting in the giant cell development for establishing host-parasite relationships. Additionally, inflicting physical harm to host plants, RKN also contributes to disease complexes creation with fungi and bacteria. This review comprehensively explores the origin, history, distribution, and physiological races of RKN, emphasizing their economic impact on plants through gall formation. Management strategies, ranging from cultural and physical to biological and chemical controls, along with resistance mechanisms and marker-assisted selection, are explored. While recognizing the limitations of traditional nematicides, recent breakthroughs in non-fumigant alternatives like fluensulfone, spirotetramat, and fluopyram offer promising avenues for sustainable RKN management. Despite the success of resistance mechanisms like the Mi gene, challenges persist, prompting the need for integrative approaches to tackle Mi-virulent isolates. In conclusion, the review stresses the importance of innovative and resilient control measures for sustainable agriculture, emphasizing ongoing research to address evolving challenges posed by RKN. The integration of botanicals, resistant cultivars, and biological controls, alongside advancements in non-fumigant nematicides, contributes novel insights to the field, laying the ground work for future research directions to ensure the long-term sustainability of agriculture in the face of persistent RKN threats.

Discovery and Mechanism of a Nematicide Candidate (W3): A Novel Amide Compound Containing a Cyclopropyl Moiety.

To find novel nematicides, we screened the nematicidal activity of compounds in our laboratory compound library. Interestingly, the compound N-((1R,2R)-2-(2-fluoro-4-(trifluoromethyl)phenyl)cyclopropyl)-2-(trifluoromethyl)benzamide (W3) showed a broad spectrum and excellent nematicidal activity. The LC50 values of compound W3 against second-stage juveniles of Bursaphelenchus xylophilus (B. xylophilus), Aphelenchoides besseyi, and Ditylenchus destructor are 1.30, 1.63, and 0.72 mg/L, respectively. Nematicidal activities of compound W3 against second-stage juveniles of Meloidogyne incognita were 87.66% at 100 mg/L. Meanwhile, compound W3 can not only observably inhibit the feeding, reproduction, and egg hatching of B. xylophilus but can also effectively promote the oxidative stress adverse reactions of nematodes and cause intestinal damage. Compound W3 can promote the production of MDA and inhibit the activities of defense enzymes SOD and GST in B. xylophilus. Compound W3 can affect the transcription of genes involved in regulating the tricarboxylic acid cycle in nematodes, resulting in weakened nematode respiration and reduced nematode activity and even death. In addition, compound W3 had good inhibitory activity against five pathogenic fungi. Among them, the EC50 of compound W3 against Fusarium graminearum was 8.4 mg/L. In the future, we will devote ourselves to the toxicological and structural optimization research of the candidate nematicide W3.

Nematicidal Activity of Phytochemicals against the Root-Lesion Nematode Pratylenchus penetrans.

Plant-parasitic nematodes (PPNs) are highly damaging pests responsible for heavy losses in worldwide productivity in a significant number of important plant crops. Common pest management strategies rely on the use of synthetic chemical nematicides, which have led to serious concerns regarding their impacts on human health and the environment. Plant natural products, or phytochemicals, can provide a good source of agents for sustainable control of PPNs, due to their intrinsic characteristics such as higher biodegradability, generally low toxicity for mammals, and lower bioaccumulation in the environment. In this work, the nematicidal activity of 39 phytochemicals was determined against the root-lesion nematode (RLN) Pratylenchus penetrans using standard direct and indirect contact methodologies. Overall, the RLN was tolerant to the tested phytochemicals at the highest concentration, 2 mg/mL, seldom reaching full mortality. However, high activities were obtained for benzaldehyde, carvacrol, 3-octanol, and thymol, in comparison to other phytochemicals or the synthetic nematicide oxamyl. These phytochemicals were seen to damage nematode internal tissues but not its cuticle shape. Also, the environmental and (eco)toxicological parameters reported for these compounds suggest lower toxicity and higher safety of use than oxamyl. These compounds appear to be good candidates for the development of biopesticides for a more sustainable pest management strategy.

Growth, Physiological, and Biochemical Variations in Tomatoes after Infection with Different Density Levels of Meloidogyne enterolobii.

Meloidogyne enterolobii is an extremely important plant parasitic nematode. Tomato (Solanum lycopersicum) is an essential worldwide vegetable, and M. enterolobii poses a major threat to its production. The present research investigated the effects of different levels of inoculum density of M. enterolobii (100, 500, 1000, 1500, and 2000 second-stage juveniles (J2s)/plant) on tomato growth, physiological, and biochemical changes at 7, 14, 21, and 28 days post-inoculation (dpi). The negative impact of M. enterolobii on plants gradually increased when the inoculum level increased. Therefore, M. enterolobii population densities (500-2000 J2s/plant) significantly (p < 0.05) reduced plant growth, photosynthetic pigmentation, gas exchange, and chlorophyll fluorescence compared to control plants, while the low population density (100 J2s/plant) showed very little influence. Furthermore, plants with the highest M. enterolobii inoculum (2000 J2s/plant) exhibited a greater number of egg masses and galls. The inoculum densities of M. enterolobii exhibited a notable correlation with the significant elevation of both malondialdehyde (MDA) and hydrogen peroxide (H2O2) levels, which are recognized as very detrimental stresses in plants. Similarly, a rise in the activity of several defensive antioxidant enzymes, namely superoxide dismutase (SOD), catalase (CAT), and peroxidase (POD), indicates the defensive mechanism used to combat the oxidative destruction produced by M. enterolobii. The specific activity of glutathione (GSH) and ascorbate (ASA) increased as potent antioxidant defense molecules in response to induced oxidative damage. In addition, our findings also demonstrated that the highest population density (2000 J2s/plant) increased the secondary metabolites responsible for scavenging oxidative stress in the plants. However, further research is required to explore the underlying reasons for this phenomenon and to develop efficient chemical or biocontrol strategies for managing M. enterolobii.

Design, Synthesis, Nematicidal Activity, and Mechanism of Novel Amide Derivatives Containing an 1,2,4-Oxadiazole Moiety.

To discover new nematicides, a series of novel amide derivatives containing 1,2,4-oxadiazole were designed and synthesized. Several compounds showed excellent nematicidal activity. The LC50 values of compounds A7, A18, and A20-A22 against pine wood nematode (Bursaphelenchus xylophilus), rice stem nematode (Aphelenchoides besseyi), and sweet potato stem nematode (Ditylenchus destructor) were 1.39-3.09 mg/L, which were significantly better than the control nematicide tioxazafen (106, 49.0, and 75.0 mg/L, respectively). Compound A7 had an outstanding inhibitory effect on nematode feeding, reproductive ability, and egg hatching. Compound A7 effectively promoted the oxidative stress of nematodes and caused intestinal damage to nematodes. Compound A7 significantly inhibited the activity of succinate dehydrogenase (SDH) in nematodes, leading to blockage of electron transfer in the respiratory chain and thereby hindering the synthesis of adenosine triphosphate (ATP), which consequently affects the entire oxidative phosphorylation process to finally cause nematode death. Therefore, compound A7 can be used as a potential SDH inhibitor in nematicide applications.

Recent developments in fluorine-containing pesticides.

To ensure ongoing sustainability, the modern agrochemical industry is faced with enormous challenges. These arise from provision of high-quality food to increasing water use and environmental impact as well as a growing world population. The loss of previous agrochemicals due to consumer perception, changing grower needs and ever-changing regulatory requirements is higher than the number of active ingredients that are being introduced into the crop protection market. Therefore, the development of novel agrochemicals is essential to provide improved efficacy and environmental profiles. In this context, the introduction of fluorine atoms and fluorine-containing motifs into a molecule is an important method to influence its physicochemical properties. These include, for example, small difluoro- and trifluoromethyl, or trifluoromethoxy groups at aryl or heterocyclic aryl moieties but also fragments like 2,2,2-trifluoroethoxycarbonyl, trifluoromethylsulfonyl, trifluoroacetyl, as well as the so far unusal rest like heptafluoro-iso-propyl. This review gives an overview of recent developments of fluorine-containing pesticides launched over the past 7 years and describes a selection of current fluorine-containing development candidates. © 2023 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Primary Screening of Microorganisms against Meloidogyne hapla (Chitwood, 1949) under the Conditions of Laboratory and Vegetative Tests on Tomato.

Highly adapted obligate endoparasites of the root system, root-knot nematodes (Meloidogyne spp.), cause great damage to agricultural crops. Our research is aimed at the assessment of nematicidal activity and effectiveness of antagonist fungal and bacterial strains against the most common type of root-knot nematode in the south of Russia. By means of molecular genetic identification, it was found that in the south of Russia, the species Meloidogyne hapla Chitwood, 1949 and Meloidogyne incognita (Kofoid and White, 1919) Chitwood, 1949 cause galls on the roots of open-ground and greenhouse tomato. Screening of microbial agents against second-stage juvenile (J2) M. hapla was carried out in the laboratory. At the end of the experiment, two liquid fungal cultures of Paecilomyces lilacinus BK-6 and Metarhizium anisopliae BK-2 were isolated, the nematicidal activity of which reached 100.0 and 70.2%, and exceeded the values of the biological standard (Nemotafagin-Mikopro) by 38.4% and 8.8%. The highest biological efficacy was noted in the liquid cultures of P. lilacinus BK-6, M. anisopliae BK-2, and Arthrobotrys conoides BK-8 when introduced into the soil before planting tomato. The number of formed galls on the roots was lower in comparison with the control by 81.0%, 75.5%, and 74.4%.

A New Biological Product Shows Promising Control of the Northern Root-Knot Nematode, Meloidogyne hapla, in Greenhouse Tomatoes.

Tomato plants are susceptible to significant yield losses when infested by the northern root-knot nematode, Meloidogyne hapla. While there are many options for conventional chemical management, few of these options offer effective control for organic growers or those who seek to adopt more environmentally considerate strategies. In this study, we showed that a new, biologically based product (referred to as "MN21.2") has potential for controlling populations of the northern root-knot nematode, Meloidogyne hapla, as a pest of susceptible tomato (cv. Rutgers) in a greenhouse trial. This is significant because if this product's efficacy is supported under field conditions, it may provide organic tomato growers with a valuable tool for fighting the plant-parasitic nematode pest, M. hapla.

Efficacy of five nematicides against root-knot nematode when applied via single and double drip tapes in a Florida sandy soil.

BACKGROUND: The efficacy of drip-applied nematicides depends on adequate product distribution, which can be difficult in sandy soils. Three new non-fumigant nematicides (fluazaindolizine, fluensulfone, fluopyram), together with two old nematicides, oxamyl and metam potassium, were evaluated when applied via single and double drip tapes to control root-knot nematode in cucumber and squash in Florida between February 2020 and December 2022. RESULTS: Nematicide applications via double drip tapes resulted in lower root gall infection (and tend to have higher yield) as compared to a single tape for fluopyram, but no difference was noted between single and double tapes for oxamyl and fluazaindolizine. Fluensulfone response was somewhere in between and metam potassium had higher squash yield when applied with double tapes. Root-knot infection was higher in cucumber than in squash, and metam potassium had the highest yields and lowest nematode infection compared to other nematicide treatments. CONCLUSION: The benefit of double versus single drip tapes depended on the type of nematicide that was applied and was evident for nematicides that have poor water solubility like fluopyram. Some benefit was noted for metam potassium, but no or limited benefit was noted for oxamyl, fluazaindolizine and fluensulfone. © 2023 Society of Chemical Industry.

Efficacy of Aspergillus tubingensis GX3' Fermentation against Meloidogyne enterolobii in Tomato (Solanum lycopersicum L.).

Meloidogyne enterolobii is one of the most virulent root-knot nematodes (RKNs). Aspergillus tubingensis Raoul Mosseray, 1934, is used to produce bioactive substances, enzymes, and secondary metabolites. However, no research has been conducted yet on the efficacy of A. tubingensis against plant-parasitic nematodes. Thus, the novel research was planned to evaluate the biocontrol efficacy of A. tubingensis fermentation against M. enterolobii. The findings showed that egg hatching inhibition and mortality of M. enterolobii increased with increasing concentration of fermentation and exposure time. The maximum second-stage juveniles (J2s) mortality was achieved via 100% fermentation at 72 h. Similarly, 100% fermentation inhibited 99.9% of egg hatching at 8 d. A. tubingensis fermentation increased plant biomass, decreased second-stage juvenile invasion, and inhibited nematode development and reproduction in greenhouse conditions. A. tubingensis reduced J2 invasion into tomato roots by 42.84% with CS+ (coated seeds plants with nematodes inoculum) and 27.04% with T+ (100% fermentation broth and nematodes inoculum both) treatments. Moreover, CS+ and T+ treatments decreased nematode development by 54.31% and 21.48%, respectively. It is concluded that the A. tubingensis GX3 strain can be used as a novel microbial biocontrol agent against M. enterolobii.

Discovery of quinazoline compound as a novel nematicidal scaffold.

With the aim of discovering novel nematicidal scaffolds, the nematicidal activities of a series of quinazoline compounds were tested, with some compounds showing excellent results. Among them, the LC50 values of compound K11 against Bursaphelenchus xylophilus, Aphelenchoides besseyi, and Ditylenchus destructor were 7.33, 6.09, and 10.95 mg/L, respectively. In addition, the nematicidal activity of compound K11 against Meloidogyne incognita was 98.77% at 100 mg/L. Compound K11 not only increased the production of reactive oxygen species and the accumulation of lipofuscin and lipids in nematodes, but it also attenuated nematode pathogenicity by reducing the nematodes' antioxidant capacity. Transcriptomic analysis showed that compound K11 had significant effects on fatty acid degradation, metabolic pathways, and the differentially expressed genes related to redox processes in nematodes. Furthermore, the expression levels of the corresponding differentially expressed genes were verified using real-time quantitative polymerase chain reaction. Quinazoline can be used as a new nematicidal scaffold, and it is expected that more work will be done on the discovery of novel nematicides based on the lead compound K11 in the future.

Evaluation of fumigant and non-fumigant nematicides for management of Rotylenchulus reniformis on sweetpotato.

Reniform nematode (Rotylenchulus reniformis) is a major pest of sweetpotato in many production regions in Southern United States. Applying soil fumigants and non-fumigant nematicides are the primary management strategies available to growers. This study compared the relative efficacy of nematicides (1,3-dichloropropene, fluopyram, oxamyl, fluazaindolizine, aldicarb, Majestene, and fluensulfone) for management of reniform nematode on sweetpotato. Fumigating soil with 1,3-dichloropropene consistently reduced soil population densities of reniform nematode at the time of planting in both trial years (31 - 36% reduction relative to the untreated control); however, the duration of suppression varied greatly by growing season. A similar trend was observed with fluopyram (56 - 67% reduction) and aldicarb (63 - 65% reduction), which provided season-long suppression of reniform nematode population development in 2021 but had no impact in 2022. In 2021, nematicide application had no impact on yield; however, in 2022, oxamyl and aldicarb increased the yield of U.S.#1 grade sweetpotato. Overall, soil fumigation with 1,3-dichloropropene and in-furrow application of fluopyram and aldicarb provided the most consistent suppression of reniform nematode on sweetpotato.

A Cost-Benefit Analysis of Soil Disinfestation Methods against Root-Knot Nematodes in Mediterranean Intensive Horticulture.

Losses caused by phytoparasitic nematodes in crops depend directly on their soil densities at the start of the crop, so reducing their populations before planting is the main aim of nematological management. Efficacies in reducing Meloidogyne soil populations of soil disinfestation methods, such as agrochemicals, botanicals, or biosolarization were estimated on multiple field trials conducted over fourteen years in intensive horticultural crops. Soil nematode populations were reduced by 87 to 78% after fumigation with 1,3-dichloropropene + chloropicrin and dimethyl-disulphide, respectively. Non-fumigant nematicides such as azadirachtin, dazomet, fenamiphos, fluopyram, fosthiazate, metam-sodium, and oxamyl showed efficacies ranging from 51 to 64%, whereas the efficacy of natural products, such as abamectin, garlic extracts, or essential oils was 41 to 48%. Biosolarization with chicken manure had an efficacy of 73%. An economic cost-benefit study of nematode management methods was performed for seven vegetable-M. incognita pathosystems. Fumigation with 1,3-dichloropropene + chloropicrin and biosolarization with chicken manure were the only treatments able to reduce RKN populations above 1000 and 750 J2 per 100 cm3 of soil, respectively, to levels below the nematode economic damage threshold, keeping profitability. Fumigation was able to manage RKN soil densities up to 350 J2 per 100 cm3 of soil in most susceptible crops as aubergine or cucumber and up to 1000 J2 per 100 cm3 of soil for more tolerant crops, such as other cucurbits, pepper, or tomato. Other nematicidal treatments were not able to reduce RKN populations above 200-300 J2/100 cm3 of soil below the economic thresholds but were profitable when RKN densities were below the limits of 200-300 J2/100 cm3 of soil.

Bio-directed Chemical Study of Pleurotus ostreatus Spent Substrate and Its Nematicidal Activity.

PURPOSE: In the present study, the nematicidal activity of the chemical fractionation of the spent substrate of the edible mushroom Pleurotus ostreatus against eggs and L3 larvae of Haemonchus contortus was evaluated. METHODS: The hydroalcoholic extract of the spent substrate was subjected to a bipartition with ethyl acetate giving two fractions: one aqueous (F. Ac) and one organic (F. AcOET). Both fractions were evaluated against eggs and L3 larvae at different concentrations (5, 2.5, 1.25, 0.625 and 0.3125 mg/mL) and 2% methanol, PBS and thiabendazole (5 mg/mL) as controls. Chemical fractionation of F. AcOET was performed in open column chromatography where 76 fractions were obtained and when analyzed by thin layer chromatography (TLC) were grouped into 11 mixtures (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11). These mixtures were evaluated at 10 mg/mL against eggs and L3 larvae. The data obtained were analyzed by ANOVA and a Tukey test in the SAS V9 program. RESULTS: The results showed that, in the evaluation of F. AcOET and F. Ac, for the inhibition of egg hatching, the highest percentages were 78.80 and 76.89% at 5 mg/mL, respectively. As for the percentage of larval mortality, F. AcOET obtained 60.91 and F. Ac 29.77% at 5 mg/mL. The results of the evaluations of the mixtures showed that mixtures R4, R5 obtained 100 and 95.41% larval mortality and mixtures R6 and R7 presented 100% inhibitory activity of egg hatching, so these were analyzed by gas chromatography mass spectrometry finding compounds such as vanillin, ß-sitosterol, ρ-methyl ρ-hydroxycinnamate and ρ-hydroxybenzaldehyde. CONCLUSION: The results of the present study demonstrate that the spent substrate of P. ostreatus has potential anthelmintic activity against H. contortus. Moreover, by reusing and taking advantage of this substrate, its environmental pollution effects can be reduced.

Effect of fumigants and non-fumigants on nematode and weed control, crop yield, and soil microbial diversity and predicted functionality in a strawberry production system.

Fumigants are commonly used to control soil-borne pathogens of high-value crops, but they may also impact non-target soil microorganisms. Increasing interest in the use of sustainable management practices to control plant- and root-parasitic nematodes has resulted in the formulation of non-fumigant nematicides (chemicals or bionematicides) which are considered environmentally friendly alternatives to fumigants. However, the impact of these new products compared to standard fumigants on soil-borne pathogens, plant production, and the diversity and composition of non-target microbial communities in all crops remains unclear. To begin to address this knowledge gap, we examined the effect of fumigants commonly used in Florida (United States) strawberry production and newly formulated non-fumigant nematicides on nematode and weed control, plant growth, crop yield, and bacterial and fungal community diversity and predicted functionality. We found the standard fumigants increased crop yields and reduced weed pressure more than non-fumigants. Both fumigants and non-fumigants were an efficient management strategy to control sting nematodes. Treatments also impacted the abundance of specific beneficial and antagonistic taxa. Both fumigants and non-fumigants reduced soil bacterial and fungal diversity, an effect that remained for six months, thus suggesting a potential residual impact of these products on soil microorganisms. However, only fumigants altered soil microbial community composition and reduced network complexity, inducing a decrease or even a loss of some predicted bacterial and fungal functions, particularly during the first weeks after fumigation. Nevertheless, soil collected at the end of the season showed significant levels of root-knot nematode suppression in a growth chamber experiment, irrespective of the previous treatment. By linking the effect of fumigants and non-fumigants on soil-borne pests, plant and production, and the soil microbiome, this study increases our knowledge regarding the environmental impact of these products.

Toxicity of Tioxazafen to Meloidogyne Incognita and Rotylenchulus Reniformis.

Tioxazafen is a seed-applied nematicide used in row crops. Currently, there are no data on nematode toxicity, nematode recovery, or effects of low concentrations of tioxazafen on nematode infection of a host root for Meloidogyne incognita or Rotylenchulus reniformis. Nematode toxicity and recovery experiments were conducted in water solutions of tioxazafen, while root infection assays were conducted on tomato. Nematode paralysis was observed after 24 hr of exposure at 27.0 µg/ml tioxazafen for both the nematode species. Based on an assay of nematode motility, 24-hr EC50 values of 57.69 µg/ml and 59.64 µg/ml tioxazafen were calculated for M. incognita and R. reniformis, respectively. Tioxazafen rates of 2.7 µg/ml and 27.0 µg/ml reduced the nematode hatch after 3 d of exposure for both the nematode species. There was no recovery in nematode motility after the 24-hr exposure of M. incognita and R. reniformis to their corresponding 48-hr EC50 values of 47.15 µg/ml and 47.25 µg/ml tioxazafen, respectively. Mortality of M. incognita continued to increase after 24 hr exposure, whereas R. reniformis mortality remain unchanged after nematodes were rinsed and removed for 48 hr from the tioxazafen solution. A 24-hr exposure to low concentrations of 0.38 to 47.15 µg/ml for M. incognita and 47.25 µg/ml for R. reniformis reduced the infectivity of each nematode species on tomato roots. The toxicity of tioxazafen was similar between nematode species; however, a greater rate of tioxazafen was needed to suppress R. reniformis infection of tomato than for M. incognita.

Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives.

Parasitic diseases, caused by intestinal helminths, remain a very serious problem in both human and veterinary medicine. While searching for new nematicides we examined a series of 1,2,4-triazole derivatives 9-22, obtained during reactions of N3-substituted amidrazones with itaconic anhydride. Two groups of compounds, 9-16 and 17-22, differed in the position of the double bond on the methacrylic acid moiety. The toxicity of derivatives 9-22 and the anti-inflammatory activity of 12 and 19-22 were studied on peripheral blood mononuclear cells (PBMC). Antiproliferative activity of compounds 12 and 19-22 was tested cytometrically in PBMC cultures stimulated by phytohemagglutinin. The influence of derivatives 12 and 19-22 on the TNF-α, IL-6, IL-10 and IFN-γ production was determined by ELISA in lipopolysaccharide-stimulated PBMC cultures. Anthelmintic activity of compounds 10-22 was studied in the Rhabditis sp. nematodes model. Most compounds (11-22) proved to be non-toxic to human PBMC. Derivatives 19-22 showed anti-inflammatory activity by inhibiting the proliferation of lymphocytes. Moreover, compounds 12 and 19-22 significantly reduced the production of TNF-α and derivatives 19-21 decreased the level of INF-γ. The strongest anti-inflammatory activity was observed for compound 21. Compounds 12 and 14 demonstrated anthelmintic activity higher than albendazole and may become promising candidates for anthelmintic drugs.