Application of a fungicide composition containing imazalil in preventing and controlling crop fungal diseases

Abstract

The present invention belongs to the field of pesticide application technology, and specifically relates to the use of a fungicidal composition containing imazalil in preventing and controlling crop fungal diseases. The effective active ingredients of the composition include a first active ingredient, imazalil, and a second active ingredient, jinggangmycin, wherein the weight ratio of imazalil to jinggangmycin is 30:1 to 1:30, and the crop fungal diseases are wheat head blight, wheat stem base rot, corn stem base rot, and rice false smut. The composition can be prepared into a variety of dosage forms permitted in agriculture, such as microemulsions, suspensions, soluble granules, soluble powders, water-dispersible granules, aqueous emulsions, wettable powders, emulsifiable concentrates, and suspension seed coatings. It can achieve the effects of reducing drug dosage, lowering costs, reducing dosage and increasing efficiency, reducing toxin residues, and protecting the environment, and is worthy of industrial promotion.

Description

Technical Field

[0001] The invention relates to application of a bactericidal composition containing imazalil in preventing and treating crop fungal diseases, belonging to the technical field of pesticide application. Background Art

[0002] Imazalil, also known as Imazalil in English, is an imidazole fungicide developed by Janssen Pharmaceuticals of Belgium in 1973. Its mechanism of action is to disrupt the pathogen's cell membrane structure by affecting its permeability, physiological functions, and lipid metabolism. It also inhibits spore formation, achieving multiple preventive, protective, and therapeutic effects. Imazalil is a broad-spectrum systemic fungicide that is effective against many fungal diseases that attack fruits, vegetables, and ornamental crops. It is particularly effective in controlling post-harvest rot in citrus, bananas, and other fruits by spraying or dipping. It also exhibits high activity against Helminthosporium, Fusarium, Septoria, and brown rust of stone fruits, making it suitable for controlling cereal diseases and seed treatment.

[0003] Validamycin, also known as Validamycin, is an antibiotic produced by actinomycetes. It is highly systemic, easily absorbed by bacterial cells and rapidly transmitted throughout the body, interfering with and inhibiting their growth and development. It is primarily used to control rice sheath blight, but can also be used to control rice false smut and diseases of crops such as vegetables and cotton. It remains an effective agent for controlling rice sheath blight. As a natural product, Validamycin can also induce immune resistance in plants. Therefore, Validamycin is one of the most widely used agricultural antibiotics in my country.

[0004] Fusarium head blight, also known as "ear rot" or "head rot," is a typical climate-related disease that primarily affects crops such as wheat, barley, and oats. Its incidence is primarily influenced by the number of fusarium sources in the field, the disease resistance of the wheat variety, air humidity, and temperature. Its primary pathogen, the Fusarium graminearum species complex, produces mycotoxins in grains that pose a serious threat to human and animal health. These mycotoxins primarily consist of two types of type B toxins: nivalenol (NIV) and deoxynivalenol (DON) and its derivatives, 3-acetyldeoxynivalenol (3-ACDON) and 15-acetyldeoxynivalenol (15-ACDON). DON is the most common mycotoxin. Low doses of DON can cause loss of appetite, weight loss, and metabolic disorders in animals, while high doses can cause vomiting. At the same time, Fusarium graminearum is also the main pathogen causing corn stalk rot.

[0005] Wheat stem rot, also known as crown rot, is caused by Fusarium graminearum as the main pathogen. It is a common and serious disease in dryland agricultural wheat production. The pathogen can survive in the soil for many years and infect wheat throughout the entire growing season.

[0006] Rice false smut, commonly known as false smut and powdery mildew, is caused by the pathogen Ustilago oryzae. The pathogen infects the rice panicles by infecting the florets during the flowering period, eventually forming yellow or dark green rice smut balls that are 3 to 5 times larger than healthy grains. In recent years, rice false smut has risen from a minor disease affecting rice productivity to a major disease, not only affecting rice yield and quality, but also producing large amounts of fungal toxins that are harmful to humans and animals, posing a serious threat to food security.

[0007] The applicant has found through experimental research that the combination of imazalil and jinggangmycin has a good control effect on wheat ergot, wheat stem base rot, corn stem base rot, and rice false smut, and has a certain synergistic effect. Summary of the Invention

[0008] The present invention aims to provide a fungicidal composition containing imazalil for use in preventing and controlling fungal diseases in crops. To achieve the above object, the technical solution of the present invention is as follows:

[0009] A fungicidal composition containing imazalil for use in preventing and controlling fungal diseases in crops, characterized in that:

[0010] (1) First active ingredient: imazalil;

[0011] (2) Second active ingredient: Jinggangmycin;

[0012] The weight ratio of the first active ingredient to the second active ingredient is 30:1 to 1:30, and the sum of their contents is 1% to 90% of the total weight of the composition. The fungal diseases are specifically wheat ergot, wheat stem base rot, corn stem base rot, and rice false smut.

[0013] Since Jinggangmycin includes AH, a total of 8 compound components, among which Jinggangmycin A is the main active ingredient, the Jinggangmycin involved in the present invention is Jinggangmycin A.

[0014] A further technical solution is that the composition containing imazalil can be prepared into various dosage forms permitted in agriculture. The types and contents of the various dosage form adjuvants are not particularly limited and are well known to those skilled in the art and can be determined according to the formulation during the specific preparation process.

[0015] The various application formulations prepared from the pesticide composition of the present invention include, in addition to the effective active ingredients, various auxiliary ingredients that are permitted and acceptable in different pesticide formulations.

[0016] The auxiliary ingredients include but are not limited to emulsifiers, dispersants, wetting agents, solvents, antifreeze agents, defoaming agents, thickeners, disintegrants, synergists, preservatives and fillers, etc., which are all commonly used or permitted ingredients in pesticide formulations and are not particularly limited. The specific ingredients and amounts are determined through experiments based on the formulation requirements.

[0017] The emulsifier can be various emulsifiers well known in the field of pesticide formulations, and can be one or more of phenylethylphenol polyoxyethylene polyoxypropylene ether, alkylaryl polyoxyethylene polyoxypropylene ether, fatty acid polyoxyethylene ether, fatty alcohol polyoxyethylene ether, glycerol laurate polyoxyethylene ether, styrylphenol polyoxyethylene ether, castor oil polyoxyethylene ether, alkylphenol polyoxypropylene polyoxyethylene ether, styrylphenyl polyoxyethylene ether, alkylphenol polyoxyethylene ether, sorbitan fatty acid ester polyoxyethylene ether, fatty alcohol polyoxyethylene ether sulfonate, alkylphenol polyoxyethylene formaldehyde condensate, calcium lauryl sulfonate, alkylphenol polyoxyethylene ether succinic acid monoester sulfonate, alkylphenol polyoxyethylene phosphate, and alkylphenol polyoxyethylene ether sulfosuccinate.

[0018] The dispersant can be various dispersants well known in the field of pesticide formulations, and can be one or more of alkylphenol polyoxyethylene ether phosphate, alkylphenol polyoxyethylene ether sulfate, phenylethylphenol polyoxyethylene ether phosphate, polyoxyethylene polyoxypropylene ether block copolymer, sodium lignin sulfonate, sodium methylene bisnaphthalene sulfonate (dispersant NNO), calcium lignin sulfonate, polycarboxylate, sodium methylene bisnaphthalene sulfonate, sodium methylene bismethylnaphthalene sulfonate, polyvinyl pyrrolidone, alkylamido taurate, sodium salt of alkylnaphthalene sulfonic acid polycondensate, and sodium methylene bisnaphthalene sulfonate formaldehyde condensate.

[0019] The wetting agent can be various wetting agents well known in the field of pesticide formulations, and can be one or more of sodium alkylnaphthalene sulfonate, sodium lauryl sulfate, sodium secondary alkyl sulfate, sodium dodecylbenzene sulfonate, fatty alcohol polyglycol ether sulfate, fatty alcohol polyoxyethylene ether, nonylphenol polyoxyethylene ether, sorbitan fatty acid ester polyoxyethylene ether, alkylnaphthalene formaldehyde condensate, alkylnaphthalene sulfonate and other wetting agents.

[0020] The solvent can be various solvents known in the field of pesticide formulations, and can be one or more of water, methanol, ethanol, N-methylpyrrolidone, N,N-dimethylformamide, N,N-dimethylacetamide, tetrahydrofurfuryl alcohol, toluene, xylene, dimethyl sulfoxide, tetrahydrofuran, cyclohexanone, n-butanol, isopropanol, solvent oil No. 100, No. 150, No. 180, and No. 200.

[0021] The antifreeze agent may be any antifreeze agent known in the field of pesticide formulations, and may be one or more of ethylene glycol, propylene glycol, glycerol, diethylene glycol, urea, and inorganic salts.

[0022] The defoaming agent can be any of various defoaming agents known in the field of pesticide formulations, and can be one or more of silicone compounds, epoxy soybean oil, emulsified silicone oil, and fatty alcohol.

[0023] The thickener may be any thickener known in the field of pesticide formulations, and may be one or more of xanthan gum, polyvinyl alcohol, sodium alginate, gum arabic, and magnesium aluminum silicate.

[0024] The disintegrant may be any disintegrant known in the field of pesticide formulations, and may be one or more of ammonium sulfate, sodium carboxymethyl starch, urea, low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl cellulose, cross-linked polyvinylpyrrolidone, sodium alginate, sodium bicarbonate, and sodium chloride.

[0025] The carrier can be various carriers known in the field of pesticide formulations, and can be one or more of glucose, white carbon black, kaolin, diatomaceous earth, light calcium carbonate, heavy calcium carbonate, attapulgite, soluble starch, urea, maltose, sucrose, citric acid, potassium carbonate, sodium carbonate, and anhydrous sodium sulfate.

[0026] The preservative may be any preservative known in the field of pesticide formulations, and may be one or more of kasone, sodium benzoate, benzoic acid, potassium sorbate, and formaldehyde.

[0027] The deionized water is industrial deionized water.

[0028] Beneficial technical effects achieved by the present invention:

[0029] 1. Compared with a single preparation, the composition has a significant synergistic effect in preventing and controlling wheat scab, wheat stem rot, corn stem rot, and rice false smut, and can significantly improve the control effect of the above diseases;

[0030] 2. The combination of these two compounds can effectively inhibit the biosynthesis of DON toxins caused by wheat fusarium head blight, thereby reducing the problem of DON toxin pollution;

[0031] 3. It can reduce the usage of chemical pesticide imazalil and delay the development of imazalil resistance in fungal diseases of crops;

[0032] 4. It can reduce the amount of medicine used, reduce costs, and reduce environmental pollution and pesticide residues. DETAILED DESCRIPTION

[0033] The following indoor toxicity test is used to illustrate the combined effect of the mixture of imazalil and jinggangmycin on ergot, stem base rot and rice false smut.

[0034] Test Method: The in-house virulence assay for the three pathogens employed the hyphal growth rate method. Each agent was dissolved and diluted to five different concentrations. The agent solution was then quantitatively pipetted from low to high concentrations, added to pre-melted culture medium, and shaken thoroughly. Equal amounts were then poured into three culture dishes to create drug-containing plates of the corresponding concentrations. A treatment without the agent served as a blank control, and each treatment was replicated three times.

[0035] For Fusarium graminearum, the preserved sensitive strain, that is, the strain that has no resistance to known drugs, is first activated in a PDA plate and cultured in the dark at 28°C for 72 hours. Then, a 4mm diameter puncher is used to cut the bacterial cake from the edge of the cultured colony and inoculate the bacterial cake into the center of the drug-containing plate with the mycelium facing up. The plate is covered and cultured in the dark at 28°C for 96 hours. The colony growth diameter is measured using the cross-cross method and the average value is taken. The mycelium growth inhibition rate is calculated, and then the virulence regression equation is obtained based on the logarithm of the drug concentration and the probability value of the inhibition rate to calculate the EC of the drug to be used. 50 The mycelial growth rate method was used for all three pathogens, with the culture method adjusted according to the characteristics of the pathogens. The co-toxicity coefficient was used to evaluate the combined effects of the compound agents on the pathogens. A co-toxicity coefficient >120 indicates a synergistic effect, a co-toxicity coefficient between 80 and 120 indicates an additive effect, and a co-toxicity coefficient <80 indicates an antagonistic effect.

[0036]

[0037] Theoretical Toxicity Index (TTI) = ∑(ATI of a drug × percentage of the active ingredient of the drug in the mixture)

[0038]

[0039] Table 1 The results of toxicity test of imazalil and jinggangmycin against Fusarium graminearum

[0040]

[0041] As shown in Table 1, when imazalil and jinggangmycin were mixed in a weight ratio of 30:1-1:40, they all showed a certain synergistic effect on Fusarium graminearum. When the mixing ratio was 1:1, the co-toxicity coefficient was the largest and the synergistic effect was the most obvious.

[0042] Table 2 The results of toxicity test of imazalil and jinggangmycin mixed against pseudo-Fusarium graminearum

[0043]

[0044]

[0045] As shown in Table 2, when imazalil and jinggangmycin were mixed in a weight ratio of 30:1-1:30, they all showed a certain synergistic effect on Fusarium graminearum. When the mixing ratio was 2:1, the co-toxicity coefficient was the largest and the synergistic effect was most obvious.

[0046] Table 3 Toxicity test results of imazalil and Jinggangmycin mixed to rice smut pathogen

[0047]

[0048] As shown in Table 3, when imazalil and jinggangmycin were mixed in a weight ratio of 30:1-1:30, they all showed a certain synergistic effect against the rice false smut fungus. When the mixing ratio was 2:1, the co-toxicity coefficient was the largest and the synergistic effect was most obvious.

[0049] The present invention will be further described below with reference to the formulation examples.

[0050] Preparation Example 1

[0051] 20% of imazalil, 10% of jinggangmycin, 13% of Nongru 160, 4% of Nongru 500#, 3% of Nongru 400#, 4% of toluene, 1.5% of cyclohexanone, 4% of isopropyl alcohol, and 2% of triphenyl phosphite were completely dissolved and mixed uniformly, and deionized water was added to 100% by weight. After stirring, a 30% imazalil-jinggangmycin microemulsion was prepared.

[0052] Preparation Example 2

[0053] 10% imazalil, 10% jinggangmycin, 3% alkylphenol formaldehyde resin polyoxyethylene ether, 5% sodium alkylnaphthalene formaldehyde condensate sulfonate, 4% sodium alkyl sulfate, 3% potassium sorbate, 2% polyethylene glycol, 2% bentonite, 2% octanol, and deionized water added to 100% by weight. These materials were mixed, dispersed at high shear speed for 30 minutes, and sand-milled to a particle size D90 of less than 10 μm to produce a 20% imazalil / jinggangmycin suspension concentrate.

[0054] Biological Example: Field trial for controlling wheat scab.

[0055] In 2023, field efficacy tests of Formulation Example 1, Formulation Example 2 and a control agent for controlling wheat fusarium wilt were carried out in Shou County, Anhui Province, and the safety of the agent on wheat was verified.

[0056] Test method: The test crop is wheat, and each plot is 30m 2The plots were randomly arranged, with 3 replicates for each treatment, and a water treatment as a blank control. Conventional spraying was used in the experiment. The first spraying was carried out during the flowering stage after the wheat ears were fully formed, and the second spraying was carried out after an interval of 7 days.

[0057] A survey was conducted once during the milky stage of wheat. Sampling was carried out at 5 diagonal points in each plot, with 100 ears surveyed at each point. The wheat was graded based on the percentage of dead ear area to the entire ear area. The number of diseased ears at each level and the total number of ears were recorded. The diseased ear rate, disease index and prevention effect of each plot were calculated.

[0058] After the wheat matured, five diagonal sampling points were used in each plot, and 0.25m was cut at each point. 2 All wheat ears were threshed manually, dried and mixed, and then the grain samples of each treatment were crushed with a high-speed grinder and passed through a 20-mesh sieve to avoid cross-contamination. The powdered samples of each treatment were then collected for DON toxin detection. Liquid chromatography tandem mass spectrometry (LC-MS) was used to detect DON toxin in the sample powder. 5g of sample powder was weighed and placed in a 50mL centrifuge tube. 25mL of 84% acetonitrile solution was added and the tube was shaken at 140r / min for 30min. The tube was centrifuged at 3000r / min for 5min, and the supernatant was filtered through a graphitized carbon column. The collected solution was dried with nitrogen, re-dissolved with 1mL of 10% methanol, and filtered through a 0.22μm microporous membrane before being tested on the machine. The DON toxin content and the control effect of different treatments on DON toxin in the grain were calculated.

[0059] Wheat scab grading standards:

[0060] Level 0: The whole ear is disease-free;

[0061] Level 1: The dead ear area accounts for less than 1 / 4 of the whole ear area;

[0062] Level 3: The dead ear area accounts for 1 / 4 to 1 / 2 of the whole ear area;

[0063] Level 5: The dead ear area accounts for 1 / 2 to 3 / 4 of the whole ear area;

[0064] Level 7: The dead ear area accounts for more than 3 / 4 of the whole ear area;

[0065] Diseased ear rate (%) = number of diseased ears / total number of surveyed ears × 100

[0066] Disease index = ∑(number of diseased ears at each level × relative level value) / (total number of ears surveyed × 7) × 100

[0067] Control effect (%) = (disease index of blank control area - disease index of drug-treated area) / disease index of blank control area × 100

[0068] DON toxin content (μg / g) = total amount of DON toxin / dry weight of sample powder

[0069] DON toxin protective effect (%) = (control DON toxin content - treatment DON toxin content) / control DON toxin content × 100%.

[0070] Table 4 Results of the control of wheat scab by mixing imazalil and Jinggangmycin

[0071]

[0072] As shown in the field efficacy test results in Table 4, the above formulation examples demonstrated excellent control efficacy against wheat scab, with efficacy exceeding 85% and DON toxin efficacy exceeding 72%. The efficacy of each treatment was significantly superior to that of the individual formulations. Safety investigations demonstrated that all test treatments were safe for wheat, with no phytotoxicity observed.

[0073] In summary, the composition of the present invention is significantly effective in controlling wheat head blight caused by Fusarium graminearum and Pseudomonas graminearum, wheat stem base rot, corn stem base rot, and rice false smut caused by U. oryzae oryzae, and can significantly reduce the production of DON toxins. Compared with existing single formulations, it has a significant synergistic effect, reduces control costs, achieves significant control effects, can reduce toxin contamination, and is safe for crops, showing broad application prospects in production.

Claims

1. A fungicidal composition containing imazalil for preventing and controlling fungal diseases in crops, characterized in that The effective active ingredients of the fungicidal composition include a first active ingredient, imazalil, and a second active ingredient, jinggangmycin, wherein the weight ratio of imazalil to jinggangmycin is 10:1 to 1:10; the crop fungal diseases are wheat fusarium ergot and corn stem rot caused by Fusarium graminearum, wheat stem rot caused by pseudofusarium graminearum, and rice false smut caused by oryzae oryzae.

2. The use according to claim 1, characterized in that: The total weight of the active ingredients accounts for 1% to 90% of the total weight of the entire preparation.

3. The use according to claim 1, characterized in that: The dosage forms of the bactericidal composition are: microemulsion, suspension, soluble granules, soluble powder, water-dispersible granules, aqueous emulsion, wettable powder, emulsifiable concentrate, and suspended seed coating agent.

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