Insecticidal and acaricidal composition, insecticidal and acaricidal agent, and use thereof
Patent Information
- Application Number
- PCT/CN2026/083040
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2025-03-15
- Filing Date
- 2026-03-12
- Publication Date
- 2026-09-24
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Figure CN2026083040_24092026_PF_FP_ABST
Abstract
Description
Insecticidal and acaricidal compositions and agents and their applications
[0001] Cross-references to related applications
[0002] This application claims the benefit of Chinese patent applications 202510306783.4, 202510306785.3, 202510306786.8, 202510306794.2 and 202510309849.5, filed on March 15, 2025, the contents of which are incorporated herein by reference. Technical Field
[0003] This invention belongs to the field of insecticides and acaricides, and relates to insecticide and acaricide compositions, insecticides and acaricides and their applications. Background Technology
[0004] In agricultural and horticultural crop production, damage caused by pests and diseases remains significant. Due to biodiversity and the simultaneous occurrence of multiple pests and diseases, the field of plant protection has a continuous need to develop new insecticides and acaricides with better activity, lower dosage, and greater environmental friendliness. Continuous use of insecticides and acaricides containing a single active ingredient in pest control easily leads to pesticide resistance in pests. Blending insecticides and acaricides with two or more active ingredients into mixed formulations plays an important role in broadening the insecticidal spectrum, controlling both pests and diseases, controlling viral diseases by controlling vector insects, reducing pesticide application costs for farmers, and delaying the development of pesticide resistance in pests. Summary of the Invention
[0005] The purpose of this invention is to meet the growing demand for insecticides and acaricides in the fields of agriculture, forestry and urban sanitation for pest control, which require increasingly higher efficacy and more diverse varieties. This invention provides insecticide and acaricide compositions and their applications.
[0006] To achieve the aforementioned technical objectives, the present invention provides the following technical solution in a first aspect: an insecticidal and acaricidal composition, comprising active component A and active component B, wherein the weight ratio of active component A to active component B is 99:1 to 1:99; active component A is selected from compound I, and active component B is selected from mitochondrial electron transport complex (Ⅰ) inhibitors, mitochondrial electron transport complex (Ⅱ) inhibitors, mitochondrial electron transport complex (Ⅲ) inhibitors, mite growth inhibitors, macrolides, ATP synthase inhibitors, or GABA-gated chloride channel allosteric modulators; the structure of compound I is as follows:
[0007] In some embodiments, the active component B is selected from mitochondrial electron transport complex (I) inhibitor insecticides / acaricides, which are selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, azoxystrobin, acetamiprid, or rotenone.
[0008] In some embodiments, the active component B is selected from mitochondrial delivery complex (II) inhibitor insecticides / acaricides, which are selected from one or more of etoxazole, cyprodinil, or diflubenzuron.
[0009] In some embodiments, the active component B is selected from mitochondrial electron transport complex (III) inhibitor insecticides / acaricides, which are selected from one or more of bifenazate, pyrimethanil, pyrimethanil, flometoquin, flufenoxuron, or mitochondrial quinone.
[0010] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, acetamiprid, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin.
[0011] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, acetamiprid, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin; the weight ratio between the active component A and the active component B is 50:1 to 1:50.
[0012] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, etoxazole, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin; the weight ratio between the active component A and the active component B is 20:1 to 1:40.
[0013] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, acetamiprid, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin; the weight ratio between the active component A and the active component B is 10:1 to 1:10.
[0014] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, etoxazole, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin; the weight ratio between the active component A and the active component B is 4:1 to 1:4.
[0015] In some embodiments, the active component B is selected from acaricides that inhibit mite growth, and the acaricides that inhibit mite growth are selected from one or more of tetradifon, thiamethoxam, etoxazole, or flufenoxam.
[0016] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole.
[0017] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole; the weight ratio of active component A to active component B is 50:1 to 1:50.
[0018] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole; the weight ratio of active component A to active component B is 5:1 to 40:1.
[0019] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole; the weight ratio of active component A to active component B is 5:1 to 20:1.
[0020] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole; the weight ratio of active component A to active component B is 1:1 to 20:1.
[0021] In some embodiments, the active ingredient B is selected from macrolide insecticides / acaricides, which are selected from one or more of abamectin, emamectin benzoate, spinosad, ethyl spinosad, dicofol, ivermectin, rapamectin, emamectin, mibamectin, Carvacrol, Doramectin, Eprinomonetin, Milbemycinoxime, Moxidectin, Sanguinarine, or Selamectin.
[0022] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of avermectin, spinosad, or emamectin benzoate.
[0023] In some embodiments, active component A in the composition is compound I, and active component B is selected from one or more of avermectin, spinosad, or emamectin benzoate; the weight ratio of active component A to active component B is 50:1 to 1:50.
[0024] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of avermectin, spinosad, or emamectin benzoate; the weight ratio of the active component A to the active component B is 5:1 to 10:1.
[0025] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of avermectin, spinosad, or emamectin benzoate; the weight ratio of the active component A to the active component B is 1:1 to 40:1.
[0026] In some embodiments, the active component B is selected from ATP synthase inhibitor insecticides / acaricides, which are selected from one or more of butyl ether urea, triazole tin, tricyclic tin, fenbutatin, propargite, or trichlorfon.
[0027] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of triazole tin, propargite, or butyl ether urea.
[0028] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of triazole tin, propargite, or butyl ether urea; the weight ratio of the active component A to the active component B is 40:1 to 1:40.
[0029] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of triazole tin, propargite, or butyl ether urea; the weight ratio of the active component A to the active component B is 20:1 to 1:40.
[0030] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of triazole tin, propargite, or butyl ether urea; the weight ratio of the active component A to the active component B is 5:1 to 1:40.
[0031] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of triazole tin, propargite, or butyl ether urea; the weight ratio of the active component A to the active component B is 1:5 to 1:20.
[0032] In some embodiments, the active component B is selected from GABA-gated chloride channel allosteric modulators, which are selected from one or more of the following: brofenoxam, acetamiprid, acetamiprid, fipronil, pyrimethanil, pyrazole, flupyrazole, butenpyram, isoxazolidinamide, cyclopropionamide, flenoproxil, afraran, afraran, fluoxazolidinamide, oxazolidinamide, sarolaner, loteran, sarolaner, flufenoxam, afraran, 1-(2,6-dichloro-a,a,a-trifluoro-p-tolyl)-4-(fluoromethylthio)-5-[(pyrazinylmethyl)amino]pyrazole-3-carboxylon, and 1-(2,6-dichloro-4-(trifluoromethyl)phenyl)-4-((difluoromethyl)thio)-5-((pyridin-2-ylmethyl)amino)-1H-pyrazole-3-carboxylon.
[0033] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of bromoxynil, isoxazolamide, cyclopyralid, fluoxazolamide, flusulfanilamide, or amphetamine.
[0034] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of bromoxynil, isoxazolam, cyclopyralid, fluoxazolamide, flusulfanilamide, or amphetamine; the weight ratio between the active component A and the active component B is 50:1 to 1:20.
[0035] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of bromoxynil, isoxazolam, cyclopyralid, fluoxazolamide, flusulfanilamide, or amphetamine; the weight ratio between the active component A and the active component B is 20:1 to 1:10.
[0036] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of bromoxynil dimethoate, isoxazolam, cycloflufenoxam, fluoxazolamide, flufenoxam, or amphetamine; the weight ratio between the active component A and the active component B is 10:1 to 1:5.
[0037] In some embodiments, the active component A is compound I, and the active component B is selected from one or more of bromoxynil, isoxaflutole, cyclopyralid, fluoxazolamide, flusulfanilamide, or amphetamine; the weight ratio of the active component A to the active component B is 5:1 to 1:5.
[0038] A second aspect of the present invention provides an insecticide and acaricide comprising the insecticide and acaricide composition described in the first aspect, wherein the method for preparing the insecticide and acaricide comprises: mixing the insecticide and acaricide composition with a carrier and any one of the adjuvants.
[0039] This invention does not impose any special restrictions on the carrier; any carrier commonly used in the field can be used.
[0040] This invention does not impose any special restrictions on the additives; commonly used additives in the field can be used.
[0041] In some embodiments, the cumulative content of the active ingredient in the insecticide and acaricide composition is between 0.5 wt% and 95 wt%.
[0042] Preferably, the cumulative content of the active component of the insecticide and acaricide composition in the insecticide and acaricide is between 1% and 85%.
[0043] The third aspect of the present invention provides the use of the insecticidal and acaricidal composition as described in the first aspect above or the insecticidal and acaricidal agent as described in the second aspect above in the control of agricultural pests or urban sanitary pests.
[0044] The above description is specifically suitable for controlling a variety of important agricultural pests, such as the carmine spider mite, hawthorn spider mite, citrus pterostilbene mite, citrus rust mite, apple spider mite, two-spotted spider mite, gall mite, and flour mites. It can be used on fruit trees such as apples, pears, citrus fruits, and lychees; cereals such as wheat and rice; legumes such as soybeans and kidney beans; cotton; vegetables such as cabbage, cauliflower, Chinese cabbage, rapeseed, tomatoes, and peppers; and flowers. When used to control urban pests, it can be applied to homes, various public places, offices, and trees.
[0045] Furthermore, the method of using the insecticide and acaricide composition involves applying the prepared insecticide and acaricide, in effective doses, to the pests that need to be controlled or to the medium in which they grow. A commonly chosen effective dose is typically 10 to 500 grams per hectare, with a preferred effective dose being 15 to 100 grams per hectare.
[0046] The present invention has the following advantages:
[0047] 1. The composition of the present invention exhibits a significant synergistic effect on insecticidal and acaricidal activity within a certain ratio range, thereby improving the control effect of the single active ingredient compound in the composition on pests.
[0048] 2. The dosage of the composition of the present invention used in insecticidal and acaricidal applications is significantly lower than that of a single compound in the composition, thereby reducing usage costs and environmental pollution.
[0049] 3. The active ingredients in the composition of the present invention have different mechanisms of action in killing insects and mites, and there is no problem of cross-resistance. Using it to control pests can delay the occurrence of pesticide resistance and improve the control effect on resistant species. Detailed Implementation
[0050] The following embodiments are intended to enable those skilled in the art to more fully understand the present invention, but are not intended to limit the invention to the scope of the embodiments described.
[0051] Indoor bioactivity assay (Part 1)
[0052] Example 1
[0053] Synergistic effect determination of compositions containing compound I against Tetranychus cinnabarinus:
[0054] Test subject: Tetranychus cinnabarinus Boisduval, adult mite, sensitive strain kept indoors.
[0055] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0056] Preparation of drug solution: According to different test requirements, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0057] Experimental method: The activity of the mites against adult Tetranychus carinata was determined by spraying potted seedlings. First, 40-60 adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding the first pair of true leaves. After the adults stabilized, the population was counted. Then, the test material was treated with 1.5 mL of the mites using the Airbrush method. A blank control was set up.
[0058] After natural air drying, the treated test materials were placed in an observation room. The temperature, humidity, and light in the observation room could be adjusted as needed. After 72 hours, the number of live mites was counted, and the mortality rate was calculated. The Bliss method was used for evaluation, which is one of the classic methods for evaluating the effects of mixtures. Based on his concept of independent combined action, Bliss believed that the theoretical mortality rate P of a mixture of insecticides and acaricides could be calculated using the following formula: P = Pm + Pn(1-Pm)
[0059] Pm represents the target mortality rate (%) of the first active component at a concentration of m; Pn represents the target mortality rate (%) of the second active component at a concentration of n.
[0060] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, it is determined that the two active components have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect.
[0061] Table 1: Synergistic effect of compound I with etoxazole, etoxazole, cyprodinil, bifenazate, or buprofen on adult Tetranychus carmine.
[0062] Example 2
[0063] Indoor activity assay of the composition containing compound I against Tetranychus carmine:
[0064] As can be seen from the synergistic effect data in Table 1 above, the composition of compound I of the present invention mixed with four agents such as etoxazole has a significant synergistic effect on adult Tetranychus cinnabarinus. Furthermore, the LC50 value and co-toxicity coefficient of the composition of compound I and etoxazole, etoxazole, cyprodinil, bifenazate or diflubenzuron were determined.
[0065] Test target: Adult Tetranychus cinnabarinus (boisduval) mite, a sensitive strain kept indoors.
[0066] Preparation of drug solution: According to different test requirements, the test samples are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0067] Experimental Methods: The activity of the pesticide against adult Tetranychus carinata was determined using a potted seedling spraying method. First, adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding their first pair of true leaves. After the adults stabilized, the population was counted. Then, the pesticide solution was sprayed evenly using the Airbrush method, from low to high doses, at a rate of 1.5 mL per plant. Each treatment was repeated four times, with a blank control included.
[0068] The treated test materials were placed in an observation room, where the temperature, humidity, and light were adjustable as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using DPS data processing software to determine the toxicity regression equations, LC50 values, and 95% confidence limits for each single test agent and each combination of different ratios. The co-toxicity coefficients for each ratio were then calculated using the Sun YP method to evaluate the combined effects.
[0069] Table 2: Results of indoor combined toxicity assay of compound I and etoxazole against Tetranychus cinnabarinus
[0070] Table 3: Results of indoor combined toxicity assay of compound I and buprofen against Tetranychus cinnabarin
[0071] Table 4: Results of indoor combined toxicity assay of compound I and cyproterone against Tetranychus cinnabarin
[0072] Table 5: Results of indoor combined toxicity assay of compound I and bifenazate against Tetranychus cinnabarinus
[0073] The results in Tables 2 to 5 show that the co-toxicity coefficients of Compound I with etoxazole, etoxazole, cyprodinil, bifenazate, or dicofol are all greater than 120, indicating that Compound I has a synergistic effect with etoxazole, etoxazole, cyprodinil, bifenazate, or dicofol.
[0074] Indoor bioactivity assay (II)
[0075] Example 3
[0076] Synergistic effect determination of compositions containing compound I on Tetranychus cinnabarinus eggs:
[0077] Test subject: Tetranychus cinnabarinus Boisduval, mite eggs, sensitive strains kept indoors, eggs laid 1 day ago.
[0078] Test conditions: Temperature: 24-28℃, Relative humidity: 30-60%, Light intensity: L:D = 12:12
[0079] Drug solution preparation: According to different test requirements, the test samples (different ratio compositions and original drugs of this invention) are accurately weighed using an electronic analytical balance. The samples are dissolved in acetone to prepare a stock solution, and then diluted with 0.1% Tween-80 according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0080] Experimental Method: Kidney bean seedlings at the first pair of true leaves unfolding stage were selected, leaving one true leaf intact. Ten female adult spider mites of uniform development were transferred to the leaf. After 24 hours, the female mites were removed, and the seedlings were sprayed with the solution. A blank control was treated first. The above procedure was repeated in ascending order of concentration, with three replicates for each treatment. After treatment, all mite eggs were transferred to an observation room. Seven days later, after all eggs in the blank control had hatched, the number of hatched eggs was counted, and the hatching inhibition rate was calculated.
[0081] The evaluation employed the Bliss method, a classic approach for evaluating the effects of mixtures. Based on his concept of independent synergistic effects, Bliss argued that the theoretical inhibition rate P of a mixture of insecticides and acaricides can be calculated using the following formula:
[0082] P = Pm + Pn(1 - Pm)
[0083] Pm represents the inhibition rate (%) of the target when the first active component is at a concentration of m; Pn represents the inhibition rate (%) of the target when the second active component is at a concentration of n.
[0084] If the actual inhibition rate of the target is greater than the theoretical inhibition rate P after the two active components are mixed at a certain concentration, it is determined that the two active components have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect.
[0085] Table 6: Synergistic effect of compound I in combination with three other agents (including thiamethoxam) on adult Tetranychus cinnabarinus.
[0086] Example 4
[0087] Indoor activity assay of the composition containing compound I against Tetranychus carmine:
[0088] As can be seen from the synergistic effect data in Table 6 above, the composition of compound I of the present invention mixed with three agents such as thiamethoxam has a significant synergistic effect on adult Tetranychus cinnabarinus. Furthermore, the LC50 value and co-toxicity coefficient of the composition composed of compound I and thiamethoxam, etoxazole and tetradifon were determined.
[0089] Test subject: Tetranychus cinnabarinus Boisduval, mite eggs, sensitive strains kept indoors, eggs laid 1 day ago.
[0090] Test conditions: Temperature: 24-28℃, Relative humidity: 30-60%, Light intensity: L:D = 12:12
[0091] Drug solution preparation: According to different test requirements, the test samples (different ratio compositions and original drugs of this invention) are accurately weighed using an electronic analytical balance. The samples are dissolved in acetone to prepare a stock solution, and then diluted with 0.1% Tween-80 according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0092] Experimental Methods: Kidney bean seedlings at the first true leaf unfolding stage were selected, leaving one true leaf. Ten female adult spider mites of uniform development were transferred to the leaf. After 24 hours, the female mites were removed, and the mixture was sprayed. A blank control was treated first. The above procedure was repeated in ascending order of concentration, with three replicates per treatment. After treatment, all mite eggs were transferred to the observation room. Seven days later, after all blank control eggs had hatched, the hatching number was recorded, and the hatching inhibition rate was calculated. Statistical analysis was performed using DPS data processing software to determine the toxicity regression equations, LC50 values, and 95% confidence limits for each tested single agent and each combination of different ratios. The co-toxicity coefficients of each ratio were calculated using the Suny-P method to evaluate the combined effects.
[0093] Table 7: Results of combined indoor toxicity assay of compound I and thiamethoxam against Tetranychus cinnabarinus
[0094] Table 8: Results of indoor combined toxicity assay of compound I and etoxazole against Tetranychus cinnabarinus.
[0095] Table 9: Results of indoor combined toxicity assay of compound I and tetradifon against Tetranychus cinnabarinus
[0096] The results in Tables 7 to 9 show that the co-toxicity coefficients of compound I with thiamethoxam, etoxazole, and tetradifon are all greater than 120, indicating that compound I has a synergistic effect with thiamethoxam, etoxazole, and tetradifon.
[0097] Indoor bioactivity assay (Part 3)
[0098] Example 5
[0099] Synergistic effect determination of compositions containing compound I on Tetranychus cinnabarinus eggs:
[0100] Test subject: Tetranychus cinnabarinus Boisduval, mite eggs, sensitive strains kept indoors, eggs laid 1 day ago.
[0101] Test conditions: Temperature: 24-28℃, Relative humidity: 30-60%, Light intensity: L:D = 12:12
[0102] Drug solution preparation: According to different test requirements, the test samples (different ratio compositions and original drugs of this invention) are accurately weighed using an electronic analytical balance. The samples are dissolved in acetone to prepare a stock solution, and then diluted with 0.1% Tween-80 according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0103] Experimental Method: Kidney bean seedlings at the first pair of true leaves unfolding stage were selected, leaving one true leaf intact. Ten female adult spider mites of uniform development were transferred to the leaf. After 24 hours, the female mites were removed, and the seedlings were sprayed with the solution. A blank control was treated first. The above procedure was repeated in ascending order of concentration, with three replicates for each treatment. After treatment, all mite eggs were transferred to an observation room. Seven days later, after all eggs in the blank control had hatched, the number of hatched eggs was counted, and the hatching inhibition rate was calculated.
[0104] The evaluation employed the Bliss method, a classic approach for evaluating the effects of mixtures. Based on his concept of independent combined action, Bliss argued that the theoretical inhibition rate P of a mixture of insecticides and acaricides can be calculated using the following formula: P = Pm + Pn(1-Pm)
[0105] Pm represents the inhibition rate (%) of the target when the first active component is at a concentration of m; Pn represents the inhibition rate (%) of the target when the second active component is at a concentration of n.
[0106] If the actual inhibition rate of the target is greater than the theoretical inhibition rate P after the two active components are mixed at a certain concentration, it is determined that the two active components have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect.
[0107] Table 10: Synergistic effect of compound I in combination with avermectin on adult Tetranychus carmine.
[0108] Example 6
[0109] Indoor activity assay of the composition containing compound I against Tetranychus carmine:
[0110] As can be seen from the synergistic effect data in Table 10 above, the combination of compound I and avermectin of the present invention has a significant synergistic effect on adult spider mites. The LC50 value and co-toxicity coefficient of the combination composed of compound I and avermectin were determined.
[0111] Test subject: Tetranychus cinnabarinus Boisduval, mite eggs, sensitive strains kept indoors, eggs laid 1 day ago.
[0112] Test conditions: Temperature: 24-28℃, Relative humidity: 30-60%, Light intensity: L:D = 12:12
[0113] Drug solution preparation: According to different test requirements, the test samples (different ratio compositions and original drugs of this invention) are accurately weighed using an electronic analytical balance. The samples are dissolved in acetone to prepare a stock solution, and then diluted with 0.1% Tween-80 according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0114] Experimental Methods: Kidney bean seedlings at the first true leaf unfolding stage were selected, leaving one true leaf. Ten female adult spider mites of uniform development were transferred to the leaf. After 24 hours, the female mites were removed, and the mixture was sprayed. A blank control was treated first. The above procedure was repeated in ascending order of concentration, with three replicates per treatment. After treatment, all mite eggs were transferred to the observation room. Seven days later, after all blank control eggs had hatched, the hatching number was recorded, and the hatching inhibition rate was calculated. Statistical analysis was performed using DPS data processing software to determine the toxicity regression equations, LC50 values, and 95% confidence limits for each tested single agent and each combination of different ratios. The co-toxicity coefficients of each ratio were calculated using the Suny-P method to evaluate the combined effects.
[0115] Table 11: Results of indoor combined toxicity assay of compound I and avermectin against Tetranychus carmine.
[0116] The results in Table 11 show that the co-toxicity coefficients of compound I and avermectin are both greater than 120, indicating that compound I and avermectin have a synergistic effect.
[0117] Indoor bioactivity assay (IV)
[0118] Example 7
[0119] Synergistic effect determination of compositions containing compound I against Tetranychus cinnabarinus:
[0120] Test subject: Tetranychus cinnabarinus Boisduval, adult mite, sensitive strain kept indoors.
[0121] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0122] Preparation of drug solution: According to different test requirements, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0123] Experimental method: The activity of the mites against adult Tetranychus carinata was determined by spraying potted seedlings. First, 40-60 adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding the first pair of true leaves. After the adults stabilized, the population was counted. Then, the test material was treated with 1.5 mL of the mites using the Airbrush method. A blank control was set up.
[0124] After natural air drying, the treated test materials were placed in an observation room. The temperature, humidity, and light in the observation room could be adjusted as needed. After 72 hours, the number of live mites was counted, and the mortality rate was calculated. The Bliss method was used for evaluation, which is one of the classic methods for evaluating the effects of mixtures. Based on his concept of independent combined action, Bliss believed that the theoretical mortality rate P of a mixture of insecticides and acaricides could be calculated using the following formula: P = Pm + Pn(1-Pm)
[0125] Pm represents the target mortality rate (%) of the first active component at a concentration of m; Pn represents the target mortality rate (%) of the second active component at a concentration of n.
[0126] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, it is determined that the two active components have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect.
[0127] Table 12: Synergistic effect of compound I with triazole tin, propargite, or diethyl urea on adult Tetranychus carmine.
[0128] Example 8
[0129] Indoor activity assay of the composition containing compound I against Tetranychus carmine:
[0130] As can be seen from the synergistic effect data in Table 12 above, the composition of compound I of the present invention mixed with three agents such as triazole tin has a significant synergistic effect on adult Tetranychus cinnabarinus. Furthermore, the LC50 value and co-toxicity coefficient of the composition composed of compound I and triazole tin, propargite, and diethyl ether urea were determined.
[0131] Test target: Adult Tetranychus cinnabarinus (boisduval) mite, a sensitive strain kept indoors.
[0132] Preparation of drug solution: According to different test requirements, the test samples are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0133] Experimental Methods: The activity of the pesticide against adult Tetranychus carinata was determined using a potted seedling spraying method. First, adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding their first pair of true leaves. After the adults stabilized, the population was counted. Then, the pesticide solution was sprayed evenly using the Airbrush method, from low to high doses, at a rate of 1.5 mL per plant. Each treatment was repeated four times, with a blank control included.
[0134] The treated test materials were placed in an observation room, where the temperature, humidity, and light were adjustable as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using DPS data processing software to determine the toxicity regression equations, LC50 values, and 95% confidence limits for each single test agent and each combination of different ratios. The co-toxicity coefficients for each ratio were then calculated using the Sun YP method to evaluate the combined effects.
[0135] Table 13: Results of indoor combined toxicity assay of compound I and triazoletin against Tetranychus cinnabarinus
[0136] Table 14: Results of indoor combined toxicity assay of compound I and propargite against Tetranychus cinnabarinus.
[0137] Table 15: Results of indoor combined toxicity assay of compound I and diethyl urea against Tetranychus cinnabarinus
[0138] The results in Tables 13 to 15 show that the co-toxicity coefficients of Compound I with triazole tin, propargite, or buprofen are all greater than 120, indicating that Compound I has a synergistic effect with triazole tin, propargite, or buprofen.
[0139] Indoor bioactivity assay (V)
[0140] Example 9
[0141] Synergistic effect determination of compositions containing compound I against Tetranychus cinnabarinus:
[0142] Test subject: Tetranychus cinnabarinus Boisduval, adult mite, sensitive strain kept indoors.
[0143] Test conditions: Temperature: 24-26℃, Relative humidity: 60%, Light intensity: L:D = 14:10
[0144] Preparation of drug solution: According to different test requirements, the test samples (different ratio compositions and original drugs of the present invention) are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to prepare a drug solution with a certain concentration.
[0145] Experimental method: The activity of the mites against adult Tetranychus carinata was determined by spraying potted seedlings. First, 40-60 adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding the first pair of true leaves. After the adults stabilized, the population was counted. Then, the test material was treated with 1.5 mL of the mites using the Airbrush method. A blank control was set up.
[0146] After natural air drying, the treated test materials were placed in an observation room. The temperature, humidity, and light in the observation room could be adjusted as needed. After 72 hours, the number of live mites was investigated, and the mortality rate was calculated. The Bliss method was used for evaluation, which is one of the classic methods for evaluating the effects of mixtures. Based on his concept of independent combined action, Bliss believed that the theoretical mortality rate P of insecticides and acaricides mixed together could be calculated using the following formula:
[0147] P = Pm + Pn(1 - Pm)
[0148] Pm represents the target mortality rate (%) of the first active component at a concentration of m; Pn represents the target mortality rate (%) of the second active component at a concentration of n.
[0149] If the actual mortality rate of the target is greater than the theoretical mortality rate P after the two active components are mixed at a certain concentration, it is determined that the two active components have a synergistic effect when used together at the set concentration; otherwise, they have an antagonistic effect.
[0150] Table 16: Synergistic effect of compound I in combination with three other agents, including isoxazolidinone, on adult Tetranychus cinnabarinus.
[0151] Example 10
[0152] Indoor activity assay of the composition containing compound I against Tetranychus carmine:
[0153] As can be seen from the synergistic effect data in Table 16 above, the combination of compound I of the present invention with three agents such as isoxazolamide has a significant synergistic effect on adult spider mites. Furthermore, the LC50 value and co-toxicity coefficient of the combination of compound I with isoxazolamide, fluoxazolamide and amphetamine were determined.
[0154] Test target: Adult Tetranychus cinnabarinus (boisduval) mite, a sensitive strain kept indoors.
[0155] Preparation of drug solution: According to different test requirements, the test samples are accurately weighed using an electronic analytical balance. The original drug is dissolved in acetone and then diluted with 0.1% Tween 80 water according to the experimental design dosage to form a series of drug solutions with a certain concentration gradient (the composition of this invention).
[0156] Experimental Methods: The activity of the pesticide against adult Tetranychus carinata was determined using a potted seedling spraying method. First, adult Tetranychus carinata of uniform size were transferred to bean seedlings (leaving one true leaf) at the stage of unfolding their first pair of true leaves. After the adults stabilized, the population was counted. Then, the pesticide solution was sprayed evenly using the Airbrush method, from low to high doses, at a rate of 1.5 mL per plant. Each treatment was repeated four times, with a blank control included.
[0157] The treated test materials were placed in an observation room, where the temperature, humidity, and light were adjustable as needed. The number of dead and live mites was investigated after 72 hours. The corrected mortality rate was calculated using the Abbott formula, and statistical analysis was performed using DPS data processing software to determine the toxicity regression equations, LC50 values, and 95% confidence limits for each single test agent and each combination of different ratios. The co-toxicity coefficients for each ratio were then calculated using the Sun YP method to evaluate the combined effects.
[0158] Table 17: Results of indoor combined toxicity assay of compound I, isoxazolamide, against Tetranychus cinnabarinus.
[0159] Table 18: Results of indoor combined toxicity assay of compound I·fluoxazolamide against Tetranychus cinnabarinus
[0160] Table 19: Results of indoor combined toxicity assay of compound I, amphetamine, against Tetranychus cinnabarinus
[0161] The results showed that the co-toxicity coefficient of compound I with isoxazoline, fluoxazoline, or amphetamine was greater than 120, indicating that compound I has a synergistic effect with isoxazoline, fluoxazoline, or amphetamine.
[0162] The preferred embodiments of the present invention have been described in detail above; however, the present invention is not limited thereto. Within the scope of the inventive concept, various simple modifications can be made to the technical solutions of the present invention, including combinations of various technical features in any other suitable manner. These simple modifications and combinations should also be considered as the content disclosed in the present invention and are all within the protection scope of the present invention.
Claims
1. An insecticidal and miticidal composition, characterized by comprising, The composition contains active component A and active component B, the weight ratio between the active component A and the active component B is 99:1-1:99; the active component A is selected from compound I, and the active component B is selected from a mitochondrial electron transport complex (I) inhibitor class of insect / mites agent, a mitochondrial transport complex (II) inhibitor class of insect / mites agent, a mitochondrial electron transport complex (III) inhibitor class of insect / mites agent, a mite growth inhibitor class of mite agent, a macrolide class of insect / mites agent, an ATP synthetase inhibitor class of insect / mites agent, or a GABA-gated chloride channel allosteric modulator; the structure of the compound I is as follows:
2. The composition of claim 1, wherein, The mitochondrial electron transport complex (I) inhibitor insecticide / acaricide is selected from one or more of pyridaben, azoxystrobin, pyrimethanil, pyridaben, azoxystrobin, acetamiprid, or rotenone. And / or, the mitochondrial delivery complex (II) inhibitor insecticide / acaricide is selected from one or more of etoxazole, cyprodinil or fenflurfen; And / or, the mitochondrial electron transport complex (III) inhibitor insecticide / acaricide is selected from one or more of bifenazate, pyrimethanil, pyrimethanil, flometoquin, flufenoxuron, or mitoxuron; And / or, the mite growth inhibitor acaricide is selected from one or more of tetradifon, thiamethoxam, etoxazole or flufenoxam; And / or, the macrolide insecticide / acaricide is selected from one or more of abamectin, emamectin benzoate, spinosad, ethyl spinosad, acaricide, ivermectin, rapamectin, emamectin, mibamectin, Carvacrol, doramectin, eprinomenctin, Milbemycinoxime, Moxidectin, Sanguinarine, or selamectin; And / or, the ATP synthase inhibitor insecticide / acaricide is selected from one or more of butyl urea, triazole tin, tricyclic tin, fenbutatin, propargite, or trichlorfon; And / or, the GABA-gated chloride channel allosteric modulator is selected from one or more of the following: bromoxynil, acetamiprid, acetamiprid, fipronil, pyridoxin, flupyrazole, butenpyram, isoxazolidinamide, cyclopropionate, flavanil, afraran, fluoxazolidinamide, oxazolidinamide, sarolaner, lotelanar, sarolaner, flusulfanilamide, afenofibrate, 1-(2,6-dichloro-a,a,a-trifluoro-p-tolyl)-4-(fluoromethylthio)-5-[(pyrazinylmethyl)amino]pyrazole-3-carboxylon, 1-(2,6-dichloro-4-(trifluoromethyl)phenyl)-4-((difluoromethyl)thio)-5-((pyridin-2-ylmethyl)amino)-1H-pyrazole-3-carboxylon.
3. The composition according to claim 1 or 2, characterized in that, The active component A is compound I, and the active component B is selected from one or more of the following: pyridaben, azoxystrobin, pyrimethanil, pyridaben, acetamiprid, cyprodinil, diflubenzuron, bifenazate, pyrimethanil, pyrimethanil, or flometoquin. Preferably, the weight ratio of active component A to active component B is 50:1-1:50, more preferably 20:1-1:40, more preferably 10:1-1:10, and even more preferably 4:1-1:
4.
4. The composition according to claim 1 or 2, characterized in that, The active component A is compound I, and the active component B is selected from one or more of tetradifon, thiamethoxam, or etoxazole. Preferably, the weight ratio of active component A to active component B is 50:1-1:50, more preferably 5:1-40:1, more preferably 5:1-20:1, and even more preferably 1:1-20:
1.
5. The composition according to claim 1 or 2, characterized in that, said active ingredient A is compound I and said active ingredient B is selected from one or more of abamectin, spinosad or emamectin benzoate; Preferably, the parts by weight ratio between said active ingredient A and said active ingredient B is from 50:1 to 1:50, preferably from 50:1 to 1:1, more preferably from 40:1 to 1:
1.
6. The composition according to claim 1 or 2, characterized in that, said active ingredient A is compound I and said active ingredient B is selected from one or more of azocyclotin, propargite or diafenthiuron; Preferably, the parts by weight ratio between said active ingredient A and said active ingredient B is from 40:1 to 1:40, preferably from 20:1 to 1:40, more preferably from 5:1 to 1:40, further preferably from 1:5 to 1:
20.
7. The composition according to claim 1 or 2, characterized in that, said active ingredient A is compound I and said active ingredient B is selected from one or more of brofenprox, isoxazoles, cycloprothrin, fluoxazamide, furametpyr or spirodiclofen; Preferably, the parts by weight ratio between said active ingredient A and said active ingredient B is from 50:1 to 1:20, preferably from 20:1 to 1:10, more preferably from 10:1 to 1:5, further preferably from 5:1 to 1:
5.
8. An insecticidal and miticidal agent comprising the insecticidal and miticidal composition according to any one of claims 1 to 7, characterized in that, said insecticidal and acaricidal composition is mixed with a carrier and any one of the auxiliary agents.
9. The insecticidal and miticidal agent according to claim 8, characterized by The cumulative content of the active ingredients of said insecticidal and acaricidal composition in said insecticidal and acaricidal agent is between 0.5% and 95%; Preferably, the cumulative content of the active ingredients of said insecticidal and acaricidal composition in said agent is between 1% and 85%.
10. Use of the insecticidal and acaricidal composition according to any one of claims 1 to 7 or of the insecticidal and acaricidal agent according to claim 8 or 9 for controlling agricultural or urban hygiene pests.
11. Use according to claim 10, characterized in that, Said insecticidal and acaricidal composition is applied in an effective dose to the pests to be controlled or to the medium in which they grow. Said insecticidal and acaricidal composition is applied in an effective dose to pests to be controlled or to the medium in which they grow.