CN114375952B - Application of hydroxy-alpha-sanshool in preparation of insecticide and/or antifeedant - Google Patents

Application of hydroxy-alpha-sanshool in preparation of insecticide and/or antifeedant Download PDF

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CN114375952B
CN114375952B CN202111647517.6A CN202111647517A CN114375952B CN 114375952 B CN114375952 B CN 114375952B CN 202111647517 A CN202111647517 A CN 202111647517A CN 114375952 B CN114375952 B CN 114375952B
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sanshool
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周先礼
陈琳
王梓旭
刘月
李翔宇
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Southwest Jiaotong University
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    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/18Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
    • A01N37/20Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof containing the group, wherein Cn means a carbon skeleton not containing a ring; Thio analogues thereof
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Abstract

The invention provides application of hydroxy-alpha-sanshool in preparation of a pesticide and/or a antifeedant, belonging to the field of pest control. The invention discovers for the first time that the hydroxyl-alpha-sanshool as an active ingredient has excellent insecticidal action on most pests of Lepidoptera and Homoptera, and the effective rate of the hydroxyl-alpha-sanshool particularly on common pests (including asparagus caterpillar, spodoptera frugiperda, plutella xylostella, cabbage caterpillar, armyworm, cnaphalocrocis medinalis, cotton aphid, wheat aphid and the like) of rice, cotton, vegetables, fruit trees and field crops reaches over 90 percent. The present inventors have also found that hydroxy- α -sanshool as an active ingredient also has excellent antifeedant activity against most pests of the orders lepidoptera and homoptera. The hydroxy-alpha-sanshool can be used as an insecticide and an antifeedant, has the advantages of multiple action modes and multiple effects, is low in toxicity, is not easy to generate drug resistance, and has wide application prospect in preparation of green insecticides and/or antifeedants.

Description

Application of hydroxy-alpha-sanshool in preparation of insecticide and/or antifeedant
Technical Field
The invention belongs to the field of pest control, and particularly relates to application of hydroxy-alpha-sanshool in preparation of a pesticide and/or a antifeedant.
Background
Pests have been one of the major disasters in the fields of agriculture, horticulture, flower culture, and the like. Through general survey for 3 years at the plant protection central station in Hubei province and 11 survey point data in the whole province, the general province finds that 158 kinds of tea plant pests are totally adopted and are insects in class Insecta and Arachnida, 150 kinds of insects are dominant and 8 kinds of Arachnida are in class Insecta. Insects that are harmful to tea tree encompass 7 orders, including lepidoptera, homoptera, coleoptera, orthoptera, hemiptera, diptera, thysanoptera, and psophila, with the largest lepidoptera, 6 in total, the suborder homoptera, 39, again the coleoptera, 21. The wide variety of pests causes significant losses to national economy, especially agricultural production, in our country.
At present, chemical pesticide control is still used as a main measure for controlling the pests, but with the long-term, large-scale and wide-range use of pesticides, the problems of chemical residues, environmental pollution, ecological change, resistance generation and the like are continuously highlighted. Old drugs are quickly adapted by insect groups, so that the effect of controlling insect pests cannot be achieved any more, and therefore, the development of novel pesticides with high efficiency, low toxicity and multiple action modes is urgent.
During the long-term co-evolution of plants with insect diseases, many secondary metabolites with defensive effects are produced. The botanical pesticide has the advantages of strong selectivity, low toxicity to natural enemies of pests and human and livestock, higher harmony with the environment, easy decomposition in natural environment, low residual quantity, unique action mode, difficult generation of drug resistance of pests and the like, and has become a research hotspot in the field of pest control at home and abroad in recent years.
Zanthoxylum bungeanum is a plant of Zanthoxylum genus of Rutaceae family, and at present, the Zanthoxylum bungeanum is proved to contain active ingredients such as volatile oil, alkaloid, amide, lignan, fatty acid and the like, and is recorded in traditional Chinese medicine that Zanthoxylum bungeanum has the effects of warming middle-jiao to relieve pain, killing parasites and relieving itching. The literature (the research on the insecticidal activity of the pepper extract, the research and the concurrence of food, 4 months in 2015, 36 th volume, 7 th period) discloses that the pepper extract has certain contact poisoning, stomach toxicity, fumigation and avoidance activities on the tribolium castaneum. Wherein the contact killing activity LC of n-butanol extraction part to tribolium castaneum 50 The value is 1.086g/mL, and the avoidance rate of the petroleum ether extraction part to the tribolium castaneum is 93.617%. However, the chemical components in the zanthoxylum bungeanum extract are quite complex and are a mixture consisting of dozens of or even hundreds of compounds, and most of the compounds in the extract have no insecticidal activity. In order to reduce the dosage of the pesticide and improve the insecticidal efficiency, it is important to develop specific compounds with insecticidal activity from plants.
Disclosure of Invention
The invention aims to provide application of hydroxy-alpha-sanshool in preparation of insecticides and/or antifeedants.
The invention provides application of hydroxy-alpha-sanshool in preparing insecticide and/or antifeedant.
Further, the pesticide can kill pests, and the antifeedant has antifeedant effect on the pests.
Further, the pests are insect pests.
Further, the insecta pests are lepidopteran pests or homopteran pests.
Further, the lepidoptera pests are noctuidae, plutella xylostella, pieris or borer;
the homoptera pests are aphididae pests.
Further, the noctuidae pests are Spodoptera exigua (Beetarmyworm), spodoptera frugiperda (Spodoptera frugiperda), or armyworm (Mythimna separata); the diamondback moth pest is diamondback moth (Plutella xylostella); the Pieris rapae pests are cabbage caterpillars (Pieris rapae); the moth-killing insect is rice borer (Chiloaauricilius dudgeno) or corn borer (pyraustanucubalis);
the pests of the aphididae are cotton aphids (Aphis gossypii Glover) or wheat aphids (Macrosiphum avenae).
Furthermore, the pesticide and/or the antifeedant is a preparation prepared by taking hydroxy-alpha-sanshool as an active ingredient and adding auxiliary materials acceptable in the field of pesticide preparations.
Furthermore, the pesticide and/or the antifeedant is a preparation prepared by taking hydroxy-alpha-sanshool and other medicines as active ingredients and adding auxiliary materials acceptable in the field of pesticide preparations; the other medicines are one or more than two of organophosphorus pesticides, pyrethroid pesticides, carbamate pesticides and plant-derived pesticides.
Such other drugs include, but are not limited to, the following: (1) organophosphorus pesticides, such as: phorate (3911), systemic forest (1059, E1059), parathion (1605, E1605), DDVP (DDV), dimethoate, trichlorfon, etc.; (2) pyrethroid type agricultural chemicals such as: deltamethrin, cypermethrin, cyhalothrin; (3) carbamate-based pesticides, such as: aldicarb, methomyl, carbosulfan, and the like; (4) plant-derived pesticides, such as: matrine, nimbin, rotenone, nicotine, celastrol, rhodojaponin, capsaicin, ricinoleic acid, stemonine, etc.
Further, the auxiliary material acceptable in the field of pesticide preparations is a pesticide auxiliary agent, and the pesticide auxiliary agent is preferably an excipient.
The pesticide adjuvant is an auxiliary substance added in the processing or use of pesticide preparations and used for improving the physicochemical property of the pesticide preparation, and is also called as a pesticide adjuvant. Pesticide adjuvants generally have no biological activity per se.
The pesticide adjuvant includes, but is not limited to, the following: silica, kaolin, bentonite, talc, diatomaceous earth, dolomite, calcium carbonate, magnesium oxide, chalk, clay, synthetic silicates, attapulgite, sepiolite and the like. Besides water, usable liquid diluents also include, for example, aromatic organic solvents (xylene or a mixture of alkylbenzenes, chlorobenzene, etc.), paraffins (petroleum fractions, alcohols (methanol, propanol, butanol, octanol, glycerol), esters (ethyl acetate, isobutyl acetate, etc.), ketones (cyclohexanone, acetone, acetophenone, isophorone, ethyl amyl ketone, etc.), amides (N, N-dimethylformamide, N-methylpyrrolidone, etc.). Usable surfactants are alkylsulfonates, alkylarylsulfonates, polyoxyethylene alkylphenols, polyoxyethylene esters of sorbitol, sodium (calcium) lignosulfonate, triethylamine or triethanolamine salts, etc.
Further, the prepared preparation is dry powder, paste, solution, emulsifiable concentrate, suspending agent, aqueous emulsion, microemulsion or granules.
The preparation method of the preparation comprises but is not limited to the following methods:
weighing hydroxy-alpha-sanshool, sodium dodecyl benzene sulfonate, pyrrolidone and other conventional auxiliary materials, and preparing the microemulsion with the concentration of the effective component of 1 percent according to the conventional process.
Weighing hydroxy-alpha-sanshool and conventional auxiliary materials such as solvent oil, pyrrolidone, xanthan gum and the like, and preparing the mixture into an aqueous emulsion with the concentration of an effective component of 1% according to a conventional process.
The water dispersible granule with the effective component concentration of 2 percent is prepared by weighing the hydroxyl-alpha-sanshool, sodium lignosulphonate, kaolin and other conventional auxiliary materials according to the conventional process.
Weighing conventional adjuvants such as hydroxy-alpha-sanshool, calcium dodecylbenzene sulfonate, phenethyl phenol polyoxyethylene ether, solvent oil, etc., and making into water dispersible granule with effective component concentration of 2% according to conventional process.
The hydroxy-alpha-sanshool, lignin, diatomite and other conventional auxiliary materials are weighed and prepared into wettable powder with the effective component concentration of 2 percent according to the conventional process.
The hydroxy-alpha-sanshool, lignin, diatomite and other conventional auxiliary materials are weighed and prepared into wettable powder with the effective component concentration of 2 percent according to the conventional process.
The hydroxy-alpha-sanshool, lignin, diatomite and other conventional auxiliary materials are weighed and prepared into wettable powder with the concentration of the effective component of 2 percent according to the conventional process.
Weighing hydroxy-alpha-sanshool and azadirachtin according to the weight ratio of 1.
According to the weight ratio of 6:1, weighing hydroxyl-alpha-sanshool and deltamethrin according to the proportion, and preparing the mixture into an aqueous emulsion with the effective component concentration of 25 percent according to the conventional process by using the mixture and conventional auxiliary materials such as solvent oil, pyrrolidone, xanthan gum and the like.
The hydroxy-alpha-sanshool of the present invention can be isolated and purified from natural plants, synthesized by a synthetic method known to those skilled in the art, or obtained by directly purchasing a commercially available product.
Hydroxy- α -sanshool (English name: hydroxy- α -sanshool, abbreviated as HAS), CAS number: 83883-10-7, chemical name: (2E, 6Z,8E, 10E) -N- (2-hydroxy-2-methylpropyl) dodeca-2,6,8, 10-tetranamide, molecular formula: c 16 H 25 NO 2 Molecular weight: 263, molecular structure shown below:
Figure GDA0003554731860000031
the invention achieves the following beneficial effects:
1. the invention discovers for the first time that the hydroxyl-alpha-sanshool as an active ingredient has excellent insecticidal action on most pests of Lepidoptera and Homoptera, and the effective rate of the hydroxyl-alpha-sanshool particularly on common pests (including asparagus caterpillar, spodoptera frugiperda, plutella xylostella, cabbage caterpillar, armyworm, cnaphalocrocis medinalis, cotton aphid, wheat aphid and the like) of rice, cotton, vegetables, fruit trees and field crops reaches over 90 percent. The hydroxy-alpha-sanshool as an agricultural insecticide has the advantages of good insecticidal effect, quick action, long persistent period and wide insecticidal spectrum.
2. The invention discovers for the first time that hydroxy-alpha-sanshool as an active ingredient also has excellent antifeedant activity against most pests of the Lepidoptera and Homoptera orders. The hydroxy-alpha-sanshool can be used as an insecticide, can also be used as an antifeedant, has the advantages of multiple action modes and multiple effects, and is not easy to generate drug resistance. Compared with chemical pesticides, the hydroxy-alpha-sanshool has various effects of contact killing, antifeedant action and the like on pests, has obvious effect and can effectively prevent the generation of insect resistance.
3. The hydroxy-alpha-sanshool is mainly derived from Zanthoxylum bungeanum of Zanthoxylum of Rutaceae, is distributed in other Rutaceae plants, has wide source and is easy to degrade, and belongs to the category of green and environment-friendly botanical pesticides.
4. The Zanthoxylum bungeanum of Zanthoxylum of Rutaceae is a medicine and food dual-purpose plant, the hydroxy-alpha-sanshool is obtained by separating and purifying the Zanthoxylum bungeanum of Rutaceae, is safe to human and livestock, nontoxic to natural enemies, pollution-free, environment-friendly, and free of three causes and three wastes, and meets the strategic objective of creating novel insecticides and the concept of green plant protection in the world at present.
Obviously, many modifications, substitutions, and variations are possible in light of the above teachings of the invention, without departing from the basic technical spirit of the invention, as defined by the following claims.
The present invention will be described in further detail with reference to the following examples. This should not be understood as limiting the scope of the above-described subject matter of the present invention to the following examples. All the technologies realized based on the above contents of the present invention belong to the scope of the present invention.
Drawings
FIG. 1: the HPLC analysis chart of hydroxy-alpha-sanshool shows that the peak at t =18.50min is hydroxy-alpha-sanshool.
FIG. 2: nuclear magnetism of hydroxy-alpha-sanshool 1 H NMR spectrum, solvent is deuterated methanol.
FIG. 3: nuclear magnetism of hydroxy-alpha-sanshool 13 C NMR spectrum, solvent is deuterated methanol.
Detailed Description
The raw materials and equipment used in the invention are known products, and are obtained by purchasing products sold in the market.
The hydroxy-alpha-sanshool used in the embodiment of the invention can be purchased from commercial products or prepared by the following method.
Preparing hydroxyl-alpha-sanshool: pulverizing dried pericarpium Zanthoxyli to 20-40 mesh, repeatedly extracting with 95% ethanol, mixing extractive solutions, and concentrating under reduced pressure to obtain fructus Zanthoxyli extract total extract. Then repeatedly carrying out column chromatography on the mixture by an RP-18 reverse phase silica gel column and a nonpolar polystyrene type macroporous adsorption resin HP20, and then carrying out reduced pressure concentration to obtain the hydroxy-alpha-sanshool with the purity of more than 98 percent. The HPLC chromatogram of hydroxy-alpha-sanshool is shown in figure 1, 1 the H NMR spectrum is shown in FIG. 2, 13 the C NMR spectrum is shown in FIG. 3.
Map data for hydroxy-alpha-sanshool: HR-ESI-MS at m/z 286.1771[ 2 ], [ M + Na ]] + (calcd.for C 16 H 25 NO 2 Na,286.1783). 1 H-NMR(CD 3 OD,400MHz)δ:1.19(6H,s,H-3'/H-4'),1.78(3H,d,J=6.4Hz,H-12),2.34(4H,m,H-4/H-5),3.27(2H,d,J=4.0Hz,H-1'),5.39(1H,dt,J=11.0,7.4Hz,H-6),5.75(1H,dd,J=13.8,6.8Hz,H-11),5.75(1H,d,J=7.0Hz,H-2),6.02-6.06(2H,dd,J=6.2,4.8Hz,H-7/H-2),6.10-6.12(2H,m,H-9/H-10),6.39(1H,dd,J=13.8,11.4Hz,H-8),6.82(1H,dt,J=15.4,6.8Hz,H-3). 13 C NMR(100MHz,CD 3 OD)δ:169.0(C-1),125.1(C-2),145.1(C-3),33.1(C-4),27.6(C-5),130.4(C-6),130.6(C-7),126.5(C-8),134.7(C-9),133.2(C-10),130.9(C-11),18.4(C-12),51.1(C-1'),71.6(C-2'),27.2(C-3'),27.2(C-4').
Example 1: contact killing effect of hydroxy-alpha-sanshool as active ingredient on agricultural pests
1. Experimental method
The test insects: in the embodiment, the test insects are collected from larvae of 3-6 th instar of field population, and are fed with artificial feed in an artificial climate chamber (25 +/-1 ℃, L/D =14/10, RH75%) until pupate and lay eggs, and are hatched and fed to 3 th instar, and the larvae with consistent and healthy sizes are selected for activity determination.
Preparing a hydroxyl-alpha-sanshool test solution: hydroxy-alpha-sanshool is precisely weighed, dissolved in ethanol and diluted to 10mg/mL concentration by 0.1% of aqueous emulsion of polyethylene glycol octyl phenyl ether (triton X-100) to be used as a hydroxy-alpha-sanshool test solution for standby.
And (3) contact activity test: healthy larvae of 3 years old and consistent size, which were raised in an artificial climate chamber, were placed in a clean petri dish. Transferring 4mL of the hydroxy-alpha-sanshool test solution, respectively placing pests in the hydroxy-alpha-sanshool test solution for 5s, taking out, sucking off excessive liquid medicine on clean filter paper, and placing in a clean culture dish for feeding with artificial feed. Each group was treated with 20 beetles, 3 replicates, a positive control group of pyrethrin (containing 1.5% pyrethroid) and a blank of ethanol plus 0.1% triton X-100 water emulsion. The death conditions of the hydroxyl-alpha-sanshool test solution after soaking various pests in the test solution are recorded at 20min,1h and 24 h. The contact killing activity (i.e., mortality) was calculated as follows:
mortality (%) = (mortality of dosing group-blank group)/(mortality of 1-blank group) × 100%;
the results are shown in Table 1.
Lethal middle concentration (LD) 50 ) And (3) determination: according to the preliminary determination result of the contact activity, hydroxyl-alpha-sanshool is precisely weighed and dissolved in ethanol, and then diluted into 5 liquid medicines with different concentrations by 0.1 percent triton X-100 aqueous emulsion according to equal ratio gradient for later use as test solutions. According to the contact activity test methodAnd measuring the contact killing activity of pests under different concentrations 1 hour after immersion.
Data processing: by utilizing origin software, taking the concentration (mu mol/mL) as an X axis and the lethality (%) as a Y axis, drawing a fitting curve, and calculating the corresponding concentration when Y is equal to 50 percent, namely the lethal middle concentration LD 50 The results are shown in Table 2.
2. Results of the experiment
Table 1: contact killing activity of test solution (10 mg/mL) to pests at different time
Figure GDA0003554731860000051
Table 2: lethal middle concentration LD of hydroxy-alpha-sanshool on various pests after 1h of action 50 (μmol/mL)
Figure GDA0003554731860000061
CI, confidence interval (confidence interval).
As can be seen from Table 1, the hydroxy-alpha-sanshool has a rapid insecticidal effect on asparagus caterpillar, spodoptera frugiperda, plutella xylostella, cabbage caterpillar, armyworm, rice stem borer, corn borer, cotton aphid and wheat aphid after 20 min; particularly, for asparagus caterpillar and plutella xylostella, the death rate reaches 100% after 20min, and the death rates of spodoptera frugiperda, armyworm, cabbage caterpillar, rice stem borer and wheat aphid also reach more than 90%, and are higher than the insecticidal activity of a positive control.
As can be seen from Table 2, about 1 hour after hydroxy-alpha-sanshool is effective against spodoptera exigua, spodoptera frugiperda, armyworm, plutella xylostella, cabbage caterpillar, rice stem borer, corn borer, cotton aphid and wheat aphid, which are all at LD of 1 hour 50 Respectively reach 3.08, 3.72, 3.82, 3.47, 3.99, 4.12, 16.32, 4.06 and 3.84 mu mol/mL, the positive control groups respectively reach 4.23, 4.54, 4.31, 4.63, 4.47, 9.44, 14.56, 5.15 and 4.39 mu mol/mL, and the insecticidal activity of the hydroxy-alpha-sanshool to the pests is higher than that of the positive control groups.
The experiment result shows that the hydroxyl-alpha-sanshool has the advantages of quick action, good insecticidal effect and wide insecticidal range when being used as an agricultural insecticide.
Example 2: antifeedant effect of hydroxy-alpha-sanshool as active ingredient on agricultural pests
The test insects: in the embodiment, the test insects are collected from larvae of 3-6 th instar in the field population, and are bred by artificial feed in an artificial climate chamber (25 +/-1 ℃, L/D =14/10, RHE 75%) until pupation and oviposition, hatched and bred to 3 rd instar, and the larvae with consistent and healthy sizes are selected for activity determination.
Preparing a hydroxy-alpha-sanshool test solution: hydroxy-alpha-sanshool is precisely weighed, dissolved in acetone and diluted into 5mg/mL concentration by 0.1 percent triton X-100 aqueous emulsion to be used as a hydroxy-alpha-sanshool test solution for standby.
Determining the antifeedant activity: healthy larvae of 3 ages and consistent size cultured in an artificial climate chamber are placed in a clean culture dish, pests are grouped and starved for 6 hours, and fresh cabbage leaves (4 x 4cm in size) are cut for standby. Transferring 15 mu L of hydroxy-alpha-sanshool test solution, uniformly coating each cabbage leaf, placing the cabbage leaves into a culture dish, placing 4 hungry pests in each dish after acetone is completely volatilized, repeating each treatment for 3 times, taking azadirachtin A as a positive control, and taking acetone triton X-100 water emulsion as a blank control. After 24h, a transparent plastic film coordinate card (with the precision of 1 mm) is adopted 2 ) Statistics of the area (mm) of leaf gnawing by pests 2 ) And calculating the food refusal rate by the following formula:
feeding rate = pest feeding area/total leaf area × 100%;
antifeedant rate = (blank gnawing rate-administration gnawing rate)/(blank gnawing rate) × 100%
The results are shown in Table 3.
Determination of antifeedant concentration (AFC) 50 ): according to the preliminary determination result of the antifeedant rate, hydroxyl-alpha-sanshool is precisely weighed and dissolved in acetone to prepare mother liquor with a certain concentration, and then 0.1 percent triton X-100 aqueous emulsion is used for diluting into at least 5 liquid medicines with different concentrations according to an equal ratio gradient for later use as test solutions. And determining the antifeedant rate of the pests under different concentrations after 24 hours according to the antifeedant rate test method.
Then, by origin software, taking an X axis as concentration and a Y axis as antifeedant rate, drawing a fitting curve, and calculating the corresponding concentration when Y is equal to 50 percent, namely half antifeedant concentration AFC 50 . The results are shown in Table 4.
2. Results of the experiment
Table 3: bite rate of hydroxyl-alpha-sanshool (5 mg/mL after 24 h) on pests
Figure GDA0003554731860000071
Table 4: half-concentration AFC of hydroxyl-alpha-sanshool against insect antifeedant 50
Figure GDA0003554731860000072
Figure GDA0003554731860000081
CI-confidence interval (confidence interval).
As can be seen from Table 3, the anti-feeding rates of the hydroxy-alpha-sanshool for spodoptera exigua, spodoptera frugiperda, armyworm, plutella xylostella, cabbage caterpillar, rice stem borer, corn borer, cotton aphid and wheat aphid within 24h are all higher than those of the positive control azadirachtin A.
As can be seen from Table 4, half of the antifeedant concentrations of the hydroxy-alpha-sanshool to spodoptera exigua, spodoptera frugiperda, armyworm, plutella xylostella, cabbage caterpillar, rice stem borer, corn borer, cotton aphid and wheat aphid within 24h are lower than those of the positive control azadirachtin A, and the antifeedant activity of the hydroxy-alpha-sanshool to the pests is higher than that of the positive control azadirachtin A again.
The experiment result shows that the hydroxyl-alpha-sanshool has the advantages of excellent effect and wide application range as the antifeedant.
Example 3: acute toxicity test of hydroxy-alpha-sanshool
1. Experimental methods
Test animals: kunming mice provided by WUDO laboratory animals GmbH have male and female halves and the body weight is 22 +/-2 g. The temperature of the animal room is kept at 23 +/-1 ℃, the humidity is 55 +/-5%, and the photoperiod is 16:8h (L: D). Mice were first acclimatized for 5 days before the experiment, and water and feed were freely supplied. No water is forbidden 12h before experiment. Animal experiments were performed strictly in accordance with national regulations on laboratory animal management.
Preparing a liquid medicine: dissolving hydroxy-alpha-sanshool in DMSO, and diluting with 0.6% Tween-80 water solution to obtain liquid medicine to be tested. A blank was prepared by adding 0.6% aqueous Tween-80 solution in the amount necessary to dissolve DMSO used.
Acute toxicity test: mice were randomly divided into 3 groups of 10 animals each, and weighed one by one. The initial dose was administered by intramascular injection of 3 times and then by increasing the dose until 100% of the animals died, the time and number of deaths were observed and recorded for 7 consecutive days after administration.
2. Results of the experiment
The experimental result shows that in the acute toxicity experiment, the blank control and the hydroxy-alpha-sanshool do not die within 7 days under the maximum dissolving dose (80 mg/mL), which indicates that the hydroxy-alpha-sanshool has no acute toxicity to rats.
In summary, the present invention provides the use of hydroxy- α -sanshool in the preparation of insecticides and/or antifeedants. The invention discovers for the first time that the hydroxy-alpha-sanshool has excellent insecticidal action on most pests of lepidoptera and homoptera as an active ingredient, and the effective rate of the hydroxy-alpha-sanshool especially on common pests (including spodoptera exigua, spodoptera frugiperda, plutella xylostella, cabbage caterpillar, armyworm, rice stem borer, cotton aphid, wheat aphid and the like) of rice, cotton, vegetables, fruit trees and field crops reaches over 90 percent; the present inventors have also found that hydroxy- α -sanshool as an active ingredient also has excellent antifeedant activity against most pests of the orders lepidoptera and homoptera; in addition, toxicity experiments show that the medicine has no acute toxicity to rats. The hydroxy-alpha-sanshool can be used as an insecticide and an antifeedant, has the advantages of multiple action modes and multiple effects, is low in toxicity, is not easy to generate drug resistance, and has wide application prospect in preparation of green insecticides and/or antifeedants.

Claims (6)

1. The application of hydroxyl-alpha-sanshool as an active ingredient in preparing pesticides is characterized in that: the pesticide can kill pests, and the pests are asparagus caterpillar, spodoptera frugiperda, armyworm, plutella xylostella, cabbage caterpillar, rice stem borer, corn borer, cotton aphid or wheat aphid.
2. Use of hydroxy-alpha-sanshool as active ingredient in the preparation of an antifeedant, characterized in that: the antifeedant has antifeedant effect on pests; the pests are asparagus caterpillar, spodoptera frugiperda, armyworm, plutella xylostella, cabbage caterpillar, rice stem borer, corn borer, cotton aphid or wheat aphid.
3. Use according to claim 1 or 2, characterized in that: the insecticide according to claim 1 or the antifeedant according to claim 2 is a preparation prepared by adding an auxiliary material acceptable in the field of pesticide preparations to a hydroxy-alpha-sanshool serving as an active ingredient.
4. Use according to claim 1 or 2, characterized in that: the insecticide according to claim 1 or the antifeedant according to claim 2 is a preparation prepared by taking hydroxy-alpha-sanshool and other medicines as active ingredients and adding auxiliary materials acceptable in the field of pesticide preparation; the other medicines are one or more of organophosphorus pesticides, pyrethroid pesticides, carbamate pesticides and plant-derived pesticides.
5. Use according to claim 3, characterized in that: the preparation formulation is dry powder, paste, solution, emulsifiable concentrate, suspending agent, aqueous emulsion, microemulsion or granules.
6. Use according to claim 4, characterized in that: the preparation formulation is dry powder, paste, solution, emulsifiable concentrate, suspending agent, aqueous emulsion, microemulsion or granules.
CN202111647517.6A 2021-12-29 2021-12-29 Application of hydroxy-alpha-sanshool in preparation of insecticide and/or antifeedant Active CN114375952B (en)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
响应面法优化花椒精油微胶囊的制备;张倩 等;《中国调味品》;20211110;第46卷(第11期);第69-76页 *
花椒精油提取及其生物活性测定研究;庄世宏;《中国优秀博硕士学位论文全文数据库 (硕士) 工程科技Ⅰ辑》;20021215(第2期);B016-180 *

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