Periplocoside P-farm-oriented insecticidal active compound having activating effect on insect trypsin

A trypsin and activation technology, applied in the field of pesticides, can solve problems such as food safety threats and excessive pesticide residues, and achieve the effects of low pressure, large output, and good field control effects

Inactive Publication Date: 2013-06-05
PESTICIDE INST XIBEI AGRI & FORESTRY TECHUNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the long-term and high-frequency application of pesticides, the pests have developed resistance or resistance to the above-mentioned pesticides to varying degrees. To achieve the ideal control effect, the only way to continuously increase the dosage of pesticides is to cause the pesticide residues in agricultural products to exceed the standard, which poses a threat to food safety. serious threat
The present invention provides a plant-derived steroidal glycoside compound, which has the advantages of novel structure and unique mechanism of action. At the same time, there is no compound of this type of structure in the current commercial insecticides

Method used

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  • Periplocoside P-farm-oriented insecticidal active compound having activating effect on insect trypsin
  • Periplocoside P-farm-oriented insecticidal active compound having activating effect on insect trypsin
  • Periplocoside P-farm-oriented insecticidal active compound having activating effect on insect trypsin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] compound separation

[0011] Put 500g of the plant root bark and crushed plant sample in a 5L round bottom flask, add 3000mL methanol for reflux extraction for 3 hours, filter the supernatant, then add 3000mL methanol for reflux extraction for 2 hours, filter the supernatant liquid, the combined filtrates were concentrated under reduced pressure to about 100 mL. The concentrate was suspended in 400 mL of water, and then extracted three times with 500 mL of n-butanol, the butanol phases were combined, and concentrated to near dryness under reduced pressure. After the concentrate 60.0g chloroform was dissolved, the sample was mixed with silica gel, transferred to a silica gel column (4.0×100cm), and eluted with sherwood oil / acetone=9 / 1, 8 / 2, 7 / 3 (volume ratio) successively. Rinse 1000mL with each solvent ratio, collect one portion per 100mL, concentrate 6 / 4 of the eluent to dryness, transfer it to a silica gel column (3.0×50cm), and use petroleum ether / acetone=7 / 3, 6 / 4 (...

Embodiment 2

[0013] The effect of the compound barrella glucoside P on insect trypsin

[0014] The tryptase activity assay employs two obligate substrates: BaPNA and TAME. The strong alkaline trypsin activity was determined with BaPNA as the substrate, and the weak alkaline tryptase activity was determined with TAME as the substrate. BAPNA was dissolved in dimethyl alum at 10 mg / mL, and 40 μL was added to 0.5 ml 0.1 mol / L pH10.5 glycine-sodium hydroxide buffer solution containing midgut enzyme solution. After 20 minutes of reaction, 0.5 mL of 30% (Volume / Volume) Acetic acid was used to terminate the reaction, and the absorbance was measured at 405nm. TAME was dissolved in 0.15mol / L NaCl solution at 2mmol / L. Take 0.25ml of this solution and add 0.25ml of 0.1mol / L Tris-Hcl buffer solution with pH8.5 containing midgut enzyme solution, measure the light absorption change value at 247nm within 5min, and take a reading every 30min. The molar extinction coefficients of BaPNA and TAME are 8800M...

Embodiment 3

[0017] The Preparation of 0.2% Glycoside P Water Emulsion

[0018] Take by weighing the crude extract 16.0g containing the compound involved in the present invention (containing the compound ≥ 0.20g involved in the present invention) and dissolve it in 35g toluene, then add nonionic surfactant agricultural milk 4005.0g, TX-55.0g, water 35g, stirred until milky, namely the water emulsion with the compound as the active ingredient, wherein the active ingredient content is 0.2%.

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Abstract

The invention provides a farm-oriented insecticidal active compound having activating effect on insect trypsin, namely periplocoside P and belongs to the technical field of pesticides. A structural formula of the active compound is shown as follows: an IUPAC chemical name is delta5-pregnen-3beta,17alpha-dyhydroxy-,20(S)-oxygen-(2-O-acetyl-beta-D-digitalose(1-4)-beta-D-cymarose-(1-4)-beta-D-cymarose-(1-4)-beta-D-digitoxose-(1-4)-((1-5)-3,7-dideoxy-4-O-methyl-alpha-D-glucose-2-heptulose(2,4)-dyhydroxy-(1-3)-beta-D-cymarose). The compound selectively has strong stomach toxicity insecticidal activity on cabbage caterpillar, diamond back moths and beet armyworms, has activation on tryptase of insects to be tested and can be processed into a farm-oriented insecticidal preparation.

Description

Technical field: [0001] The invention relates to the technical field of pesticides, in particular to the use of a new compound of bark willow new glycosides for preventing and treating cabbage caterpillar, diamondback moth and beet armyworm. technical background: [0002] Lepidoptera insects such as cabbage caterpillar, diamondback moth, and beet armyworm are important pests that threaten the production of cruciferous vegetables such as cabbage and cabbage. Generally, there are 3-4 generations a year, and even more than 10 generations in the southern region, resulting in a 20% reduction in production. %-30%, severe production reduction can reach more than 60%. The main technical method currently used to control such pests is still chemical control, mainly insecticides such as beta-cyhalothrin, beta-cypermethrin, abamectin, and emamectin. Due to the long-term and high-frequency application of pesticides, the pests have developed resistance or resistance to the above-mentione...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/00A01N45/00A01P7/04
Inventor 师宝君高履桐陈翠翠孙文聪吴文君胡兆农姬志勤
Owner PESTICIDE INST XIBEI AGRI & FORESTRY TECHUNIV
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