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Application of annosquacin B in preparation of pesticide preparations

A technology for pesticide preparations and organic solvents is applied in the field of bisphenol lactone compounds, which can solve the problems of complex methods, low yield, low efficiency and the like, and achieve the effects of good poisoning activity and little environmental pollution.

Inactive Publication Date: 2015-06-03
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Annoscortin B is an ortho-ditype annonaceous acetogenins (as reported in the literature Yong Chen,.Six cytotoxic annonaceous acetogenins from Annona squamosa seeds, Food Chem.2012,135,960-966), the preparation method in the prior art In order to adopt high-efficiency preparation of liquid phase, the method is complicated, the yield is low, and the efficiency is low, and industrial production cannot be realized.
At present, there are no reports on the simple and efficient preparation method of Anoxetin B and its use in the preparation of killing agricultural diseases and insect pests, etc.

Method used

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  • Application of annosquacin B in preparation of pesticide preparations
  • Application of annosquacin B in preparation of pesticide preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take 2kg of custard apple seeds, crush them, and percolate the coarse powder twice with 5 times the amount of ethyl acetate, combine the percolation liquid, recover under reduced pressure below 60°C to obtain the concentrated liquid, let it stand overnight, and centrifuge at 3000r / min to obtain the obtained product The upper layer (123g), mixed with 120g of silica gel, was subjected to 500g silica gel column chromatography, and was eluted with petroleum ether-ethyl acetate gradient, the ratios were 10:1, 5:1, 2:1, 1:1, 0:1 , 10 fractions were collected for each ratio, each fraction was 500 mL, tracked by thin-layer chromatography, 23-30 fractions were combined, concentrated and dried under reduced pressure at less than 60°C. Recrystallize with 5 times the amount of petroleum ether-ethyl acetate (7:1) to obtain 0.14 g of refined anoxetine B. According to 1H-NMR data and MS, its molecular weight was determined to be 606.4, and it was identified as annonacetin anoxetine B....

Embodiment 2

[0025] Take 1.8kg of custard apple seeds, crush them, and pass the coarse powder through 20 meshes, and perform supercritical carbon dioxide extraction under the conditions of extraction temperature 35°C, extraction pressure 30Mpa, extraction time 3 hours and entrainer ethanol consumption 180mL. The extract was obtained, which was recovered under reduced pressure below 60°C to obtain 98 g of concentrated liquid. After mixing 100g of silica gel, carry out 500g of silica gel column chromatography, and use chloroform-methanol gradient elution, the ratio is 100:1, 50:1, 25:1, 10:1, each ratio collects 10 fractions, each fraction is 500mL , followed by thin-layer chromatography, combined 10-15 fractions, concentrated and dried under reduced pressure at less than 60°C. Recrystallize with 5 times the amount of chloroform-methanol (65:1) to obtain 0.19 g of refined aristomethoxin B. Its molecular weight was determined to be 606.4 by 1H-NMR data and MS, and it was determined to be ann...

Embodiment 3

[0026] The biological activity of embodiment 3 Anoxetin B

[0027] 1. Determination of the contact effect on bean aphid:

[0028] Use a micro-dropper to drip 10% distilled acetone aqueous solution containing different concentrations of anoxetin B on the abdomen and back of the bean aphid, and the amount of dripping per insect is 0.05 μL. After the dripping was completed, each was put into a biochemical incubator for cultivation. After 24 hours, the death situation was checked and the death rate was calculated. Immersion with 10% acetone distilled water was used as a control. The mortality rate of the control group was less than 10% for effective determination, and the mortality rate of the treatment group was corrected by Abbott's formula. Measured 3 times in parallel. The test results were analyzed using SPSS 13.0 to calculate the lethal concentration LC 50 .

[0029] 2. Determination of contact killing effect on Tetranychus cinnabarinus:

[0030] Paste the double-side...

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Abstract

The invention discloses an annonaceous acetogenin compound annosquacin B which is prepared from sweetsop seeds and can prevent and treat agricultural pests. A plenty of biological activity assay results verify that sweetsop annosquacin B has poisonous activities to different extends on aphis craccivora and T. cinnabarinus and particularly shows a better poisonous activity than that of abamectin, and moreover, annosquacin B is extracted from the sweetsop seeds, so that annosquacin B is low in environmental pollution and environmental-friendly, and can be developed to form novel pesticide preparations which prevent and treat agricultural pests.

Description

technical field [0001] The invention relates to a method for preparing ortho-ditype anemone lactone compounds from the seeds of the traditional Chinese medicine custard apple, and the application of anoxacin B in the preparation of pesticide preparations. Background technique [0002] At present, there are about 500 kinds of artificially synthesized chemical pesticides. The widespread use of these pesticides not only causes serious environmental pollution, but also causes harm to human health. Botanical pesticides are an important part of biological pesticides. Botanical pesticides have the advantages of fast biodegradation in the environment, low biological toxicity to humans and animals, and less resistance to pests and diseases. Searching for compounds with pesticide activity, especially novel molecular structure and special mechanism of action, from traditional Chinese medicines has become an important approach for the research of new pesticides. With the advancement of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/08A01P7/02A01P7/04C07D307/58
CPCY02P20/54
Inventor 陈勇李祥陈建伟邱燕
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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