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Application of betulinic acid and derivatives thereof in control of rice planthoppers

A technology of betulinic acid and its derivatives, applied in the field of pesticides, can solve the problems of insufficient activity and high toxicity, and achieve high biological activity

Active Publication Date: 2018-10-30
GAUNGXI TIANYUAN BIOCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In order to further search for high-efficiency and low-toxic betulinic acid pesticides, the present invention designs and synthesizes a series of betulinic acid compounds with novel functions on the basis of mastering the structure-activity relationship of betulinic acid. Finding some highly active pesticides will not only solve the problem of insufficient activity and high toxicity of pesticides on the market, but also enrich the types of pesticides on the market, and effectively control rice planthoppers, a pest that is harmful to agriculture.

Method used

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  • Application of betulinic acid and derivatives thereof in control of rice planthoppers
  • Application of betulinic acid and derivatives thereof in control of rice planthoppers
  • Application of betulinic acid and derivatives thereof in control of rice planthoppers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation of Betulinic Acid and Its Derivatives BHZ-1~BHZ-33

[0035] Compound BHZ-1 was prepared with reference to the literature Bioorganic&Medicinal Chemistry Letters, 2010,20(18):5389-5393;

[0036] Compound BHZ-2 was prepared with reference to the literature European Journal of Medicinal Chemistry, 2015, 95, 240-248;

[0037] Compound BHZ-3 was prepared with reference to Medchemcomm, 2014, 5(4):445-451;

[0038] Compound BHZ-4 was prepared with reference to Medchemcomm, 2014, 5(4):445-451;

[0039] Compound BHZ-5 was prepared with reference to the literature Bioorganic & Medicinal Chemistry Letters, 2007, 17(5): 1475-1478;

[0040] Compound BHZ-6 was prepared with reference to the literature Bioorganic & Medicinal Chemistry Letters, 2004, 14(15): 4087-4091;

[0041] Compound BHZ-7 was prepared with reference to the literature Bioorganic & Medicinal Chemistry Letters, 2003, 13(20): 3549-3552;

[0042] Compound BHZ-8 was prepared with reference to Medchemcomm, ...

Embodiment 2

[0070] Determination and Results of Lethal Activity in Controlling Rice Planthopper

[0071] (1) Test insects: rice planthopper (mainly brown planthopper), collected from rice seedlings of Guangxi Tianyuan Biochemical Co., Ltd.;

[0072] (2) Drugs to be tested: the drugs are compounds BHZ-1 to BHZ-33 (prepared according to Example 1), and toosendanin and clothianidin are reference substances.

[0073] (3) Determination of biological activity: the method of soaking rice stalks was used. Dissolve 30 mg of the compound in 10 mL of methanol, NMP and NP-10 mixed solution (volume ratio 80:19:1) to prepare a drug solution with a mass concentration of 3000 μg / mL, take 10 mL of it and dilute it with water to 25 , 50, 100, 250 and 500 μg / mL of the test solution. Take 20mL of the test drug solution and place it in a test tube with a capacity of 25mL, and put rice seedlings of appropriate length whose roots have been subjected to moisturizing treatment into the test tube containing the ...

Embodiment 3

[0082] Preparation of 1% betulinic acid granules

[0083] 1% betulinic acid, 2.6% sodium lauryl sulfate, 1% naphthalenesulfonic acid formaldehyde condensate sodium salt, 5% methylcellulose, 10% white carbon black, 10% chitin, and kaolin make up 100%. The above materials were mixed in a mixer for 20 minutes, and then jet milled. After the pulverization is completed, stir for 10 minutes, and then granulate to obtain 1% betulinic acid granules.

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Abstract

The invention discloses application of betulinic acid and derivatives thereof in control of rice planthoppers and provides novel application of betulinic acid and derivatives thereof for agriculturalproduction, namely application of betulinic acid and derivatives thereof serving as pesticides in control of rice planthoppers. The pesticide preparations prepared from the betulinic acid and derivatives thereof are high in activity and low in toxicity, have excellent control effects on the rice planthoppers, and are ideal pesticides for controlling the rice planthoppers.

Description

technical field [0001] The invention belongs to the technical field of pesticides, and in particular relates to the application of betulinic acid and its derivatives in preventing and treating rice planthoppers. Background technique [0002] Betulinic acid can be extracted from rose apple leaves, white birch bark, jujube seed, and can also be synthesized by chemical methods using betulin as raw material. Studies in recent years have found that betulinic acid has a wide range of biological activities: betulinic acid can selectively kill human melanoma cells without killing healthy cells; betulinic acid has an inhibitory effect on HIV-1 infection; betulinic acid It also has inhibitory effect on malignant tumor cells such as brain tumor, neuroectodermal tumor and leukemia. With the continuous improvement of synthesis technology, there are more and more reports on the synthesis of betulinic acid analogues. Since betulin, an analogue of betulinic acid, has a high content in birc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07J73/00C07J71/00A01P7/04
CPCC07J63/008C07J71/0005C07J71/0047C07J71/0063C07J73/003C07J73/005
Inventor 李卫国刘映前张君香陈诚李俊采零春华
Owner GAUNGXI TIANYUAN BIOCHEM
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