Natural sesquiterpene guaiol compound and medicinal application thereof

A technology of guaiacol and compounds, which is applied in the field of pharmacy and can solve problems such as complex mechanism of action

Inactive Publication Date: 2012-11-28
SHIHEZI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insecticidal active ingredients in plants are secondary metabolites formed during the long-term co-evolution of plants and insects. They have unique symptoms, diverse modes of action, and complex mechanisms of action on pests.

Method used

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  • Natural sesquiterpene guaiol compound and medicinal application thereof
  • Natural sesquiterpene guaiol compound and medicinal application thereof
  • Natural sesquiterpene guaiol compound and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 prepares guaiol (guaiol) by ferulicum ferulae

[0033] 2.0 kg of root parts of dried plant Ferula ferulaeoides (Steud.) Korov. were crushed and mixed with 20 times the amount of 95% ethanol at 45 o C soaking and extracting for 3 times, the extracts were combined and evaporated to dryness under reduced pressure to obtain extract, which was then extracted with dichloromethane 3 times, and evaporated to dryness under reduced pressure to obtain 400 g of extract. The sample was subjected to silica gel column chromatography, using 200-300 mesh silica gel (Qingdao Ocean Chemical Factory, China), petroleum ether-ethyl acetate (100:0 ~ 0:100) gradient elution, and silica gel thin-layer chromatography detection. Combine the fractions eluted with petroleum ether-ethyl acetate 97:3, evaporate to dryness to obtain a white solid, and repeatedly use 300-400 mesh silica gel column chromatography, the eluent is petroleum ether-acetone (99:1 ~ 97:3), and finally Recrysta...

Embodiment 2

[0034] Example 2 Contact test of compound (I) on armyworm and diamondback moth

[0035] Dilute the reagent to be tested with acetone to the required concentration, and use a micro capillary to quantitatively drip the drug on the pronotum of the larvae of the test insects, and drip 10 larvae for each treatment. Insects are reared in the insect culture room [T=(25±1)°C, RH=75%±5%, D / L=12h / 12h], and the number of dead insects is investigated after 24 hours, and the corrected mortality rate is calculated (as shown in Table 1. Show).

[0036] Table 1 is the contact toxicity of guaiol (guaiol) to armyworm and diamondback moth.

[0037]

[0038] Table 1

[0039]

Embodiment 3

[0040] Example 3 Fumigation insecticidal experiment of compound (I) against armyworm and housefly

[0041] Fumigation container is with 250ml triangular flask (capacity is 330m1), fixes the rubber stopper of 9 cm * 1 cm filter paper with pin and seals; Place 10 insects for testing in the triangular flask and give a small amount of food, dilute the test agent with acetone to the desired level. After the concentration is required, use a micro-sampler to measure 1 μL-5 μL of the drug solution and drop it on the filter paper, quickly cover the triangular flask tightly, and investigate the number of dead insects 12 hours after the treatment; 10 test insects are treated as one, and each treatment is repeated Three times to calculate the mortality rate and corrected mortality rate; use the probability value analysis method to obtain the toxicity curve and the lethal median dose of the essential oil to the test insects.

[0042] Activity test results show that the contact toxicity o...

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Abstract

The invention belongs to the field of pharmacy, and relates to a natural sesquiterpene guaiol compound, in particular to a natural sesquiterpene guaiol compound of a formula (I) and a preparation method thereof and application in preparation of a botanical insecticide. Insecticidal experiment results display that the guaiol compound shows eating refusal, contact killing, fumigation and juvenile hormone analog activity on experimental insects, and the acting mode of the guaiol compound is closely related with the using dose; the contact effect LD50 on 4-age armyworms and 3-age plutella xylostella is respectively 0.072 mg / piece, 24 hours and 8.920 mg / piece, 24 hours; the fumigation virulence LC50 on houseflies and 4-age adult armyworms is respectively 3.52 muL / L, 12 hours and 16.95 muL / L, 12 hours; and the results show that the compound has high insecticidal activity and can be used as an insecticidal active ingredient for preparing the botanical insecticide in a form of spray or fumigant and the like.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a natural sesquiterpene compound guaiol, in particular to a natural sesquiterpene compound guaiol (guaiol), a preparation method thereof and an application in preparing plant pesticides. Background technique [0002] With the emergence of problems such as environmental pollution, pesticide residues and pest resistance, as well as the rapid development of organic agriculture in the world, higher requirements have been placed on the pesticide industry. It is known that the direction of pesticide development is to develop environment-friendly pesticides with high efficiency, low toxicity, low residue and low resistance risk, and botanical pesticides meet this development requirement. Generally speaking, botanical pesticides come from nature and have a smooth degradation path in the environment, so they do not pollute the environment and have little adverse impact on the environment; practice sh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C33/16C07C29/76A01N31/04A01P7/04
Inventor 谢慧琴刘涛王春娟穆青
Owner SHIHEZI UNIVERSITY
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