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A kind of honeysuckle diterpenoid compound and its preparation method and anti-agricultural fungus use

A technology of compounds and diterpenoids, applied in the field of natural products, can solve the problems of endangering human and animal health, poor selectivity, long residual time, etc.

Active Publication Date: 2021-02-05
河南金陵金银花药业有限公司 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional chemical pesticides usually have poor selectivity, high toxicity, and long residual time. During use, there are problems such as serious pesticide residues, endangering human and animal health, and polluting the environment.

Method used

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  • A kind of honeysuckle diterpenoid compound and its preparation method and anti-agricultural fungus use
  • A kind of honeysuckle diterpenoid compound and its preparation method and anti-agricultural fungus use
  • A kind of honeysuckle diterpenoid compound and its preparation method and anti-agricultural fungus use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: Cut 5 kg of dried Lonicera pilosulae into 0.2-0.3 cm sections, add 95% ethanol with 6 times the volume of the crude drug, reflux extraction twice, each time for 2 hours, combine the crude extracts, and decompose at 70 ° C. Concentrate under reduced pressure to 0.5 times the volume of the medicinal material, then add petroleum ether and ethyl acetate in sequence according to the volume of 1:2 to extract 3 times respectively, combine the petroleum ether and ethyl acetate extracts, concentrate under reduced pressure, and obtain 14 g of petroleum ether extract and acetic acid Ethyl ester extract 200g. Get the ethyl acetate extract, use silica gel column chromatography to segment, and use petroleum ether-ethyl acetate (20:1), petroleum ether-ethyl acetate (10:1), petroleum ether-ethyl acetate (4:1 ), petroleum ether-ethyl acetate (1:1) solution, combined eluents with similar components, and concentrated to obtain 4 fractions of F2-1 to F2-4. Then, by comprehensiv...

Embodiment 2

[0022] Example 2: Cut 5 kg of dried Lonicera chinensis roots into 0.2-0.3 cm sections, add 5 times the volume of crude drug methanol, reflux extraction for 3 times, each time for 1.5 h, combine the crude extracts, and depressurize at 50 ° C Concentrate to 0.5 times the volume of the medicinal material, then add petroleum ether and ethyl acetate in sequence according to the volume of 1:1 to extract 3 times respectively, combine the petroleum ether and ethyl acetate extracts, concentrate under reduced pressure, and obtain 16 g of petroleum ether extract and ethyl acetate Ester extract 220g. Using methods such as silica gel column chromatography, gel LH-20 column chromatography, and recrystallization, the compound Lonicera cinereus (160 mg) was isolated from the ethyl acetate extract, with a yield of 0.0032%, UPLC- The purity of the product detected by HRESI-MS was 98.8%.

Embodiment 3

[0023] Example 3: Cut 10 kg of dried Lonicera pilosula root into 0.2-0.3 cm sections, add 80% methanol / water 6 times the volume of the crude drug, reflux extraction twice, each time for 2 hours, combine the crude extracts, 50 Concentrate under reduced pressure at ℃ to 1.5 times the volume of the medicinal material, then add petroleum ether and ethyl acetate to extract 5 times in sequence at a volume of 1:2, combine petroleum ether and ethyl acetate extracts, concentrate under reduced pressure, and obtain petroleum ether extract and Ethyl acetate extract. Using methods such as silica gel column chromatography, gel LH-20 column chromatography, and recrystallization, the compound Lonicera cinereus (315 mg) was isolated from the ethyl acetate extract, with a yield of 0.00315%, UPLC- The purity of the product detected by HRESI-MS was 98.4%.

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PUM

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Abstract

The present invention relates to the field of natural products. Specifically, it relates to a new compound, lonimacranthoidin A, which is obtained by using the roots of Lonicera vulgaris as raw material, and extracted and separated by a natural product chemical method. Its skeleton belongs to syn ‑Pimarane type ( syn ‑pimarane) diterpenes, the compound has a strong inhibitory effect on agricultural pathogenic fungi, and can be used to prepare anti-agricultural pathogenic fungi drugs.

Description

technical field [0001] The present invention relates to the field of natural products. It is characterized by taking the root of Lonicera macranthoides Hand.-Mazz. as a raw material, and extracting and separating it through natural product chemical methods to obtain a new compound whose skeleton belongs to the syn-pimarane type (syn-pimarane) di Terpene, the compound has a strong inhibitory effect on agricultural pathogenic fungi, and can be used to prepare anti-agricultural pathogenic fungal drugs. Background technique [0002] my country is a large agricultural country, and pesticides are the main tool for preventing and controlling agricultural diseases. Traditional chemical pesticides usually have poor selectivity, high toxicity, and long residual time. During use, there are problems such as serious pesticide residues, endangering human and animal health, and polluting the environment. Biopesticides refer to those products with pesticide properties made from plant extr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C29/76C07C35/42A01N31/06A01P3/00
CPCA01N31/06C07C29/76C07C35/42C07C2603/26
Inventor 陈雨冯煦吕慧徐曙单宇赵友谊王鸣
Owner 河南金陵金银花药业有限公司
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