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Extraction method and application of indole monoterpene compound

A technology of terpenoids and extraction methods, which is applied in the field of traditional Chinese medicine extraction and can solve the problems that the extraction methods and uses of indole monoterpenoids have not yet been reported.

Active Publication Date: 2020-02-04
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the extraction of indole monoterpenoids, extraction methods and uses from Uncaria uncaria has not been reported yet.

Method used

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  • Extraction method and application of indole monoterpene compound
  • Extraction method and application of indole monoterpene compound
  • Extraction method and application of indole monoterpene compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The extraction method of indole monoterpenoid compound comprises the steps:

[0036] (1) Take Uncaria ( Uncariarhynchophylla (Miq.) Miq .ex Havil.) (18kg) as the raw material, add 6 mass times of the raw material with a volume fraction of 95% ethanol aqueous solution, reflux extraction twice, each extraction for 2 hours, combine to obtain the extract, recover the solvent under reduced pressure, and concentrate to obtain the total extract (1360g);

[0037] (2) Disperse the total extract into 5 times the mass of water, sequentially extract with equal volumes of petroleum ether and ethyl acetate, recover the solvent from the ethyl acetate extract under reduced pressure, and obtain 300 g of ethyl acetate layer extract;

[0038] (3) The ethyl acetate layer extract was separated by silica gel column chromatography, using dichloromethane-methanol with a volume ratio of 100:1, 50:1, 20:1, 10:1 and 1:1 as the eluent gradient Elution gave fractions Fr. 1, Fr. 2, Fr. 3, Fr. 4,...

Embodiment 2

[0053] The extraction method of indole monoterpenoid compound comprises the steps:

[0054] (1) Using the hooked stems of Uncaria uncaria as raw material, add 85% ethanol aqueous solution with a volume fraction of 7 times the mass of the raw material, reflux extraction for 3 times, each time for 2 hours, combine to obtain the extract, recover the solvent under reduced pressure, and concentrate After obtaining the total extract;

[0055] (2) Disperse the total extract into 5 times the mass of water, sequentially extract with equal volumes of petroleum ether and ethyl acetate, recover the solvent from the ethyl acetate extract under reduced pressure, and obtain the ethyl acetate layer extract;

[0056] (3)-(8) are the same as Embodiment 1 (3)-(8).

Embodiment 3

[0058] The extraction method of indole monoterpenoid compound comprises the steps:

[0059] (1) Using the hooked stems of Uncaria vine as the raw material, add 75% ethanol aqueous solution with a volume fraction of 10 times the mass of the raw material, reflux extraction for 3 times, and extract for 2 hours each time, combine to obtain the extract, recover the solvent under reduced pressure, and concentrate After obtaining the total extract;

[0060] (2) Disperse the total extract into 10 times the mass of water, sequentially extract with equal volumes of petroleum ether and ethyl acetate, recover the solvent from the ethyl acetate extract under reduced pressure, and obtain the ethyl acetate layer extract;

[0061] (3)-(8) are the same as Embodiment 1 (3)-(8).

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PUM

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Abstract

The invention discloses an extraction method and application of an indole monoterpene compound, and belongs to the technical field of traditional Chinese medicine extraction. A pharmacodynamic substance in uncaria rhynchophylla that has a significant agitation effect on a 5-HT1A receptor is clarified, it is found that a compound 1 and a compound 2 have the strong agitation effect on the 5-HT1A receptor. The indole monoterpene compound obtained by extracting can effectively agitate the 5-HT1A receptor, and it is indicated that the compound can be used as an agonist drug for the 5-HT1A receptor.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine extraction, and relates to an indole monoterpene compound, an extraction method and application. Background technique [0002] Uncaria was first recorded in "Bielu of Famous Doctors", and it was listed as a low-grade product. It has the effects of clearing away heat and calming the liver, calming wind and calming convulsions. The 2015 edition of the "Chinese Pharmacopoeia" stipulates that the traditional Chinese medicine Uncaria uncaria is the Rubiaceae plant Uncaria Uncariarhynchophylla (Miq.) Miq. exHavil., Uncaria chinensis Uncariasinens (Oliv.) Havil., Uncaria Uncaria macrophylla Wall., Uncaria Uncaria hirsute Havil .and Uncaria uncaria Uncariases silifructus Dry hooked stems of Roxb. Through in vivo and in vitro experiments, the antihypertensive effect of Uncaria was confirmed (Ndagijimana, A.; et al. A review onindole alkaloids isolated from Uncariarhynchophylla and th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14A61K31/4375A61P25/24
CPCC07D471/14A61P25/24
Inventor 孙成鹏马骁驰王超霍晓奎田象阁冯磊宁静于振龙
Owner DALIAN MEDICAL UNIVERSITY
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