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Compound with cholesterol lowering activity extracted from burdock leaves as well as preparation method and application thereof

A technology of burdock leaves and compounds, applied in the field of compounds with cholesterol-lowering activity and their preparation

Pending Publication Date: 2021-05-28
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The long history of both medicine and food and folk usage of burdock leaves provide a basis for its blood lipid regulation, and it is expected to become a new resource for regulating blood lipids, but safe and effective compounds for regulating blood lipids can be obtained from it, and used to prepare Drugs regulating dyslipidemia have not been publicly reported so far

Method used

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  • Compound with cholesterol lowering activity extracted from burdock leaves as well as preparation method and application thereof
  • Compound with cholesterol lowering activity extracted from burdock leaves as well as preparation method and application thereof
  • Compound with cholesterol lowering activity extracted from burdock leaves as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A preparation method of a compound with cholesterol-lowering activity extracted from burdock leaves of the present invention comprises the following steps:

[0031] (1) Grind 15 kg of dried burdock leaves, add water, immerse and boil for extraction twice, each time for 2.5 hours, combine the extracts, and concentrate to a concentrated solution equivalent to 0.15 g / mL of crude drug;

[0032] (2) Load the concentrated solution on the AB-8 column with an inner diameter of 15cm and a height of 150cm, and carry out gradient elution at a flow rate of 1BV / h with 200L of water, 300L of mass concentration 30% ethanol, and 400L of 70% ethanol in sequence, and collect 70% ethanol Eluent, the solvent was recovered under reduced pressure to obtain extract (600g);

[0033] (3) Add 1L of water to the extract to disperse, extract 4 times with n-butanol 1L, 1L, 0.5L, 0.5L, combine the n-butanol extracts, recover the solvent under reduced pressure, and obtain component Fr.A (50g); compon...

Embodiment 2

[0038] A preparation method of a compound with cholesterol-lowering activity extracted from burdock leaves of the present invention comprises the following steps:

[0039] (1) Grind 15 kg of dried burdock leaves, add water, immerse and boil to extract twice, extract for 2 hours each time, combine the extracts, and concentrate to a concentrated solution equivalent to crude drug 0.3g / mL;

[0040] (2) Load the concentrated solution on the AB-8 column with an inner diameter of 20cm and a height of 120cm. Carry out gradient elution with 300L of water, 450L of mass concentration 30% ethanol, and 600L of 70% ethanol in sequence at a flow rate of 2BV / h, and collect 70% ethanol The eluent was recovered under reduced pressure to obtain a solvent extract (800g);

[0041](3) Add 1.5L of water to the extract to disperse, extract 4 times with 1.5L, 1L, 0.5L, and 0.5L of n-butanol, combine the n-butanol extracts, recover the solvent under reduced pressure, and obtain component Fr.A (50g); C...

Embodiment 3

[0046] A preparation method of a compound with cholesterol-lowering activity extracted from burdock leaves of the present invention comprises the following steps:

[0047] (1) Grind 15 kg of dried burdock leaves, add water, immerse and boil for extraction 3 times, extracting for 1.5 hours each time, combine the extracts, and concentrate to a concentrated solution equivalent to 0.4 g / mL of crude drug;

[0048] (2) Load the concentrated solution on the AB-8 column with an inner diameter of 25cm and a height of 100cm. Carry out gradient elution at a flow rate of 3BV / h with 400L of water, 600L of 30% ethanol and 800L of 70% ethanol in sequence, and collect 70% ethanol Eluent, solvent recovery under reduced pressure, to obtain extract (1100g);

[0049] (3) Add 2L of water to the extract to disperse, extract 4 times with 2L, 1L, 0.5L, 0.5L of n-butanol, combine the n-butanol extracts, recover the solvent under reduced pressure, and obtain the component Fr.A (58g); Fr.A was subjecte...

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Abstract

The invention relates to a compound with cholesterol lowering activity extracted from burdock leaves and a preparation method and application thereof, can effectively solve the problem of extracting a new compound with lipid lowering activity from the burdock leaves and realize the application of the new compound in preparing lipid lowering medicaments. The preparation method comprises the steps of adding water into burdock leaves, conducting boiling and extraction, conducting concentration, feeding an obtained concentrate into an AB-8 column, conducting elution with water, 30% ethanol and 70% ethanol in sequence, collecting 70% ethanol eluent, recovering the solvent under reduced pressure, dispersing an obtained extractum by adding water, conducting extracting with n-butyl alcohol, recovering the solvent under reduced pressure, carrying out silica gel column chromatography, carrying out dichloromethane / methanol gradient elution, recovering the solvent under reduced pressure, carrying out secondary silica gel column chromatography, carrying out gradient elution with petroleum ether-ethyl acetate, collecting 100:70 eluate, recovering the solvent under reduced pressure, carrying out MCI column chromatography, carrying out methanol aqueous solution gradient elution, collecting 40% methanol eluate, recovering the solvent under reduced pressure, and carrying out reverse semi-preparation by using a YMC-Pack ODS-A column to obtain the compound with the activity of reducing cholesterol. The preparation method is easy to operate, high in guidance quality, high in separation speed and high in product purity.

Description

technical field [0001] The invention relates to medicine, in particular to a compound with cholesterol-lowering activity extracted from burdock leaves and its preparation method and application. Background technique [0002] Burdock leaves are the dry basal leaves of Arctiumlappa, a plant in the Compositae family. It is widely distributed throughout the country and has a long history of edible and medicinal uses. Burdock leaves have been recorded in dietotherapy in ancient herbal medicines, and they are used to prevent stroke and hand and foot paralysis. Many books on herbal medicine have recorded the dietotherapy experience of burdock leaf. For example: "The Prescription in the Box" of the Tang Dynasty recorded that burdock leaves were edible for the first time, and "Sheng Hui Fang" recorded: "One catty of burdock leaves, one or two crisps, boiled for three to five boils, drained, made soup, and eaten. Cure stroke, hand and foot paralysis" ; Burdock leaves are used to trea...

Claims

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Application Information

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IPC IPC(8): C07D307/92A61K36/28A61P3/06
CPCC07D307/92A61K36/28A61P3/06Y02A50/30
Inventor 代丽萍许菲斐朱利利梁韩晶冯庆梅吕江南张玲霞
Owner HENAN UNIV OF CHINESE MEDICINE
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