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Compound D with hypoglycemic effect extracted from wine-processed cornel, and preparation method and application thereof

The technology of a compound and cornelian root, applied in the field of medicine, can solve the problems such as no public reports, and achieve the effects of developing medicinal value, huge economic and social benefits, and easy preparation method.

Active 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

Combined with the traditional efficacy characteristics of Cornus officinalis, through systematic research on the chemical components of Cornus officinalis, it is expected to obtain new compounds with novel structures that have hypoglycemic effects, but there has been no public report so far

Method used

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  • Compound D with hypoglycemic effect extracted from wine-processed cornel, and preparation method and application thereof
  • Compound D with hypoglycemic effect extracted from wine-processed cornel, and preparation method and application thereof
  • Compound D with hypoglycemic effect extracted from wine-processed cornel, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of preparation method of the present invention extracts the compound D that has hypoglycemic effect from wine Cornus officinalis, comprises the following steps:

[0028] (1) Take 10kg of dried Cornus officinalis, add 120L of ethanol solution with a volume concentration of 30%, cold-soak at 4-6°C for 9 days, filter to obtain the extract, concentrate under reduced pressure, and obtain a product with a relative density of 1.2-1.4 at 50°C thick extract (1.5kg);

[0029] (2) Add 2.0L of water to the thick extract to disperse into a suspension, extract 6 times with ethyl acetate, 1L to 2L each time, combine the above extracts, concentrate under reduced pressure, and obtain an extract Fr. ETOAC (100g);

[0030] (3) The extract Fr.ETOAC is chromatographed on a silica gel column with 200-300 mesh sieves, r=3cm, H=7cm, gradient elution with volume ratio 100:0, 100:2, 100:5 dichloromethane-methanol (Natural flow rate), elute 6 column volumes in each ratio, collect the 100...

Embodiment 2

[0035] A kind of preparation method of the present invention extracts the compound D that has hypoglycemic effect from wine Cornus officinalis, comprises the following steps:

[0036] (1) Take 10kg of dried Cornus officinalis, add 100L of ethanol solution with a volume concentration of 30%, extract by cold immersion at 4°C for 12 days, filter to obtain the extract, concentrate under reduced pressure to obtain a thick extract with a relative density of 1.2 at 50°C ( 1.1kg);

[0037] (2) Add 2L of water to the thick extract to disperse into a suspension, extract 4 times with ethyl acetate, 2.5L each time, and concentrate the extract solution under reduced pressure to obtain an extract Fr.ETOAC (95g) with a relative density of 1.2 at 50°C;

[0038] (3) Extraction Fr.ETOAC is subjected to silica gel column chromatography with 300 mesh sieve, r=2.5cm, H=6cm, gradient elution is carried out with volume ratio 100:0, 100:2, 100:5 dichloromethane-methanol ( natural flow rate), each ra...

Embodiment 3

[0043]A kind of preparation method of the present invention extracts the compound D that has hypoglycemic effect from wine Cornus officinalis, comprises the following steps:

[0044] (1) Take 10kg of dried Cornus officinalis, add 60L of ethanol solution with a volume concentration of 30%, extract by cold soaking at 6°C for 8 days, filter to obtain the extract, concentrate under reduced pressure to obtain a thick extract with a relative density of 1.3 at 50°C ( 950g);

[0045] (2) Add 1L of water to the thick extract to disperse into a suspension, extract 6 times with ethyl acetate, 1L each time, and concentrate the extract solution under reduced pressure to obtain extract Fr.ETOAC (78g) with a relative density of 1.3 at 50°C;

[0046] (3) Extraction Fr.ETOAC is subjected to silica gel column chromatography with 200 mesh sieve, r=4cm, H=9cm, gradient elution is carried out with dichloromethane-methanol with volume ratio 100:0, 100:2, 100:5 (natural flow rate), 4 column volumes...

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Abstract

The invention relates to a compound D with a hypoglycemic effect extracted from wine-processed cornel, and a preparation method and application thereof. The problems of extracting a new compound from wine-processed cornel and realizing application of the new compound in preparation of drugs for treating diabetes mellitus are effectively solved. 30% ethanol is added into wine-processed cornel for cold soaking extraction, an extract solution is concentrated into thick extract under reduced pressure, water is added into the thick extract for dispersion, extraction is performed with ethyl acetate, and the extract solution is concentrated under reduced pressure to obtain an extract Fr.ETOAC; the extract Fr.ETOAC goes through a silica gel column chromatograph, and undergoes gradient elution with dichloromethane-methanol, 100: 5 elate is collected, vacuum concentration is performed to obtain an extract Fr.ETOAC-4, ODS column chromatography is performed, gradient elution is performed with methanol-water, c20: 80 eluate is collected, vacuum concentration is performed to obtain an extract Fr.ETOAC-4-2, Sephadex LH-20 column chromatography is performed, methanol elution is performed, vacuum concentration is performed to obtain an extract Fr.ETOAC-4-2-2, separation on semi-preparative HPLC is performed with an ODS-C18 column, acetonitrile-water elution is performed, a chromatographic peak in 25 minutes is collected, and the solvents are recovered under reduced pressure to obtain the compound D. The method disclosed by the invention is easy to operate, high in guidance quality and high in product purity, and develops new application and medicinal value of the wine-processed cornel.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a compound D with hypoglycemic effect extracted from Cornus officinalis and its preparation method and application. Background technique [0002] Malignant tumors, cardiovascular and cerebrovascular diseases, and diabetes are the three major chronic diseases that seriously threaten human health. As of 2015, the number of diabetic patients in China has exceeded 100 million, ranking first in the world. It is estimated that by 2040, the number of diabetic patients in my country will exceed 150 million. So far there is no curative treatment option. Deficiency of both qi and yin, deficiency of liver and kidney are the main causes of diabetic nephropathy. In recent years, it has been a research hotspot to obtain monomeric compounds with good hypoglycemic activity from traditional Chinese medicines. Cornus officinalis (Cornus officin alis) is the dried and mature pulp of Cornus officinalis Si...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/46A61P3/10
CPCC07D307/46A61P3/10
Inventor 许二平代丽萍冯庆梅李红彬张玲霞陈随清王智民
Owner HENAN UNIV OF CHINESE MEDICINE
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